BR112018009279B1 - OXADIAZAESPIRO COMPOUNDS, PROCESS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITION AND THEIR USE IN THE PREPARATION OF A MEDICATION FOR THE TREATMENT OF DRUG ABUSE OR ADDICTION - Google Patents

Abstract

OXADIAZAESPIRO COMPOUNDS FOR THE TREATMENT OF DRUG ABUSE AND ADDICTION. The present invention relates to compounds having pharmacological activity for the sigma receptor (s), and more particularly to oxadiazaspiro compounds having this pharmacological activity, to processes for preparing such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular against drug abuse and addiction.

Description

FIELD OF INVENTION

[001] The present invention relates to new oxadiazaspiro compounds having affinity for sigma receptors, especially sigma-1 (GI) receptors, as well as processes for preparing them, compositions comprising them, and their use as medicines. against drug abuse and addiction.

BACKGROUND OF THE INVENTION

[002] Research into new therapeutic agents has been greatly aided in recent years by a better understanding of the structure of proteins and other biomolecules associated with target diseases. An important class of these proteins are sigma (G) receptors, receptors on the cell surface of the central nervous system (CNS) that may be related to dysphoric, hallucinogenic and cardiac stimulant effects of opioids. From studies of the biology and function of sigma receptors, evidence has been presented that sigma receptor ligands may be useful in the treatment of psychosis and movement disorders, such as dystonia and tardive dyskinesia, and motor disorders associated with Huntington's chorea or Huntington's syndrome. Tourette's and in Parkinson's disease (Walker, J.M. et al, Pharmacological Reviews, 1990, 42, 355). The known sigma receptor ligand rimcazole has been reported to clinically show effects in the treatment of psychosis (Snyder, S. H., Largent, B. L. J. Neuropsychiatry 1989, 1, 7).

[003] The sigma receptor has at least two subtypes, the sigma-1 site (g1), and the sigma-2 site (g2).

[004] The g1 receptor is a non-opioid type receptor expressed in numerous adult mammalian tissues (e.g., central nervous system, ovary, testis, placenta, adrenal gland, spleen, liver, kidney, gastrointestinal tract) as well as in developing embryos from its earliest stages, and is apparently involved in a large number of physiological functions. Its high affinity for several pharmaceutical products has been described, such as (+)SKF-10047, (+)-pentazocine, haloperidol and rimcazole, among others, known ligands with analgesic, anxiolytic, antidepressant, antiamnestic, antipsychotic and neuroprotective activities.

[005] The G2 receptor is also expressed in numerous adult mammalian tissues (e.g., nervous system, immune system, endocrine system, liver, kidney). Receptors may be components in a new apoptosis routine that may play an important role in regulating cell proliferation or cell development. This routine appears to consist of G2 receptors linked to intracellular membranes, located in calcium-storing organelles, such as the endoplasmic reticulum and mitochondria, which also have the capacity to release calcium from these organelles. Calcium signals can be used in routine signaling for normal cells and/or in induction of apoptosis.

[006] Endogenous sigma ligands are not known, although progesterone has been suggested to be one of them. Possible sigma site-mediated drug effects include modulation of glutamate receptor function, neurotransmitter response, neuroprotection, behavior, and cognition (Quirion, R. et al. Trends Pharmacol. Sci., 1992, 13:85-86). Most studies have suggested that sigma binding sites (receptors) are plasma elements of the signal transduction cascade. Drugs reported to be selective sigma ligands have been evaluated as antipsychotics (Hanner, M. et al. Proc. Natl. Acad. Sci., 1996, 93:8072-8077). The existence of sigma receptors in the CNS, immune and endocrine systems has suggested a likelihood that it may serve as a link between the three systems.

[007] In view of the potential therapeutic applications of sigma receptor agonists or antagonists, a great effort has been directed to finding selective ligands. Thus, the prior art describes different sigma receptor ligands.

[008] For example, international patent application WO 2007/098961 describes 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives having pharmacological activity for the sigma receptor.

[009] Spiro[benzopyran] or spiro[benzofuran] derivatives were also described in EP1847542, as well as pyrazole derivatives (EP1634873) with pharmacological activity on sigma receptors.

[0010] WO 2009/071657 describes some tricyclic triazole compounds although structurally different from those of the present invention with activity for sigma receptors.

[0011] Furthermore, receiving AI becomes a promising goal for developing new therapies aimed at treating the effects of a variety of abused drugs (Robson et al., Curr Pharm Des. 2012;18(7 ):902-19). The a1 receptor is known to be expressed in brain regions involved in addictive processes, e.g., hippocampus, striatal nucleus, nucleus accumbens, and amygdala (Alonso et al., Neuroscience. 2000;97(1): 155-70). It is also expressed in organs such as the heart (Ela et al., J Pharmacol Exp Ther 1994; 269: 1300-9), liver (Samovilova and Vinogradov, Eur J Pharmacol 1992; 225: 69-74.) or gastrointestinal system (Roman et al., Gastroenterology 1989; 97:76-82.), organs involved in some of the side effects and many toxicities of substances they abused. Drugs such as cocaine (Matsumoto et al., Neuropharmacology 2001; 41: 878-86, 2007), methamphetamine (Nguyen et al., Neuropharmacology 2005; 49: 638-45), or phencyclidine (Morris et al., Curr Opin Pharmacol 2005 ; 5: 101-6.) interact directly with the ai receptor, which is involved in some of the effects of these substances. However, the a1 receptor can also modulate the effects of other drugs, even if they do not have affinity for the a1 receptor. This is the case for opiates such as morphine (Chen et al., Drug Alcohol Depend 2011;117:164-9), ethanol (Blasio et al., Behav Brain Res 2015;287:315-22) or nicotine (Horan et al. al., Eur J Pharmacol 2001; 426: R1-2).

[0012] Modulation of the a1 receptor is known to be effective in blocking the reinforcing effects of cocaine (Romieu et al., Neuroreport 2000; 11: 2885-8), ethanol (Maurice et al., Pharmacol Biochem Behav 2003; 74: 869-76) or nicotine (Horan et al., Eur J Pharmacol 2001; 426: R1-2.) in Rodents, assessed in the place conditioning test, and may also attenuate cocaine reinstatement (Martin-Fardon et al., Neuropsychopharmacology. September 2007; 32(9):1967-73) or ethanol (Martin-Fardon et al., Neuroreport. 2012 Oct 3;23(14):809-13) response to self-administration. It also inhibits the stimulation effects on locomotor activity induced by cocaine (McCracken et al., Eur J Pharmacol 1999; 370(3):225-32) or methamphetamine (Okuyama et al., Life Sci. 1993; 53(18) :PL285-90).

[0013] The precise mechanisms by which a1 receptor ligands exert the observed effects are not fully elucidated. It is well known that the a1 receptor modulates neurotransmitter systems such as dopaminergic, serotonergic and glutamatergic, as well as the activity of ion channels, signaling pathways and expression of certain genes, all processes involved in the actions of drugs of which it has been used. abusive (Matsumoto, Expert Rev Clin Pharmacol. 2009 Jul;2(4):351-8.).

[0014] Drug addiction is one of the most serious health problems in the world, which impacts society on multiple levels. Drug abuse is responsible for significant medical, economic and social health costs. The effectiveness in some cases of current treatments, or even the absence of treatments, also aggravates the problem. All together supports the need for deeper understanding of the neurobiological effects of drugs of abuse and mechanisms of addiction in order to discover new therapeutic targets for the development of alternative treatments.

[0015] Additionally, there is still a need to find compounds having pharmacological activity for the sigma receptor, being effective, selective, and/or having good "toxic dependence" properties, that is, good pharmaceutical properties related to administration, distribution, metabolism and excretion.

[0016] Surprisingly, it was observed that the new oxadiazaspiro compounds with general formula (I) show an affinity for the ai receptor ranging from good to excellent. These compounds are therefore particularly suitable as pharmacologically active agents in medicines for the prophylaxis and/or treatment of disorders or diseases related to sigma receptors, in particular against drug abuse and addiction.

SUMMARY OF THE INVENTION

[0017] The present invention describes new compounds with high affinity for sigma receptors and having high solubility in a physiological medium that can be used for the treatment of sigma-related disorders and diseases, in particular against drug use and addiction.

[0018] As this invention is directed to providing a compound or series of chemically related compounds that act as ai receptor ligands, it is a very preferred embodiment that the compound has a bond expressed as Ki which is preferably < i000 nM, more preferably < 500 nM, even more preferably < 100 nM.

[0019] The invention is directed in a main aspect to a compound of general formula (I),

[0020] wherein R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', X, Y, m, n and p are as defined below in the detailed description.

[0021] Another object of the invention relates to processes for preparing compounds of general formula (I).

[0022] Yet another object of the invention relates to the use of intermediate compounds for the preparation of a compound of general formula (I).

[0023] A pharmaceutical composition comprising a compound of formula (I) is also an object of the invention.

[0024] Finally, it is an object of the invention to use the compound as a medicine and more particularly for the treatment of pain and pain-related conditions.

DETAILED DESCRIPTION OF THE INVENTION

[0025] The present invention describes new compounds with affinity for sigma receptors and having high solubility in a physiological medium that can be used for the treatment of sigma-related disorders or diseases.

[0026] As this invention is directed to providing a compound or series of chemically related compounds that act as ligands for the receptor, it is a most preferred embodiment that the compound has a bond expressed as Ki which is preferably < i000 nM, more preferably < 500 nM, even more preferably < 100 nM.

[0027] Advantageously, the compounds according to the present invention in addition show one or more of the following functionalities: ai receptor antagonism. It should be noted, however, that the functionalities "antagonism" and "agonism" are also subdivided in their effects into subfunctionalities such as partial agonism or inverse agonism. Consequently, the functionalities of the compound must be considered within a relatively wide range.

[0028] An antagonist blocks or decreases agonist-mediated responses. Known subfunctionalities are neutral antagonists or inverse agonists.

[0029] An agonist increases receptor activity above its basal level. Known subfunctionalities are full agonists, or partial agonists.

[0030] The invention is directed in a main aspect to a compound of general formula (I).

[0031] In a particular aspect, the present invention is directed to compounds of general formula (I):

[0032] in which

[0033] p is 0 or 1 or 2; preferably p is 0 or 1;

[0034] m is 1, 2 or 3;

[0035] n is 0, 1 or 2;

[0036] Y is -CH2- or -C(O)-;

[0037] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[0038] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[0039] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0040] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0041] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[0042] wherein said cycloalkyl in R1 if substituted, is substituted with one or more selected halogen substituents, - R11, -OR11, -NO2, -NR11R11''', NR11C(O)R11', -NR11S(O )2R11', - S(O)2NR11R11', -NR11C(O)NR11'R11'', -SR11 , -S(O)R11, S(O)2R11, -CN, haloalkyl, haloalkoxy, -C(O )OR11, -C(O)NR11R11', -OCH2CH2OH, - NR11S(O)2NR11'R11'' and C(CH3)2OR11;

[0043] additionally, cycloalkyl in R1, if substituted, can also be substituted with or =O;

[0044] wherein the alkyl, alkenyl or alkynyl in R1, if substituted, is replaced with one or more substituents selected from -OR11, halogen, -CN, haloalkyl, haloalkoxy and -NR11R11''';

[0045] wherein R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[0046] and in which R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[0047] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[0048] wherein said cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituents selected from halogen, -R12, -OR12, -NO2, -NR12R12''', NR12C(O)R12' , -NR12S(O)2R12', -S(O)2NR12R12', -NR12C(O)NR12'R12'', -SR12, -S(O)R12, S(O)2R12, -CN, haloalkyl, haloalkoxy , -C(O)OR12, -C(O)NR12R12', -OCH2CH2OH, - NR12S(O)2NR12'R12'' and C(CH3)2OR12;

[0049] additionally, non-aromatic cycloalkyl or heterocyclyl in R2, if substituted, can also be substituted with or =O;

[0050] wherein the alkyl, alkenyl or alkynyl in R2, if substituted, is replaced with one or more substituents selected from -OR12, halogen, -CN, haloalkyl, haloalkoxy and -NR12R12''';

[0051] wherein R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[0052] and in which R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[0053] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0054] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[0055] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[0056] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[0057] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[0058] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0059] alternatively, R5 and R5' taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[0060] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, - CHOR10 and -C(O )OR10;

[0061] wherein R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0062] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof;

[0063] In a particular aspect, the present invention is directed to compounds of general formula (I):

[0064] in which:

[0065] p is 0 or 1;

[0066] m is 1, 2 or 3;

[0067] n is 0, 1 or 2;

[0068] Y is -CH2- or -C(O)-;

[0069] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[0070] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[0071] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0072] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0073] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[0074] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced;

[0075] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0076] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[0077] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[0078] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[0079] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[0080] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0081] alternatively, R5 and R5' taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[0082] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, - CHOR10 and -C(O )OR10;

[0083] wherein R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[0084] These compounds according to the invention are optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any ratio mixture, or a corresponding salt thereof, or a corresponding solvate thereof.

[0085] In another embodiment, these compounds according to the invention are optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers , in any mixing ratio, or a corresponding salt thereof.

[0086] In another modality the following condition applies:

[0087] when Y is -C(O)- and R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl, then m is 1, X is a bond, n is 0 and R3 is not hydrogen.

[0088] In another modality the following condition applies:

[0089] when Y is -C(O)- and R2 is substituted or unsubstituted monocyclic aryl or substituted or unsubstituted monocyclic heterocyclyl, then m is 1, X is a bond, n is 0 and R3 is not hydrogen.

[0090] In another modality the following condition applies:

[0091] when Y is -C(O)- and R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl, then m is 1, X is a bond and n is 0.

[0092] In another modality the following condition applies:

[0093] when Y is -C(O)- and R2 is substituted or unsubstituted monocyclic aryl or substituted or unsubstituted monocyclic heterocyclyl, then m is 1, X is a bond and n is 0.

[0094] In another modality the following condition applies:

[0095] when Y is -C(O)- and R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl, then -[CR5R5']m-X- [CR6R6']n- is neither -CH2CH2- nor -CH2CH (OH)- , and R3 is not hydrogen.

[0096] For the sake of clarity regarding -CH2CH(OH)-, this means that when Y is -C(O)- and R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl, then - [CR5R5' ]m-X-[CR6R6']n- cannot be -CH2CH(OH)- read in the "N" direction from the spiro part of the nucleus to R2.

[0097] In another embodiment, the following compound is also excluded:

[0098] In another embodiment, the following compound is excluded:

[0099] In another embodiment, both of the following compounds are also excluded:

[00100] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I')

[00101] in which, R1, R2, R3, R3', R4, R4', R5, R5', X, Y, m and p are as defined in the description.

[00102] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (Ia')

[00103] in which, R1, R2, R3, R3', R4, R4', R5, R5', X, Y, m and p are as defined in the description.

[00104] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (Ib')

[00105] in which, Ri, R2, R4, R4', R5, R5', X, Y, m and p are as defined in the description.

[00106] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (Ic')

[00107] in which, R1, R2, R4, R4', R5, R5', X, Y, m and p are as defined in the description.

[00108] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I2')

[00109] wherein R1, R2, R4, R4', R5, R5', X,Y, m and p are as defined in the description.

[00110] In another embodiment, for compounds of general formula (I) they are compounds of general formula (I3')

[00111] in which R1, R2, R4, R4', R5, R5', X, m and p are as defined in the description.

[00112] In another embodiment, for compounds of general formula (I) they are compounds of general formula (I4')

[00113] in which R1, R2, m and p are as defined in the description.

[00114] In another embodiment, for compounds of general formula (I) they are compounds of general formula (I5')

[00115] in which R1, R2, and m are as defined in the description.

[00116] In another embodiment, the compound according to the invention of general formula (I) is a compound of general formula (I6')

[00117] in which, R1, R2, R3, R3', R5, R5', X, Y, and m are as defined in the description.

[00118] For the purposes of clarity, reference is also made to the following statements below in the definitions of alkyl substitutions etc. or arila etc. that "wherein when different radicals R1 to R14'''' and Rx, Rx' are present simultaneously in formula I they may be identical or different". This statement is reflected in the general formula below (I7') being derived from and included in the general formula (I).

[00119] wherein R1, R2, R3, R3', R4, R4', R5, R5', X, Y and p are as defined in the description. Additionally, m' (being 0 or 1), R5'' and R5''' are added. As stated above, this statement is thus reflected in the fact that R5'' and R5''' are or may be different from R5 and R5' or not and - consequently - m' being 0 or 1 is naturally resulting from m ( in general formulas (I) to (I6') being 1 or 2).

[00120] The same would apply mutatis mutandis to general formulas such as general formula (I) as well as the other general formulas (I') to (I6') above, as well as to all synthetic intermediates.

[00121] For the purposes of clarity, all groups and definitions described in the description and referring to compounds of general formula (I), also apply to compounds of general formula (I'), (Ia'), (Ib '), (Ic'), (I2'), (I3'), (I4'), (I5'), or (I6') and also (I7'), as well as all synthesis intermediates, when those groups are present in the general Markush formulas, since compounds with the general formula (I'), (Ia'), (Ib'), (Ic'), (I2'), (I3'), (I4'), (I5'), (I6') or (I7') are included in the general formula (I).

[00122] For the purposes of clarity, the general formula Markush (I)

[00123] is equivalent to

[00124] wherein only -C(R4R4')-, -C(R5R5')- and -C(R6R6')- are included in the parentheses and p, m and n mean the number of times -C(R4R4')-, -C(R5R5')- and -C(R6R6')- are repeated, respectively. The same would apply to the general Markush formulas (I'), (Ia'), (Ib'), (Ic'), (I2'), (I3'), (I4'), (I5') or (I6 ') as well as all synthetic intermediates.

[00125] In this way, the general formula (I') can also be expressed as the general formula (IZ') etc.:

[00126] In addition, and for the purposes of clarity, it should also be understood that naturally if p, m or n are 0, then R1, X or R2 are still present in the general formulas Markush (I'), (Ia') , (Ib'), (Ic'), (I2'), (I3'), (I4'), (I5') or (I6') as well as in all synthesis intermediates.

[00127] In the context of this invention, alkyl is understood to mean saturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It covers, for example, -CH3 and -CH2-CH3. In these radicals, C1-2-alkyl represents C1- or C2-alkyl, C1-3-alkyl represents C1-, C2- or C3-alkyl, C1-4-alkyl represents C1-, C2-, C3- or C4-alkyl , C1-5-alkyl represents C1-, C2-, C3-, C4-, or C5-alkyl, C1-6-alkyl represents C1-, C2-, C3-, C4-, C5- or C6-alkyl, C1 -7-alkyl represents C1-, C2-, C3-, C4-, C5-, C6- or C7-alkyl, C1-8-alkyl represents C1-, C2-, C3-, C4-, C5-, C6- , C7- or C8-alkyl, C1-10-alkyl represents C1, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9- or C10-alkyl and C1-18-alkyl represents C1-, C2-, C3-, C4-, C5-, C6-, C7-, C8-, C9-, C10-, C11-, C12, C13-, C14-, C15-, C16-, C17- or C18-alkyl. the alkyl radicals are preferably methyl, ethyl, propyl, methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl , 1-methylpentyl, if also substituted CHF2, CF3 or CH2OH etc. Preferably alkyl is understood in the context of this invention as C1-8 alkyl such as methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, or octyl; preferably it is C1-6 alkyl such as methyl, ethyl, propyl, butyl, pentyl, or hexyl; more preferably it is C1-4 alkyl such as methyl, ethyl, propyl or butyl.

[00128] Alkenyl is understood to mean unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It covers groups such as -CH=CH-CH3. The alkenyl radicals are preferably vinyl (ethenyl), allyl (2-propenyl). Preferably in the context of this invention alkenyl is C2-10-alkenyl or C2-8-alkenyl such as ethylene, propylene, butylene, pentylene, hexylene, heptylene or octylene; or is C2-6-alkenyl such as ethylene, propylene, butylene, pentylene, or hexylene; or is C2-4-alkenyl, such as ethylene, propylene, or butylenes.

[00129] Alkynyl is understood to mean unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It covers groups such as, for example, -C=C-CH3 (1-propynyl). Preferably alkynyl in the context of this invention is C2-10-alkynyl or C2-8-alkynyl such as ethyne, propyne, butyene, pentyne, hexin, heptin, or octine; or is C2-6-alkynyl such as ethyne, propyne, butyene, pentyne, or hexin; or is C2-4-alkynyl such as ethyne, propyne, butyene, pentyne, or hexin.

[00130] With respect to alkyl (also in alkylaryl, alkyl-heterocyclyl or alkylcycloalkyl), alkenyl, alkynyl and O-alkyl - unless otherwise defined - the term substituted in the context of this invention is understood to mean the replacement of by least one hydrogen radical on a carbon atom per halogen (F, Cl, Br, I), -NRcRc''', -SRc, -S(O)Rc, -S(O)2Rc, -ORc, -C( O)ORc, -CN, - C(O)NRcRc', haloalkyl, haloalkoxy or -OC1-6 alkyl, with Rc represented by R11, R12, R13, (with Rc' represented by R11', R12', R13'; with Rc'' being represented by R11'', R12'', R13''; with Rc''' being represented by R11''', R12''', R13''', with Rc'''' being represented by R11'. ''', R12'''', R13'''') wherein R1 to R14'''' and Rx, Rx' and Rn are as defined in the description, and wherein when different radicals R1 to R14''' ' and Rx, Rx' and Rn are present simultaneously in formula I and they can be identical or different.

[00131] More preferably with respect to alkyl (also in alkylaryl, alkyl heterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl, substituted, it is understood in the context of this invention that any alkyl (also in alkylaryl, alkyl heterocyclyl or alkylcycloalkyl) , alkenyl, alkynyl or O-alkyl that is substituted is substituted with one or more halogen (F, Cl, Br, I), -ORc, -CN, -NRcRc''', haloalkyl, haloalkoxy or -OC1-6alkyl, with Rc represented by R11, R12, R13, (with Rc' represented by R11', R12', R13'; with Rc'' represented by R11'', R12'', R13''; with Rc''' represented by R11''', R12''', R13''', with Rc'''' represented by R11'''', R12'''', R13''''), where R1 to R14''' ' and Rx, Rx'and Rn are as defined in the description, and wherein when different radicals R1 to R14'''' and Rx, Rx' and Rn are present simultaneously in formula I, they may be identical or different.

[00132] More than one substitution in the same molecule and also on the same carbon atom is possible with the same or different substituents. This includes, for example, 3 hydrogens being substituted on the same C atom, as in the case of CF3, or in different locations on the same molecule, as in the case of, for example, -CH(OH)-CH=CH- CHCl2.

[00133] In the context of this invention, haloalkyl is understood to mean an alkyl being replaced once or several times by a halogen (selected from F, Cl, Br, I). It encompasses, for example, -CH2Cl, -CH2F, -CHCl2, -CHF2, -CCl3, -CF3 and -CH2-CHCl2. Preferably haloalkyl is understood in the context of this invention as halogen-substituted C1-4 alkyl representing C1-, C2-, C3- or halogen-substituted C4-alkyl. The halogen-substituted alkyl radicals are therefore preferably methyl, ethyl, propyl, and butyl. Preferred examples include -CH2Cl, -CH2F, -CHCl2, -CHF2, and -CF3.

[00134] In the context of this invention, haloalkoxy is understood to mean an -O-alkyl being replaced once or several times by a halogen (selected from F, Cl, Br, I). It encompasses, for example, -OCH2Cl, -OCH2F, -OCHCl2, -OCHF2, -OCCl3, -OCF3 and - OCH2-CHCI2. Preferably haloalkyl is understood in the context of this invention as -OC1-4-alkyl substituted by halogen, representing C1-, C2-, C3- or C4-alkoxy substituted by halogen. The halogen-substituted alkyl radicals are therefore preferably O-methyl, O-ethyl, O-propyl, and O-butyl. Preferred examples include -OCH2Cl, -OCH2F, -OCHCl2, -OCHF2, and -OCF3.

[00135] In the context of this invention, cycloalkyl is understood to mean saturated and unsaturated (but non-aromatic) cyclic hydrocarbons (without a heteroatom in the ring), which can be unsubstituted once or substituted several times. Furthermore, C3-4 cycloalkyl represents C3- or C4-cycloalkyl, C3-5 cycloalkyl represents C3-, C4- or C5-cycloalkyl, C3-6 cycloalkyl represents C3-, C4-, C5- or C6-cycloalkyl, C3- 7 cycloalkyl represents C3-, C4-, C5-, C6- or C7-cycloalkyl, C3-8-cycloalkyl represents C3-, C4-, C5-, C6-, C7- or C8-cycloalkyl, C4-5-cycloalkyl represents C4- or C5-cycloalkyl, C4-6-cycloalkyl represents C4-, C5- or C6-cycloalkyl, C4-7-cycloalkyl represents C4-, C5-, C6- or C7-cycloalkyl, C5-6-cycloalkyl represents C5- or C6-cycloalkyl and C5-7-cycloalkyl represents C5-, C6- or C7-cycloalkyl. Examples are cyclopropyl, 2-methylcyclopropyl, cyclopropylmethyl, cyclobutyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cycloheptyl, cyclooctyl, and also adamantly. Preferably in the context of this invention cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; or is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or is C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, especially cyclopentyl or cyclohexyl.

[00136] Aryl is understood to mean mono- or polycyclic ring systems of 5 to 18 members with at least one aromatic ring, however, without heteroatoms even in just one of the rings. Examples are phenyl, naphthyl, fluoranthenyl, fluorenyl, tetralinyl or indanyl, 9H-fluorenyl or anthracenyl radicals, which may be unsubstituted or once or several times substituted. More preferably aryl is understood in the context of this invention as phenyl, naphthyl or anthracenyl, preferably it is phenyl.

[00137] A heterocyclyl group or radical (also called heterocyclyl hereinafter) is understood to mean 5- to 18-membered heterocyclic, mono- or polycyclic ring systems, such as at least one saturated or unsaturated ring that contains one or more heteroatoms of the group consisting in nitrogen, oxygen and/or sulfur in the ring. A heterocyclic group can also be substituted once or several times.

[00138] Examples include non-aromatic heterocyclyls, such as tetrahydropyran, oxazepane, morpholine, piperidine, pyrrolidine, as well as heteroaryls, such as furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazole, benzothiazole, indole, benzotriazole, carbazole and quinazoline.

[00139] Subgroups within heterocyclyls as understood herein include heteroaryls and non-aromatic heterocyclyls.

[00140] - heteroaryl (being equivalent to heteroaromatic radicals or aromatic heterocyclyls) is a heterocyclic, mono or polycyclic 5 to 18 membered, aromatic ring system of one or more rings of which at least one aromatic ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a 5- to 18-membered heterocyclic, mono- or polycyclic, aromatic ring system of one or two rings of which at least one aromatic ring contains one or more heteroatoms of the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, quinazoline, thiazole, imidazole, pyrazole, oxazole, thiophene and benzimidazole;

[00141] - non-aromatic heterocyclyl is a 5- to 18-membered mono- or polycyclic heterocyclic ring system of one or more rings of which at least one ring - with this ring(s) then being non-aromatic ) - contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a 5- to 18-membered mono- or polycyclic heterocyclic ring system of one or two rings of which one or both rings - with this one or two rings then being non-aromatic - contains/contains one or more heteroatoms of the group consisting in nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from oxazepam, pyrrolidine, piperidine, piperazine, tetrahydropyran, morpholine, indoline, oxopyrrolidine, benzodioxane, oxetane, especially benzodioxane, morpholine, tetrahydropyran, piperidine, oxopyrrolidine, oxetane and pyrrolidine.

[00142] Preferably, in the context of this invention, heterocyclyl is defined as a 5- to 18-membered mono- or polycyclic heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms of the group consisting in nitrogen, oxygen and/or sulfur in the ring. Preferably, it is a 5- to 18-membered mono- or polycyclic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring.

[00143] Preferred examples of heterocyclyls include oxetane, oxazepane, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole, oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline, especially are pyridine, pyrazine, indazole, benzodioxane, thiazole, benzothiazole, morpholine, tetrahydropyran, pyrazole, imidazole, piperidine, thiophene, indole, benzimidazole, pyrrolo[2,3b]pyridine, benzoxazole, oxopyrrolidine, pyrimidine, oxazepane, oxetane and pyrrolidine.

[00144] In the context of this invention, oxopyrrolidine is understood to mean pyrrolidin-2-one.

[00145] With respect to aromatic heterocyclyls (heteroaryls), non-aromatic heterocyclyls, aryls and cycloalkyls, when a ring system falls into two or more of the above-mentioned cycle definitions simultaneously, then the ring system is first defined as a aromatic heterocyclyl (heteroaryl) if at least one aromatic ring contains a heteroatom. If the aromatic ring contains a heteroatom, then the ring system is defined as a non-aromatic heterocyclyl if at least one non-aromatic ring contains a heteroatom. If no non-aromatic ring contains a heteroatom, then the ring system is defined as an aryl if it contains at least one aryl cycle. If no aryl is present, then the ring system is defined as a cycloalkyl if at least one non-aromatic cyclic hydrocarbon is present.

[00146] In the context of this invention, alkylaryl is understood to mean an aryl group (see above) being connected to another atom through a C1-6-alkyl (see above) that can be branched or linear and is unsubstituted or substituted a once or several times. Preferably, alkylaryl is understood to mean an aryl group (see above) being connected to another atom through 1 to 4 groups (-CH2-). More preferably, alkylaryl is benzyl (i.e., -CH2- phenyl).

[00147] In the context of this invention, alkyl heterocyclyl is understood to mean a heterocyclyl group being connected to another atom through a C1-6 alkyl (see above) that can be branched or linear and is unsubstituted or substituted once or several times. times. Preferably, alkyl heterocyclyl is understood to mean a heterocyclyl group (see above) being connected to another atom through 1 to 4 groups (-CH2-). More preferably, alkyl heterocyclyl is -CH2- pyridine.

[00148] In the context of this invention, alkylcycloalkyl is understood to mean a cycloalkyl group being connected to another atom through a C1-6-alkyl (see above) that may be branched or linear and is unsubstituted or substituted once or multiple times . Preferably, alkylcycloalkyl is understood to mean a cycloalkyl group (see above) being connected to another atom through 1 to 4 groups (-CH2-). More preferably, alkylcycloalkyl is -CH2- cyclopropyl.

[00149] Preferably, the aryl is a monocyclic aryl. More preferably, the aryl is a 5-, 6- or 7-membered monocyclic aryl. Even more preferably, the aryl is a 5- or 6-membered monocyclic aryl.

[00150] Preferably, the heteroaryl is a monocyclic heteroaryl. More preferably, the heteroaryl is a 5-, 6- or 7-membered monocyclic heteroaryl. Even more preferably, the heteroaryl is a 5- or 6-membered monocyclic heteroaryl.

[00151] Preferably, the non-aromatic heterocyclyl is a non-aromatic, monocyclic heterocyclyl. More preferably, the non-aromatic heterocyclyl is a 4-, 5-, 6- or 7-membered monocyclic non-aromatic heterocyclyl. Even more preferably, the non-aromatic heterocyclyl is a non-aromatic, 5- or 6-membered monocyclic heterocyclyl.

[00152] Preferably, the cycloalkyl is a monocyclic cycloalkyl. More preferably, the cycloalkyl is a 3-, 4-, 5-, 6-, 7- or 8-membered monocyclic cycloalkyl. Even more preferably, the cycloalkyl is a 3-, 4-, 5- or 6-membered monocyclic cycloalkyl.

[00153] With respect to aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), substituted is understood - unless otherwise defined - to mean replacement of the ring system aryl or alkyl-aryl, cycloalkyl or alkyl-cycloalkyl; heterocyclyl or alkyl heterocyclyl with one or more halogen (F, Cl, Br, I), -Rc, -ORc, -CN, -NO2, -NRcRc''', -C(O)ORc, NRcC(O) Rc' , -C(O)NRcRc' , -NRcS(O)2Rc' , =O, -OCH2CH2OH, -NRcC(O)NRc'Rc'', -S(O)2NRcRc', -NRcS(O)2NRc 'Rc'', haloalkyl, haloalkoxy, -SRc, -S(O)Rc, -S(O)2Rc or C(CH3)ORc; NRcRc''', with Rc, Rc', Rc'' and Rc''' independently being H or a saturated or unsaturated, linear or branched, substituted or unsubstituted C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted -O-C1-6-alkyl (alkoxy); a saturated or unsaturated, linear or branched, substituted or unsubstituted -S-C1-6-alkyl; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(O)-C1-6-alkyl group; a saturated or unsaturated, linear or branched, substituted or unsubstituted -C(O)-O-C1-6-alkyl group; a substituted or unsubstituted aryl or alkyl aryl; a substituted or unsubstituted cycloalkyl or alkyl cycloalkyl; a substituted or unsubstituted heterocyclyl or alkylheterocyclyl, Rc being one of R11, R12 or R14, (Rc' being one of R11', R12' or R14'; Rc'' being one of R11'', R12'' or R14'''; Rc''' being one of R11'''', R12''' or R14'''; '), wherein R1 to R14'''' and Rx, Rx' and Rn are as defined in the description, and wherein when different radicals R1 to R14'''' and Rx, Rx' and Rn are present simultaneously in the formula I they can be identical or different.

[00154] More preferably, with respect to substituted aryl (including alkyl-aryl), cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), it is understood in the context of this invention that any aryl, cycloalkyl and heterocyclyl that is substituted is substituted (also in an allylaryl, alkylcycloalkyl or alkylheterocyclyl) with one or more halogen (F, Cl, Br, I), -Rc, -ORc, -CN, -NO2, -NRcRc''', NRcC (O)Rc', -NRcS(O)2Rc' , =O, haloalkyl, haloalkoxy, or C(CH3)ORc; -OC1-4alkyl being unsubstituted or substituted with one or more of ORc or halogen (F, Cl, I, Br), -CN, or -C1-4 alkyl being unsubstituted or substituted with one or more of ORc or halogen ( F, Cl, I, Br), Rc being one of R11, R12 or R14, (Rc' being one of R11', R12' or R14'; Rc'' being one of R11'', R12'' or R14' '; Rc''' being one of R11''', R12'''' or R14'''; Rc'''' being one of R11'''', R12'''' or R14'''') , wherein R1 to R14'''' and Rx, Rx' and Rn are as defined in the description, and wherein when different radicals R1 to R14'''' and Rx, Rx' and Rn are present simultaneously in formula I they they can be identical or different.

[00155] In addition to the above-mentioned substitutions, with respect to cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), namely, non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl), substituted is also understood - the unless otherwise defined - as meaning replacement of the ring system of a cycloalkyl or alkyl-cycloalkyl; non-aromatic heterocyclyl or non-aromatic alkyl heterocyclyl with or =O.

[00156] With respect to cycloalkyl (including alkyl-cycloalkyl), or heterocyclyl (including alkyl-heterocyclyl), namely, non-aromatic heterocyclyl (including non-aromatic alkyl-heterocyclyl), substituted is also understood - unless otherwise defined - as meaning replacement of the ring system of a cycloalkyl or alkyl-cycloalkyl; non-aromatic heterocyclyl or non-aromatic alkyl heterocyclyl with (leading to a spiro structure) or with =O.

[00157] A ring system is a system consisting of at least one ring of connected atoms, however, also including systems in which two or more connected rings of atoms are joined with "joined" meaning that the respective rings are sharing a (like a spiro structure), two or more atoms being a member or members of both joined rings.

[00158] The term "leaving group" means a molecular fragment that leaves with a pair of electrons in heterolytic bond cleavage. Leaving groups can be neutral molecules or anions. Common anionic leaving groups are halides, such as Cl-, Br-, and I-, and sulfonate esters, such as tosylate (TsO-) or mesylate.

[00159] The term "salt" should be understood to mean any form of the active compound used according to the invention in which it assumes an ionic form or is charged and is coupled with a counterion (a cation or anion) or is in solution . Therefore, complexes of the active compound with other molecules and ions, in particular complexes through ionic interactions, must also be understood.

[00160] The term "physiologically acceptable salt" means, in the context of this invention, any salt that is physiologically tolerated (most often meaning not being especially toxic because of the counterion) if used appropriately for a treatment, especially if used or applied to humans and/or mammals.

[00161] These physiologically acceptable salts can be formed with cations or bases and in the context of this invention are understood to mean salts of at least one of the compounds used according to the invention - usually a (deprotonated) acid - as an anion with at least a preferably inorganic cation that is physiologically tolerated - especially if used in humans and/or mammals. Salts of alkali metals and alkaline earth metals are particularly preferred, and also those with NH4, but in particular salts of (mono)- or (di)sodium, (mono)- or (di)potassium, magnesium or calcium.

[00162] Physiologically acceptable salts can also be formed with anions or acids and in the context of this invention are understood to mean salts of at least one of the compounds used according to the invention as the cation with at least one anion that are physiologically tolerated - especially if used in humans and/or mammals. By this is meant in particular, in the context of this invention, the salt formed with a physiologically tolerated acid, that is to say salts of the particular active compound with inorganic or organic acids that are physiologically tolerated - especially if used in humans and/or mammals. Examples of physiologically tolerated salts of particular acids are salts of: hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid or citric acid.

[00163] The compounds of the invention can be present in crystalline form or in the form of free compounds such as a free acid or base.

[00164] Any compound that is a solvate of a compound according to the invention like a compound according to general formula I defined above is understood to also be covered by the scope of the invention. Solvation methods are generally known in the art. Suitable solvates are pharmaceutically acceptable solvates. The term "solvate" according to this invention is to be understood as meaning any form of the active compound according to the invention in which this compound has bonded via non-covalent bonding to another molecule (most likely a polar solvent). Especially, preferred examples include hydrates and alcoholates, such as methanolates or ethanolates.

[00165] Any compound that is a prodrug of a compound according to the invention like a compound according to general formula I defined above is understood to also be covered by the scope of the invention. The term "prodrug" is used in its broadest sense and encompasses those derivatives that are converted in vivo to the compounds of the invention. Such derivatives would readily occur to those skilled in the art, and include, depending on the functional groups present in the molecule and without limitation, the following derivatives of the present compounds: esters, amino acid esters, phosphate esters, sulfonate esters of metal salts, carbamates , and amides. Examples of well-known methods of producing a prodrug of a given active compound are known to those skilled in the art and can be found, for example, in Krogsgaard-Larsen et al. "Textbook of Drug Design and Discovery" Taylor & Francis (April 2002).

[00166] Any compound that is an N-oxide of a compound according to the invention like a compound according to general formula I defined above is understood to also be covered by the scope of the invention.

[00167] Unless otherwise stated, the compounds of the invention are also intended to include compounds that differ only in the presence of one or more isotopically enriched atoms. For example, compounds having the present structures except for the substitution of a hydrogen for a deuterium or tritium, or the substitution of a carbon for a carbon enriched in 13C or 14C or of a nitrogen for a nitrogen enriched for 15N are within the scope of this invention. . This especially would also apply to the caveats outlined above, so that any mention of hydrogen or any "H" in a formula would also cover deuterium or tritium.

[00168] The compounds of formula (I), as well as their salts or solvates of the compounds, are preferably in pharmaceutically acceptable or substantially pure form. By pharmaceutically acceptable form is intended, inter alia, to have a pharmaceutically acceptable level of purity excluding normal pharmaceutical additives, such as diluents and carriers, and not including any material considered toxic at normal dosage levels. Purity levels for the drug substance are preferably above 50%, more preferably above 70%, most preferably above 90%. In a preferred embodiment they are above 95% of the compound of formula (I), or its salts. This also applies to their solvates or prodrugs.

[00169] In another embodiment, the compound according to the invention of general formula (I)

[00170] is a compound in which:

[00171] p is 0 or 1;

[00172] m is 1, 2 or 3;

[00173] n is 0, 1 or 2;

[00174] Y is -CH2- or -C(O)-;

[00175] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00176] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00177] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00178] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00179] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00180] wherein said cycloalkyl in R1 if substituted, is substituted with one or more selected halogen substituents, - R11, -OR11, -NO2, -NR11R11''', NR11C(O)R11', -NR11S(O )2R11', - S(O)2NR11R11', -NR11C(O)NR11'R11'', -SR11 , -S(O)R11, S(O)2R11, -CN, haloalkyl, haloalkoxy, -C(O )OR11, -C(O)NR11R11', -OCH2CH2OH, - NR11S(O)2NR11'R11'' and C(CH3)2OR11;

[00181] additionally, cycloalkyl in R1, if substituted, can also be substituted with or =O;

[00182] wherein the alkyl, alkenyl or alkynyl in R1, if substituted, is replaced with one or more substituents selected from -OR11, halogen, -CN, haloalkyl, haloalkoxy and -NR11R11''';

[00183] wherein R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00184] and in which R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00185] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00186] wherein said cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituents selected from halogen, -R12, -OR12, -NO2, -NR12R12''', NR12C(O)R12' , -NR12S(O)2R12', -S(O)2NR12R12', -NR12C(O)NR12'R12'', -SR12, -S(O)R12, S(O)2R12, -CN, haloalkyl, haloalkoxy , -C(O)OR12, -C(O)NR12R12', -OCH2CH2OH, - NR12S(O)2NR12'R12'' and C(CH3)2OR12;

[00187] additionally, non-aromatic cycloalkyl or heterocyclyl in R2, if substituted, can also be substituted with or =O;

[00188] wherein the alkyl, alkenyl or alkynyl in R2, if substituted, is substituted with one or more substituents selected from -OR12, halogen, -CN, haloalkyl, haloalkoxy and -NR12R12''';

[00189] wherein R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00190] and in which R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00191] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00192] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[00193] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00194] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00195] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00196] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00197] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00198] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, - CHOR10 and -C(O )OR10;

[00199] wherein R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00200] the alkyl, alkenyl or alkynyl, other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from -OR13, halogen, -CN, haloalkyl, haloalkoxy and - NR13R13''';

[00201] wherein R13 is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, and C2-6 unsubstituted alkynyl;

[00202] R13''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00203] aryl, heterocyclyl or cycloalkyl other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from halogen, -R14, -OR14, -NO2, -NR14R14''', NR14C(O )R14', -NR14S(O)2R14', -S(O)2NR14R14', - NR14C(O)NR14'R14'', -SR14 , -S(O)R14, S(O)2R14, -CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14', - OCH2CH2OH, -NR14S(O)2NR14'R14'' and C(CH3)2OR14;

[00204] additionally, where non-aromatic cycloalkyl or heterocyclyl, other than those defined in R1 or R2, if substituted, can also be substituted with or =O;

[00205] wherein R14, R14' and R14'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl replaced;

[00206] and wherein R14''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00207] These preferred compounds, according to the invention are optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.

[00208] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00209] m is 1, 2 or 3;

[00210] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00211] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00212] n is 0, 1 or 2;

[00213] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00214] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00215] p is 0 or 1;

[00216] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00217] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00218] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00219] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00220] In another preferred embodiment, the compound according to the invention of general formula (I) is a compound in which

[00221] X is a link;

[00222] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00223] In another preferred embodiment, the compound according to the invention of general formula (I) is a compound in which

[00224] X is -C(RxRx')-;

[00225] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00226] In another preferred embodiment, the compound according to the invention of general formula (I) is a compound in which

[00227] X is -O-;

[00228] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00229] In another preferred embodiment, the compound according to the invention of general formula (I) is a compound in which

[00230] X is -C(O)-;

[00231] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00232] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00233] Y is -CH2- or -C(O)-;

[00234] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00235] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00236] Y is -CH2-;

[00237] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00238] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00239] Y is -C(O)-;

[00240] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00241] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00242] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00243] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00244] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00245] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00246] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00247] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00248] R1 is substituted or unsubstituted C1-6 alkyl;

[00249] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00250] In another embodiment, the compound according to the invention of general formula (I) is a compound in which:

[00251] R1 is selected from C1-6 substituted or unsubstituted alkyl and substituted or unsubstituted cycloalkyl;

[00252] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00253] In another embodiment, the compound according to the invention of general formula (I) is a compound in which

[00254] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00255] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00256] In another embodiment, the compound according to the invention of general formula (I) is a compound in which:

[00257] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl,

[00258] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00259] In another embodiment, the compound according to the invention of general formula (I) is a compound in which:

[00260] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl,

[00261] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00262] In another embodiment, the compound according to the invention of general formula (I) is a compound in which:

[00263] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl,

[00264] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00265] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00266] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00267] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00268] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00269] R3 and R3' are independently selected from substituted or unsubstituted hydrogen and C1-6 alkyl;

[00270] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00271] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00272] R3 and R3', taken together with the C atom in connection, form a substituted or unsubstituted cycloalkyl;

[00273] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00274] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00275] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00276] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00277] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00278] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00279] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00280] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00281] R4 and R4' are independently selected from substituted or unsubstituted hydrogen and C1-9 alkyl;

[00282] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00283] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00284] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00285] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00286] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00287] R5 and R5' taken together with the C atom in connection, form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00288] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00289] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00290] R5 and R5' taken together with the C atom in connection, form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl, m is 1, X is a bond, n is 0 and R2 is hydrogen ;

[00291] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00292] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00293] R5 and R5' taken together with the C atom in connection, form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted saturated heterocyclyl, m is 1, X is a bond, n is 0 and R2 is hydrogen;

[00294] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00295] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00296] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, - CHOR10 and -C(O )OR10;

[00297] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00298] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00299] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00300] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00301] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00302] R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00303] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00304] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00305] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00306] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00307] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00308] R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00309] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00310] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00311] R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00312] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00313] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00314] R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00315] and wherein R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00316] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00317] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00318] R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00319] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00320] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00321] R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00322] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00323] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00324] R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00325] and wherein R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00326] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00327] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00328] R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00329] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00330] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00331] R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00332] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00333] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00334] R13 is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, and C2-6 unsubstituted alkynyl;

[00335] R13''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00336] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00337] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00338] R13 is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, and C2-6 unsubstituted alkynyl;

[00339] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00340] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00341] R13''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00342] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00343] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00344] R14, R14' and R14'' are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

[00345] and wherein R14''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00346] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00347] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00348] R14, R14' and R14'' are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

[00349] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00350] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00351] R14''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00352] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00353] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00354] Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00355] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00356] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00357] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00358] Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00359] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00360] In another preferred embodiment of the compound according to the invention of general formula (I) is a compound in which

[00361] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00362] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00363] In another preferred embodiment of the compound according to the invention of general formula (I), it is a compound in which

[00364] p is 0 or 1;

[00365] m is 1, 2 or 3;

[00366] n is 0, 1 or 2;

[00367] Y is -CH2- or -C(O)-;

[00368] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00369] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00370] in which

[00371] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably the C1-6 alkyl is methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl or neopentyl;

[00372] and/or

[00373] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00374] and/or

[00375] C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00376] and/or

[00377] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;

[00378] and/or

[00379] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00380] in which

[00381] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably the C1-6 alkyl is methyl, ethyl, propyl, isopropyl, isobutyl, tert-butyl or neopentyl;

[00382] and/or

[00383] C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00384] and/or

[00385] C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00386] and/or

[00387] aryl is selected from phenyl, naphthyl, or anthracene; preferably it is naphthyl or phenyl; more preferably it is phenyl;

[00388] and/or

[00389] heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrole[ 2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; more preferably it is pyridine;

[00390] and/or

[00391] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;

[00392] and/or

[00393] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00394] in which

[00395] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; preferably it is methyl;

[00396] and/or

[00397] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00398] and/or

[00399] C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00400] and/or

[00401] R3 and R3', taken together with the C atom in connection, can form a substituted or unsubstituted cycloalkyl;

[00402] where

[00403] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; more preferably the cycloalkyl is cyclopropyl;

[00404] and/or

[00405] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00406] where

[00407] C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; preferably it is methyl;

[00408] and/or

[00409] C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00410] and/or

[00411] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00412] and/or

[00413] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00414] in which

[00415] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00416] and/or

[00417] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00418] and/or

[00419] C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00420] and/or

[00421] R5 and R5' taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00422] in which

[00423] non-aromatic heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a non-aromatic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from piperidine, piperazine, tetrahydropyran, morpholine, oxopyrrolidine; preferably, the non-aromatic heterocyclyl is tetrahydropyran;

[00424] and/or

[00425] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; more preferably it is cyclobutyl, cyclopentyl or cyclohexyl;

[00426] and/or

[00427] R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, - CHOR10 and -C(O )OR10;

[00428] in which

[00429] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00430] and/or

[00431] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00432] and/or

[00433] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00434] and/or

[00435] R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00436] in which

[00437] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00438] and/or

[00439] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00440] and/or

[00441] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00442] and/or

[00443] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00444] in which

[00445] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00446] and/or

[00447] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00448] and/or

[00449] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00450] and/or

[00451] R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00452] where

[00453] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00454] and/or

[00455] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00456] and/or

[00457] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00458] and/or

[00459] R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00460] where

[00461] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00462] and/or

[00463] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00464] and/or

[00465] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00466] and/or

[00467] R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00468] R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00469] where

[00470] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00471] and/or

[00472] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00473] and/or

[00474] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00475] and/or

[00476] R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00477] R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00478] where

[00479] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; preferably the C1-6 alkyl is methyl;

[00480] and/or

[00481] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00482] and/or

[00483] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00484] and/or

[00485] R13 is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, and C2-6 unsubstituted alkynyl;

[00486] R13''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00487] where

[00488] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00489] and/or

[00490] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00491] and/or

[00492] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00493] and/or

[00494] R14, R14' and R14'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;

[00495] R14''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00496] in which

[00497] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00498] and/or

[00499] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00500] and/or

[00501] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00502] and/or

[00503] aryl is selected from phenyl, naphthyl and anthracene; preferably it is naphthyl or phenyl;

[00504] and/or

[00505] heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, , benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrole [2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;

[00506] and/or

[00507] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

[00508] and/or

[00509] Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00510] where

[00511] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00512] and/or

[00513] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00514] and/or

[00515] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00516] and/or

[00517] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00518] in which

[00519] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00520] and/or

[00521] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00522] and/or

[00523] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00524] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00525] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R1 as defined in any of the embodiments of the present invention,

[00526] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably the C1-6 alkyl is methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl or neopentyl;

[00527] and/or

[00528] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00529] and/or

[00530] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00531] and/or

[00532] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;

[00533] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00534] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R2 as defined in any of the embodiments of the present invention,

[00535] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably the C1-6 alkyl is methyl, ethyl, propyl, isopropyl, isobutyl, tert-butyl or neopentyl;

[00536] and/or

[00537] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00538] and/or

[00539] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00540] and/or

[00541] aryl is selected from phenyl, naphthyl, or anthracene; preferably it is naphthyl or phenyl; more preferably it is phenyl;

[00542] and/or

[00543] heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, , benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrole [2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline; preferably it is pyridine;

[00544] and/or

[00545] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;

[00546] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00547] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R3 and R3' as defined in any of the embodiments of the present invention,

[00548] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably it is methyl;

[00549] and/or

[00550] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00551] and/or

[00552] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00553] and/or

[00554] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; more preferably the cycloalkyl is cyclopropyl;

[00555] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00556] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R4 and R4'as defined in any of the embodiments of the present invention,

[00557] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; more preferably it is methyl;

[00558] and/or

[00559] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00560] and/or

[00561] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00562] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00563] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R5 and R5' as defined in any of the embodiments of the present invention,

[00564] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00565] and/or

[00566] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00567] and/or

[00568] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00569] and/or

[00570] non-aromatic heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a non-aromatic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from piperidine, piperazine, tetrahydropyran, morpholine, oxopyrrolidine; preferably, the non-aromatic heterocyclyl is tetrahydropyran;

[00571] and/or

[00572] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; more preferably it is cyclobutyl, cyclopentyl or cyclohexyl;

[00573] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00574] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R6 and R6'as defined in any of the embodiments of the present invention,

[00575] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00576] and/or

[00577] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00578] and/or

[00579] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00580] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00581] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R7 as defined in any of the embodiments of the present invention,

[00582] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00583] and/or

[00584] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00585] and/or

[00586] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00587] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00588] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R8 as defined in any of the embodiments of the present invention,

[00589] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00590] and/or

[00591] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00592] and/or

[00593] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00594] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00595] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R9 as defined in any of the embodiments of the present invention,

[00596] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00597] and/or

[00598] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00599] and/or

[00600] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00601] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00602] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R10 as defined in any of the embodiments of the present invention,

[00603] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00604] and/or

[00605] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00606] and/or

[00607] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00608] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00609] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R11, R11' and R11'' as defined in any of the embodiments of the present invention,

[00610] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00611] and/or

[00612] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00613] and/or

[00614] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00615] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00616] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R11''' as defined in any of the embodiments of the present invention,

[00617] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00618] and/or

[00619] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00620] and/or

[00621] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00622] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00623] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R12, R12' and R12'' as defined in any of the embodiments of the present invention,

[00624] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl; preferably the C1-6 alkyl is methyl;

[00625] and/or

[00626] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00627] and/or

[00628] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00629] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00630] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R12''' as defined in any of the embodiments of the present invention,

[00631] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00632] and/or

[00633] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00634] and/or

[00635] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00636] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00637] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R13 and R13''' as defined in any of the embodiments of the present invention,

[00638] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00639] and/or

[00640] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00641] and/or

[00642] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00643] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00644] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R14, R14' and R14'' as defined in any of the embodiments of the present invention,

[00645] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00646] and/or

[00647] C2-6 alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00648] and/or

[00649] C2-6 alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00650] and/or

[00651] aryl is selected from phenyl, naphthyl and anthracene; preferably it is naphthyl or phenyl;

[00652] and/or

[00653] heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably it is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably it is selected from imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, , benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrole [2,3b]pyridine, quinoline, isoquinoline, phthalazine, benzo-1,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carbazole and quinazoline;

[00654] and/or

[00655] cycloalkyl is C3-8 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably it is C3-7 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably C3-6 cycloalkyl such as cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;

[00656] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00657] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in R14''' as defined in any of the embodiments of the present invention,

[00658] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00659] and/or

[00660] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00661] and/or

[00662] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00663] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00664] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in Rx as defined in any of the embodiments of the present invention,

[00665] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00666] and/or

[00667] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00668] and/or

[00669] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00670] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00671] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein in Rx' as defined in any of the embodiments of the present invention,

[00672] the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl and 2-methylpropyl;

[00673] and/or

[00674] C2-6-alkenyl is preferably selected from ethylene, propylene, butylene, pentylene and hexylene;

[00675] and/or

[00676] C2-6-alkynyl is preferably selected from ethyne, propyne, butyne, pentyne and hexin;

[00677] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00678] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein

[00679] n is 0, 1 or 2; preferably, n is 0;

[00680] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00681] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein

[00682] m is 1, 2 or 3; preferably m is 1 or 2;

[00683] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00684] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein

[00685] p is 0 or 1 or 2;

[00686] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00687] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, in which

[00688] p is 0 or 1;

[00689] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00690] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein

[00691] X is a bond, -C(RxRx')-, -C(O)- or -O-; preferably, X is a bond or -O-;

[00692] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00693] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, wherein

[00694] Y is -CH2- or -C(O)-;

[00695] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00696] In another preferred embodiment of the invention according to general formula (I) the compound is a compound, in which

[00697] X is a bond, -C(RxRx')-, -C(O)- or -O-; preferably X is a bond or -O- and/or

[00698] m is 1, 2 or 3; preferably m is 1 or 2; and/or

[00699] n is 0, 1 or 2; preferably n is 0; and/or

[00700] p is 0 or 1; preferably p is 0;

[00701] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00702] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I')

[00703] wherein R1, R2, R3 R3', R4, R4', R5, R5', X, Y, m and p are as described above or as described below.

[00704] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I')

[00705] where

[00706] p is 0 or 1;

[00707] m is 1, 2 or 3;

[00708] Y is -CH2- or -C(O)-;

[00709] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00710] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00711] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00712] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00713] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00714] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00715] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00716] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[00717] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00718] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00719] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00720] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00721] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00722] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00723] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (Ia')

[00724] in which:

[00725] p is 0 or 1;

[00726] m is 1, 2 or 3;

[00727] Y is -CH2- or -C(O)-;

[00728] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00729] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00730] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00731] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00732] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00733] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00734] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00735] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[00736] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00737] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00738] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00739] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00740] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00741] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00742] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (Ib')

[00743] in which

[00744] p is 0 or 1;

[00745] m is 1, 2 or 3;

[00746] Y is -CH2- or -C(O)-;

[00747] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00748] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00749] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00750] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00751] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00752] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00753] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00754] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00755] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00756] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00757] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00758] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00759] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (Ic')

[00760] in which:

[00761] p is 0 or 1;

[00762] m is 1, 2 or 3;

[00763] Y is -CH2- or -C(O)-;

[00764] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00765] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00766] Rx' is selected from hydrogen, halogen or substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

[00767] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00768] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00769] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00770] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00771] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00772] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00773] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00774] alternatively, R5 and R5' taken together with the connecting C atom may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00775] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00776] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I2'),

[00777] in which R1, R2, R4, R4', R5, R5', X, Y, m and p are as described above or as described below.

[00778] In another preferred embodiment of the invention according to general formula (I) the compound is a compound of formula (I2'),

[00779] in which

[00780] p is 0 or 1;

[00781] m is 1, 2 or 3;

[00782] Y is -CH2- or -C(O)-;

[00783] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00784] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00785] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00786] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00787] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00788] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00789] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00790] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00791] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00792] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00793] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00794] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00795] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I3'),

[00796] wherein R1, R2, R4, R4', R5, R5', X, Y, m and p are as described above or as described below.

[00797] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I3'),

[00798] where

[00799] p is 0 or 1;

[00800] m is 1, 2 or 3;

[00801] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00802] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00803] Rx' is selected from hydrogen, halogen or substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;

[00804] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00805] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00806] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00807] R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl, C2-9 substituted or unsubstituted alkynyl, -CHOR9 and -C(O)OR9;

[00808] wherein R9 is selected from hydrogen, C1-9 substituted or unsubstituted alkyl, C2-9 substituted or unsubstituted alkenyl and C2-9 substituted or unsubstituted alkynyl;

[00809] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00810] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00811] alternatively, R5 and R5' taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00812] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00813] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I4'),

[00814] wherein R1, R2, m and p are as described above or as described below.

[00815] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I4'),

[00816] in which:

[00817] p is 0 or 1;

[00818] m is 1, 2 or 3;

[00819] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00820] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00821] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00822] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I5'),

[00823] (I5'),

[00824] in which:

[00825] m is 1, 2 or 3;

[00826] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00827] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00828] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00829] In another preferred embodiment of the invention according to general formula (I), the compound is a compound of formula (I6')

[00830] in which:

[00831] m is 1, 2 or 3;

[00832] Y is -CH2- or -C(O)-;

[00833] X is a bond, -C(RxRx')-, -C(O)- or -O-;

[00834] wherein Rx is selected from halogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, and -OR8;

[00835] Rx' is selected from hydrogen, halogen or C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00836] R8 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00837] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00838] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00839] R3 and R3' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00840] alternatively, R3 and R3', taken together with the C atom in connection can form a substituted or unsubstituted cycloalkyl;

[00841] R5 and R5' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -CHOR7 and -C(O)OR7;

[00842] wherein R7 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl and C2-6 substituted or unsubstituted alkynyl;

[00843] alternatively, R5 and R5' taken together with the C atom in connection may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl;

[00844] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00845] In a preferred embodiment

[00846] R1 is a substituted or unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, neopentyl and cyclopropyl.

[00847] In a preferred embodiment

[00848] R1 is an unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, neo-pentyl and cyclopropyl.

[00849] In a preferred embodiment

[00850] R1 is a substituted or unsubstituted cyclopropyl, preferably unsubstituted cyclopropyl.

[00851] In a preferred embodiment

[00852] R2 is hydrogen or a substituted or unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, tert-butyl, neo-pentyl, cyclopropyl, phenyl and pyridine; more preferably hydrogen or an unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, tert-butyl, neo-pentyl, cyclopropyl, or a substituted or unsubstituted group selected from phenyl and pyridine.

[00853] In a preferred embodiment

[00854] R3 and R3' taken together with the C atom in connection can form a substituted or unsubstituted cyclopropyl: preferably unsubstituted cyclopropyl.

[00855] In a preferred embodiment

[00856] R3 is hydrogen or substituted or unsubstituted methyl, preferably R3 is hydrogen or unsubstituted methyl.

[00857] In a preferred embodiment

[00858] R3' is hydrogen or substituted or unsubstituted methyl, preferably R3' is hydrogen or unsubstituted methyl.

[00859] In a preferred embodiment

[00860] R3' is hydrogen while R3 is substituted or unsubstituted methyl, preferably R3' is hydrogen while R3 is unsubstituted methyl.

[00861] In a preferred embodiment

[00862] R3 is hydrogen while R3' is substituted or unsubstituted methyl, preferably R3 is hydrogen while R3' is unsubstituted methyl.

[00863] In a preferred embodiment

[00864] R3 and R3' are both substituted or unsubstituted methyl, preferably R3 and R3' are both unsubstituted methyl.

[00865] In a preferred embodiment

[00866] R3 and R3' are both hydrogen.

[00867] In a preferred embodiment

[00868] R4 is hydrogen or substituted or unsubstituted methyl, preferably R4 is hydrogen or unsubstituted methyl.

[00869] In a preferred embodiment

[00870] R4' is hydrogen.

[00871] In a preferred embodiment

[00872] R4' is hydrogen while R4 is substituted or unsubstituted methyl, preferably R4' is hydrogen while R4 is unsubstituted methyl.

[00873] In a preferred embodiment

[00874] R4 and R4' are both hydrogen.

[00875] In a preferred embodiment

[00876] R5 and R5' are both hydrogen.

[00877] In a preferred embodiment

[00878] R5 and R5' taken together with the C atom in connection, form a substituted or unsubstituted group selected from cyclobutyl, cyclopentyl, cyclohexyl or tetrahydropyran, preferably an unsubstituted group selected from cyclobutyl, cyclopentyl, cyclo - hexyl or tetrahydropyran.

[00879] In a preferred embodiment

[00880] R6 and R6' are both hydrogen.

[00881] In a preferred embodiment

[00882] X is a link.

[00883] In a preferred embodiment

[00884] X is -O-.

[00885] In a preferred embodiment

[00886] Y is -CH2-;

[00887] In a preferred embodiment

[00888] Y is -C(O)-;

[00889] In another preferred embodiment

[00890] n is 0.

[00891] In another preferred embodiment

[00892] n is 1.

[00893] In another preferred embodiment

[00894] n is 2.

[00895] In another preferred embodiment

[00896] m is 1 or 2;

[00897] In another preferred embodiment

[00898] p is 0, 1 or 2.

[00899] In another preferred embodiment

[00900] p is 0 or 1.

[00901] In another preferred embodiment

[00902] p is 0.

[00903] In a particular embodiment

[00904] the halogen is fluorine or chlorine.

[00905] In another preferred embodiment, the compounds of general formula (I) are selected from

[00906] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00907] In another preferred embodiment, the compounds of general formula (I) are selected from

[00908] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00909] In a preferred embodiment of the compound according to the invention of general formula (I),

[00910] R1 is selected from C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl and substituted or unsubstituted cycloalkyl;

[00911] wherein said cycloalkyl in R1 if substituted, is substituted with one or more selected halogen substituents, - R11, -OR11, -NO2, -NR11R11''', NR11C(O)R11', -NR11S(O )2R11', - S(O)2NR11R11', -NR11C(O)NR11'R11'', -SR11 , -S(O)R11, S(O)2R11, -CN, haloalkyl, haloalkoxy, -C(O )OR11, -C(O)NR11R11', -OCH2CH2OH, - NR11S(O)2NR11'R11'' and C(CH3)2OR11;

[00912] additionally, cycloalkyl in R1, if substituted, can also be substituted with or =O;

[00913] wherein the alkyl, alkenyl or alkynyl in R1, if substituted, is replaced with one or more substituents selected from -OR11, halogen, -CN, haloalkyl, haloalkoxy and -NR11R11''';

[00914] wherein R11, R11' and R11'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00915] and wherein R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00916] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00917] In another embodiment of the invention, the compound of general formula (I),

[00918] R2 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted heterocyclyl or not replaced,

[00919] wherein said cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituents selected from halogen, -R12, -OR12, -NO2, -NR12R12''', NR12C(O)R12' , -NR12S(O)2R12', -S(O)2NR12R12', -NR12C(O)NR12'R12'', -SR12, -S(O)R12, S(O)2R12, -CN, haloalkyl, haloalkoxy , -C(O)OR12, -C(O)NR12R12', -OCH2CH2OH, - NR12S(O)2NR12'R12'' and C(CH3)2OR12;

[00920] additionally, non-aromatic cycloalkyl or heterocyclyl in R2, if substituted, can also be substituted with or =O;

[00921] wherein the alkyl, alkenyl or alkynyl in R2, if substituted, is replaced with one or more substituents selected from -OR12, halogen, -CN, haloalkyl, haloalkoxy and -NR12R12''';

[00922] wherein R12, R12' and R12'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl and C2-6 unsubstituted alkynyl;

[00923] and wherein R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00924] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00925] In another embodiment of the invention, the compound of general formula (I),

[00926] the alkyl, alkenyl or alkynyl, other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from -OR13, halogen, -CN, haloalkyl, haloalkoxy and - NR13R13''';

[00927] wherein R13 is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, and C2-6 unsubstituted alkynyl;

[00928] R13''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00929] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00930] In another embodiment of the invention, the compound of general formula (I),

[00931] aryl, heterocyclyl or cycloalkyl other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from halogen, -R14, -OR14, -NO2, -NR14R14''', NR14C(O )R14', -NR14S(O)2R14', -S(O)2NR14R14', - NR14C(O)NR14'R14'', -SR14 , -S(O)R14, S(O)2R14, -CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14', - OCH2CH2OH, -NR14S(O)2NR14'R14'' and C(CH3)2OR14;

[00932] additionally, where non-aromatic cycloalkyl or heterocyclyl, other than those defined in R1 or R2, if substituted, can also be substituted with or =O;

[00933] wherein R14, R14' and R14'' are independently selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl replaced;

[00934] and wherein R14''' is selected from hydrogen, C1-6 unsubstituted alkyl, C2-6 unsubstituted alkenyl, C2-6 unsubstituted alkynyl and -Boc;

[00935] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00936] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R1 of any of the embodiments of the present invention,

[00937] the cycloalkyl in R1 if substituted, is substituted with one or more selected halogen substituents, -R11, -OR11, -NO2, - NR11R11''', NR11C(O)R11', -NR11S(O)2R11' , -S(O)2NR11R11', - NR11C(O)NR11'R11'', -SR11 , -S(O)R11, S(O)2R11, -CN, haloalkyl, haloalkoxy, -C(O)OR11, -C(O)NR11R11', -OCH2CH2OH, - NR11S(O)2NR11'R11'' and C(CH3)2OR11;

[00938] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00939] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R1 of any of the embodiments of the present invention,

[00940] the cycloalkyl in R1, if substituted, can also be substituted with or =O;

[00941] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00942] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R1 of any of the embodiments of the present invention,

[00943] the alkyl, alkenyl or alkynyl in R1, if substituted, is substituted with one or more substituents selected from -OR11, halogen, -CN, haloalkyl, haloalkoxy and -NR11R11''';

[00944] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00945] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R2 of any of the embodiments of the present invention,

[00946] the cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more selected halogen substituents, - R12, -OR12, -NO2, -NR12R12''', NR12C(O)R12', -NR12S (O)2R12', - S(O)2NR12R12', -NR12C(O)NR12'R12'', -SR12, -S(O)R12, S(O)2R12, -CN, haloalkyl, haloalkoxy, -C (O)OR12, -C(O)NR12R12', -OCH2CH2OH, - NR12S(O)2NR12'R12'' and C(CH3)2OR12;

[00947] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00948] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R2 of any of the embodiments of the present invention,

[00949] the non-aromatic cycloalkyl or heterocyclyl in R2, if substituted, can also be substituted with or =O;

[00950] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00951] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to R2 of any of the embodiments of the present invention,

[00952] the alkyl, alkenyl or alkynyl in R2, if substituted, is substituted with one or more substituents selected from -OR12, halogen, -CN, haloalkyl, haloalkoxy and -NR12R12''';

[00953] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00954] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to alkyls other than those defined in R1 or R2 of any of the embodiments of the present invention,

[00955] the alkyl, alkenyl or alkynyl, other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from -OR13, halogen, -CN, haloalkyl, haloalkoxy and - NR13R13''';

[00956] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00957] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to a cycloalkyl, aryl or heterocyclyl other than those defined in R1 or R2 of any of the embodiments of the present invention,

[00958] aryl, heterocyclyl or cycloalkyl other than those defined in R1 or R2, if substituted, is substituted with one or more substituents selected from halogen, -R14, -OR14, -NO2, -NR14R14''', NR14C(O )R14', -NR14S(O)2R14', -S(O)2NR14R14', - NR14C(O)NR14'R14'', -SR14 , -S(O)R14, S(O)2R14, -CN, haloalkyl, haloalkoxy, -C(O)OR14, -C(O)NR14R14', - OCH2CH2OH, -NR14S(O)2NR14'R14'' and C(CH3)2OR14;

[00959] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00960] In a preferred embodiment of the compound according to the invention of general formula (I) and in relation to cycloalkyl, aryl or heterocyclyl other than those defined in R1 or R2 of any of the embodiments of the present invention,

[00961] non-aromatic cycloalkyl or heterocyclyl, other than those defined in R1 or R2, if substituted, can also be substituted with or =O;

[00962] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00963] In one embodiment of the compound according to the invention of general formula (I),

[00964] the halogen is fluorine, chlorine, iodine or bromine, preferably fluorine or chlorine; more preferably fluorine;

[00965] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00966] In one embodiment of the compound according to the invention of general formula (I),

[00967] the haloalkyl is -CF3;

[00968] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00969] In another embodiment of the compound according to the invention of general formula (I),

[00970] haloalkoxy is -OCF3;

[00971] optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt of the same, or a corresponding solvate thereof.

[00972] As this invention aims to provide a compound or a series of chemically related compounds that act as ligands for the ai receptor, it is a very preferred embodiment, in which compounds are selected, which act as ligands for the ai receptor. and especially compounds that have a binding expressed as Ki that is preferably < i000 nM, more preferably < 500 nM, even more preferably < i00 nM.

[00973] In the following sentence "compound of the invention" is used. This is to be understood as any compound according to the invention as described above according to the general formula (I), (I'), (Ia'), (Ib'), (Ic'), (I2'), (I3'), (I4'), (I5'), (I6') or (I7').

[00974] The compounds of the invention represented by the above-described formula (I) may include enantiomers depending on the presence of chiral centers or isomers depending on the presence of multiple bonds (for example, Z, E). Simple isomers, enantiomers or diastereoisomers and mixtures thereof fall within the scope of the present invention.

[00975] In general, the processes are described below in the experimental part. The starting materials are commercially available or can be prepared by conventional methods.

[00976] A preferred aspect of the invention is also a process for producing a compound according to formula (I).

[00977] A preferred aspect of the invention is a process for producing a compound according to formula (I),

[00978] and in which R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', m, n, p, X and Y are as defined in the description, following schemes 1 to 4.

[00979] In all processes and uses described below, the values of R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', m, n, p, X and Y are as defined in the description (unless otherwise stated), LG represents a leaving group, such as halogen, mesylate, tosylate or triflate, with the proviso that when Y= CO, it can only be chlorine or bromine, V represents an aldehyde or other leaving group (such as halogen, mesylate, tosylast or triflate) and P' represents a suitable protecting group (preferably 4-methoxybenzyl or benzyl).

[00980] A preferred embodiment of the invention is a process for preparing compounds of general formula (I), said process comprising:

[00981] a) an intramolecular cyclization of a compound of formula VIIa

[00982] or

[00983] b) the reaction of a compound of formula VIIIH

[00984] with a compound of formula IX, X or XI,

[00985] or

[00986] c1) when Y is CH2, by an alkylation of a compound of formula XIV

[00987] with a compound of formula XV

[00988] the compound of formula XV being an alkylating agent and V a leaving group, or alternatively by the reductive amination reaction of a compound of formula XIV with a compound of formula XV, the compound of formula XV being an aldehyde and V a C(O)H group;

[00989] or

[00990] c2) when Y is C(O), by an alkylation of a compound of formula XIV

[00991] with a compound of formula XV

[00992] with the compound of formula XV being an alkylating agent and V being a leaving group.

[00993] In another embodiment of the invention is a process for the preparation of compounds of general formula (I), said process comprising an intramolecular cyclization of a compound of formula VIIa

[00994] In another embodiment of the invention is a process for the preparation of compounds of general formula (I) said process comprises the reaction of a compound of formula VIIIH

[00995] with a compound of formula IX, X or XI,

[00996] In another embodiment of preparation of compounds of general formula (I) in which Y is CH2, said process comprises the alkylation of a compound of formula XIV

[00997] with a compound of formula XV

[00998] the compound of formula XV being an alkylating agent and V a leaving group, or alternatively by the reductive amination reaction of a compound of formula XIV with a compound of formula XV, the compound of formula XV being an aldehyde and V a C(O)H group;

[00999] In another embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y is C(O), by alkylation of a compound of formula XIV

[001000] with a compound of formula XV

[001001] with the compound of formula XV being an alkylating agent and V being a leaving group.

[001002] In another preferred embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' taken together with the C atom in connection, form a cyclopropyl (compounds of formula Ic),

[001003] said process comprises

[001004] a) treatment with a strong base of a compound of formula Ib in which Rs=Rs'=H and s=1

[001005] or

[001006] b) a cyclopropanation reaction in a compound of formula XXI

[001007] or

[001008] c) alkylation of a compound of formula XXV

[001009] with a compound of formula XV

[001010] the compound of formula XV being an alkylating agent and V being a leaving group;

[001011] or

[001012] d) the reaction of a compound of formula XIXH

[001013] with a compound of formula IX, X or XI,

[001014] In another preferred embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' taken together with the C atom in connection, form a cyclopropyl (compounds of formula Ic),

[001015] said process comprises

[001016] treatment with a strong base of a compound of formula Ib in which Rs=Rs'=H and s=1

[001017] In another preferred embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' taken together with the C atom in connection, form a cyclopropyl (compounds of formula Ic),

[001018] said process comprises a cyclopropanation reaction in a compound of formula XXI

[001019] In another preferred embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' taken together with the C atom in connection, form a cyclopropyl (compounds of formula Ic),

[001020] said process comprises the alkylation of a compound of formula XXV

[001021] with a compound of formula XV

[001022] with the compound of formula XV being an alkylating agent and V being a leaving group.

[001023] In another preferred embodiment of the invention is a process for the preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' taken together with the C atom in connection, form a cyclopropyl (compounds of formula Ic),

[001024] said process comprises the reaction of a compound of formula XIXH

[001025] with a compound of formula IX, X or XI,

[001026] In another particular embodiment, a compound of formula II, IIP, III, IIIP, IVa, IVb, Vb, VbP, Va, VaP, VI, VIIa, VIIb, VIIb, VIIbP, VIIIP, VIIIH, IX, X, XI , XII, XIIP, XIII, XIIIP, XIV, XIVP, XIVH, , XXII, XXIIP, XXIIH, XXIII, XXIIIP, XXIIIH, XXIV, XXIVP, XXIVH, XXV, XXVP, XXVH, Ie, XXVIP, XXVIH, XXVIIa, XXVIIb, XXVIIc, If, XXVIIIP, XXVIIIH, Ig, XXIXP, XXIXH, Ih , XXXP, XXXH, XXXI, XXXIP, XXXIH, XXXII, XXXIIP, XXXIIH, XXXIII, XXXIIIP, XXXIIIH, XXXIV, XXXIVP or XXXIVH,

[001027] is used for the preparation of a compound of formula (I).

[001028] The reaction products obtained can, if desired, be purified by conventional methods, such as crystallization and chromatography. Where the processes described above for preparing compounds of the invention give rise to mixtures of stereoisomers, these isomers can be separated by conventional techniques such as preparative chromatography. If chiral centers exist, the compounds can be prepared in racemic form, or individual enantiomers can be prepared either by enantiospecific synthesis or by resolution.

[001029] A preferred pharmaceutically acceptable form of a compound of the invention is the crystalline form, including such form in pharmaceutical composition. In the case of salts and also solvates of the compounds of the invention, the ionic moieties and additional solvents must also be non-toxic. The compounds of the invention may have different polymorphic forms, and the invention is intended to encompass all such forms.

[001030] Another aspect of the invention relates to a pharmaceutical composition comprising a compound according to the invention as described above according to general formula I or a pharmaceutically acceptable salt or stereoisomer thereof, and a carrier, pharmaceutically acceptable adjuvant or vehicle. The present invention, therefore, provides pharmaceutical compositions comprising a compound of this invention, or a pharmaceutically acceptable salt or stereoisomers thereof together with a pharmaceutically acceptable carrier, adjuvant, or vehicle, for administration to a patient.

[001031] Examples of pharmaceutical compositions include any solid (tablets, pills, capsules, granules, etc.) or liquid (solutions, suspensions or emulsions) composition for oral, topical or parenteral administration.

[001032] In a preferred embodiment, the pharmaceutical compositions are in oral form, either solid or liquid. Dosage forms suitable for oral administration may be tablets, capsules, syrups or solutions and may contain conventional excipients known in the art such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone; fillers, for example lactose, sugar, corn starch, calcium phosphate, sorbitol or glycine; tablet lubricants, for example magnesium stearate; disintegrants, for example starch, polyvinylpyrrolidone, sodium starch glycolate or microcrystalline cellulose; or pharmaceutically acceptable wetting agents such as sodium lauryl sulfate.

[001033] Solid oral compositions can be prepared by conventional mixing, loading or tableting methods. Repeated mixing operations can be used to distribute the active agent throughout these compositions employing large amounts of fillers. Such operations are conventional in the art. Tablets may, for example, be prepared by wet or dry granulation and optionally coated according to methods well known in normal pharmaceutical practice, in particular with an enteric coating.

[001034] Pharmaceutical compositions can also be adapted for parenteral administration, such as sterile solutions, suspensions or lyophilized products in appropriate unit dosage form. Suitable excipients can be used, such as bulking agents, buffering agents or surfactants.

[001035] The mentioned formulations will be prepared using standard methods such as those described or referred to in the Spanish and North American Pharmacopoeias and similar reference texts.

[001036] Administration of the compounds or compositions of the present invention can be by any suitable method, such as intravenous infusion, oral preparations, and intraperitoneal and intravenous administration. Oral administration is preferred because of convenience for the patient and the chronic nature of the diseases to be treated.

[001037] Generally, an effective administered amount of a compound of the invention will depend on the relative effectiveness of the chosen compound, the severity of the disorder being treated and the weight of the patient. However, active compounds will typically be administered once or more times in a day, e.g., 1, 2, 3, or 4 times a day, with typical total daily doses in the range of about 0.1 to 1000 mg/kg/day. .

[001038] The compounds and compositions of this invention can be used with other drugs to provide a combination therapy. The other drugs may form part of the same composition, or be provided as a separate composition for administration at the same or different times.

[001039] Another aspect of the invention relates to the use of a compound of the invention or a pharmaceutically acceptable salt or isomer thereof in the manufacture of a medicament.

[001040] Another aspect of the invention relates to a compound of the invention as described above, according to general formula I, or a pharmaceutically acceptable salt or isomer thereof, for use as a medicament for the treatment of abuse of drugs or addiction.

[001041] Another aspect of the invention relates to the use of a compound of the invention in the manufacture of a medicine for the treatment or prophylaxis of drug abuse or addiction.

[001042] Another aspect of this invention relates to a method of treating or preventing drug abuse or addiction which method comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound as defined above or a pharmaceutical composition thereof. .

[001043] The present invention is illustrated below with the aid of examples. These illustrations are provided by way of example only and do not limit the general spirit of the present invention.

General Experimental Part (Methods and Equipment for synthesis and analysis SCHEME 1:

[001044] A 4-step process is described for the preparation of compounds of general formula (I) starting from a ketone of formula II, as shown in the following scheme: Scheme 1

[001045] wherein R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', X, Y, m, n and p have the meanings as defined above by a compound of formula (I) , LG represents a leaving group such as halogen, mesylate, tosylate or triflate, with the caveat that when Y=CO it can only be chlorine or bromine, V represents an aldehyde or other leaving group (such as halogen, mesylate, tosylate or triflate), P represents a suitable protecting group (preferably Boc) and P' represents an orthogonal protecting group (preferably 4-methoxybenzyl or benzyl).

[001046] The 4-step process is carried out as described below:

[001047] Step 1: a compound of formula III is prepared by treating a compound of formula II with a suitable methyl transfer reagent such as trimethylsulfoxonium iodide or trimethylsulfonium iodide, in a suitable aprotic solvent such as dimethylsulfoxide or 1,2- dimethoxyethane or mixtures, and in the presence of a strong base such as sodium hydride or potassium tert-butoxide, at a suitable temperature, preferably between 0 °C and 60 °C.

[001048] Step 2: a compound of formula Va is prepared by reacting a compound of formula III with an amine of formula IVa, in a suitable solvent such as an alcohol, preferably ethanol-water mixtures, at a suitable temperature between room temperature and the reflux temperature.

[001049] Step 3: a compound of formula Vila is prepared by reacting a compound of formula Va with a compound of formula VI. Depending on the meaning of Y, the compound of formula VI may be of different nature and different reaction conditions will apply:

[001050] a) When Y represents CO, VI is an acylating agent. The acylation reaction is carried out in a suitable solvent, such as dichloromethane or ethyl acetate-water mixtures; in the presence of an organic base such as triethylamine or diisopropylethylamine or an inorganic base such as K2CO3; and at a suitable temperature, preferably between -78 °C and room temperature.

[001051] b) When Y represents CH2, VI is an alkylating agent. The alkylation reaction can be carried out in a suitable solvent, such as acetonitrile, dichloromethane, tetrahydrofuran, 1,4-dioxane or dimethylformamide; in the presence of an inorganic base such as K2CO3, Cs2CO3 or NaH, or an organic base such as triethylamine or diisopropylethylamine, at a suitable temperature between room temperature and reflux temperature. The OH group present may need prior protection for the alkylation reaction.

[001052] Step 4: Intramolecular cyclization of a compound of formula VIIa yields a compound of formula I. The cyclization reaction is carried out in a suitable solvent, such as tetrahydrofuran; in the presence of a strong base such as potassium tert-butoxide or sodium hydride; and at a suitable temperature, between -78 °C and the reflux temperature, preferably cooling.

[001053] Alternatively, the group -(CR5R5')mX(CR6R6')nR2 can be incorporated in the last step of the synthesis by reacting a compound of formula VIIIH with a compound of formula IX, X or XI, as shown in Scheme 1 A compound of formula VIIIH is obtained by deprotection of a compound of formula VIIIP, where P represents a suitable protecting group, preferably Boc (tert-butoxycarbonyl). When the protecting group is Boc, deprotection can be carried out by adding a solution of a strong acid such as HCl, in a suitable solvent such as diethyl ether, 1,4-dioxane or methanol, or with trifluoroacetic acid in dichloromethane. A compound of formula VIIIP is prepared from a compound of formula IIP following the same sequence described for the synthesis of compounds of formula I.

[001054] The alkylation reaction between a compound of formula VIIIH (or a suitable salt such as trifluoroacetate or hydrochloride) and a compound of formula IX is carried out in a suitable solvent, such as acetonitrile, dichloromethane, 1,4-dioxane or dimethylformamide , preferably in acetonitrile; in the presence of an inorganic base such as K2CO3 or Cs2CO3, or an organic base such as triethylamine or diisopropylethylamine, preferably K2CO3; at a suitable temperature between room temperature and reflux temperature, preferably heating, or alternatively, the reactions can be carried out in a microwave reactor. Additionally, an activating agent such as NaI can be used.

[001055] The reductive amination reaction between a compound of formula VIIIH and a compound of formula X is carried out in the presence of a reductive reagent, preferably sodium triacetoxyborohydride, in an aprotic solvent, preferably tetrahydrofuran or dichloroethane, optionally in presence of an acid, preferably acetic acid.

[001056] The condensation reaction between a compound of general formula VIIIH and a compound of formula XI is preferably carried out in a suitable solvent, such as ethanol, isopropanol, n-butanol or 2-methoxyethanol, optionally in the presence of an organic base such as such as triethylamine or diisopropylethylamine, at a suitable temperature between room temperature and reflux temperature, preferably heating, or alternatively, the reactions can be carried out in a microwave reactor.

[001057] In another alternative approach, the -(CR4R4')pR1 substituent can be incorporated later in the sequence by a reaction of a compound of formula XIV with a compound of formula XV. Depending on the meaning of Y, V may be of different nature and different reaction conditions will apply:

[001058] a) When Y is CH2, compound XV is an alkylating agent and V represents a leaving group such as halogen, mesylate, tosylate or triflate. The alkylation reaction is carried out under the same reaction conditions described above for the reaction of a compound of formula VIIIH and a compound of formula IX. Alternatively, compound XV may be an aldehyde in which V represents a C(O)-H group. The reductive amination reaction is carried out under the same reaction conditions described above for the reaction of a compound of formula VIIIH and a compound of formula X.

[001059] b) When Y is C(O), compound XV is an alkylating agent and V represents a leaving group such as halogen, mesylate, tosylate or triflate. This alkylation reaction is carried out in an aprotic solvent, preferably dimethylformamide, in the presence of an inorganic base such as NaH, at a suitable temperature, preferably between room temperature and 60°C.

[001060] A compound of formula XIV is synthesized following an analogous sequence as described for the synthesis of compounds of formula I, but carrying out step 2 using ammonia instead of an amine IVa. Alternatively, when Y is C(O), a compound of formula XIV may be prepared by reacting a compound of formula XIVH (prepared from a compound of formula XIVP, wherein P represents a suitable protecting group) with a compound of formula IX, X or XI, as described above.

[001061] Additionally, a compound of formula XIV can be prepared from a compound of formula XVI, in which P' represents an orthogonal protecting group. When Y is C(O), P' is preferably a 4-methoxybenzyl group and the deprotection reaction is carried out with cerium ammonium nitrate in a suitable solvent such as acetonitrile-water mixtures or by heating in trifluoroacetic acid or hydrochloric acid. . When Y is -CH2-, P' is preferably a 4-methoxybenzyl or a benzyl group, and the deprotection reaction is preferably carried out by hydrogenation under a hydrogen atmosphere and metal catalysis, preferably by using palladium on charcoal as a catalyst in a suitable solvent such as methanol or ethanol, optionally in the presence of an acid such as acetic acid or hydrochloric acid.

[001062] A compound of formula XVI is synthesized from a compound of formula III following an analogous sequence as described for the synthesis of compounds of formula I. Alternatively, a compound of formula XVI can be prepared by reacting a compound of formula XVIH ( prepared from a compound of formula XVIP, where P represents a suitable protecting group) with a compound of formula IX, X or XI, as described above.

[001063] Compounds of general formula II, IIP, IVa, IVb, VI, IX, X, XI and XV in which R1, R2, R3, R3', R4, R4', R5, R5', R6, R6' , X, Y, m, n and p have the meanings as defined above, are commercially available or can be prepared by conventional methods described in the bibliography.

SCHEME 2

[001064] The preparation of compounds of general formula (I) in which Y represents CO and R3 and R3' are used together with the connecting C atom to form a cycloalkyl (compounds of formula Ia) is described in the following scheme: Scheme 2

[001065] wherein R1, R2, R4, R4', R5, R5', R6, R6', X, Y, m, n and p have the meanings as defined above for a compound of formula (I), s represents 1, 2, 3 or 4, Rs and Rs' represents hydrogen or alkyl, LG represents a leaving group such as halogen, mesylate, tosylate or triflate, V represents another leaving group (such as halogen, mesylate, tosylate or triflate), P represents a suitable protecting group (preferably Boc), P' represents an orthogonal protecting group (preferably 4-methoxybenzyl), and Q represents methyl or benzyl.

[001066] A compound of formula Ia can be prepared from a compound of formula Ib by treating with a strong base such as lithium diisopropylamide or potassium tert-butoxide, in an aprotic solvent such as tetrahydrofuran, at a temperature Suitably, preferably by cooling and analogously, a compound of formula Ic (where Rs=Rs'=H and s=1) can be prepared from a compound of formula Ib under the same reaction conditions.

[001067] Alternatively, compounds of formula Ic can be prepared from compounds of formula XXI. The cyclopropanation reaction is carried out using a suitable methyl transfer reagent such as trimethylsulfoxonium iodide or trimethylsulfonium iodide, in a suitable aprotic solvent such as dimethylsulfoxide, and in the presence of a strong base such as sodium hydride or sodium tert-butoxide. potassium, at a suitable temperature, preferably between room temperature and 60 °C. Alternatively, typical Simmons-Smith reaction conditions may be used, comprising treating a compound of formula XXI with diiodomethane, a zinc source such as zinc-copper, zinc iodide or diethylzinc, in a suitable aprotic solvent such as diethyl ether.

[001068] Compounds of formula XXI can be prepared from a compound of formula Id in which Q represents methyl or benzyl. The elimination reaction is carried out in the presence of a base, such as potassium tert-butoxide, in a suitable solvent, such as tetrahydrofuran.

[001069] In another alternative approach, the -(CR4R4')pR1 substituent can be incorporated later in the synthesis. Thus, compounds of formula Ia and Ic can be prepared from compounds of formula XXIII and XXV, respectively, by following the reaction conditions described in Scheme 1 for the preparation of compounds of formula I from compounds of formula XIV. Compounds of formula XXIII and XXV can be prepared from suitable protected precursors XXII and XXIV, respectively, following the conditions described in Scheme 1.

[001070] Furthermore, the group -(CR5R5')mX(CR6R6')nR2 can be incorporated in the last step of the synthesis to prepare compounds of formula Ia and Ic from suitable protected precursors, by deprotection followed by reaction with a compound of formula IX or X or XI, as described in Scheme 1 for the preparation of compounds of formula I.

[001071] Compounds of general formula Ib and Id can be prepared by the procedures described in Scheme 1 from a compound of formula Va using suitable starting materials. Compounds of general formula XXII and XXIV can be prepared by following the procedures described in Scheme 2 for the preparation of compounds of formula Ia and Ic using the corresponding protected starting materials.

SCHEME 3 and SCHEME 4

[001072] Compounds of formula (I) can also be prepared starting from other compounds of formula (I), as described in Schemes 3 and 4 below.

[001073] Compounds of formula Ia, If and Ig can be prepared from a compound of formula Ie as shown in Scheme 3: Scheme 3

[001074] wherein R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', X, m, n and p have the meanings as defined above for a compound of formula (I), s represents 1, 2, 3 or 4, Rs and Rs' represent hydrogen or alkyl, LG, X' and X'' independently represent a leaving group such as halogen, mesylate, tosylate or triflate, and P represents a suitable protecting group (preferably Boc).

[001075] A compound of formula If can be prepared by treating a compound of formula Ie with an alkylating agent of formula XXVIIa in the presence of a strong base such as lithium diisopropylamide or potassium tert-butoxide, in an aprotic solvent such as as tetrahydrofuran, at a suitable temperature, preferably between -78 °C and room temperature. A second alkylation can be carried out under the same reaction conditions to prepare a compound of formula Ig. An analogous double alkylation process can be used for the preparation of compounds of formula Ia by reacting a compound of formula Ie with an alkylating agent of formula XXVIIc, as an alternative to the procedure described in Scheme 2 for preparing compounds of formula Go.

[001076] Furthermore, the group -(CR5R5')mX(CR6R6')nR2 can be incorporated in the last step of the synthesis to prepare compounds of formula Ia, Ie, If and Ig from suitable protected precursors, by deprotection followed by reaction with a compound of formula IX or X or XI, under the reaction conditions described in Scheme 1 for the preparation of compounds of formula I.

[001077] Compounds of general formula Ie and If can be prepared by the procedures described in Scheme 1 using suitable starting materials.

[001078] The compounds of general formula XXVIIa, XXVIIb and XXVIIc in which R3, R3', Rs, Rs', X', X'' and s have meanings as defined above, are commercially available or can be prepared by conventional methods described in bibliography.

[001079] Scheme 4 shows the preparation of compounds of formula (I) in which Y is CH2 from compounds of formula (I) in which Y is C(O): Scheme 4

[001080] wherein R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', X, m, n and p have the meanings as defined above for a compound of formula (I), LG represents a leaving group such as halogen, mesylate, tosylate or triflate, V represents an aldehyde or other leaving group (such as halogen, mesylate, tosylate or triflate), P represents a suitable protecting group (preferably Boc) and P' represents an orthogonal protecting group (preferably 4-methoxybenzyl or benzyl).

[001081] The reduction reaction of a compound of formula Ig to produce a compound of formula Ih can be carried out using a suitable reducing agent such as lithium aluminum hydride, borane-tetrahydrofuran complex or borane-dimethyl sulfide complex , in a suitable solvent such as tetrahydrofuran or diethyl ether, at a suitable temperature between room temperature and reflux temperature, preferably heating.

[001082] The reduction reaction can also be carried out on a suitable precursor (compounds of formula XXXI or XXXII) or a protected derivative (compounds of formula XXIXP, XXXIP or XXXIIP, where A=P). When P represents Boc, borane is the preferred reducing agent.

[001083] Compounds of general formula Ig can be prepared by the procedures described in Schemes 1 to 3 using suitable starting materials, or they can be prepared from a compound of formula XXXI or XXXII. Deprotection of a compound of formula XXXII to provide a compound of formula XXXI and subsequent reaction with a compound of formula XV to produce a compound of formula Ig are carried out following the procedures described in Scheme 1.

[001084] Compounds of general formula XXXI and XXXII can be prepared according to the procedures described in Scheme 1 using suitable starting materials.

[001085] Consequently, compounds of general formula Ih can be prepared from a compound of formula XXXIII or XXXIV following an analogous procedure.

[001086] Furthermore, the group -(CR5R5')mX(CR6R6')nR2 can be incorporated at different stages of the synthesis to prepare compounds of formula Ig and Ih from suitable protected precursors, by deprotection followed by reaction with a compound of formula IX or X or XI, as described in Scheme 1 for the preparation of compounds of formula I.

[001087] Furthermore, certain compounds of the present invention can also be obtained from other compounds of formula (I) by appropriate conversion reactions of functional groups, in one or several steps, using well-known reactions in organic chemistry under standard experimental conditions. .

[001088] Furthermore, a compound of formula I that shows chirality can also be obtained by resolving a racemic compound of formula I or by chiral preparative HPLC or by crystallization of a diastereomeric salt or co-crystal. Alternatively, the resolution step can be carried out at an earlier stage using any suitable intermediary.

EXAMPLES Intermediaries and Examples

[001089] The following abbreviations are used in the examples: ACN: acetonitrile AcOH: acetic acid Boc: tert-butoxycarbonyl Conc: concentrate DCM: dichloromethane DIPEA: N,N-diisopropylethylamine DMF: dimethylformamide DMSO: dimethylsulfoxide EtOH: ethanol EX: example h: hour/s HPLC: high performance liquid chromatography INT: intermediate LDA: lithium diisopropylamide MeOH: methanol MS: mass spectrometry Min.: minutes Quantity: quantitative Ret.: retention t.a.: room temperature Sat: saturated s.m.: starting material TFA: trifluoroacetic acid THF: tetrahydrofuran P: weight

[001090] The following methods were used to determine the HPLC-MS spectra: Method A

[001091] Column: Gemini-NX 30 x 4.6 mm, 3um

[001092] Temperature: 40 °C

[001093] Flow: 2.0 mL/min

[001094] Gradient: NH4HCO3 pH 8: ACN (95:5)---0.5min---(95:5)--- 6.5min---(0:100)---1min--- (0:100)

[001095] The sample dissolved approx. 1mg/mL in NH4HCO3 pH 8/ACN Method B

[001096] Speaker: Xbridge C18 XP 30 x 4.6 mm, 2.5 m

[001097] Temperature: 40 °C

[001098] Flow: 2.0 mL/min

[001099] Gradient: NH4HCO3 pH 8: ACN (95:5)---0.5min---(95:5)--- 6.5min---(0:100)---1min--- (0:100)

[001100] The sample dissolved approx. 1mg/ mL in NH4HCO3 pH 8/ACN Method C

[001101] Column: Kinetex EVO 50 x 4.6 mm 2.6um

[001102] Temperature: 40 °C

[001103] Flow: 2.0 mL/min

[001104] Gradient: NH4HCO3 pH 8: ACN (95:5)---0.5min---(95:5)--- 6.5min---(0:100)---1min--- (0:100)

[001105] The sample dissolved approx. 1mg/ mL in NH4HCO3 pH 8/ACN Method D

[001106] Column: Kinetex EVO 50 x 4.6 mm 2.6um

[001107] Temperature: 40°C

[001108] Flow: 1.5 mL/min

[001109] Gradient: NH4HCO3 pH 8: ACN (95:5)---0.5min---(95:5)--- 6.5min---(0:100)---2min--- (0:100)

[001110] The sample dissolved approx. 1mg/ mL in NH4HCO3 pH 8/ACN Synthesis of Intermediates Intermediate 1A: tert-Butyl 1-oxa-6-azaspiro[2.5]octane-6-carboxylate

[001111] To a suspension of trimethylsulfoxonium iodide (24.3 g, 110 mmol) and NaH (4.4 g, 60% weight in mineral oil, 110 mmol) in DMSO (140 mL), a solution of tert. butyl 4-oxopiperidine-1-carboxylate (20.0 g, 100 mmol) in DMSO (140 mL) was added dropwise. The reaction mixture was stirred at room temperature for 30 minutes, then heated at 50 °C for 1 hour. After cooling to room temperature, ice was slowly added, and the reaction mixture was extracted three times with ethyl acetate. The organic phases were combined, washed with water, dried over MgSO4 and concentrated in vacuo to provide the title compound (17.6 g, 82% yield) as a white solid.

[001112] This method was used for the preparation of intermediate 1B using suitable starting materials: Intermediate 2A: tert-Butyl 4-hydroxy-4-((methylamino)methyl)piperidine-1-carboxylate

[001113] A solution of intermediate 1A (0.50 g, 2.34 mmol) in a mixture of EtOH-water 5.5:1 (14 mL), methylamine (4.1 mL, 40% solution in water , 47 mmol) was added. The reaction mixture was stirred at room temperature overnight in a sealed tube. The solvent was removed in vacuo to provide the title compound (0.534 g, 93% yield) as a white solid.

[001114] This method was used for the preparation of intermediates 2B-2I using suitable starting materials: Intermediate 3A: tert-butyl 12-(4-methoxybenzyl)-13-oxo-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane-8-carboxylate

[001115] Step 1. Tert-butyl 4-((2-bromo-4-chloro-N-(4-methoxybenzyl)butanamido)methyl)-4-hydroxypiperidine-1-carboxylate: To a 2D intermediate solution (9.94 g, 28.4 mmol) and triethylamine (9.5 mL, 68.1 mmol) in DCM (500 mL), a solution of 2-bromo-4-chlorobutanoyl chloride (prepared as described in US 6114541A1 (2000) Ex1) (9.35 g, 20.2 mmol) in DCM (200 mL) was added dropwise at 0 °C. The reaction mixture was stirred at 0 °C for 3 h. DCM and saturated aqueous NaHCO3 solution were added and the phases were separated. The aqueous phase was extracted with DCM and the organic phases were combined, dried over MgSO4, filtered and concentrated to dryness to give the title compound (17.6 g, crude product).

[001116] Step 2. Title compound: a solution of the crude product obtained in step 1 (14.8 g, 27.7 mmol) in THF (185 mL) was cooled under nitrogen to 0 °C. After addition of potassium tert-butoxide solution (111 mL, 1 M in THF, 111 mmol), the reaction mixture was stirred at 0 °C for 2 h. Saturated NH4Cl solution was then added, and the aqueous phase was extracted with ethyl acetate. The organic phases were combined, dried over MgSO4, filtered and concentrated in vacuo. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (5.51 g, 48% yield over 2 steps).

[001117] This method was used for the preparation of intermediates 3B-3E using suitable starting materials: Intermediate 4: 13-oxo-4-oxa-8,12-diazadiespiro[2.1.5.3' tridecane-8- tert-Butyl carboxylate

[001118] Step 1. 4-Oxa-8,12-diazadiespiro-[2.1.5.3]tridecan-13-one trifluoroacetate: a solution of intermediate 3A (1.78 g, 4.26 mmol) in TFA (20 mL ) was stirred in a sealed tube at 80 °C for 4 days. The reaction mixture was concentrated to dryness and water was added to the residue. The acidic aqueous phase was washed with ethyl ether, which was discarded. The aqueous layer was evaporated to dryness to provide the title compound (1.17 g).

[001119] Step 2. Title compound: a mixture of the crude product obtained in step 1, di-tert-butyl dicarbonate (1.40 g, 6.40 mmol), 1,4-dioxane (40 mL) and solution 1 M NaOH aqueous solution (10 mL) was stirred at room temperature overnight. Water was added and the resulting mixture was extracted with ethyl acetate. The organic phases were combined, dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to provide the title compound (0.872 g, 69% yield over 2 steps). Intermediate 5A: tert-Butyl 13-oxo-12-propyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane-8-carboxylate

[001120] To a solution of intermediate 4 (0.200 g, 0.641 mmol) in dry DMF (6.7 mL), NaH (54 mg, 60 wt% in mineral oil, 1.35 mmol) was added at 0 °C . The reaction mixture was stirred at 0 °C for 30 minutes, then 1-bromopropane (0.092 mL, 1.012 mmol) was added and the resulting mixture was stirred at room temperature for 3 h. Saturated aqueous NaHCO3 solution was added to the reaction mixture and it was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over MgSO4, filtered and concentrated to dryness to provide the title compound as a crude product which was used as such (229 mg, quantitative yield).

[001121] This method was used for the preparation of intermediates 5B-5F using suitable starting materials: Intermediate 6A: (S)-tert-Butyl 4-ethyl-2-methyl-3-oxo-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate

[001122] Step 1. (R)-tert-Butyl 4-((2-chloro-N-methylpropanamido)methyl)-4-hydroxypyperidine-1-carboxylate: To a solution of intermediate 2B (0.700 g, 2 .71 mmol) in ethyl acetate (7 mL), a solution of K2CO3 (1.05 g, 7.59 mmol) in water (7.7 mL) was added. After cooling to 0 °C, a solution of (R)-2-chloropropanoyl chloride (0.461 g, 3.63 mmol) in ethyl acetate (3.5 mL) was added dropwise. The reaction mixture was stirred at 0 to 5 °C for 30 minutes and then it was diluted with water. The layers were separated and the aqueous phase was extracted with ethyl acetate. The organic phases were combined, washed with 0.5 M aqueous HCl solution and then saturated NaHCO3 solution, dried over MgSO4, filtered and concentrated to dryness to provide the title compound (0.775 g, 82% yield).

[001123] Step 2. Title compound: a solution of the crude product obtained in step 1 (0.775 g, 2.22 mmol) in THF (15.5 mL) was cooled to -78 ° C using a dry ice bath/ acetone. After addition of potassium tert-butoxide solution (2.4 mL, 1 M in THF, 2.4 mmol), the reaction mixture was stirred at -78 °C for 30 minutes. Saturated NH4Cl solution was then added, and the aqueous phase was extracted with ethyl acetate. The organic phases were combined, dried over MgSO4, filtered and concentrated in vacuo to provide the title compound (0.683 g, 98% yield).

[001124] This method was used for the preparation of 6B-6P intermediates using suitable starting materials: Intermediate 7A: tert-Butyl 12-isopropyl-4-oxa-8,12-diazadiespiro[2.1.5.3]-tridecane-8-carboxylate

[001125] To a solution of intermediate 3B (1.00 g, 2.95 mmol) in THF (5 mL), solution of borane-tetrahydrofuran complex (11.8 mL, 1 M in THF, 11.8 mmol) was added dropwise at room temperature. The reaction mixture was stirred at 65 °C for 2 h, then it was cooled to room temperature. 1 M NaOH aqueous solution (5 mL) was carefully added, cooling the mixture with an ice-water bath, and then it was heated to 70 °C for 2 h. After cooling to room temperature, it was diluted with ethyl acetate. The phases were separated and the aqueous phase was extracted again with ethyl acetate. The organic phases were combined, dried over MgSO4, filtered and concentrated to dryness to provide the title compound as a crude product which was used as such (960 mg, quantitative yield).

[001126] This method was used for the preparation of intermediates 7B-7H using suitable starting materials: Intermediate 8: tert-Butyl 4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane-8-carboxylate

[001127] A mixture of intermediate 7E (7.4 g, 19.9 mmol), AcOH (1.14 mL, 19.9 mmol) and palladium (1.31 g, 10% weight on carbon, wet) in MeOH (37 mL) was stirred under 3 bars of H2 at room temperature for 1 day. The solids were filtered and the solvent was removed under vacuum. The residue was diluted with DCM and 1 M aqueous NaOH solution. The phases were separated and the aqueous phase was extracted several times with DCM. The organic phases were combined, dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (3.57 g, 64% yield). Intermediate 9A: tert-Butyl 4-ethyl-2,2-dimethyl-3-oxo-1-oxa-4,9-diazaspiro[5.5]undecane-9-carboxylate

[001128] A solution of intermediate 6B (18.15 g, 58.1 mmol) in dry THF (82 mL) was cooled to 0 °C. After slow addition of LDA solution (77 mL, 1.5 M in THF/n-heptane/ethylbenzene, 115.5 mmol), the reaction mixture was stirred at 0 °C for 30 minutes. Iodomethane (10.9 mL, 174.2 mmol) was then added and the reaction mixture was stirred at 0 to 5 °C for a further 60 min. Again, LDA solution (77 mL, 1.5 M in THF/n-heptane/ethylbenzene, 115.5 mmol) was slowly added and the reaction mixture was stirred at 0 °C for 30 minutes. Additional iodomethane (10.9 mL, 174.2 mmol) was then added and the reaction mixture was stirred at 0 to 5 °C for an additional 60 minutes to achieve complete conversion. Saturated NH4Cl solution was then added, and the aqueous phase was extracted three times with ethyl acetate. The combined organic phases were dried over Na2SO4, filtered and concentrated in vacuo. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (8.42 g, 44% yield).

[001129] This method was used for the preparation of intermediates 9B-9C using suitable starting materials: Intermediate 10A: tert-Butyl 12-isobutyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane-8-carboxylate

[001130] A mixture of intermediate 8 (1.5 g, 5.31 mmol), 1-bromo-2-methylpropane (0.69 mL, 6.37 mmol) and K2CO3 (1.468 g, 10.62 mmol) in ACN (18 mL) was heated at 80 °C in a sealed tube overnight. 1 M NaOH was added, and the reaction mixture was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (679 mg, 38% yield).

[001131] This method was used for the preparation of intermediate 10B using suitable starting materials: Intermediate 11A: tert-Butyl 12-neopentyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane-8-carboxylate

[001132] To a solution of intermediate 8 (0.300 g, 1.06 mmol) in dry THF (7.2 mL), pivalaldehyde (0.15 mL, 1.38 mmol) and acetic acid (0.12 mL, 2 .12 mmol) were added. The reaction mixture was stirred at room temperature for 15 minutes and then sodium triacetoxyborohydride (0.675 g, 3.19 mmol) was added in portions. The resulting mixture was stirred at room temperature overnight. Water and concentrated NH3 were carefully added and it was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over Na2SO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH:DCM (1:4) to give the title compound (184 mg, 49% yield).

[001133] This method was used for the preparation of intermediate 11B using suitable starting materials: Synthesis of Examples Example 1: 12-Ethyl-8-isopentyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecan-13-one

[001134] Step 1. 12-ethyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecan-13-one trifluoroacetate. To a solution of intermediate 3C (1.75 g, 5.39 mmol) in DCM (65 mL), TFA (4.2 mL, 53.9 mmol) was added, and the reaction mixture was heated to 40 °C for 2 h. The solvent was evaporated to dryness to provide the title compound as a crude product (3.59 g, 50% weight, quantitative production), which was used in the next step without further purification.

[001135] Step 2. Title compound: a mixture of the crude product obtained in step 1 (0.200 g, 50% weight, 0.297 mmol), 1-bromo-3-methylbutane (0.043 mL, 0.357 mmol), NaI (0.026 g , 0.178 mmol) and K2CO3 (0.205 g, 1.49 mmol) in ACN (2.5 mL) was heated at 80 °C in a sealed tube overnight. Water was added, and the reaction mixture was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (45 mg, 51% yield).

[001136] HPLC retention time (method B): 3.48 min; MS: 295.2 (M+H).

[001137] This method was used to prepare examples 215 using suitable starting materials: Example 16: 12-Ethyl-8-(4-fluorobenzyl)-4-oxa-8,12-diazadiespiro [2.1.5.3]tridecan-13-one

[001138] To a solution of the crude product obtained in step 1 of example 1 (0.173 g, 59% weight, 0.30 mmol) in dry THF (2 mL), 4-fluorobenzaldehyde (0.042 mL, 0.39 mmol) was added. The reaction mixture was stirred at room temperature for 15 minutes and then sodium triacetoxyborohydride (0.190 g, 0.91 mmol) was added in portions. The resulting mixture was stirred at room temperature overnight. Water and concentrated NH3 were carefully added and it was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over Na2SO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH:DCM (1:4) to give the title compound (55 mg, 55% yield).

[001139] HPLC retention time (method A): 3.08 min; DM: 333.1 (M+H).

[001140] This method was used to prepare examples 17-35 using suitable starting materials: Example 36: 8-(2-(3-Fluoropyridin-2-yl)ethyl)-12-isopropyl-4-oxa-8,12-diazadiespiro[2.1.5.3]tridecane

[001141] Step 1. 12-isopropyl-4-oxa-8,12-diazadiespiro [2.1.5.3]tridecane dihydrochloride. To a solution of intermediate 7A (156 mg, 0.48 mmol) in MeOH (2 mL), HCl (2 M solution in diethyl ether, 2.4 mL, 4.8 mmol) was added, and the mixture was stirred. at room temperature for 4 h. The solvent was evaporated under vacuum to provide the corresponding di-HCl salt (143 mg, quantitative yield).

[001142] Step 2. Title compound: a solution of the crude product obtained in step 1 (0.125 g, 0.42 mmol), DIPEA (0.366 mL, 2.1 mmol) and 3-fluoro-2-vinylpyridine hydrochloride ( 0.115 g, 0.72 mmol) in EtOH (1.2 mL) was heated at 90 °C in a sealed tube for 1 day. Additional 3-fluoro-2-vinylpyridine hydrochloride (0.034 g, 0.210 mmol) was added and the mixture heated at 90°C for another day. The reaction mixture was allowed to cool to room temperature and the solvent was evaporated. It was diluted with DCM and washed twice with 1N NaOH. The organic phase was dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (44 mg, 30% yield).

[001143] HPLC retention time (method A): 3.70 min; MS: 348.2 (M+H).

[001144] This method was used to prepare examples 37-43 using suitable starting materials:

[001145] The method described in Example 1 was used to prepare examples 44-65 using suitable starting materials:

[001146] The method described in Example 16 was used to prepare examples 67 to 100 using suitable starting materials:

[001147] The method described in Example 36 was used to prepare examples 101 to 108 using suitable starting materials: Example 109: 4-Isopropyl-2-methyl-9-phenethyl-1-oxa-4,9-diazaspiro[5.5] Undecane

[001148] Step 1. 4-Isopropyl-2-methyl-9-phenethyl-1-oxa-4,9-diazaspiro[5.5] undecan-3-one. To a solution of intermediate 6L (0.168 g, 0.58 mmol) in dry DMF (5 mL), NaH (47 mg, 60 wt% in mineral oil, 1.17 mmol) was added. The reaction mixture was stirred at room temperature for 30 minutes, then 2-bromopropane (0.054 mL, 0.58 mmol) was added and the resulting mixture was stirred at room temperature overnight. Water was added and it was extracted with ethyl acetate. The organic phases were combined, washed with brine, dried over MgSO4, filtered and concentrated to dryness. The residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH/DCM (1:4) to give the title compound (84 mg, 43% yield).

[001149] Step 2. Title compound: To a solution of the product obtained in step 1 (50 mg, 0.15 mmol) in dry THF (1 mL), cooled to 0 °C, lithium aluminum hydride solution ( 0.6 mL, 1 M in THF, 0.6 mmol) was added dropwise. The reaction mixture was stirred at 50 °C for 3 h and then at room temperature overnight. 1 M NaOH was added and the heterogeneous mixture was filtered through a celite pad, washing with THF. The filtrate was concentrated to dryness and the residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH:DCM (1:4) to give the title compound (36 mg, 76% yield).

[001150] HPLC retention time (method B): 4.45 min; DM: 317.2 (M+H).

[001151] This method was used to prepare examples 110 to 111 using suitable starting materials: Example 112: 4-Ethyl-2-methyl-9-phenethyl-1-oxa-4,9-diazaspiro[5.5] undecane

[001152] Step 1. 4-Ethyl-2-methyl-9-phenethyl-1-oxa-4,9-diazaspiro[5.5]undecan-3-one. Following the method described for the preparation of Example 1 but starting from intermediate 5F (220 mg, 0.70 mmol), the title compound was obtained (162 mg, 73% yield).

[001153] Step 2. Title compound: To a solution of the product obtained in step 1 (101 mg, 0.32 mmol) in dry THF (2 mL), cooled to 0 °C, lithium aluminum hydride solution ( 1.28 mL, 1M in THF, 1.28 mmol) was added dropwise. The reaction mixture was stirred at 50 °C overnight. 1 M NaOH was added and the heterogeneous mixture was filtered through a celite pad, washing with THF. The filtrate was concentrated to dryness and the residue was purified by flash chromatography, silica gel, Gradient DCM to MeOH:DCM (1:4) to give the title compound (55 mg, 57% yield).

[001154] HPLC retention time (method B): 3.91 min; MS: 303.2 (M+H).

[001155] This method was used to prepare example 113 using suitable starting materials:

Table of Examples with connection to the g1-Receiver: BIOLOGICAL ACTIVITY Pharmacological study Human g receptor radioligand assay

[001156] To investigate binding properties of test compounds to the human g1 receptor, transfected HEK-293 membranes and [3H](+)-pentazocine (Perkin Elmer, NET-1056), as the radioligand, were used. The assay was performed with 7 μg of membrane suspension, 5 nM [3H](+)-pentazocine in the absence or presence of buffer or 10 μM Haloperidol for total and non-specific binding, respectively. Binding buffer contained 50 mM Tris-HCl at pH 8. Plates were incubated at 37°C for 120 minutes. After the incubation period, the reaction mixture was then transferred to MultiScreen HTS, FC plates (Millipore), filtered and the plates were washed 3 times with ice-cold 10 mM Tris-HCL (pH 7.4). Filters were dried and counted at approximately 40% efficiency on a MicroBeta scintillation recorder (Perkin-Elmer) using EcoScint liquid scintillation cocktail.

Results:

[001157] As this invention is directed to providing a compound or a series of chemically related compounds that act as g1 receptor ligands, it is a very preferred embodiment in which compounds are selected that act as αi receptor ligands and especially compounds that have a binding expressed as Ki which is preferably < 1000 nM, more preferably < 500 nM, even more preferably < 100 nM.

[001158] The following scale was adopted to represent binding to the ai receptor expressed as K: + Ki-ai >= 500 nM ++ Ki-ai < 500 nM +++ Ki-ai < i00 nM

[001159] All compounds prepared in the present application exhibit binding to the ai receptor, in particular the following binding results as shown:

Claims (16)

1. Compound, characterized by the fact that it has the general formula (I): where p is 0 or 1; m is 1, 2 or 3; n is 0, 1 or 2; Y is -CH2- or -C(O)-; X is a bond or -O-; R1 is selected from C1-6 substituted or unsubstituted alkyl, and substituted or unsubstituted monocyclic cycloalkyl; wherein said cycloalkyl in R1, if substituted, is replaced with one or more selected halogen substituents, -R11, -OR11, -NO2, -NR11R11''', NR11C(O)R11', -NR11S(O )2R11', 1. (O)2NR11R11', -NR11C(O)NR11'R11'', -SR11 , -S(O)R11, S(O)2R11, -CN, haloalkyl, haloalkoxy, -C(O )OR11, -C(O)NR11R11', -OCH2CH2OH, -NR11S(O)2NR11'R11'' and C(CH3)2OR11; Additionally, cycloalkyl in R1, if substituted, can also be substituted with or =O; wherein the alkyl, alkenyl or alkynyl in R1, if substituted, is substituted with one or more substituents selected from -OR11, halogen, -CN, haloalkyl, haloalkoxy and -NR11R11'''; wherein R11, R11' and R11'' are independently selected from hydrogen, unsubstituted C1-6 alkyl; and wherein R11''' is selected from hydrogen, C1-6 unsubstituted alkyl, and -Boc; R2 is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heterocyclyl, wherein said cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more selected halogen substituents, -R12, -OR12, -NO2, -NR12R12''', NR12C(O)R12', -NR12S(O)2R12', -S(O)2NR12R12', -NR12C( O)NR12'R12'', -SR12, -S(O)R12, S(O)2R12, -CN, haloalkyl, haloalkoxy, -C(O)OR12, -C(O)NR12R12', -OCH2CH2OH, - NR12S(O)2NR12'R12'' and C(CH3)2OR12; Additionally, non-aromatic cycloalkyl or heterocyclyl in R2, if substituted, may also be substituted with or =O; wherein the alkyl, alkenyl or alkynyl in R2, if substituted, is substituted with one or more substituents selected from -OR12, halogen, -CN, haloalkyl, haloalkoxy and -NR12R12'''; wherein R12, R12' and R12'' are independently selected from hydrogen, unsubstituted C1-6 alkyl; and wherein R12''' is selected from hydrogen, C1-6 unsubstituted alkyl, and -Boc; R3 and R3' are independently selected from hydrogen, or substituted or unsubstituted C1-6 alkyl; alternatively, R3 and R3', taken together with the connecting C atom, may form a substituted or unsubstituted cycloalkyl; R4 and R4' are independently selected from hydrogen, C1-9 substituted or unsubstituted alkyl, -CHOR9 and -C(O)OR9; wherein R9 is selected from hydrogen, or C1-9 unsubstituted alkyl; R5 and R5' are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, -CHOR7 and -C(O)OR7; wherein R7 is selected from hydrogen, or C1-6 unsubstituted alkyl; alternatively, R5 and R5' taken together with the connecting C atom may form a substituted or unsubstituted cycloalkyl or a substituted or unsubstituted non-aromatic heterocyclyl; R6 and R6' are independently selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, C2-6 substituted or unsubstituted alkynyl, -OR10, -CHOR10 and -C(O)OR10; wherein R10 is selected from hydrogen, C1-6 substituted or unsubstituted alkyl, C2-6 substituted or unsubstituted alkenyl, and C2-6 substituted or unsubstituted alkynyl; optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof , or a corresponding solvate thereof; with the following condition applying: when Y is -C(O)- and R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl, then m is 1, X is a bond, n is 0, and R3 is not hydrogen ; the following compounds are also excluded: 2. Compound according to claim 1, characterized by the fact that R3 is selected from hydrogen or unsubstituted methyl; R3' is selected from hydrogen or unsubstituted methyl; alternatively, R3 and R3', taken together with the connecting C atom, can form an unsubstituted cyclopropyl. 3. Compound according to claim 1 or 2, characterized by the fact that the compound of formula (I) is a compound of formula (I'), (Ia'), (Ib') or (Ic') 4. Compound according to any one of claims 1 to 3, characterized in that the compound of formula (I) is a compound of formula (I2') 5. Compound according to any one of claims 1 to 4, characterized in that the compound of formula (I) is a compound of formula (I3') 6. Compound according to any one of claims 1 to 4, characterized by the fact that Y is -C(O)-. 7. Compound according to any one of claims 1 to 6, characterized in that the compound of formula (I) is a compound of formula (I4') 8. Compound according to any one of claims 1 to 7, characterized by the fact that R1 is an unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, sec-butyl, isopentyl, neopentyl and cyclopropyl. 9. Compound according to any one of claims 1 to 8, characterized in that R2 is selected from hydrogen or a substituted or unsubstituted group selected from methyl, ethyl, propyl, isopropyl, isobutyl, tert-butyl, neopentyl, cyclopropyl , phenyl and pyridine. 10. Compound according to any one of claims 1 to 9, characterized in that the compound is selected from optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof . 11. Compound according to any one of claims 1 to 9, characterized in that the compound is selected from optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof . 12. Process for preparing compounds of Formula (I) as defined in any one of claims 1 to 11, characterized in that it comprises: a) an intramolecular cyclization of a compound of formula VIIa or b) the reaction of a compound of formula VIIIH with a compound of formula IX, X or XI, or c1) when Y is CH2, by alkylation of a compound of formula XIV with a compound of formula XV the compound of formula XV being an alkylating agent and V a leaving group, or alternatively by the reductive amination reaction of a compound of formula XIV with a compound of formula XV, the compound of formula XV being an aldehyde and V a C(O)H group; or c2) when Y is C(O), by alkylation of a compound of formula XIV with a compound of formula XV the compound of formula XV being an alkylating agent and V being a leaving group. 13. Use of one or more compounds of Formulas II, IIP, III, IIIP, IVa, IVb, Vb, VbP, Va, VaP, VI, VIIa, VIIb, VIIb, VIIbP, VIIIP, VIIIH, IX, X, XI, XII, XIIP, XIII, XIIIP, XIV, XIVP, XIVH, XXII, XXIIP, XXIIH, XXIII, XXIIIP, XXIIIH, XXIV, XXIVP, XXIVH, XXV, XXVP, XXVH, Ie, XXVIP, XXVIH, XXVIIa, XXVIIb, XXVIIc, If, XXVIIIP, XXVIIIH, Ig, XXIXP, XXIXH, Ih, XXXP, XXXH, XXXI, XXXIP, XXXIH, XXXII, XXXIIP, XXXIIH, XXXIII, XXXIIIP, XXXIIIH, XXXIV, XXXIVP or XXXIVH, wherein R1, R2, R3, R3', R4, R4', R5, R5', R6, R6', X, Y, m, n and p have the meanings as defined in claim 1 for a compound of formula (I), LG represents a leaving group, such as halogen, mesylate, tosylate, or triflate, V represents an aldehyde or other leaving group, such as halogen, mesylate, tosylate, or triflate, Q represents methyl or benzyl, P represents a suitable protecting group, preferably Boc, and P' represents an orthogonal protecting group, preferably 4-methoxybenzyl or benzyl, characterized in that it is for the preparation of compounds of Formula (I) as defined in any one of claims 1 to 10. 14. Pharmaceutical composition, characterized in that it comprises a compound of Formula (I) as defined in any one of claims 1 to 10 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier, adjuvant or vehicle. 15. Use of a compound as defined in any one of claims 1 to 10, characterized by the fact that it is in the preparation of a medicament for the treatment of drug abuse or addiction. 16. Compounds, characterized by the fact that they are selected from among optionally, in the form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in the form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof .