AR069480A1 - DERIVATIVES OF 2-AMINO-PYRIMIDINE - Google Patents
DERIVATIVES OF 2-AMINO-PYRIMIDINEInfo
- Publication number
- AR069480A1 AR069480A1 ARP080105118A ARP080105118A AR069480A1 AR 069480 A1 AR069480 A1 AR 069480A1 AR P080105118 A ARP080105118 A AR P080105118A AR P080105118 A ARP080105118 A AR P080105118A AR 069480 A1 AR069480 A1 AR 069480A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- atoms
- optionally substituted
- atom
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Estos compuestos son utiles como antagonistas del receptor H4. Se describen además intermediarios y procesos de preparacion de los compuestos. Reivindicacion 1: Un compuesto caracterizado por Ia formula (1) donde: R1 representa C2-8 alquilo o C3-7 cicloalquilo-C0-4 alquilo, donde dicho grupo C3-7 cicloalquilo puede estar opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados entre C1-4 alquilo, fenilo y fluoro; R2 y R3 forman, junto con el átomo de N al cual están unidos, un grupo heterocíclico saturado que puede ser monocíclico de 4 a 7 átomos, bicíclico con puente de 7 a 8 átomos o bicíclico fusionado de 8 a 12 átomos, donde dicho grupo heterocíclico puede contener un máximo de dos átomos de N y no contiene ningun otro heteroátomo, y puede estar opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados entre C1-4 alquilo y NRaRb, con la condicion de que el grupo heterocíclico o bien contenga 2 átomos de N y no esté sustituido por un grupo NRaRb, o bien contenga un 1 átomo de N y esté sustituido por un grupo NRaRb; o bien R2 representa H o C1-4 alquilo, y R3 representa azetidinilo, pirrolidinilo, piperidinilo o azepanilo, que pueden estar opcionalmente sustituidos por uno o más grupos C1-4 alquilo; y Ra representa H o C1-4 alquilo; Rb representa H o C1-4 alquilo; o bien Ra y Rb forman, junto con el átomo de N al cual están unidos, un grupo azetidinilo, pirrolidinilo, piperidinilo o azepanilo, que puede estar opcionalmente sustituido por uno o más grupos C1-4 alquilo; con la condicion de que el compuesto de formula 1 no es 4-(4-etil-piperazin-1-il)-6-propil-pirimidin-2-amina; o una sal del mismo. Reivindicacion 17: Un compuesto caracterizado por la formula (2) donde: R1' representa C1-6 alquilo o C3-7 cicloalquilo-C0-2 alquilo, donde dicho grupo C3-7 cicloalquilo puede estar opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados entre C1-4 alquilo, fenilo y fluoro; R2 y R3 forman, junto con el átomo de N al cual están unidos, un grupo heterocíclico saturado que puede ser monocíclico de 4 a 7 átomos, bicíclico con puente de 7 a 8 átomos o bicíclico fusionado de 8 a 12 átomos, donde dicho grupo heterocíclico puede contener un máximo de dos átomos de N y no contiene ningun otro heteroátomo, y puede estar opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados entre C1-4 alquilo y NRaRb, con la condicion de que el grupo heterocíclico o bien contenga 2 átomos de N y no esté sustituido por un grupo NRaRb, o bien contenga un 1 átomo de N y esté sustituido por un grupo NRaRb; o bien R2 representa H o C1-4 alquilo, y R3 representa azetidinilo, pirrolidinilo, piperidinilo o azepanilo, que pueden estar opcionalmente sustituidos por uno o más grupos C1-4 alquilo; y R2 representa H o C1-4 alquilo; Rb representa H o C1-4 alquilo; o bien Ra y Rb forman, junto con el átomo de N al cual están unidos, un grupo azetidinilo, pirrolidinilo, piperidinilo o azepanilo, que puede estar opcionalmente sustituido por uno o más grupos C1-4 alquilo; o una sal del mismo.These compounds are useful as H4 receptor antagonists. Intermediates and preparation processes of the compounds are also described. Claim 1: A compound characterized by the formula (1) wherein: R1 represents C2-8 alkyl or C3-7 cycloalkyl-C0-4 alkyl, wherein said C3-7 cycloalkyl group may be optionally substituted by one or more substituents independently selected from C1-4 alkyl, phenyl and fluoro; R2 and R3 form, together with the N atom to which they are attached, a saturated heterocyclic group that can be monocyclic of 4 to 7 atoms, bicyclic with bridge of 7 to 8 atoms or bicyclic fused of 8 to 12 atoms, where said group heterocyclic may contain a maximum of two N atoms and does not contain any other heteroatom, and may be optionally substituted by one or more substituents independently selected from C1-4 alkyl and NRaRb, with the proviso that the heterocyclic group or contains 2 atoms of N and is not substituted by an NRaRb group, or contains a 1 N atom and is substituted by an NRaRb group; or R2 represents H or C1-4 alkyl, and R3 represents azetidinyl, pyrrolidinyl, piperidinyl or azepanyl, which may be optionally substituted by one or more C1-4 alkyl groups; and Ra represents H or C1-4 alkyl; Rb represents H or C1-4 alkyl; or Ra and Rb together with the N atom to which they are attached, an azetidinyl, pyrrolidinyl, piperidinyl or azepanyl group, which may be optionally substituted by one or more C1-4 alkyl groups; with the proviso that the compound of formula 1 is not 4- (4-ethyl-piperazin-1-yl) -6-propyl-pyrimidin-2-amine; or a salt thereof. Claim 17: A compound characterized by the formula (2) wherein: R1 'represents C1-6 alkyl or C3-7 cycloalkyl-C0-2 alkyl, wherein said C3-7 cycloalkyl group may be optionally substituted by one or more independently selected substituents between C1-4 alkyl, phenyl and fluoro; R2 and R3 form, together with the N atom to which they are attached, a saturated heterocyclic group that can be monocyclic of 4 to 7 atoms, bicyclic with bridge of 7 to 8 atoms or bicyclic fused of 8 to 12 atoms, where said group heterocyclic may contain a maximum of two N atoms and does not contain any other heteroatom, and may be optionally substituted by one or more substituents independently selected from C1-4 alkyl and NRaRb, with the proviso that the heterocyclic group or contains 2 atoms of N and is not substituted by an NRaRb group, or contains a 1 N atom and is substituted by an NRaRb group; or R2 represents H or C1-4 alkyl, and R3 represents azetidinyl, pyrrolidinyl, piperidinyl or azepanyl, which may be optionally substituted by one or more C1-4 alkyl groups; and R2 represents H or C1-4 alkyl; Rb represents H or C1-4 alkyl; or Ra and Rb together with the N atom to which they are attached, an azetidinyl, pyrrolidinyl, piperidinyl or azepanyl group, which may be optionally substituted by one or more C1-4 alkyl groups; or a salt thereof.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07381074 | 2007-11-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069480A1 true AR069480A1 (en) | 2010-01-27 |
Family
ID=39197144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080105118A AR069480A1 (en) | 2007-11-30 | 2008-11-25 | DERIVATIVES OF 2-AMINO-PYRIMIDINE |
Country Status (5)
| Country | Link |
|---|---|
| AR (1) | AR069480A1 (en) |
| CL (1) | CL2008003537A1 (en) |
| PE (1) | PE20091035A1 (en) |
| TW (1) | TW200936570A (en) |
| WO (1) | WO2009068512A1 (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101054325B1 (en) | 2006-03-31 | 2011-08-04 | 얀센 파마슈티카 엔.브이. | Benzoimidazol-2-yl pyrimidine and pyrazine as histamine H4 receptor modulators |
| KR20090028819A (en) | 2006-07-11 | 2009-03-19 | 얀센 파마슈티카 엔.브이. | Benzofuro- and benzothienopyryimidine modulators of the histamine h4 receptor |
| TW200904437A (en) | 2007-02-14 | 2009-02-01 | Janssen Pharmaceutica Nv | 2-aminopyrimidine modulators of the histamine H4 receptor |
| CA2705719C (en) | 2007-09-14 | 2016-10-11 | Janssen Pharmaceutica N.V. | Thieno-and furo-pyrimidine modulators of the histamine h4 receptor |
| MY158927A (en) | 2008-06-12 | 2016-11-30 | Janssen Pharmaceutica Nv | Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine h4 receptor |
| US9371311B2 (en) | 2008-06-30 | 2016-06-21 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine derivatives |
| EP2201982A1 (en) | 2008-12-24 | 2010-06-30 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Histamine H4 receptor antagonists for the treatment of vestibular disorders |
| TWI478714B (en) | 2009-10-29 | 2015-04-01 | Vectura Ltd | N-containing heteroaryl derivatives as jak3 kinase inhibitors |
| WO2011076878A1 (en) * | 2009-12-23 | 2011-06-30 | Palau Pharma, S.A. | Aminoalkylpyrimidine derivatives as histamine h4 receptor antagonists |
| EP2746265B1 (en) | 2011-08-18 | 2015-11-18 | Nippon Shinyaku Co., Ltd. | HETEROCYCLIC DERIVATIVE AS MICROSOMAL PROSTAGLANDIN E SYNTHASE (mPGEs) INHIBITOR |
| PT2858647T (en) | 2012-06-08 | 2018-10-03 | Sensorion | H4 receptor inhibitors for treating tinnitus |
| WO2014010748A1 (en) * | 2012-07-10 | 2014-01-16 | Shionogi & Co., Ltd. | Cyclopropane derivative having bace1 inhibiting activity |
| SG11201507117XA (en) | 2013-03-06 | 2015-10-29 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor |
| WO2017160925A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| WO2017160922A1 (en) * | 2016-03-16 | 2017-09-21 | Kalyra Pharmaceuticals, Inc. | Analgesic compounds |
| GB202005858D0 (en) * | 2020-04-22 | 2020-06-03 | Heptares Therapeutics Ltd | H4 Antagonist compounds |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1505064A1 (en) * | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| WO2005054239A1 (en) * | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| AU2006290715A1 (en) * | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 2-aminopyrimidine derivatives as modulators of the histamine H4 receptor activity |
| NL2000323C2 (en) * | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine derivatives. |
| WO2008031556A2 (en) * | 2006-09-12 | 2008-03-20 | Ucb Pharma, S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| US7985745B2 (en) * | 2006-10-02 | 2011-07-26 | Abbott Laboratories | Method for pain treatment |
| TW200904437A (en) * | 2007-02-14 | 2009-02-01 | Janssen Pharmaceutica Nv | 2-aminopyrimidine modulators of the histamine H4 receptor |
-
2008
- 2008-11-25 WO PCT/EP2008/066110 patent/WO2009068512A1/en active Application Filing
- 2008-11-25 PE PE2008001971A patent/PE20091035A1/en not_active Application Discontinuation
- 2008-11-25 AR ARP080105118A patent/AR069480A1/en unknown
- 2008-11-26 TW TW097145757A patent/TW200936570A/en unknown
- 2008-11-27 CL CL2008003537A patent/CL2008003537A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW200936570A (en) | 2009-09-01 |
| WO2009068512A1 (en) | 2009-06-04 |
| CL2008003537A1 (en) | 2009-03-06 |
| PE20091035A1 (en) | 2009-07-16 |
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| FB | Suspension of granting procedure |