Nothing Special   »   [go: up one dir, main page]

HRP20040178B1 - Derivati piperidina kao antagonisti nmda receptora - Google Patents

Derivati piperidina kao antagonisti nmda receptora

Info

Publication number
HRP20040178B1
HRP20040178B1 HRP20040178AA HRP20040178A HRP20040178B1 HR P20040178 B1 HRP20040178 B1 HR P20040178B1 HR P20040178A A HRP20040178A A HR P20040178AA HR P20040178 A HRP20040178 A HR P20040178A HR P20040178 B1 HRP20040178 B1 HR P20040178B1
Authority
HR
Croatia
Prior art keywords
group
formula
compounds
oxo
alkyl
Prior art date
Application number
HRP20040178AA
Other languages
English (en)
Inventor
György DOMÁNY
Csilla HORVÁTH
Sándor FARKAS
Gisella Bartáné Szalai
József Nagy
Sándor KOLOK
Éva KOVÁCSNÉ BOZÓ
István BORZA
István VÁGÓ
Attila Bielik
Györgyi Ingáczné Szendrei
György Keserú
Original Assignee
Richter Gedeon Vegyészeti Gyár RT
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from HU0103055A external-priority patent/HU226978B1/hu
Priority claimed from HU0202213A external-priority patent/HU225905B1/hu
Application filed by Richter Gedeon Vegyészeti Gyár RT filed Critical Richter Gedeon Vegyészeti Gyár RT
Publication of HRP20040178A2 publication Critical patent/HRP20040178A2/hr
Publication of HRP20040178B1 publication Critical patent/HRP20040178B1/hr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Biochemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)

Abstract

Prezentirani izum se prvo odnosi na nove derivate amida karboksilne kiseline formule (I)gdje su oba -(CHR)- i -(CHR)-CH-CH-skupina, susjedne V i U skupine zajedno formiraju i s jednim ili više identičnih ili različitih dodatnih hetero atoma i -CH= i/ili -CH-skupinama po izboru substituiranim 4-7 članim homo- ili heterociklični prstenom, preferirano morfolin, pirol, pirolidin, okso- ili tiokso-pirolidin, pirazol, pirazolidin, itnidazol, imidazolidin, okso- ili tiokso-imidazol ili imidazolidin, 1,4-oksazolin, oksazol, oksazolidin, okso- ili tiokso-oksazolidin, ili 3-okso-1,4-oksazin prsten, X je -CO-skupina, W je -CO-, -CH- ili -CH(-alkil)- skupina - gdje je alkil C-Calkil skupina, Y je atom kisika, također C-Calkilen, C-Calkinilen, cikloalkilen, aminokarbonil, -NH-, -N(alkil)-, -CHO-, CH(OH)-, -OCH- skupina, -gdje alkil je C-Calkil skupina, Z je vodik ili atom halogena, nitro, amino, C-Calkil, C-Calkoksi, cijano, trifluormetil, hidroksil ili karboksil skupina, i optički antipodi ili racemati i/ili njihove farmaceutski prihvatljive soli formirane s kiselinama ili bazama i na farmaceutske sastave koji sadržavaju spojeve amida karboksilne kiseline formule (I) ili njihove optičke antipode ili racemate ili, soli kao aktivne tvari. Nadalje predmet izuma su postupci proizvodnje spojeva amida karboksilne kiseline formule (I), i farmaceutska proizvodnja lijekova koji sadržavaj u te spojeve kao i na postupak tretiranja s tim spojevima, što znači aplikaciju sisavcima - uključujući ljude - učinkovite količine/količina aktivnih tvari formule (I) prezentiranog izuma isto tako i lijekovi. Novi derivati amida karboksilne kiseline formule (I) prezentiranog i
HRP20040178AA 2001-07-24 2004-02-23 Derivati piperidina kao antagonisti nmda receptora HRP20040178B1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
HU0103055A HU226978B1 (en) 2001-07-24 2001-07-24 New carboxylic acid amide compounds, process for their preparation and pharmaceutical compositions containing them and their use
HU0202213A HU225905B1 (en) 2002-07-10 2002-07-10 Solid-supported parallel synthesis of new carboxylic acid amide derivatives
PCT/HU2002/000071 WO2003010159A1 (en) 2001-07-24 2002-07-23 Piperidine derivatives as nmda receptor antagonists

Publications (2)

Publication Number Publication Date
HRP20040178A2 HRP20040178A2 (en) 2005-04-30
HRP20040178B1 true HRP20040178B1 (hr) 2013-05-31

Family

ID=90001553

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20040178AA HRP20040178B1 (hr) 2001-07-24 2004-02-23 Derivati piperidina kao antagonisti nmda receptora

Country Status (33)

Country Link
US (1) US7435744B2 (hr)
EP (1) EP1409477B1 (hr)
JP (1) JP4322113B2 (hr)
KR (1) KR100890676B1 (hr)
CN (1) CN100413860C (hr)
AT (1) ATE408611T1 (hr)
AU (1) AU2002313566B2 (hr)
BG (1) BG66441B1 (hr)
BR (1) BR0211393A (hr)
CA (1) CA2453383C (hr)
CO (1) CO5560570A2 (hr)
CY (1) CY1109401T1 (hr)
CZ (1) CZ2004233A3 (hr)
DE (1) DE60228969D1 (hr)
DK (1) DK1409477T3 (hr)
EA (1) EA010162B1 (hr)
EE (1) EE05429B1 (hr)
ES (1) ES2312603T3 (hr)
HK (1) HK1063464A1 (hr)
HR (1) HRP20040178B1 (hr)
IL (1) IL159393A (hr)
IS (1) IS7066A (hr)
MX (1) MXPA04000737A (hr)
NO (1) NO327099B1 (hr)
NZ (1) NZ530055A (hr)
PL (1) PL216636B1 (hr)
PT (1) PT1409477E (hr)
RS (1) RS50767B (hr)
SI (1) SI1409477T1 (hr)
SK (1) SK287726B6 (hr)
UA (1) UA77684C2 (hr)
WO (1) WO2003010159A1 (hr)
ZA (1) ZA200400417B (hr)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10210779A1 (de) * 2002-03-12 2003-10-09 Merck Patent Gmbh Cyclische Amide
PA8575901A1 (es) * 2002-07-18 2004-07-20 Pfizer Prod Inc Derivados de piperidina novedosos
ES2222833B1 (es) * 2003-07-30 2006-03-01 Laboratorios Del Dr. Esteve, S.A. Compuestos piperidinicos 1,4-disustituidos, su preparacion y su uso como medicamentos.
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
JP4737418B2 (ja) * 2003-09-25 2011-08-03 塩野義製薬株式会社 Ｎｍｄａ受容体拮抗作用を有するピペリジン誘導体
WO2005039564A1 (en) * 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
HUP0401522A2 (en) * 2004-07-29 2006-04-28 Richter Gedeon Vegyeszet New 4-benzylidene-piperidine derivatives, pharmaceutical compositions containing the same and process for their preparation
HU227000B1 (en) * 2004-07-29 2010-04-28 Richter Gedeon Nyrt Nmda receptor antagonist benzoyl urea derivatives, and pharmaceutical compositions containing them
EP2520567A3 (en) * 2006-02-23 2012-12-12 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
HUP0600809A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
HUP0600810A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
HUP0600808A3 (en) * 2006-10-27 2008-09-29 Richter Gedeon Nyrt New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them
EP1918281A1 (en) * 2006-11-02 2008-05-07 Laboratorios del Dr. Esteve S.A. Phenylamino-substituted piperidine compounds, their preparation and use as medicaments
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
DK2091948T3 (da) 2006-11-30 2012-07-23 Probiodrug Ag Nye inhibitorer af glutaminylcyclase
ZA200905537B (en) 2007-03-01 2010-10-27 Probiodrug Ag New use of glutaminyl cyclase inhibitors
US9656991B2 (en) 2007-04-18 2017-05-23 Probiodrug Ag Inhibitors of glutaminyl cyclase
US20110251212A1 (en) * 2007-08-21 2011-10-13 Shionogi & Co., Ltd. Piperazine derivatives
DE102007047737A1 (de) * 2007-10-05 2009-04-30 Merck Patent Gmbh Piperidin- und Piperazinderivate
MX2010004431A (es) * 2007-10-27 2010-05-13 Richter Gedeon Nyrt Nuevos derivados no peptidicos como antagonistas b1 de la bradiquinina.
US20100010044A1 (en) * 2008-07-08 2010-01-14 Forest Laboratories Holdings Limited Novel crystalline form of 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-n-(2-oxo-2,3-dihydro-benzoxazol-6-yl)-acetamide
EP2331097A4 (en) * 2008-08-21 2011-12-28 Richter Gedeon Nyrt METHOD FOR TREATING CNS DISEASES
WO2010022300A1 (en) * 2008-08-21 2010-02-25 Forest Laboratories Holdings Limited Methods for treating neuropathic pain
WO2010068794A2 (en) 2008-12-10 2010-06-17 The General Hospital Corporation Hif inhibitors and use thereof
HUP0900130A3 (en) 2009-03-03 2012-02-28 Richter Gedeon Nyrt Novel crystalline hydrate, amorphous and polymorphic forms of dihydro-benzoxazole-6-yl-acetamide derivative and processes for their preparation
JP5934645B2 (ja) 2009-09-11 2016-06-15 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体
EP2512241A4 (en) 2009-12-15 2013-04-03 Neurop Inc COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL DISEASES
AU2011216950A1 (en) 2010-02-16 2012-08-23 Pfizer Inc. (R)-4-((4-((4-(tetrahydrofuran-3-yloxy) benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol, a partial agonist of 5-HT4 receptors
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
MX2012010470A (es) 2010-03-10 2012-10-09 Probiodrug Ag Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5).
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
HUP1000424A2 (en) 2010-08-11 2012-05-02 Richter Gedeon Nyrt Use of radiprodil in attention deficit hyperactivity disorder
WO2012123563A1 (en) 2011-03-16 2012-09-20 Probiodrug Ag Benz imidazole derivatives as inhibitors of glutaminyl cyclase
DK2921485T3 (en) * 2011-12-27 2018-11-12 Bayer Cropscience Ag isoxazole
JP6042968B2 (ja) 2012-04-20 2016-12-14 ユセベ ファルマ ソシエテ アノニム パーキンソン病の処置方法
US9868730B2 (en) 2013-02-18 2018-01-16 The Trustees Of Columbia University In The City Of New York Kappa opioid receptor selective compounds, compositions, and uses thereof
JP2017538678A (ja) * 2014-11-05 2017-12-28 フレクサス・バイオサイエンシーズ・インコーポレイテッドＦｌｅｘｕｓ Ｂｉｏｓｃｉｅｎｃｅｓ， Ｉｎｃ． 免疫調節剤
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
CN108271370B (zh) * 2015-09-25 2021-03-19 (由卫生与公众服务部部长代表的)美利坚合众国 作为p2y14受体拮抗剂的三唑衍生物
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
CA3083331A1 (en) 2017-12-08 2019-06-13 Boehringer Ingelheim International Gmbh Imidazopyridine derivatives and the use thereof as medicament
EP3724177A1 (en) * 2017-12-12 2020-10-21 Phenex Discovery Verwaltungs-GmbH Oxalamides as modulators of indoleamine 2,3-dioxygenase
JP7093469B2 (ja) 2018-10-17 2022-06-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ４－ピリジニルメチル－モルホリン誘導体および医薬としてのその使用
IL282142B2 (en) 2018-10-17 2024-04-01 Boehringer Ingelheim Int The history of 4-pyrazine-2-ilmethyl-morpholine and its use as a medicine
US11104670B2 (en) 2018-10-17 2021-08-31 Boehringer Ingelheim International Gmbh 4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament
WO2020245136A1 (en) 2019-06-04 2020-12-10 Boehringer Ingelheim International Gmbh Purine derivatives, as nr2b negative modulators and the use thereof as medicament, in particular for treating depressive disorders
CN113234036B (zh) * 2021-05-12 2023-07-14 斯莱普泰(上海)生物医药科技有限公司 Nmda受体拮抗剂及其用途
WO2023014956A1 (en) 2021-08-06 2023-02-09 Grin Therapeutics, Inc. Formulations of radiprodil
CN114163388A (zh) * 2021-12-15 2022-03-11 陕西汉江药业集团股份有限公司 芬苯达唑中的杂质i、杂质ⅱ和杂质ⅲ的制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2672286A1 (fr) * 1991-01-31 1992-08-07 Synthelabo Derives de 1-(4-chlorophenyl)-2-[4-(phenylmethyl)piperidin-1-yl]ethanol, leur preparation et leur application en therapeutique.
EP0648744A1 (en) * 1993-09-02 1995-04-19 F. Hoffmann-La Roche Ag Phenylalkanolamine derivatives as antagonists of the NMDA receptor
WO1997023216A1 (en) * 1995-12-22 1997-07-03 Warner-Lambert Company 4-substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
EP0824098A1 (en) * 1996-07-19 1998-02-18 F. Hoffmann-La Roche Ag 4-hydroxy-piperidine derivatives
US6048900A (en) * 1998-02-13 2000-04-11 Bayer Corporation Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE254999C (hr)
US2324123A (en) 1941-07-08 1943-07-13 Eastman Kodak Co Fog inhibitor for photographic developers
US3260723A (en) 1963-08-27 1966-07-12 Parke Davis & Co 4-phenoxy piperidines; alpha4-phenoxy piperideines
NL6501323A (hr) 1965-02-02 1966-08-03
US3632767A (en) 1968-02-12 1972-01-04 Mallinckrodt Chemical Works Treatment of depression with 4-substituted piperidines
AU639529B2 (en) 1987-03-04 1993-07-29 Higuchi, Yoshinari Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
WO1990014087A1 (en) 1989-05-17 1990-11-29 Pfizer Inc. 2-piperidino-1-alkanol derivatives as antiischemic agents
US5436255A (en) 1992-07-23 1995-07-25 Pfizer Inc. Method of treating diseases susceptable to treatment by blocking NMDA-receptors
ZA9610736B (en) 1995-12-22 1997-06-27 Warner Lambert Co 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists
ZA9610738B (en) 1995-12-22 1997-06-24 Warner Lambert Co Subtype selective nmda receptor ligands and the use thereof
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
AU1463997A (en) 1995-12-22 1997-07-17 Acea Pharmaceuticals, Inc. Subtype-selective nmda receptor ligands and the use thereof
DE19643790A1 (de) 1996-10-30 1998-05-07 Merck Patent Gmbh Benzoxazol-Derivat
WO1998035944A1 (en) * 1997-02-14 1998-08-20 Bayer Corporation Amides as npy5 receptor antagonists
AU760800B2 (en) 1997-10-24 2003-05-22 Warner-Lambert Company Method for treating disease-related or drug-induced dyskinesias
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
WO2000025109A1 (en) 1998-10-28 2000-05-04 Scofield Dillon F Electrodynamic particle size analyzer
US6399631B1 (en) * 1999-07-23 2002-06-04 Pfizer Inc. Carbazole neuropeptide Y5 antagonists
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
US6316474B1 (en) 1999-10-29 2001-11-13 Merck & Co., Inc. 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists
US6291499B1 (en) 1999-10-29 2001-09-18 Merck & Co., Inc. 2-cyclohexyl benzimidazole NMDA/NR2B antagonists
CA2386441A1 (en) 1999-10-29 2001-05-03 Merck Sharp & Dohme Limited Method to treat pain utilizing benzimidazole nmda/nr2b antagonists
US6432976B1 (en) 1999-10-29 2002-08-13 Merck & Co., Inc. 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
US6369076B1 (en) 1999-10-29 2002-04-09 Merck & Co. Inc. 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
US6489477B1 (en) 1999-10-29 2002-12-03 Merck & Co., Inc. 2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2672286A1 (fr) * 1991-01-31 1992-08-07 Synthelabo Derives de 1-(4-chlorophenyl)-2-[4-(phenylmethyl)piperidin-1-yl]ethanol, leur preparation et leur application en therapeutique.
EP0648744A1 (en) * 1993-09-02 1995-04-19 F. Hoffmann-La Roche Ag Phenylalkanolamine derivatives as antagonists of the NMDA receptor
WO1997023216A1 (en) * 1995-12-22 1997-07-03 Warner-Lambert Company 4-substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
EP0824098A1 (en) * 1996-07-19 1998-02-18 F. Hoffmann-La Roche Ag 4-hydroxy-piperidine derivatives
US6048900A (en) * 1998-02-13 2000-04-11 Bayer Corporation Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists

Also Published As

Publication number Publication date
BR0211393A (pt) 2004-08-17
WO2003010159A8 (en) 2004-02-12
SK287726B6 (en) 2011-07-06
HK1063464A1 (en) 2004-12-31
EA010162B1 (ru) 2008-06-30
NO327099B1 (no) 2009-04-20
UA77684C2 (en) 2007-01-15
CA2453383A1 (en) 2003-02-06
RS103903A (en) 2007-02-05
JP2005515968A (ja) 2005-06-02
US7435744B2 (en) 2008-10-14
IL159393A0 (en) 2004-06-01
NO20040307L (no) 2004-03-23
NZ530055A (en) 2005-07-29
SI1409477T1 (sl) 2009-02-28
CN100413860C (zh) 2008-08-27
CA2453383C (en) 2010-04-06
EA200400213A1 (ru) 2004-08-26
EP1409477B1 (en) 2008-09-17
ES2312603T3 (es) 2009-03-01
CO5560570A2 (es) 2005-09-30
KR100890676B1 (ko) 2009-03-26
PL216636B1 (pl) 2014-04-30
AU2002313566B2 (en) 2007-05-24
KR20040041152A (ko) 2004-05-14
WO2003010159A1 (en) 2003-02-06
PT1409477E (pt) 2008-11-20
ATE408611T1 (de) 2008-10-15
BG108592A (bg) 2005-03-31
MXPA04000737A (es) 2004-07-08
CN1556805A (zh) 2004-12-22
IL159393A (en) 2011-01-31
SK1022004A3 (en) 2004-07-07
RS50767B (sr) 2010-08-31
EE05429B1 (et) 2011-06-15
HRP20040178A2 (en) 2005-04-30
CY1109401T1 (el) 2014-07-02
DK1409477T3 (da) 2008-12-08
DE60228969D1 (hr) 2008-10-30
US20040157886A1 (en) 2004-08-12
ZA200400417B (en) 2005-07-27
JP4322113B2 (ja) 2009-08-26
PL367259A1 (en) 2005-02-21
BG66441B1 (bg) 2014-08-29
CZ2004233A3 (cs) 2004-12-15
IS7066A (is) 2003-12-05
EE200400058A (et) 2004-04-15
EP1409477A1 (en) 2004-04-21
AU2002313566B8 (en) 2003-02-18

Similar Documents

Publication Publication Date Title
HRP20040178B1 (hr) Derivati piperidina kao antagonisti nmda receptora
ES2380904T3 (es) Composiciones farmacéuticas que tienen un efecto analgésico y contienen 1-bencil-1-hidroxi-2,3-diamino-propil aminas, amidas del ácido 3-bencil-3-hidroxi-2-amino propiónico o compuestos relacionados
HUP0400992A2 (hu) Karbonsavval helyettesített oxazol-származékok, eljárás előállításukra és PPAR-alfa- és -gamma-aktivátorként való alkalmazásuk diabétesz kezelésére felhasználható gyógyszerek készítésére
TNSN07018A1 (en) New 4-benzylidene-piperidin derivatives
RU2003105805A (ru) Производные 4-фенилпиридина в качестве антагонистов рецепторов нейрокинина-1
SE9703377D0 (sv) New compounds
HUP0003577A2 (hu) Tetrahidro-gamma-karbolinok, eljárás előállításukra, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
US20120101129A1 (en) Methylphenidate Derivatives and Uses of Them
AR009374A1 (es) Compuestos novedosos antagonistas de nmda (n-metil-d-aspartato), composicion farmaceutica y usos para fabricar medicamentos.
JPS6117544A (ja) 新規化合物，その製造方法及び用途
US4518783A (en) Process for producing (-)-2-[1-(2,6-dichlorophenoxy)-ethyl]-1,3-diazacyclopent-2-ene
ZA200300262B (en) Carboxamide compounds and their use as antagonists of a human 11CBy receptor.
AR009556A1 (es) Compuestos derivados de indazol triciclico, procedimiento de preparacion del mismo; medicamento y composicion farmaceutica que lo contienen
RU2008149076A (ru) Действующее вещество для лечения алкогольной зависимости, фармацевтическая композиция, лекарственное средство, способ получения фармацевтической композиции и лекарственного средства и способ лечения
BR112019024155A2 (pt) Compostos analgésicos
AU2018203022B2 (en) 3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and/or immunostimulant activity
TW202416973A (zh) Ｋｉｆ１８ａ抑制劑及其用途
DE69806248D1 (de) Pharmazeutische zubereitung zur behandlung sogenannter rastloser beine
JPS61210092A (ja) ジヒドロピリジン−５−ホスホン酸ジアミド誘導体
KR800001680B1 (ko) 벤질아민의 제조방법
JPS61140581A (ja) １，４‐ジヒドロピリジン誘導体
YU115491A (sh) Novi ergolinski derivati 2-propihilamina i postupak za njihovo pripremanje
FR2633292B1 (fr) Nouveaux derives de la 20,21-dinoreburnamenine substitues en 15 par un groupement amine, leur procede de preparation et les intermediaires ainsi obtenus, leur application comme medicaments et les compositions pharmaceutiques les reenfermant
HRP20120434T2 (hr) Spojevi 4-oksadiazolil-piperidina i njihova uporaba
AU2012241156A1 (en) 3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and/or immunostimulant activity

Legal Events

Date Code Title Description
A1OB Publication of a patent application
AIPI Request for the grant of a patent on the basis of a substantive examination of a patent application
B1PR Patent granted
PNAN Change of the applicant name, address/residence

Owner name: RICHTER GEDEON NYRT., HU

PPPP Transfer of rights

Owner name: UCB PHARMA S.A., BE

ODRP Renewal fee for the maintenance of a patent

Payment date: 20190624

Year of fee payment: 18

ODRP Renewal fee for the maintenance of a patent

Payment date: 20200721

Year of fee payment: 19

ODRP Renewal fee for the maintenance of a patent

Payment date: 20210722

Year of fee payment: 20

PB20 Patent expired after termination of 20 years

Effective date: 20220723