RU2341515C2 - Ацетиленовые производные, способ их получения, фармацевтическая композиция на их основе и их применение в качестве антагонистов метаботропных глутаматных рецепторов (mglur5) - Google Patents

Ацетиленовые производные, способ их получения, фармацевтическая композиция на их основе и их применение в качестве антагонистов метаботропных глутаматных рецепторов (mglur5) Download PDF

Info

Publication number
RU2341515C2
RU2341515C2 RU2004120781/04A RU2004120781A RU2341515C2 RU 2341515 C2 RU2341515 C2 RU 2341515C2 RU 2004120781/04 A RU2004120781/04 A RU 2004120781/04A RU 2004120781 A RU2004120781 A RU 2004120781A RU 2341515 C2 RU2341515 C2 RU 2341515C2
Authority
RU
Russia
Prior art keywords
hydroxy
carboxylic acid
meta
ethyl
3ars
Prior art date
Application number
RU2004120781/04A
Other languages
English (en)
Russian (ru)
Other versions
RU2004120781A (ru
Inventor
Фабрицио ГАСПАРИНИ (CH)
Фабрицио ГАСПАРИНИ
Ив ОБЕРСОН (CH)
Ив Оберсон
Сильвио ОФНЕР (CH)
Сильвио Офнер
Каспар ЦИММЕРМАНН (CH)
Каспар Циммерманн
Терэнс В. ХАРТ (GB)
Терэнс В. ХАРТ
Original Assignee
Новартис Аг
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=9926969&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2341515(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU2004120781A publication Critical patent/RU2004120781A/ru
Application granted granted Critical
Publication of RU2341515C2 publication Critical patent/RU2341515C2/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/23Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
RU2004120781/04A 2001-12-04 2002-12-03 Ацетиленовые производные, способ их получения, фармацевтическая композиция на их основе и их применение в качестве антагонистов метаботропных глутаматных рецепторов (mglur5) RU2341515C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0128996.6 2001-12-04
GBGB0128996.6A GB0128996D0 (en) 2001-12-04 2001-12-04 Organic compounds

Publications (2)

Publication Number Publication Date
RU2004120781A RU2004120781A (ru) 2006-01-10
RU2341515C2 true RU2341515C2 (ru) 2008-12-20

Family

ID=9926969

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2004120781/04A RU2341515C2 (ru) 2001-12-04 2002-12-03 Ацетиленовые производные, способ их получения, фармацевтическая композиция на их основе и их применение в качестве антагонистов метаботропных глутаматных рецепторов (mglur5)

Country Status (31)

Country Link
US (4) US7348353B2 (https=)
EP (1) EP1453512B8 (https=)
JP (2) JP4176020B2 (https=)
KR (2) KR100980901B1 (https=)
CN (2) CN101366714B (https=)
AR (2) AR037682A1 (https=)
AT (1) ATE327755T1 (https=)
AU (1) AU2002358585B2 (https=)
BR (1) BR0214666A (https=)
CA (1) CA2466560C (https=)
CO (1) CO5590929A2 (https=)
CY (1) CY1105460T1 (https=)
DE (1) DE60211944T2 (https=)
DK (1) DK1453512T3 (https=)
EC (1) ECSP045139A (https=)
EG (1) EG24936A (https=)
ES (1) ES2263842T3 (https=)
GB (1) GB0128996D0 (https=)
HU (1) HU229429B1 (https=)
IL (1) IL161990A0 (https=)
MX (1) MXPA04005456A (https=)
MY (1) MY137774A (https=)
NO (1) NO327005B1 (https=)
NZ (1) NZ533266A (https=)
PE (1) PE20030640A1 (https=)
PL (1) PL212996B1 (https=)
PT (1) PT1453512E (https=)
RU (1) RU2341515C2 (https=)
TW (1) TWI328578B (https=)
WO (1) WO2003047581A1 (https=)
ZA (1) ZA200403713B (https=)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0128996D0 (en) * 2001-12-04 2002-01-23 Novartis Ag Organic compounds
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
GB0325956D0 (en) * 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING PEOPLE WITH METABOLIC AND ANTHROPOMETRIC DISORDER
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508314D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
JP2010502664A (ja) 2006-09-11 2010-01-28 ノバルティス アクチエンゲゼルシャフト 代謝型グルタミン酸受容体の調節剤としてのニコチン酸誘導体
MX354786B (es) 2007-06-04 2018-03-21 Synergy Pharmaceuticals Inc Agonistas de guanilato ciclasa utiles para el tratamiento de trastornos gastrointestinales, inflamacion, cancer y otros trastornos.
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
AU2008309621A1 (en) * 2007-10-12 2009-04-16 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's Disease
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
ES2522968T3 (es) 2008-06-04 2014-11-19 Synergy Pharmaceuticals Inc. Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
MX2010014222A (es) * 2008-06-30 2011-03-29 Novartis Ag Star Combinaciones que comprenden moduladores de mglur para el tratamiento de enfermedad de parkinson.
MX2011001664A (es) 2008-08-12 2011-03-25 Novartis Ag Procesos para la preparacion del metil-ester del acido 4-oxo-octahidro-indol-1-carbociclico y derivados del mismo.
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
EP2959902A1 (en) 2009-07-23 2015-12-30 Novartis AG Use of azabicycloalkyl derivatives for the treatment or prevention of ataxia
JO3250B1 (ar) 2009-09-22 2018-09-16 Novartis Ag إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7
EP2490691A1 (en) 2009-10-20 2012-08-29 Novartis AG Use of 1h-quinazoline-2,4-diones
US20130052644A1 (en) 2010-04-30 2013-02-28 Baltazar Gomez-Mancilla Predictive Markers Useful in the Treatment of Fragile X Syndrome (FXS)
AU2011268865A1 (en) 2010-06-24 2013-01-31 Novartis Ag Use of 1H-quinazoline-2,4-diones
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2655326A1 (en) * 2010-12-20 2013-10-30 Novartis AG 4- (hetero) aryl - ethynyl - octahydro - indole - 1 - carboxylic acid esters
EP2668159A1 (en) 2011-01-24 2013-12-04 Novartis AG 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
WO2012101060A1 (en) 2011-01-27 2012-08-02 Novartis Ag Use of nicotinic acetylcholine receptor alpha 7 activators
AU2012232711B2 (en) 2011-03-18 2016-04-28 Novartis Ag Combinations of alpha 7 nicotinic acetylcholine receptor activators and mGluR5 antagonists for use in dopamine induced dyskinesia in Parkinson's Disease
MX2014002693A (es) 2011-09-07 2014-06-04 Novartis Ag Uso de 1h-quinazolina-2,4-dionas para usarse en la prevencion o el tratamiento de epilepsia fotosensible.
WO2013131981A1 (en) 2012-03-08 2013-09-12 Novartis Ag Predictive markers useful in the diagnosis and treatment of fragile x syndrome (fxs)
GB201215033D0 (en) 2012-08-23 2012-10-10 Novartis Ag Diazepinone derivatives
KR101879919B1 (ko) 2013-01-15 2018-07-18 노파르티스 아게 알파 7 니코틴성 아세틸콜린 수용체 작용물질의 용도
MX362819B (es) 2013-01-15 2019-02-18 Novartis Ag Uso de agonistas del receptor nicotinico de acetilcolina alfa 7 para el tratamiento de la narcolepsia.
AU2014235215A1 (en) 2013-03-15 2015-10-01 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
AU2014235209B2 (en) 2013-03-15 2018-06-14 Bausch Health Ireland Limited Guanylate cyclase receptor agonists combined with other drugs
BR112015030326A2 (pt) 2013-06-05 2017-08-29 Synergy Pharmaceuticals Inc Agonistas ultrapuros de guanilato ciclase c, método de fabricar e usar os mesmos
BR112015030431B1 (pt) * 2013-06-12 2023-02-28 Novartis Ag Formulação de liberação modificada, e seu processo de produção
GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
CN105669686B (zh) * 2014-11-19 2018-08-03 上海合全药业股份有限公司 一种6-(叔丁氧羰基)八氢呋喃[2,3-c]吡啶-4-羧酸的合成方法
EP3661500B1 (en) 2017-07-31 2026-01-07 Novartis AG Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use
CA3067688A1 (en) 2017-07-31 2019-02-07 Novartis Ag Use of mavoglurant in the reduction of alcohol use or in preventing relapse into alcohol use
KR20210120011A (ko) * 2019-01-29 2021-10-06 노파르티스 아게 오피오이드 진통제 내약성을 치료하기 위한 mglur5 길항제의 용도
KR20220097405A (ko) * 2019-11-05 2022-07-07 클라에스 툴린 포유동물에서의 혹사의 예방 및/또는 치료에 사용하기 위한 4-[5-[(rac)-1-[5-(3-클로로페닐)-3-이속사졸일]에톡시]-4-메틸-4H-1,2,4-트리아졸-3-일]피리딘
JP7620694B2 (ja) * 2020-07-17 2025-01-23 ノバルティス アーゲー オピオイド使用の低減用医薬品及びオピオイド禁断の促進用医薬品
IL303248A (en) 2020-12-11 2023-07-01 Novartis Ag Use of mglur5 antagonists for treating amphetamine addiction
AU2021404023A1 (en) 2020-12-14 2023-06-29 Novartis Ag Use of mglur5 antagonists for treating gambling disorder

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4129658A (en) * 1976-09-22 1978-12-12 Sandoz Ltd. 4-Styryl-hexahydro-4-indolinols
WO1999002497A2 (en) * 1997-07-11 1999-01-21 Novartis Ag Pyridine derivatives

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2802833A1 (de) 1978-01-23 1979-07-26 Sandoz Ag 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung
US5264456A (en) * 1989-12-29 1993-11-23 Allergan, Inc. Acetylenes disubstituted with a furyl group and a substituted phenyl group having retinoid like activity
US5284957A (en) 1992-09-03 1994-02-08 Eli Lilly And Company Excitatory amino acid receptor antagonists
US5593994A (en) 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
EP0849256B1 (en) 1995-08-22 2005-06-08 Japan Tobacco Inc. Amide compounds and use of the same
JP4373497B2 (ja) 1996-06-19 2009-11-25 ローン−プーラン・ロレ・リミテツド 置換されたアザビシクロ化合物、ならびにtnfおよびサイクリックampホスホジエステラーゼ産生の阻害剤としてのそれらの使用
EP1085010B1 (en) 1998-06-04 2004-03-10 Kumiai Chemical Industry Co., Ltd. Phenylacetylene derivatives and agricultural/horticultural bactericides
ID29095A (id) 1998-10-02 2001-07-26 Novartis Ag Cs Antagonis mglur5 untuk pengobatan rasa sakit dan kegelisahan
PT1200073E (pt) 1999-07-06 2007-03-30 Lilly Co Eli Antagonistas selectivos do receptor de iglur5 para o tratamento de enxaqueca
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
CA2426430C (en) 2000-10-20 2014-10-07 Biocryst Pharmaceuticals, Inc. Biaryl compounds as serine protease inhibitors
WO2002046166A1 (en) 2000-12-04 2002-06-13 F. Hoffmann-La Roche Ag Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists
GB0103045D0 (en) * 2001-02-07 2001-03-21 Novartis Ag Organic Compounds
US7138404B2 (en) 2001-05-23 2006-11-21 Hoffmann-La Roche Inc. 4-aminopyrimidine derivatives
HUP0402344A2 (hu) 2001-12-04 2005-02-28 F. Hoffmann-La Roche Ag Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
TW200303309A (en) 2001-12-04 2003-09-01 Bristol Myers Squibb Co Novel n-[4-(1h-imidazol-1-yl)-2-fluorophenyl]-3-trifluoromethyl)-1h-pyrazole-5-carboxamides as factor Xa inhibitors
GB0128996D0 (en) * 2001-12-04 2002-01-23 Novartis Ag Organic compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4129658A (en) * 1976-09-22 1978-12-12 Sandoz Ltd. 4-Styryl-hexahydro-4-indolinols
WO1999002497A2 (en) * 1997-07-11 1999-01-21 Novartis Ag Pyridine derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
GASPARINI F. et al. «2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist Neuropharmacology. 1999. V. 38(10). P. 1493-1503. *
MOVESYAN V.А. ет al. «mGluR5 antagonists 2-methyl-6-(phenylethynyl)-pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl-D-aspartate receptors» J. Pharmaco.l Exp. Ther. 2001. V. 296(1). P.41-47. O'LEARY D.M. et al. «Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antag onism» Br. J. Pharmacol. 2000. V. 131(7). P. 1429-1437. BRUNO V. et al. «Selective blockade of metabotropic glutamate receptor subtype 5 is neuroprotective» Neuropharmacology. 2000. V. 39(12). P. 2223-2230. *

Also Published As

Publication number Publication date
NO327005B1 (no) 2009-04-06
PE20030640A1 (es) 2003-09-12
BR0214666A (pt) 2004-11-03
ECSP045139A (es) 2004-07-23
TW200304910A (en) 2003-10-16
TWI328578B (en) 2010-08-11
EP1453512B8 (en) 2006-07-19
US20120010263A1 (en) 2012-01-12
DK1453512T3 (da) 2006-08-28
US20130331568A1 (en) 2013-12-12
CN101366714A (zh) 2009-02-18
NZ533266A (en) 2005-02-25
HU229429B1 (en) 2013-12-30
DE60211944T2 (de) 2007-05-16
AU2002358585A1 (en) 2003-06-17
ES2263842T3 (es) 2006-12-16
GB0128996D0 (en) 2002-01-23
JP4176020B2 (ja) 2008-11-05
KR20050044657A (ko) 2005-05-12
CN100430059C (zh) 2008-11-05
DE60211944D1 (de) 2006-07-06
CO5590929A2 (es) 2005-12-30
US20050065191A1 (en) 2005-03-24
KR100980901B1 (ko) 2010-09-07
EP1453512B1 (en) 2006-05-31
EP1453512A1 (en) 2004-09-08
ATE327755T1 (de) 2006-06-15
KR100959204B1 (ko) 2010-05-19
AR088921A2 (es) 2014-07-16
IL161990A0 (en) 2005-11-20
EG24936A (en) 2011-01-11
MY137774A (en) 2009-03-31
NO20042673L (no) 2004-06-25
HUP0402191A3 (en) 2010-03-29
RU2004120781A (ru) 2006-01-10
US20080146647A1 (en) 2008-06-19
JP5036648B2 (ja) 2012-09-26
AR037682A1 (es) 2004-12-01
CN1592623A (zh) 2005-03-09
HUP0402191A2 (hu) 2005-02-28
CY1105460T1 (el) 2010-04-28
JP2008303226A (ja) 2008-12-18
PL212996B1 (pl) 2012-12-31
HK1071510A1 (en) 2005-07-22
MXPA04005456A (es) 2004-10-11
JP2005514381A (ja) 2005-05-19
CA2466560A1 (en) 2003-06-12
PT1453512E (pt) 2006-10-31
PL368739A1 (en) 2005-04-04
CN101366714B (zh) 2014-09-17
AU2002358585B2 (en) 2006-01-19
ZA200403713B (en) 2005-10-26
KR20100020044A (ko) 2010-02-19
CA2466560C (en) 2010-07-27
WO2003047581A1 (en) 2003-06-12
US7348353B2 (en) 2008-03-25
US8536229B2 (en) 2013-09-17

Similar Documents

Publication Publication Date Title
RU2341515C2 (ru) Ацетиленовые производные, способ их получения, фармацевтическая композиция на их основе и их применение в качестве антагонистов метаботропных глутаматных рецепторов (mglur5)
EP0672031B1 (en) Catechol diethers as selective pde iv inhibitors
KR100586349B1 (ko) 아릴술폰아미드 및 그의 유사체, 및 신경 변성 질병 치료에있어서 그의 용도
JP2004532229A (ja) 脂肪酸アミド加水分解酵素阻害剤
JP4322685B2 (ja) イソキノリン誘導体
EP0538080A1 (fr) Dérivés de l'aminométhyl-4 pipéridine, leur préparation et leur application en thérapeutique
EP0346207B1 (fr) Dérivés d'amino-4 carboxy-3 naphtyridines, leur préparation et compositions pharmaceutiques qui les contiennent
JP3908798B2 (ja) ベンゾシクロアルケン類、その製造法および剤
HK1071510B (en) Acetylene derivatives having mglur 5 antagonistic activity
EP0929525B1 (fr) Heteroaryloxyethylamines comme ligands du recepteur 5-ht1a
FR2741071A1 (fr) Derives de 3-(benzofuran-5-yl)oxazolidin-2-one, leur preparation et leur application en therapeutique
FR2757161A1 (fr) Diphenylalkyl-tetrahydropyridines
JPH10273464A (ja) 置換カテコール誘導体
JPH06345695A (ja) リグナン類縁体の製法

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20171204