ECSP045139A - DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTICA DE MGluR5 - Google Patents

DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTICA DE MGluR5

Info

Publication number
ECSP045139A
ECSP045139A EC2004005139A ECSP045139A ECSP045139A EC SP045139 A ECSP045139 A EC SP045139A EC 2004005139 A EC2004005139 A EC 2004005139A EC SP045139 A ECSP045139 A EC SP045139A EC SP045139 A ECSP045139 A EC SP045139A
Authority
EC
Ecuador
Prior art keywords
mglur5
antagonistic activity
acetylene derivatives
formula
acetylene
Prior art date
Application number
EC2004005139A
Other languages
English (en)
Inventor
Fabrizio Gasparini
Yves Auberson
Silvio Ofner
Original Assignee
Novartis Ag
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=ECSP045139(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of ECSP045139A publication Critical patent/ECSP045139A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters 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
    • C07C271/16—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters 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
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • A61P25/34—Tobacco-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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic 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
    • C07C233/23—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/04—Heterocyclic 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
    • C07D215/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

La invención proporciona compuestos de la fórmula (I), en donde m, n, A, R, R', R'', R0, X e Y son como se definen en la descripción, y su preparación. Los compuestos de la fórmula (I) son útiles como farmacéuticos en el tratamiento de, por ejemplo, trastornos del sistema nervioso
EC2004005139A 2001-12-04 2004-06-04 DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTICA DE MGluR5 ECSP045139A (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ECSP045139A true ECSP045139A (es) 2004-07-23

Family

ID=9926969

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2004005139A ECSP045139A (es) 2001-12-04 2004-06-04 DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTICA DE MGluR5

Country Status (31)

Country Link
US (4) US7348353B2 (es)
EP (1) EP1453512B8 (es)
JP (2) JP4176020B2 (es)
KR (2) KR100959204B1 (es)
CN (2) CN101366714B (es)
AR (2) AR037682A1 (es)
AT (1) ATE327755T1 (es)
AU (1) AU2002358585B2 (es)
BR (1) BR0214666A (es)
CA (1) CA2466560C (es)
CO (1) CO5590929A2 (es)
CY (1) CY1105460T1 (es)
DE (1) DE60211944T2 (es)
DK (1) DK1453512T3 (es)
EC (1) ECSP045139A (es)
EG (1) EG24936A (es)
ES (1) ES2263842T3 (es)
GB (1) GB0128996D0 (es)
HU (1) HU229429B1 (es)
IL (1) IL161990A0 (es)
MX (1) MXPA04005456A (es)
MY (1) MY137774A (es)
NO (1) NO327005B1 (es)
NZ (1) NZ533266A (es)
PE (1) PE20030640A1 (es)
PL (1) PL212996B1 (es)
PT (1) PT1453512E (es)
RU (1) RU2341515C2 (es)
TW (1) TWI328578B (es)
WO (1) WO2003047581A1 (es)
ZA (1) ZA200403713B (es)

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
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 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
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
EP2272509A1 (en) 2006-09-11 2011-01-12 Novartis AG New Uses of metabotropic glutamate receptors
WO2008151257A2 (en) 2007-06-04 2008-12-11 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
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
MX2010003913A (es) * 2007-10-12 2010-04-27 Novartis Ag Moduladores de los receptores de glutamato metabotropicos para el tratamiento de enfermedades de parkinson.
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
ES2627848T3 (es) 2008-06-04 2017-07-31 Synergy Pharmaceuticals Inc. Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos
WO2010000763A2 (en) * 2008-06-30 2010-01-07 Novartis Ag Combination products
NZ590753A (en) * 2008-08-12 2012-06-29 Novartis Ag Processes for the preparation of 4-oxo-octahydro-indole-1-carbocylic acid methyl ester and derivatives thereof
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
EP2456438A2 (en) 2009-07-23 2012-05-30 Novartis AG Use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives
TWI558398B (zh) 2009-09-22 2016-11-21 諾華公司 菸鹼乙醯膽鹼受體α7活化劑之用途
WO2011048150A1 (en) 2009-10-20 2011-04-28 Novartis Ag Use of 1h-quinazoline-2,4-diones
WO2011137206A1 (en) * 2010-04-30 2011-11-03 Novartis Ag Predictive markers useful in the treatment of fragile x syndrome (fxs)
CA2800970A1 (en) 2010-06-24 2011-12-29 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
US20130274294A1 (en) * 2010-12-20 2013-10-17 David Carcache 4-(Hetero)Aryl-Ethynyl-Octahydro-Indole-1-Esters
EP2668159A1 (en) 2011-01-24 2013-12-04 Novartis AG 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
US20140171448A1 (en) 2011-01-27 2014-06-19 Novartis Ag Use of nicotinic acetylcholine receptor alpha 7 activators
EA201391348A8 (ru) 2011-03-18 2014-11-28 Новартис Аг КОМБИНАЦИИ АКТИВАТОРОВ АЛЬФА-7 НИКОТИНОВОГО АЦЕТИЛХОЛИНОВОГО РЕЦЕПТОРА И АНТАГОНИСТОВ mGluR5, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ПРИМЕНЕНИЯ ПРИ ВЫЗВАННОЙ ДОПАМИНОМ ДИСКИНЕЗИИ, СВЯЗАННОЙ С БОЛЕЗНЬЮ ПАРКИНСОНА
CA2846503A1 (en) 2011-09-07 2013-03-14 Novartis Ag Use of 1h-quinazoline-2,4-diones for use in the prevention or treatment of photosensitive epilepsy
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
MX379289B (es) 2013-01-15 2025-03-10 Novartis Ag Uso de agonistas del receptor nicotinico de acetilcolina alfa 7.
JP6137336B2 (ja) 2013-01-15 2017-05-31 ノバルティス アーゲー ナルコレプシーの処置のためのアルファ7ニコチン性受容体アゴニストの使用
EP2968439A2 (en) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
US9708367B2 (en) 2013-03-15 2017-07-18 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
PL3004138T3 (pl) 2013-06-05 2024-07-29 Bausch Health Ireland Limited Ultra-oczyszczeni agoniści peptydowi cyklazy guanylanowej C, sposób ich uzyskiwania i ich zastosowanie
SG11201509178TA (en) * 2013-06-12 2015-12-30 Novartis Ag Modified release formulation
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
AU2018310882C1 (en) 2017-07-31 2021-12-09 Novartis Ag Use of mavoglurant in the reduction of alcohol use or in preventing relapse into alcohol use
KR20200035035A (ko) 2017-07-31 2020-04-01 노파르티스 아게 코카인 사용 감소 또는 코카인 사용 재발 예방에 있어서 마보글루란트의 용도
KR20210120011A (ko) * 2019-01-29 2021-10-06 노파르티스 아게 오피오이드 진통제 내약성을 치료하기 위한 mglur5 길항제의 용도
EP4007575B1 (en) * 2019-11-05 2023-09-27 Claes THULIN 4-[5-[(rac)-1-[5-(3-chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4h-1,2,4-triazol-3-yl]pyridine for use in prevention and/or treatment of stress
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
WO2022123482A1 (en) 2020-12-11 2022-06-16 Novartis Ag Use of mglur5 antagonists for treating amphetamine addiction
CA3204360A1 (en) 2020-12-14 2022-06-23 Novartis Ag Use of mglur5 antagonists for treating gambling disorder

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2741009A1 (de) * 1976-09-22 1978-03-23 Sandoz Ag 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung
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
CA2502764A1 (en) 1995-08-22 1997-03-06 Japan Tobacco Inc. Amide compounds
CA2258728C (en) 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
AU4059199A (en) 1998-06-04 1999-12-20 Ihara 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
DZ3209A1 (fr) 1999-07-06 2001-01-11 Lilly Co Eli Antagonistes selectifs du recepteur iGLuR5 utilises dans le traitement de la migraine.
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
NZ525917A (en) * 2000-12-04 2005-11-25 F Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists and their use in treating mGLuR5 receptor mediated disorders
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
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
PL370766A1 (en) 2001-12-04 2005-05-30 F.Hoffmann-La Roche Ag Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors
GB0128996D0 (en) 2001-12-04 2002-01-23 Novartis Ag Organic compounds

Also Published As

Publication number Publication date
HUP0402191A2 (hu) 2005-02-28
PT1453512E (pt) 2006-10-31
KR100959204B1 (ko) 2010-05-19
ATE327755T1 (de) 2006-06-15
CN101366714A (zh) 2009-02-18
BR0214666A (pt) 2004-11-03
DE60211944D1 (de) 2006-07-06
CN1592623A (zh) 2005-03-09
HUP0402191A3 (en) 2010-03-29
AR037682A1 (es) 2004-12-01
DK1453512T3 (da) 2006-08-28
US20130331568A1 (en) 2013-12-12
KR20100020044A (ko) 2010-02-19
CY1105460T1 (el) 2010-04-28
ES2263842T3 (es) 2006-12-16
ZA200403713B (en) 2005-10-26
GB0128996D0 (en) 2002-01-23
NO20042673L (no) 2004-06-25
US20120010263A1 (en) 2012-01-12
CN100430059C (zh) 2008-11-05
NO327005B1 (no) 2009-04-06
NZ533266A (en) 2005-02-25
US20080146647A1 (en) 2008-06-19
IL161990A0 (en) 2005-11-20
HU229429B1 (en) 2013-12-30
AR088921A2 (es) 2014-07-16
CN101366714B (zh) 2014-09-17
CA2466560C (en) 2010-07-27
EP1453512B8 (en) 2006-07-19
JP2005514381A (ja) 2005-05-19
RU2004120781A (ru) 2006-01-10
TWI328578B (en) 2010-08-11
US7348353B2 (en) 2008-03-25
EP1453512A1 (en) 2004-09-08
PE20030640A1 (es) 2003-09-12
WO2003047581A1 (en) 2003-06-12
AU2002358585A1 (en) 2003-06-17
CO5590929A2 (es) 2005-12-30
MXPA04005456A (es) 2004-10-11
JP2008303226A (ja) 2008-12-18
CA2466560A1 (en) 2003-06-12
EG24936A (en) 2011-01-11
KR100980901B1 (ko) 2010-09-07
JP5036648B2 (ja) 2012-09-26
US20050065191A1 (en) 2005-03-24
HK1071510A1 (en) 2005-07-22
JP4176020B2 (ja) 2008-11-05
EP1453512B1 (en) 2006-05-31
MY137774A (en) 2009-03-31
PL212996B1 (pl) 2012-12-31
PL368739A1 (en) 2005-04-04
DE60211944T2 (de) 2007-05-16
AU2002358585B2 (en) 2006-01-19
TW200304910A (en) 2003-10-16
RU2341515C2 (ru) 2008-12-20
KR20050044657A (ko) 2005-05-12
US8536229B2 (en) 2013-09-17

Similar Documents

Publication Publication Date Title
MXPA04005456A (es) Derivados de acetileno que tienen actividad antagonistica de mglur5.
ECSP066391A (es) [1,8] naftiridin-2-onas y compuestos relacionados para el tratamiento de la esquizofrenia
ATE433447T1 (de) Pyrimiidinverbindungen
CO6331473A2 (es) Derivados de 2,3-dihidrobenzo[1,4]dioxin-2-ilmetilo como antagonistas alfa2c para uso en el tratamiento de enfermedades del sistema nervioso central y periferico
ATE296826T1 (de) Pyrazolo(1,5)pyridinderivate
BRPI0409701A (pt) ligantes de receptores de canabinóides e seus usos
DE60235083D1 (de) Substituierte tetracyclin-verbindungen zur behandlung von malaria
ATE353888T1 (de) Chinazolinderivate
ECSP066311A (es) Derivados de la piperazina y su uso como agentes terapéuticos
BR0314393A (pt) Piperazinas heterocìclicas substituìdas para o tratamento de esquizofrenia
BR0307058A (pt) N-óxidos de derivados de n-fenil-2-pirimidina-amina
ATE301653T1 (de) Pyrazolopyridine
UY28150A1 (es) Agentes terapeuticos
UY28186A1 (es) N-arilheterociclos sustituidos, procedimientos para su preparación, y su empleo como medicamentos.
BR0313676A (pt) Derivados de pirimidina e uso destes como moduladores cb2
SE0201544D0 (sv) Novel compounds and thier use
BR0210028A (pt) Agentes antibacterianos
ES2243579T3 (es) Derivados de pirazolopirideno.
BRPI0409376A (pt) derivados de indeno como agentes farmacêuticos
ATE479657T1 (de) N-(aryl)-2-arylethensulfonamide und ihre therapeutischen anwendungen
BRPI0412843A (pt) lactamas substituìdas e uso das mesmas como agentes anticáncer
UY27451A1 (es) 2,5-diamidoindoles sustituidos y su utilización
UY27998A1 (es) Piperazinas sustituidas sustituidas heterocíclicas para el tratamiento de la esquizofrenia
GT200800066A (es) Derivados de 9-cloro-15-deoxiprostaglandina, procedimiento para su preparacion y su uso como medicamento.
ECSP044971A (es) Isoxazolopiridinonas y su uso en el tratamiento de enfermedad de parkinson