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=***_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

  • 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)
  • Pyridine Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic 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 (32)

Country Link
US (4) US7348353B2 (es)
EP (1) EP1453512B8 (es)
JP (2) JP4176020B2 (es)
KR (2) KR100980901B1 (es)
CN (2) CN100430059C (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)
HK (1) HK1071510A1 (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 (44)

* 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
WO2005097127A2 (en) 2004-04-02 2005-10-20 Merck & Co., Inc. Method of treating men with metabolic and anthropometric disorders
GB0503646D0 (en) * 2005-02-22 2005-03-30 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
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
KR20090061041A (ko) * 2006-09-11 2009-06-15 노파르티스 아게 대사성 글루타메이트 수용체의 조절제로서의 니코틴산 유도체
US20100120694A1 (en) 2008-06-04 2010-05-13 Synergy Pharmaceuticals, Inc. Agonists of Guanylate Cyclase Useful for the Treatment of Gastrointestinal Disorders, Inflammation, Cancer and Other Disorders
EP2527360B1 (en) 2007-06-04 2015-10-28 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
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
SG185293A1 (en) * 2007-10-12 2012-11-29 Novartis Ag Organic compounds
RU2496494C2 (ru) * 2008-06-30 2013-10-27 Новартис Аг КОМБИНАЦИИ, СОДЕРЖАЩИЕ МОДУЛЯТОРЫ mGluR, ДЛЯ ЛЕЧЕНИЯ БОЛЕЗНИ ПАРКИНСОНА
JP5468608B2 (ja) * 2008-08-12 2014-04-09 ノバルティス アーゲー ４−オキソ−オクタヒドロ−インドール−１−カルボサイリックアシッドメチルエステルとその誘導体の調製方法
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
WO2011009890A2 (en) 2009-07-23 2011-01-27 Novartis Ag Use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives
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
BR112012027816A2 (pt) * 2010-04-30 2017-08-08 Novartis Ag marcadores preditivos úteis no tratamento da síndrome do x frágil (fxs).
MX2012015090A (es) 2010-06-24 2013-02-12 Novartis Ag Uso de 1h-quinazolina-2,4-dionas.
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
WO2012084873A1 (en) 2010-12-20 2012-06-28 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
BR112013018726A2 (pt) 2011-01-27 2016-10-25 Novartis Ag uso de ativadores de alfa 7 do receptor nicotínico de acetilcolina
KR20140018286A (ko) 2011-03-18 2014-02-12 노파르티스 아게 파킨슨병에서의 도파민 유발 이상운동증에서 사용하기 위한 알파 7 니코틴성 아세틸콜린 수용체 활성화제 및 mGluR5 길항제의 조합물
WO2013036224A1 (en) 2011-09-07 2013-03-14 Novartis Ag Use of 1h-quinazoline- 2, 4 -diones for use in the prevention or treatment 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
EP2945637B1 (en) 2013-01-15 2021-03-10 Novartis AG Use of alpha 7 nicotinic acetylcholine receptor agonists
CN105263492B (zh) 2013-01-15 2018-04-10 诺华有限公司 α7烟碱型乙酰胆碱受体激动剂在治疗发作性睡病中的应用
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
US10011637B2 (en) 2013-06-05 2018-07-03 Synergy Pharmaceuticals, Inc. Ultra-pure agonists of guanylate cyclase C, method of making and using same
EA031395B1 (ru) 2013-06-12 2018-12-28 Новартис Аг Состав с модифицированной кинетикой высвобождения
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
JP2020529978A (ja) 2017-07-31 2020-10-15 ノバルティス アーゲー アルコール使用の低減又はアルコール使用再燃の予防におけるマボグルラントの使用
CA3066711A1 (en) 2017-07-31 2019-02-07 Novartis Ag Use of mavoglurant in the reduction of ***e use or in preventing relapse into ***e use
CN113301894A (zh) 2019-01-29 2021-08-24 诺华股份有限公司 mGluR5拮抗剂用于治疗阿片类物质镇痛耐受性的用途
AU2021307607A1 (en) 2020-07-17 2022-11-17 Novartis Ag Mavoglurant, a mGluR5 antagonist, for use in the treatment in the reduction of opioid use
CA3203607A1 (en) 2020-12-11 2022-06-16 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

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
USRE39088E1 (en) 1995-08-22 2006-05-02 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
TW544448B (en) 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
US6313071B1 (en) 1998-06-04 2001-11-06 Kumiai Chemical Industry Co., Ltd. Phenylacetylene derivatives and agricultural/horticultural fungicides
PT1117403E (pt) 1998-10-02 2004-04-30 Sibia Neurosciences Inc Antagonistas de mglurs para o tratamento da dor e ansiedade
CZ20014488A3 (cs) 1999-07-06 2003-01-15 Eli Lilly And Company Selektivní antagonisté iGluR5 receptoru pro léčení migrény
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
IL155202A0 (en) 2000-10-20 2003-11-23 Biocryst Pharm Inc Biaryl compounds as serine protease inhibitors
BR0115871A (pt) * 2000-12-04 2003-10-28 Hoffmann La Roche Derivados de feniletenila ou feniletinila como antagonistas de receptores de glutamato
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
EP1453801B1 (en) 2001-12-04 2007-03-21 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
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

Also Published As

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

Similar Documents

Publication Publication Date Title
ECSP045139A (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
DE60235083D1 (de) Substituierte tetracyclin-verbindungen zur behandlung von malaria
ATE353888T1 (de) Chinazolinderivate
ECSP066311A (es) Derivados de la piperazina y su uso como agentes terapéuticos
UY28150A1 (es) Agentes terapeuticos
UY28186A1 (es) N-arilheterociclos sustituidos, procedimientos para su preparación, y su empleo como medicamentos.
ATE369372T1 (de) 42-o-alkoxyalkylrapamycinderivate und diese enthaltende zusammensetzungen
BR0313676A (pt) Derivados de pirimidina e uso destes como moduladores cb2
UY26130A1 (es) Compuestos para tratar la obesidad
ATE538124T1 (de) Imidazokondensierte tricyclische verbindungen auf thiazoloä4,5-büpyridin-basis und pharmazeutische zusammensetzungen damit
ES2243579T3 (es) Derivados de pirazolopirideno.
SE0302139D0 (sv) Novel compounds
UY29999A1 (es) "n-pirazinil-fenilsulfonamidas, procedimientos y compuestos intemedios utilizados en su preparacion, composiciones farmaceuticas que las contienen y aplicaciones"
UY27232A1 (es) Nuevos compuestos de dihidropirimidina ciano substituidos y su uso para tratar padecimientos
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
SE0303280D0 (sv) Novel compounds
GT200800066A (es) Derivados de 9-cloro-15-deoxiprostaglandina, procedimiento para su preparacion y su uso como medicamento.
UY27998A1 (es) Piperazinas sustituidas sustituidas heterocíclicas para el tratamiento de la esquizofrenia