KR100959204B1 - ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체 - Google Patents

ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체 Download PDF

Info

Publication number
KR100959204B1
KR100959204B1 KR1020047008477A KR20047008477A KR100959204B1 KR 100959204 B1 KR100959204 B1 KR 100959204B1 KR 1020047008477 A KR1020047008477 A KR 1020047008477A KR 20047008477 A KR20047008477 A KR 20047008477A KR 100959204 B1 KR100959204 B1 KR 100959204B1
Authority
KR
South Korea
Prior art keywords
hydroxy
octahydro
carboxylic acid
phenylethynyl
formula
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
KR1020047008477A
Other languages
English (en)
Korean (ko)
Other versions
KR20050044657A (ko
Inventor
파브리치오 가스파리니
야베스 아우베르존
질비오 오프너
카스파르 침머만
테란스 더블유. 하트
Original Assignee
노파르티스 아게
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=KR100959204(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20050044657A publication Critical patent/KR20050044657A/ko
Application granted granted Critical
Publication of KR100959204B1 publication Critical patent/KR100959204B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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)
KR1020047008477A 2001-12-04 2002-12-03 ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체 Expired - Fee Related KR100959204B1 (ko)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020107002745A Division KR100980901B1 (ko) 2001-12-04 2002-12-03 ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체

Publications (2)

Publication Number Publication Date
KR20050044657A KR20050044657A (ko) 2005-05-12
KR100959204B1 true KR100959204B1 (ko) 2010-05-19

Family

ID=9926969

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020047008477A Expired - Fee Related KR100959204B1 (ko) 2001-12-04 2002-12-03 ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체
KR1020107002745A Expired - Fee Related KR100980901B1 (ko) 2001-12-04 2002-12-03 ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020107002745A Expired - Fee Related KR100980901B1 (ko) 2001-12-04 2002-12-03 ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체

Country Status (31)

Country Link
US (4) US7348353B2 (https=)
EP (1) EP1453512B8 (https=)
JP (2) JP4176020B2 (https=)
KR (2) KR100959204B1 (https=)
CN (2) CN100430059C (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
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
GB0508314D0 (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
EP2272509A1 (en) * 2006-09-11 2011-01-12 Novartis AG New Uses of metabotropic glutamate receptors
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
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
KR101572280B1 (ko) * 2007-10-12 2015-11-26 노파르티스 아게 파킨슨병의 치료를 위한 대사성 글루타메이트 수용체 조절제
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
EP2810951B1 (en) 2008-06-04 2017-03-15 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2320892A2 (en) * 2008-06-30 2011-05-18 Novartis AG Combination products
RU2513856C2 (ru) * 2008-08-12 2014-04-20 Новартис Аг Способы получения метилового эфира 4-оксооктагидроиндол-1-карбоновой кислоты и ее производные
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
CN102573842A (zh) 2009-07-23 2012-07-11 诺瓦提斯公司 氮杂双环烷基衍生物或吡咯烷-2-酮衍生物的用途
JO3250B1 (ar) 2009-09-22 2018-09-16 Novartis Ag إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7
WO2011048150A1 (en) 2009-10-20 2011-04-28 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)
JP2013529622A (ja) 2010-06-24 2013-07-22 ノバルティス アーゲー １ｈ−キナゾリン−２，４−ジオンの使用
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
WO2012101058A1 (en) 2011-01-24 2012-08-02 Novartis Ag 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
KR20140003580A (ko) 2011-01-27 2014-01-09 노파르티스 아게 니코틴성 아세틸콜린 수용체 알파 7 활성화제의 용도
WO2012127393A1 (en) 2011-03-18 2012-09-27 Novartis Ag COMBINATIONS OF ALPHA 7 NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVATORS AND mGluR5 ANTAGONISTS FOR USE IN DOPAMINE INDUCED DYSKINESIA IN PARKINSON'S DISEASE
CN103889427A (zh) 2011-09-07 2014-06-25 诺华股份有限公司 1h-喹唑啉-2,4-二酮用于预防或治疗光敏性癫痫的应用
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
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
BR112015016992A8 (pt) 2013-01-15 2018-01-23 Novartis Ag uso de agonistas do receptor alfa 7 nicotínico de acetilcolina
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
CA2905438A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
SI3004138T1 (sl) 2013-06-05 2024-07-31 Bausch Health Ireland Limited Ultra čisti agonisti gvanilat ciklaze C, postopek za njihovo pripravo in uporabo
KR102290249B1 (ko) 2013-06-12 2021-08-17 노파르티스 아게 변형 방출 제제
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
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
CA3066711A1 (en) 2017-07-31 2019-02-07 Novartis Ag Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use
CA3124931A1 (en) 2019-01-29 2020-08-06 Novartis Ag The use of an mglur5 antagonist for treating opioid analgesic tolerance
BR112022005579A2 (pt) * 2019-11-05 2022-06-21 Claes Thulin 4-[5-[(rac)-1-[5-(3-clorofenil)-3-isoxazolil]etoxi]-4-metil-4h-1,2,4-triazol-3-il]piridina para uso na prevenção e/ou no tratamento de surmenage em um mamífero
MX2023000664A (es) * 2020-07-17 2023-02-27 Novartis Ag Uso de antagonistas de mglur5.
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

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
DE69634822T2 (de) 1995-08-22 2006-04-27 Japan Tobacco Inc. Amid-verbindungen und ihre anwendung
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
DE69915472T2 (de) 1998-06-04 2004-08-19 Kumiai Chemical Industry Co., Ltd. Phenylacetylenderivate und bakterizide für landwirtschaft und gartenbau
EP1117403B1 (en) 1998-10-02 2003-12-10 Novartis AG Mglur5 antagonists for the treatment of pain and anxiety
EP1200073B1 (en) 1999-07-06 2007-01-10 Eli Lilly And Company SELECTIVE iGluR 5? RECEPTOR ANTAGONISTS FOR THE TREATMENT OF MIGRAINE
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
MXPA03009130A (es) 2000-10-20 2004-02-26 Biocryst Pharm Inc Compuestos de biarilo que funcionan como inhibidores de proteasa serina.
MXPA03004862A (es) * 2000-12-04 2005-02-14 Hoffmann La Roche Derivados de feniletenilo o feniletinilo como antagonistas del receptor 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
JP2005517640A (ja) 2001-12-04 2005-06-16 エフ．ホフマン−ラ　ロシュ　アーゲー 置換２−アミノ−シクロアルカンカルボキサアミドならびにシステインプロテアーゼインヒビターとしてのその使用
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
해당사항없음

Also Published As

Publication number Publication date
US20080146647A1 (en) 2008-06-19
CA2466560C (en) 2010-07-27
AR037682A1 (es) 2004-12-01
NZ533266A (en) 2005-02-25
DK1453512T3 (da) 2006-08-28
US20120010263A1 (en) 2012-01-12
ATE327755T1 (de) 2006-06-15
HU229429B1 (en) 2013-12-30
MXPA04005456A (es) 2004-10-11
CY1105460T1 (el) 2010-04-28
JP2008303226A (ja) 2008-12-18
NO327005B1 (no) 2009-04-06
EP1453512B8 (en) 2006-07-19
ZA200403713B (en) 2005-10-26
GB0128996D0 (en) 2002-01-23
TW200304910A (en) 2003-10-16
CN1592623A (zh) 2005-03-09
HUP0402191A2 (hu) 2005-02-28
IL161990A0 (en) 2005-11-20
PL212996B1 (pl) 2012-12-31
ECSP045139A (es) 2004-07-23
KR20100020044A (ko) 2010-02-19
US20130331568A1 (en) 2013-12-12
PL368739A1 (en) 2005-04-04
CN100430059C (zh) 2008-11-05
EG24936A (en) 2011-01-11
AR088921A2 (es) 2014-07-16
JP2005514381A (ja) 2005-05-19
AU2002358585B2 (en) 2006-01-19
KR20050044657A (ko) 2005-05-12
DE60211944D1 (de) 2006-07-06
US8536229B2 (en) 2013-09-17
PE20030640A1 (es) 2003-09-12
HK1071510A1 (en) 2005-07-22
CO5590929A2 (es) 2005-12-30
EP1453512B1 (en) 2006-05-31
CA2466560A1 (en) 2003-06-12
CN101366714B (zh) 2014-09-17
BR0214666A (pt) 2004-11-03
ES2263842T3 (es) 2006-12-16
EP1453512A1 (en) 2004-09-08
HUP0402191A3 (en) 2010-03-29
NO20042673L (no) 2004-06-25
RU2004120781A (ru) 2006-01-10
MY137774A (en) 2009-03-31
DE60211944T2 (de) 2007-05-16
TWI328578B (en) 2010-08-11
JP4176020B2 (ja) 2008-11-05
AU2002358585A1 (en) 2003-06-17
PT1453512E (pt) 2006-10-31
JP5036648B2 (ja) 2012-09-26
RU2341515C2 (ru) 2008-12-20
WO2003047581A1 (en) 2003-06-12
CN101366714A (zh) 2009-02-18
US20050065191A1 (en) 2005-03-24
US7348353B2 (en) 2008-03-25
KR100980901B1 (ko) 2010-09-07

Similar Documents

Publication Publication Date Title
KR100959204B1 (ko) ｍＧｌｕＲ５ 안타고니스트 활성을 갖는 아세틸렌 유도체
EP0672031B1 (en) Catechol diethers as selective pde iv inhibitors
KR100586349B1 (ko) 아릴술폰아미드 및 그의 유사체, 및 신경 변성 질병 치료에있어서 그의 용도
US5728712A (en) 3,4-disubstituted-phenylsulphonamides and their therapeutic use
US5532372A (en) Imide derivatives, and their production and use
US5583149A (en) Antimigraine derivatives of indolylcycloalkanylamines
KR100546534B1 (ko) 아릴술폰아미드 및 그의 동족체, 및 신경 변성 질병 치료에 있어서 그의 용도
US7250434B2 (en) CCK-1 receptor modulators
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
JPH0342276B2 (https=)
JP3467072B2 (ja) リグナン類縁体の製法
JP3161948B2 (ja) ビシクロラクタム化合物

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

A201 Request for examination
AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

J201 Request for trial against refusal decision
PJ0201 Trial against decision of rejection

St.27 status event code: A-3-3-V10-V11-apl-PJ0201

A107 Divisional application of patent
AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

PB0901 Examination by re-examination before a trial

St.27 status event code: A-6-3-E10-E12-rex-PB0901

B701 Decision to grant
PB0701 Decision of registration after re-examination before a trial

St.27 status event code: A-3-4-F10-F13-rex-PB0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

FPAY Annual fee payment

Payment date: 20130419

Year of fee payment: 4

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

FPAY Annual fee payment

Payment date: 20140422

Year of fee payment: 5

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

FPAY Annual fee payment

Payment date: 20150416

Year of fee payment: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

FPAY Annual fee payment

Payment date: 20160419

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

FPAY Annual fee payment

Payment date: 20170504

Year of fee payment: 8

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20180514

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20180514

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000