DE60223720D1 - Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5 - Google Patents

Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5

Info

Publication number
DE60223720D1
DE60223720D1 DE60223720T DE60223720T DE60223720D1 DE 60223720 D1 DE60223720 D1 DE 60223720D1 DE 60223720 T DE60223720 T DE 60223720T DE 60223720 T DE60223720 T DE 60223720T DE 60223720 D1 DE60223720 D1 DE 60223720D1
Authority
DE
Germany
Prior art keywords
modulators
heteroaryl
glutamate receptor
metabotropic glutamate
substituted pyrazol
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 - Lifetime
Application number
DE60223720T
Other languages
English (en)
Other versions
DE60223720T2 (de
Inventor
Nicholas D Cosford
Chixu Chen
Brian W Eastman
Dehua Huang
Benito Munoz
Petpiboon Prasit
Nicholas D Smith
Essa Hu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck and Co Inc
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of DE60223720D1 publication Critical patent/DE60223720D1/de
Application granted granted Critical
Publication of DE60223720T2 publication Critical patent/DE60223720T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/34—Tobacco-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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
DE60223720T 2001-12-18 2002-12-13 Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5 Expired - Lifetime DE60223720T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34138201P 2001-12-18 2001-12-18
US341382P 2001-12-18
PCT/US2002/040147 WO2003051833A2 (en) 2001-12-18 2002-12-13 Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5

Publications (2)

Publication Number Publication Date
DE60223720D1 true DE60223720D1 (de) 2008-01-03
DE60223720T2 DE60223720T2 (de) 2008-10-30

Family

ID=23337314

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60223720T Expired - Lifetime DE60223720T2 (de) 2001-12-18 2002-12-13 Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5

Country Status (8)

Country Link
US (1) US7569592B2 (de)
EP (1) EP1458383B1 (de)
JP (1) JP4286146B2 (de)
AU (1) AU2002359714B2 (de)
CA (1) CA2469813C (de)
DE (1) DE60223720T2 (de)
ES (1) ES2295441T3 (de)
WO (1) WO2003051833A2 (de)

Families Citing this family (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60227794D1 (de) * 2001-04-26 2008-09-04 Eisai R&D Man Co Ltd Stickstoffhaltige verbindung mit kondensiertem ring und pyrazolylgruppe als substituent und medizinische zusammensetzung davon
ATE486600T1 (de) * 2002-03-12 2010-11-15 Merck Sharp & Dohme Di-aryl-substituierte tetrazol-modulatoren des metabotropen glutamat-rezeptors-5
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
EP1613614A2 (de) * 2003-04-03 2006-01-11 Merck & Co., Inc. Diarylsubstituierte pyrazolmodulatoren des metabotropen glutamatrezeptors-5
WO2004087653A2 (en) * 2003-04-03 2004-10-14 Merck & Co., Inc. 4-ring imidazole derivatives as modulators of metabotropic glutamate receptor-5
CA2537141A1 (en) * 2003-09-02 2005-03-10 Merck And Co., Inc. Bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5
AU2005215379A1 (en) * 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
US20070197549A1 (en) * 2004-02-18 2007-08-23 Astrazeneca Ab Tetrazole compounds and their use as metabotropic glutamate receptor antagonists
AU2005219791B2 (en) * 2004-03-05 2011-06-09 Msd K.K. Diaryl-substituted five-membered heterocycle derivative
AU2005223483B2 (en) 2004-03-18 2009-04-23 Zoetis Llc N-(1-arylpyrazol-4l)sulfonamides and their use as parasiticides
EP2305352A1 (de) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-Reduktaseinhibitoren zur Behandlung von Stoffwechsel- und anthropometrischen Störungen
EP1812071A2 (de) 2004-10-13 2007-08-01 PTC Therapeutics, Inc. Verbindungen zur nonsense-unterdrückung und verwendung dieser verbindungen für die herstellung eines medikaments zur behandlung somatischer mutationsbedingter erkrankungen
DE102008020113A1 (de) 2008-04-23 2009-10-29 Bayer Schering Pharma Aktiengesellschaft Substituierte Dihydropyrazolone und ihre Verwendung
AU2005322173A1 (en) * 2004-12-27 2006-07-06 Astrazeneca Ab Pyrazolone compounds as metabotropic glutamate receptor agonists for the treatment of neurological and psychiatric disorders
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
AU2006227729B2 (en) * 2005-03-16 2011-10-13 Aventis Pharmaceuticals Inc. Dipyrazoles as central nervous system agents
DE102005019712A1 (de) 2005-04-28 2006-11-09 Bayer Healthcare Ag Dipyridyl-dihydropyrazolone und ihre Verwendung
CA2609783A1 (en) * 2005-05-27 2006-12-07 Pfizer Products Inc. Combination of a cannabinoid-1- receptor-antagonist and a microsomal triglyceride transfer protein inhibitor for treating obesity or mainataining weight loss
EP2258359A3 (de) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenese durch Modulation des Muscarinrezeptors mit Sabcomelin
JP2009506069A (ja) 2005-08-26 2009-02-12 ブレインセルス，インコーポレイティド ムスカリン性受容体調節による神経発生
AU2006304787A1 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US7951824B2 (en) * 2006-02-17 2011-05-31 Hoffman-La Roche Inc. 4-aryl-pyridine-2-carboxyamide derivatives
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007223036A1 (en) * 2006-03-08 2007-09-13 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2026813A2 (de) * 2006-05-09 2009-02-25 Braincells, Inc. 5-ht-rezeptor-vermittelte neurogenese
EP2377531A2 (de) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenese mittels Angiotensin-Modulation
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
US7998971B2 (en) * 2006-09-08 2011-08-16 Braincells Inc. Combinations containing a 4-acylaminopyridine derivative
EP2066355A2 (de) * 2006-09-19 2009-06-10 Braincells, Inc. Kombination aus einem durch einen peroxisom-proliferator aktivierten rezeptor-mittel und einem zweiten neurogenen mittel zur behandlung von erkrankungen des nervensystems sowie zur förderung von neuraler differenzierung und neurogenese
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
DE102006050516A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dihydropyrazolone und ihre Verwendung
DE102006050515A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dipyridiyl-dihydropyrazolone und ihre Verwendung
DE102006050513A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substitiuierte Dihydropyrazolone und ihre Verwendung
CA2687306A1 (en) 2007-05-18 2008-11-27 Bayer Schering Pharma Aktiengesellschaft Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
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
US7879802B2 (en) 2007-06-04 2011-02-01 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
MX2010002266A (es) * 2007-08-30 2010-03-25 Takeda Pharmaceutical Derivados de pirazol sustituidos.
EP3239170B1 (de) 2008-06-04 2019-03-20 Synergy Pharmaceuticals Inc. Für die behandlung von gastrointestinalen erkrankungen, entzündungen, krebs und anderen erkrankungen geeignete agonisten von guanylatcyclase
EP3241839B1 (de) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Zur behandlung von erkrankungen des magen-darm-trakts, entzündlichen erkrankungen, krebs und anderen erkrankungen geeignete agonisten von guanylatcyclase
KR20110092266A (ko) 2008-08-04 2011-08-17 씨에이치디아이 파운데이션, 인코포레이티드 소정 키누레닌-3-모노옥시게나아제 억제제, 약학적 조성물, 및 그의 사용 방법
EP2352725A1 (de) * 2008-11-07 2011-08-10 Wyeth LLC Lxr-modulatoren auf chinoxalinbasis
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN102573478B (zh) * 2009-10-12 2015-12-16 拜尔农作物科学股份公司 作为杀虫剂的1-(吡啶-3-基)-吡唑和1-(嘧啶-5-基)-吡唑
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
US9090632B2 (en) * 2010-08-31 2015-07-28 Vanderbilt University Bicyclic oxazole and thiazole compounds and their use as allosteric modulators of mGluR5 receptors
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
DE102010044131A1 (de) 2010-11-18 2012-05-24 Bayer Schering Pharma Aktiengesellschaft Substituiertes Natrium-1H-pyrazol-5-olat
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
BR112014004845A2 (pt) 2011-08-30 2017-04-04 Chdi Foundation Inc pelo menos uma entidade química; pelo menos um composto; composição farmacêutica; uso de uma quantidade terapeuticamente eficaz de pelo menos uma entidade química; composição farmacêutica embalada
CN106518845B (zh) 2011-08-30 2019-09-13 Chdi基金会股份有限公司 犬尿氨酸-3-单加氧酶抑制剂、药物组合物及其使用方法
UA111754C2 (uk) 2011-10-06 2016-06-10 Байєр Фарма Акцієнгезелльшафт Заміщені бензиліндазоли для застосування як інгібіторів bub1-кінази для лікування гіперпроліферативних захворювань
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
US8822464B2 (en) 2011-11-28 2014-09-02 Boehringer Ingelheim International Gmbh N-aryl-piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors
US8741892B2 (en) 2011-12-05 2014-06-03 Boehringer Ingelheim International Gmbh Compounds
US8642774B2 (en) 2011-12-08 2014-02-04 Boehringer Ingelheim International Gmbh Compounds
US8846948B2 (en) 2011-12-13 2014-09-30 Boehringer Ingelheim International Gmbh Compounds
US8796467B2 (en) 2011-12-13 2014-08-05 Boehringer Ingelheim International Gmbh Compounds
US8716277B2 (en) 2011-12-14 2014-05-06 Boehringer Ingelheim International Gmbh Substituted imidazole compounds useful as positive allosteric modulators of mGlu5 receptor activity
US8883789B2 (en) 2011-12-14 2014-11-11 Boehringer Ingelheim International Gmbh Piperazine derivatives and their use as positive allosteric modulators of mGluR5 receptors
US8937176B2 (en) 2011-12-14 2015-01-20 Boehringer Ingelheim International Gmbh Compounds
ES2638144T3 (es) 2011-12-21 2017-10-18 Bayer Intellectual Property Gmbh Bencilpirazoles sustituidos
US8889677B2 (en) 2012-01-17 2014-11-18 Boehringer Ingellheim International GmbH Substituted triazoles useful as mGlu5 receptor modulators
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
EP2914587A1 (de) * 2012-10-31 2015-09-09 Bayer CropScience AG Neue heterocylische verbindungen als schädlingsbekämpfungsmittel
CA2905435A1 (en) 2013-03-15 2014-09-25 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
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
HUE053654T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR- és CMET-inhibitorok kombinációi a rák kezelésére
JP6980385B2 (ja) 2014-03-26 2021-12-15 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited Ｆｇｆｒ阻害剤とｉｇｆ１ｒ阻害剤の組合せ
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
WO2015161014A1 (en) * 2014-04-17 2015-10-22 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
DK3152199T3 (en) 2014-06-03 2018-11-26 Idorsia Pharmaceuticals Ltd PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS
SG11201700341PA (en) 2014-07-17 2017-02-27 Chdi Foundation Inc Methods and compositions for treating hiv-related disorders
AU2015317022B2 (en) 2014-09-15 2020-01-16 Idorsia Pharmaceuticals Ltd Triazole compounds as T-type calcium channel blockers
KR20170049604A (ko) 2014-09-19 2017-05-10 바이엘 파마 악티엔게젤샤프트 Bub1 억제제로서의 벤질 치환된 인다졸
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
WO2016202935A1 (en) 2015-06-19 2016-12-22 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
KR20180052631A (ko) 2015-09-23 2018-05-18 얀센 파마슈티카 엔.브이. 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도
BR112018005637B1 (pt) 2015-09-23 2023-11-28 Janssen Pharmaceutica Nv Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos
CA3046846A1 (en) 2016-12-16 2018-06-21 Idorsia Pharmaceuticals Ltd Pharmaceutical combination comprising a t-type calcium channel blocker
TWI808960B (zh) 2017-02-06 2023-07-21 瑞士商愛杜西亞製藥有限公司 用於合成1-芳基-1-三氟甲基環丙烷之新穎方法
KR20210033503A (ko) * 2018-07-18 2021-03-26 아르커스 바이오사이언시즈 인코포레이티드 아졸로피리미딘 화합물의 고체 형태

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2833779A (en) * 1956-10-29 1958-05-06 American Cyanamid Co Substituted pyrazoles
US5859215A (en) * 1995-10-25 1999-01-12 Wallac Oy Biospecific binding reactants labelled with luminescent lanthanide chelates and their use
US6660753B2 (en) * 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
DK1210344T3 (da) * 1999-08-19 2006-03-06 Nps Pharma Inc Heteropolycykliske forbindelser og anvendelser deraf som metabotrope glutamatreceptorantagonister
WO2003029210A2 (en) * 2001-10-04 2003-04-10 Merck & Co. Inc. Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5
AU2002365892A1 (en) * 2001-11-30 2003-06-17 Merck & Co., Inc. Metabotropic glutamate receptor-5 modulators
CA2469821C (en) * 2001-12-18 2009-10-20 Merck & Co., Inc. Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5
JP4357965B2 (ja) * 2001-12-21 2009-11-04 メルク エンド カムパニー インコーポレーテッド メタボトロピックグルタミン酸受容体−５のヘテロアリール置換ピロールモジュレーター
ATE486600T1 (de) * 2002-03-12 2010-11-15 Merck Sharp & Dohme Di-aryl-substituierte tetrazol-modulatoren des metabotropen glutamat-rezeptors-5
WO2004087653A2 (en) * 2003-04-03 2004-10-14 Merck & Co., Inc. 4-ring imidazole derivatives as modulators of metabotropic glutamate receptor-5
EP1613614A2 (de) * 2003-04-03 2006-01-11 Merck & Co., Inc. Diarylsubstituierte pyrazolmodulatoren des metabotropen glutamatrezeptors-5
WO2004089308A2 (en) * 2003-04-04 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrrole modulators of metabotropic glutamate receptor-5
US7268151B2 (en) * 2003-04-04 2007-09-11 Merck & Co., Inc. Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5
CA2537141A1 (en) * 2003-09-02 2005-03-10 Merck And Co., Inc. Bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5
US20060189661A1 (en) * 2003-11-03 2006-08-24 Wagenen Bradford V Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
AU2005215379A1 (en) 2004-02-12 2005-09-01 Merck & Co., Inc. Bipyridyl amides as modulators of metabotropic glutamate receptor-5
WO2007070563A2 (en) * 2005-12-13 2007-06-21 Harkness Pharmaceuticals, Inc. Stable solid forms of enterostatin

Also Published As

Publication number Publication date
US20050026963A1 (en) 2005-02-03
WO2003051833A3 (en) 2003-10-30
EP1458383A4 (de) 2005-05-25
US7569592B2 (en) 2009-08-04
WO2003051833A2 (en) 2003-06-26
ES2295441T3 (es) 2008-04-16
CA2469813C (en) 2009-02-24
AU2002359714A1 (en) 2003-06-30
DE60223720T2 (de) 2008-10-30
AU2002359714B2 (en) 2006-12-21
CA2469813A1 (en) 2003-06-26
JP4286146B2 (ja) 2009-06-24
EP1458383A2 (de) 2004-09-22
EP1458383B1 (de) 2007-11-21
JP2005516934A (ja) 2005-06-09

Similar Documents

Publication Publication Date Title
DE60223720D1 (de) Heteroaryl-substituierte pyrazol-modulatoren des metabotropen glutamatrezeptors-5
EP1453815A4 (de) Modulatoren des metabotropen glutamatrezeptors-5
ZA200501101B (en) Oxadiazoles as modulators of metabotropic glutamate receptor-5.
EP1458385A4 (de) Heteroaryl-substituierte imidazol-modulatoren des metabotropen glutamat-rezeptors-5
ATE369330T1 (de) O-desmethyl-venlafaxine succinat salz
DE60325025D1 (de) Modulatoren des vanilloidrezeptors
ATE451348T1 (de) N-(3-amino-2-hydroxy-propyl)substituierte alkylamidverbindungen
EP1458710A4 (de) Heteroarylsubstituierte pyrrolmodulatoren des metabotropen glutamatrezeptors 5
DE60239146D1 (de) Neue kristalline verbindung
IL166510A0 (en) 1,2,4"oxadiazole as modulators of metabotropic glutamate receptor-5
DK1563100T3 (da) Fortrængningssandwich-immuno-PCR
NO20041767L (no) Pyrrolidinonderivater
NO20023677L (no) Sementeringsmanifold-enhet
DE60219284D1 (de) Dreischichtige maschenware
EP1613617A4 (de) Diarylsubstituierte triazolmodulatoren des metabotropen glutamatrezeptors-5
EP1613265A4 (de) Di-aryl-substituierte pyrrol-modulatoren von metabotropischem glutamat-rezeptor-5
ATE335740T1 (de) Ringannelierte pyrazolderivate
DE60221187D1 (de) Bandraupe
DE60201256D1 (de) Elektrooptischer wanderwellenmodulator
DK1483451T3 (da) Betonblok
ATE346045T1 (de) Heteroaryl-substituierte aminocyclohexan-derivate
FI20010129A0 (fi) Kaksiviiraformeri
FI5259U1 (fi) Kehto
DE60211574D1 (de) Seriendruckgerät
ATA5002002A (de) Vibrator

Legal Events

Date Code Title Description
8327 Change in the person/name/address of the patent owner

Owner name: MERCK & CO., INC., RAHWAY, N.J., US

8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: MERCK SHARP & DOHME CORP., RAHWAY, N.J., US

8328 Change in the person/name/address of the agent

Representative=s name: MARKS & CLERK (LUXEMBOURG) LLP, LUXEMBOURG, LU

R081 Change of applicant/patentee

Ref document number: 1458383

Country of ref document: EP

Owner name: SCHERING CORPORATION, US

Free format text: FORMER OWNER: MERCK SHARP & DOHME CORP., RAHWAY, US

Effective date: 20121213

R082 Change of representative

Ref document number: 1458383

Country of ref document: EP

Representative=s name: MARKS & CLERK (LUXEMBOURG) LLP, LU

Effective date: 20121213