ES2295441T3 - Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato. - Google Patents

Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato. Download PDF

Info

Publication number
ES2295441T3
ES2295441T3 ES02794267T ES02794267T ES2295441T3 ES 2295441 T3 ES2295441 T3 ES 2295441T3 ES 02794267 T ES02794267 T ES 02794267T ES 02794267 T ES02794267 T ES 02794267T ES 2295441 T3 ES2295441 T3 ES 2295441T3
Authority
ES
Spain
Prior art keywords
pyrazol
pyridine
pyridin
benzonitrile
heteroaril
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
ES02794267T
Other languages
English (en)
Spanish (es)
Inventor
Nicholas D. P. 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 and Co Inc
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
Application granted granted Critical
Publication of ES2295441T3 publication Critical patent/ES2295441T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/38Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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

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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
ES02794267T 2001-12-18 2002-12-13 Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato. Expired - Lifetime ES2295441T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34138201P 2001-12-18 2001-12-18
US341382P 2001-12-18

Publications (1)

Publication Number Publication Date
ES2295441T3 true ES2295441T3 (es) 2008-04-16

Family

ID=23337314

Family Applications (1)

Application Number Title Priority Date Filing Date
ES02794267T Expired - Lifetime ES2295441T3 (es) 2001-12-18 2002-12-13 Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato.

Country Status (8)

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

Families Citing this family (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7074801B1 (en) * 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
DE60334781D1 (de) * 2002-03-12 2010-12-16 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
CN100422175C (zh) * 2003-04-03 2008-10-01 麦克公司 作为代谢型谷氨酸受体-5调制剂的四环咪唑衍生物
AU2004228057A1 (en) * 2003-04-03 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
JP2007504229A (ja) * 2003-09-02 2007-03-01 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体−5のモジュレーターとしてのビピリジルアミン類およびエーテル類
EP1715867A4 (en) * 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
TW200533664A (en) * 2004-02-18 2005-10-16 Astrazeneca Ab Tetrazole compounds and their use as metabotropic glutamate receptor antagonists
WO2005085214A1 (ja) * 2004-03-05 2005-09-15 Banyu Pharmaceutical Co., Ltd ジアリール置換複素5員環誘導体
EP1735284A1 (en) 2004-03-18 2006-12-27 Pfizer Limited N-(1-arylpyrazol-4l)sulfonamides and their use as parasiticides
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
EP1799659A1 (en) 2004-10-13 2007-06-27 PTC Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
DE102008020113A1 (de) 2008-04-23 2009-10-29 Bayer Schering Pharma Aktiengesellschaft Substituierte Dihydropyrazolone und ihre Verwendung
KR20070106690A (ko) * 2004-12-27 2007-11-05 아스트라제네카 아베 피라졸론 화합물 및 대사성 글루타메이트 수용체길항제로서 그들의 용도
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
CA2601098C (en) * 2005-03-16 2011-07-05 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
JP2008542255A (ja) * 2005-05-27 2008-11-27 ファイザー・プロダクツ・インク 肥満症の治療または体重減量の維持のためのカンナビノイド−1受容体アンタゴニストおよびミクロソームトリグリセリド輸送タンパク質阻害物質の併用
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP1928437A2 (en) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 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
EP1991212A1 (en) * 2006-03-08 2008-11-19 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
US20100009983A1 (en) * 2006-05-09 2010-01-14 Braincells, Inc. 5 ht receptor mediated neurogenesis
WO2007134077A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2068872A1 (en) * 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
AU2007299920A1 (en) * 2006-09-19 2008-03-27 Braincells, Inc. PPAR Mediated Modulation of Neurogenesis
DE102006050516A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dihydropyrazolone und ihre Verwendung
DE102006050513A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substitiuierte Dihydropyrazolone und ihre Verwendung
DE102006050515A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte Dipyridiyl-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
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
CN101842357A (zh) * 2007-08-30 2010-09-22 武田药品工业株式会社 取代的吡唑衍生物
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
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
JP5693452B2 (ja) 2008-08-04 2015-04-01 シーエイチディーアイ ファウンデーション,インコーポレーテッド 特定のキヌレニン−3−モノオキシゲナーゼインヒビター、医薬組成物およびそれらの使用方法
US20100120778A1 (en) * 2008-11-07 2010-05-13 Wyeth Quinoxaline-based lxr modulators
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
WO2011045224A1 (de) 2009-10-12 2011-04-21 Bayer Cropscience Ag 1- (pyrid-3-yl) -pyrazole und 1- (pyrimid-5-yl) -pyrazole als schädlingsbekämpfungsmittel
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
EP2611298A4 (en) * 2010-08-31 2014-07-30 Univ Vanderbilt BICYCLIC OXAZOLE AND THIAZOL COMPOUNDS AND THEIR USE AS ALLOSTERIC MODULATORS OF MGLUR-5 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
EP2651405A2 (en) 2010-12-14 2013-10-23 Electrophoretics Limited Casein kinase 1 (ck1 ) inhibitors
SI2750677T1 (sl) 2011-08-30 2017-10-30 Chdi Foundation, Inc. Inhibitorji kinurenin-3-monooksigenaze, farmacevtski sestavki in postopki njihove uporabe
MX2014002459A (es) 2011-08-30 2014-04-10 Chdi Foundation Inc Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodos de uso de los mismos.
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
GB201118652D0 (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
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
US8937176B2 (en) 2011-12-14 2015-01-20 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
WO2013092512A1 (en) 2011-12-21 2013-06-27 Bayer Intellectual Property Gmbh Substituted benzylpyrazoles
US8889677B2 (en) 2012-01-17 2014-11-18 Boehringer Ingellheim International GmbH Substituted triazoles useful as mGlu5 receptor modulators
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
CN104884449A (zh) * 2012-10-31 2015-09-02 拜尔农作物科学股份公司 作为害虫防治剂的新的杂环化合物
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
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
SI3004138T1 (sl) 2013-06-05 2024-07-31 Bausch Health Ireland Limited Ultra čisti agonisti gvanilat ciklaze C, postopek za njihovo pripravo in uporabo
GB201312800D0 (en) 2013-07-17 2013-08-28 Heptares Therapeutics Ltd mGlu5 modulators
MX373150B (es) 2014-03-26 2020-04-21 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JP6752715B2 (ja) 2014-03-26 2020-09-09 アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited 組合せ
WO2015161014A1 (en) * 2014-04-17 2015-10-22 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
JP6195684B2 (ja) 2014-06-03 2017-09-13 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd ピラゾール化合物及びt型カルシウムチャンネルブロッカーとしてのそれらの使用
CN106715421A (zh) 2014-07-17 2017-05-24 Chdi基金会股份有限公司 用于治疗hiv相关病症的方法和组合物
WO2016041892A1 (en) 2014-09-15 2016-03-24 Actelion Pharmaceuticals Ltd Triazole compounds as t-type calcium channel blockers
MA39484A (fr) 2014-09-19 2016-03-24 Bayer Pharma AG Indazoles à substituants benzyle utilisés comme inhibiteurs de bub1
TWI719960B (zh) 2015-02-10 2021-03-01 英商阿斯迪克治療公司 新穎組成物
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
DK3353177T3 (da) 2015-09-23 2020-08-24 Janssen Pharmaceutica Nv Tricykliske heterocykler til behandling af cancer
AU2016328693B2 (en) 2015-09-23 2021-03-11 Janssen Pharmaceutica Nv Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
CN110072521B (zh) 2016-12-16 2022-11-29 爱杜西亚药品有限公司 包含t型钙通道阻断剂的药物组合
MA47409A (fr) 2017-02-06 2019-12-11 Idorsia Pharmaceuticals Ltd Nouveau procédé de synthèse de 1-aryl-1-trifluorométhylcyclopropanes
EP3823614A4 (en) 2018-07-18 2022-03-30 Arcus Biosciences, Inc. SOLID FORMS OF AN AZOLOPYRIMIDINE COMPOUND
JP2024506858A (ja) 2021-02-02 2024-02-15 リミナル・バイオサイエンシーズ・リミテッド Gpr84アンタゴニストおよびその使用

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
NZ517221A (en) * 1999-08-19 2004-01-30 Nps Pharma Inc Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
US6660753B2 (en) * 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
DE60226756D1 (de) * 2001-10-04 2008-07-03 Merck & Co Inc Heteroarylsubstituierte tetrazolmodulatoren des metabotropischen glutamatrezeptors-5
EP1453815A4 (en) * 2001-11-30 2005-04-06 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
CA2470519C (en) * 2001-12-21 2009-11-17 Merck & Co., Inc. Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5
DE60334781D1 (de) * 2002-03-12 2010-12-16 Merck Sharp & Dohme Di-aryl-substituierte tetrazol-modulatoren des metabotropen glutamat-rezeptors-5
AU2004228057A1 (en) * 2003-04-03 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
CN100422175C (zh) * 2003-04-03 2008-10-01 麦克公司 作为代谢型谷氨酸受体-5调制剂的四环咪唑衍生物
CA2521396A1 (en) * 2003-04-04 2004-10-21 Merck & Co., Inc. Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5
JP2006522137A (ja) * 2003-04-04 2006-09-28 メルク エンド カムパニー インコーポレーテッド 代謝型グルタミン酸受容体−5のジ−アリール置換ピロールモジュレーター
JP2007504229A (ja) * 2003-09-02 2007-03-01 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体−5のモジュレーターとしてのビピリジルアミン類およびエーテル類
US20060189661A1 (en) * 2003-11-03 2006-08-24 Wagenen Bradford V Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE 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
EP1458383A2 (en) 2004-09-22
EP1458383A4 (en) 2005-05-25
US7569592B2 (en) 2009-08-04
DE60223720T2 (de) 2008-10-30
WO2003051833A3 (en) 2003-10-30
DE60223720D1 (de) 2008-01-03
JP4286146B2 (ja) 2009-06-24
AU2002359714A1 (en) 2003-06-30
JP2005516934A (ja) 2005-06-09
AU2002359714B2 (en) 2006-12-21
CA2469813C (en) 2009-02-24
CA2469813A1 (en) 2003-06-26
EP1458383B1 (en) 2007-11-21
WO2003051833A2 (en) 2003-06-26

Similar Documents

Publication Publication Date Title
ES2295441T3 (es) Moduladores de pirazol heteroaril sustituido de receptor 5 metabotropico de glutamato.
RU2451673C2 (ru) ПРОИЗВОДНЫЕ ПИРИДИНА И ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2
CA2462289A1 (en) Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5
RU2020113350A (ru) Модуляторы белка регулятора трансмембранной проводимости при муковисцидозе и способ применения
CA2469821A1 (en) Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5
RU2008141509A (ru) Mglur5 модуляторы 1
HRP20160172T1 (hr) Spojevi koji su inhibitori metaloenzima
JP2019518036A5 (https=)
JP2005527625A5 (https=)
RU2015132181A (ru) Фтор-[1,3]-оксазины в качестве ингибиторов васе1
PE20080545A1 (es) Isoxazolinas insecticidas
JP2005516934A5 (https=)
JP2017502049A5 (https=)
JP2019504854A5 (https=)
NZ609955A (en) Sgc stimulators
JP2018535999A5 (https=)
JP2007523208A5 (https=)
RU2006133909A (ru) Производные азабицикло {3. 1. 0}гексана, применимые в качестве модуляторов допаминовых рецепторов d3
JP2020515575A5 (https=)
SI2513053T1 (en) Pyrrolidine carboxylic acid derivatives as G-protein-coupled receptor 43 agonists (GPR43), pharmaceutical composition and methods for use in the treatment of metabolic disorders
JP2004536814A5 (https=)
HRP20120240T1 (hr) Piridil piperidin antagonisti receptora za oreksin
JP2016512259A5 (https=)
CA2486399A1 (en) Calcium receptor modulating agents
ME02437B (me) Disupstituirani oktahidropirolo[3,4-c]piroli kao modulatori oreksin receptora