ATE392421T1 - Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung - Google Patents

Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung

Info

Publication number
ATE392421T1
ATE392421T1 AT02756943T AT02756943T ATE392421T1 AT E392421 T1 ATE392421 T1 AT E392421T1 AT 02756943 T AT02756943 T AT 02756943T AT 02756943 T AT02756943 T AT 02756943T AT E392421 T1 ATE392421 T1 AT E392421T1
Authority
AT
Austria
Prior art keywords
sup
kinase inhibitors
pyrazole
derived kinase
compounds
Prior art date
Application number
AT02756943T
Other languages
English (en)
Inventor
Michael Hale
James Janetka
Francois Maltais
Qing Tang
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE392421T1 publication Critical patent/ATE392421T1/de

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P25/08—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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Toxicology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
AT02756943T 2001-08-03 2002-08-02 Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung ATE392421T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30986501P 2001-08-03 2001-08-03

Publications (1)

Publication Number Publication Date
ATE392421T1 true ATE392421T1 (de) 2008-05-15

Family

ID=23200008

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02756943T ATE392421T1 (de) 2001-08-03 2002-08-02 Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung

Country Status (9)

Country Link
US (2) US6750239B2 (de)
EP (1) EP1423382B1 (de)
JP (1) JP4357295B2 (de)
AT (1) ATE392421T1 (de)
AU (1) AU2002321910A1 (de)
CA (1) CA2456192A1 (de)
DE (1) DE60226154T2 (de)
MX (1) MXPA04001087A (de)
WO (1) WO2003011855A2 (de)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1423382B1 (de) * 2001-08-03 2008-04-16 Vertex Pharmaceuticals Incorporated Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
UA79804C2 (en) * 2002-07-03 2007-07-25 Janssen Pharmaceutica Nv Cck-1 receptor modulators
US7094791B2 (en) * 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
DE602004012578T2 (de) 2003-08-15 2008-12-11 Vertex Pharmaceuticals Inc., Cambridge Als inhibitoren von c-met geeignete pyrrolzusammensetzungen
NZ547696A (en) 2003-12-23 2009-12-24 Astex Therapeutics Ltd Pyrazole derivatives as protein kinase modulators
WO2005102346A2 (en) * 2004-04-23 2005-11-03 Ab Science Use of c-kit inhibitors for treating fibrosis
TW200639163A (en) * 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
PT1853588E (pt) * 2005-02-16 2008-08-25 Astrazeneca Ab Compostos químicos
KR20080015409A (ko) * 2005-05-16 2008-02-19 아스트라제네카 아베 티로신 키나제 억제제로서 유용한 피라졸릴아미노피리미딘 유도체
WO2006136823A1 (en) * 2005-06-21 2006-12-28 Astex Therapeutics Limited Heterocyclic containing amines as kinase b inhibitors
EP1902032A1 (de) * 2005-06-22 2008-03-26 Astex Therapeutics Limited Pharmazeutische verbindungen
EP1933832A2 (de) 2005-06-23 2008-06-25 Astex Therapeutics Limited Pharmazeutische kombinationen mit pyrazol-derivaten als proteinkinase-modulatoren
EP1945631B8 (de) * 2005-10-28 2013-01-02 AstraZeneca AB 4-(3-aminopyrazol)pyrimidinderivate zur verwendung als tyrosinkinaseinhibitoren bei der behandlung von krebs
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
CN101389324A (zh) * 2005-12-23 2009-03-18 史密丝克莱恩比彻姆公司 Aurora激酶的氮杂吲哚抑制剂
CA2642762A1 (en) 2006-02-16 2007-08-30 Schering Corporation Pyrrolidine derivatives as erk inhibitors
US8173365B2 (en) 2006-03-24 2012-05-08 The University Of Tokyo Method for inhibiting signal transduction, signal transduction inhibitor to be used therein and use thereof
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
ES2543325T3 (es) * 2007-02-07 2015-08-18 Glaxosmithkline Llc Inhibidores de la actividad de Akt
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
CN101679429A (zh) * 2007-04-18 2010-03-24 阿斯利康(瑞典)有限公司 5-氨基吡唑-3-基-3h-咪唑并[4,5-b]吡啶衍生物及其治疗癌的用途
ES2369596T3 (es) * 2007-05-04 2011-12-02 Astrazeneca Ab Derivados de amino-tiazolil-pirimidina y su uso para el tratamiento del cáncer.
UA99459C2 (en) * 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
JP5276676B2 (ja) 2008-02-21 2013-08-28 メルク・シャープ・アンド・ドーム・コーポレーション Ｅｒｋ阻害剤である化合物
CA2727073A1 (en) * 2008-06-11 2009-12-17 Astrazeneca Ab Tricyclic 2,4-diamin0-l,3,5-triazine derivatives useful for the treatment of cancer and myeloproliferative disorders
US20110129455A1 (en) * 2008-06-26 2011-06-02 Hong Lin Inhibitors of akt activity
EP2303277A4 (de) * 2008-06-26 2011-08-17 Glaxosmithkline Llc Hemmer der akt-aktivität
RU2011116928A (ru) * 2008-09-30 2012-11-20 Астразенека Аб (Se) Гетероциклические ингибиторы jак киназы
US20110288142A1 (en) 2009-01-30 2011-11-24 Chen Pingyun Y CRYSTALLINE N--5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
EP2642856B1 (de) 2010-11-24 2017-07-19 The Ohio State University Research Foundation Integrin-gekoppelte kinasehemmer
US9303024B2 (en) 2011-10-11 2016-04-05 Dana-Farber Cancer Institute, Inc. Pyrazol-3-ones that activate pro-apoptotic BAX
WO2014138661A1 (en) 2013-03-08 2014-09-12 Mayo Foundation For Medical Education And Research Methods and materials for identifying and treating mammals having lung adenocarcinoma characterized by neuroendocrine differentiation

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Publication number Priority date Publication date Assignee Title
US5837719A (en) * 1995-08-10 1998-11-17 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
US6087496A (en) * 1998-05-22 2000-07-11 G. D. Searle & Co. Substituted pyrazoles suitable as p38 kinase inhibitors
AU7726898A (en) * 1997-05-22 1998-12-11 G.D. Searle & Co. Pyrazole derivatives as p38 kinase inhibitors
BR0104424A (pt) 2000-02-05 2002-01-08 Vertex Pharma Composições de pirazol úteis como inibidores de erk
EP1423382B1 (de) * 2001-08-03 2008-04-16 Vertex Pharmaceuticals Incorporated Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung

Also Published As

Publication number Publication date
WO2003011855A3 (en) 2003-09-25
JP4357295B2 (ja) 2009-11-04
CA2456192A1 (en) 2003-02-13
DE60226154T2 (de) 2009-05-20
AU2002321910A1 (en) 2003-02-17
WO2003011855A2 (en) 2003-02-13
US6750239B2 (en) 2004-06-15
DE60226154D1 (de) 2008-05-29
EP1423382A2 (de) 2004-06-02
US20030144337A1 (en) 2003-07-31
MXPA04001087A (es) 2004-07-08
US7183307B2 (en) 2007-02-27
EP1423382B1 (de) 2008-04-16
JP2005500353A (ja) 2005-01-06
US20040209935A1 (en) 2004-10-21

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