ATE296809T1 - 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren - Google Patents

3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren

Info

Publication number
ATE296809T1
ATE296809T1 AT00980587T AT00980587T ATE296809T1 AT E296809 T1 ATE296809 T1 AT E296809T1 AT 00980587 T AT00980587 T AT 00980587T AT 00980587 T AT00980587 T AT 00980587T AT E296809 T1 ATE296809 T1 AT E296809T1
Authority
AT
Austria
Prior art keywords
csbp
kinase inhibitors
compounds
chinazoline
dihydro
Prior art date
Application number
AT00980587T
Other languages
English (en)
Inventor
Jerry L Adams
Michael J Bower
Jeffrey Charles Boehm
Don E Griswold
David C Underwood
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Application granted granted Critical
Publication of ATE296809T1 publication Critical patent/ATE296809T1/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
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    • A61P33/06—Antimalarials
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
AT00980587T 1999-11-23 2000-11-21 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren ATE296809T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16697599P 1999-11-23 1999-11-23
PCT/US2000/031894 WO2001038314A1 (en) 1999-11-23 2000-11-21 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors

Publications (1)

Publication Number Publication Date
ATE296809T1 true ATE296809T1 (de) 2005-06-15

Family

ID=22605428

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00980587T ATE296809T1 (de) 1999-11-23 2000-11-21 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren

Country Status (8)

Country Link
US (1) US7053098B1 (de)
EP (1) EP1233951B1 (de)
JP (1) JP2003514900A (de)
AT (1) ATE296809T1 (de)
AU (1) AU1783201A (de)
DE (1) DE60020595T2 (de)
ES (1) ES2241675T3 (de)
WO (1) WO2001038314A1 (de)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6548503B1 (en) 1998-11-04 2003-04-15 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
JP2003514900A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物
DE60023025T2 (de) 1999-11-23 2006-07-13 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
WO2001037837A1 (en) * 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)-QUINAZOLIN-2-ONES AND THEIR USE AS CSBP/p38 KINASE INHIBITORS
ES2230171T3 (es) 1999-11-23 2005-05-01 Smithkline Beecham Corporation Compuestos 3,4-dihidro-(1h)quinazolin-2-ona como inhibidores de csbp/p38 quinasa.
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
AUPR213700A0 (en) 2000-12-18 2001-01-25 Biota Scientific Management Pty Ltd Antiviral agents
AU2003245989A1 (en) 2002-07-09 2004-01-23 Boehringer Ingelheim Pharma Gmbh And Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
US8426429B2 (en) 2004-08-06 2013-04-23 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8383637B2 (en) 2004-08-06 2013-02-26 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
WO2006137421A1 (ja) * 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
ES2360957T3 (es) 2005-10-25 2011-06-10 Janssen Pharmaceutica Nv Derivados de 2-amino-3,4-dihidro-pirido(3,4-d)-pirimidina utiles como inhibidores de la beta-secretasa (bace).
US7932261B2 (en) 2006-02-06 2011-04-26 Janssen Pharmaceutica Nv Macrocycle derivatives useful as inhibitors of β-secretase (BACE)
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
CA2656507C (en) * 2006-07-17 2012-03-20 Amgen Inc. Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors
EP1992344A1 (de) 2007-05-18 2008-11-19 Institut Curie P38 Alpha als therapeutisches Target für Erkrankungen, die mit einer FGFR3- Mutation assoziiert sind
WO2009097278A1 (en) 2008-01-28 2009-08-06 Janssen Pharmaceutica N.V. 6-SUBSTITUTED-THIO-2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US8916704B1 (en) 2013-10-02 2014-12-23 King Fahd University Of Petroleum And Minerals Dihydroquinone derivatives of piperidine and piperazine
US20190060286A1 (en) 2016-02-29 2019-02-28 University Of Florida Research Foundation, Incorpo Chemotherapeutic Methods
ES2927715T3 (es) 2017-10-05 2022-11-10 Fulcrum Therapeutics Inc Inhibidores de la quinasa p38 reducen la expresión de dux4 y de los genes que le siguen para el tratamiento de la FSHD

Family Cites Families (148)

* 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
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
US3929807A (en) 1971-05-10 1975-12-30 Ciba Geigy Corp 2-Substituted-4(5)-(aryl)-5(4)-(2,3 or -4-pyridyl)-imidazoles
US3940486A (en) 1971-05-10 1976-02-24 Ciba-Geigy Corporation Imidazole derivatives in the treatment of pain
US3703475A (en) 1971-06-21 1972-11-21 Continental Oil Co Preparation of oil soluble sulfonic acids useful as dispersant additives
US4058614A (en) 1973-12-04 1977-11-15 Merck & Co., Inc. Substituted imidazole compounds and therapeutic compositions therewith
US4199592A (en) 1978-08-29 1980-04-22 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-2-nitroimidazoles
GR75287B (de) 1980-07-25 1984-07-13 Ciba Geigy Ag
WO1983002613A1 (fr) 1981-07-20 1983-08-04 Sallmann, Alfred Composes oxazoiques a triple substitution
US4503065A (en) 1982-08-03 1985-03-05 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl 1-2-halo imidazoles
JPS60226882A (ja) 1984-04-24 1985-11-12 Nippon Zoki Pharmaceut Co Ltd 新規ピリミドピリミジン誘導体
US4565875A (en) 1984-06-27 1986-01-21 Fmc Corporation Imidazole plant growth regulators
US4686231A (en) 1985-12-12 1987-08-11 Smithkline Beckman Corporation Inhibition of 5-lipoxygenase products
IL83467A0 (en) 1986-08-15 1988-01-31 Fujisawa Pharmaceutical Co Imidazole derivatives,processes for their preparation and pharmaceutical compositions containing the same
EP0533837A4 (en) 1990-06-12 1994-11-17 Smithkline Beecham Corp Inhibition of 5-lipoxygenase and cyclooxygenase pathway mediated diseases
FR2665898B1 (fr) 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
IE913473A1 (en) 1990-10-15 1992-04-22 Fujisawa Pharmaceutical Co Quinazoline derivatives and their preparation
EP0563286A4 (en) 1990-12-13 1995-01-11 Smithkline Beecham Corp Novel csaids
JPH06504779A (ja) 1990-12-13 1994-06-02 スミスクライン・ビーチャム・コーポレイション 新規ｃｓａｉｄｓ
WO1992012154A1 (en) 1990-12-31 1992-07-23 Fujisawa Pharmaceutical Co., Ltd. Imidazotriazine derivatives
JP3375659B2 (ja) 1991-03-28 2003-02-10 テキサス インスツルメンツ インコーポレイテツド 静電放電保護回路の形成方法
IL102764A0 (en) 1991-08-16 1993-01-31 Merck & Co Inc Quinazoline derivatives,and pharmaceutical compositions containing them
GB9816837D0 (en) 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
US6008235A (en) 1992-01-13 1999-12-28 Smithkline Beecham Corporation Pyridyl substituted imidazoles
JP3264492B2 (ja) 1992-01-13 2002-03-11 スミスクライン・ビーチャム・コーポレイション ピリジル置換イミダゾール
US5716972A (en) 1993-01-13 1998-02-10 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US5656644A (en) 1994-07-20 1997-08-12 Smithkline Beecham Corporation Pyridyl imidazoles
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
GB9303993D0 (en) 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
IL110296A (en) 1993-07-16 1999-12-31 Smithkline Beecham Corp Imidazole compounds process for their preparation and pharmaceutical compositions containing them
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5593991A (en) 1993-07-16 1997-01-14 Adams; Jerry L. Imidazole compounds, use and process of making
AU7629594A (en) 1993-07-21 1995-02-20 Smithkline Beecham Corporation Imidazoles for treating cytokine mediated disease
US5783664A (en) 1993-09-17 1998-07-21 Smithkline Beecham Corporation Cytokine suppressive anit-inflammatory drug binding proteins
US5871934A (en) 1993-09-17 1999-02-16 Smithkline Beecham Corporation Screening methods using cytokine suppressive anti-inflammatory drug (CSAID) binding proteins
US5869043A (en) 1993-09-17 1999-02-09 Smithkline Beecham Corporation Drug binding protein
US5543520A (en) 1993-10-01 1996-08-06 Ciba-Geigy Corporation Pyrimidine derivatives
PT672042E (pt) 1993-10-01 2006-08-31 Novartis Ag Derivados de pirimidinoamina farmacologicamente activos e processos para a sua preparacao
AU693475B2 (en) 1993-10-01 1998-07-02 Novartis Ag Pyrimidineamine derivatives and processes for the preparation thereof
DE69429078T2 (de) 1993-10-01 2002-07-11 Novartis Ag, Basel Pharmacologisch wirksame pyridinderivate und verfahren zu deren herstellung
AU1046895A (en) * 1993-11-05 1995-05-23 Merck & Co., Inc. New quinazolines as inhibitors of hiv reverse transcriptase
EP1306377A3 (de) 1993-11-08 2003-05-07 Smithkline Beecham Corporation Pyridyl-Oxazole und ihre Verwendung als Cytokine-Inhibitoren
US5559137A (en) 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5545669A (en) 1994-06-02 1996-08-13 Adams; Jerry L. Anti-inflammatory compounds
PL321292A1 (en) 1995-01-12 1997-11-24 Smithkline Beecham Corp Novel xchemical compounds
IL118544A (en) 1995-06-07 2001-08-08 Smithkline Beecham Corp History of imidazole, the process for their preparation and the pharmaceutical preparations containing them
US5739143A (en) 1995-06-07 1998-04-14 Smithkline Beecham Corporation Imidazole compounds and compositions
CA2228050A1 (en) 1995-08-10 1997-02-20 Harold G. Selnick 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
JP3294616B2 (ja) 1995-08-10 2002-06-24 メルク エンド カンパニー インコーポレーテッド ２−置換アリールピロール、このような化合物を含む組成物及び使用方法
IL123950A (en) 1995-10-06 2001-04-30 Merck & Co Inc Substituted imidazoles having anti-cancer and cytokine inhibitory activity and pharmaceutical compositions containing them
AU7482396A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
AU7529096A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
WO1997016442A1 (en) 1995-10-31 1997-05-09 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
ZA9610687B (en) 1995-12-22 1997-09-29 Smithkline Beecham Corp Novel synthesis.
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
EP0883402A4 (de) 1996-01-11 1999-08-11 Smithkline Beecham Corp Neue cycloalkyl substituierte imidazole
US5756499A (en) 1996-01-11 1998-05-26 Smithkline Beecham Corporation Substituted imidazole compounds
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
EP1005343A4 (de) 1996-03-08 2000-06-07 Smithkline Beecham Corp Verwendung von csaids als inhibitoren der angiogenese
US6096748A (en) * 1996-03-13 2000-08-01 Smithkline Beecham Corporation Pyrimidine compounds useful in treating cytokine mediated diseases
WO1997035856A1 (en) 1996-03-25 1997-10-02 Smithkline Beecham Corporation Novel treatment for cns injuries
WO1997035855A1 (en) 1996-03-25 1997-10-02 Smithkline Beecham Corporation Novel treatment for cns injuries
JP2000504023A (ja) 1996-04-03 2000-04-04 メルク エンド カンパニー インコーポレーテッド 癌治療方法
US6875769B2 (en) 1996-05-23 2005-04-05 Pfizer Inc. Substituted6,6-hetero-bicyclicderivatives
AU708883B2 (en) 1996-06-10 1999-08-12 Merck & Co., Inc. Substituted imidazoles having cytokine inhibitory activity
SI0912518T1 (en) 1996-07-18 2003-12-31 Merck Frosst Canada & Co. Substituted pyridines as selective cyclooxygenase-2 inhibitors
WO1998006715A1 (en) 1996-08-09 1998-02-19 Smithkline Beecham Corporation Novel piperazine containing compounds
WO1998007425A1 (en) 1996-08-21 1998-02-26 Smithkline Beecham Corporation Imidazole compounds, compositions and use
AU5147598A (en) 1996-10-17 1998-05-11 Smithkline Beecham Corporation Methods for reversibly inhibiting myelopoiesis in mammalian tissue
HUP9903330A2 (hu) 1996-11-19 2000-03-28 Amgen Inc. Gyulladásgátló hatású, aril- és heteroaril csoporttal szubsztituált kondenzált pirrolszármazékok, valamint ezeket tartalmazó gyógyászati készítmények
CA2271893A1 (en) 1996-11-20 1998-05-28 Linda L. Chang Triaryl substituted imidazoles as glucagon antagonists
CA2274093C (en) 1996-12-05 2006-11-07 Amgen Inc. Substituted pyrimidinone and pyridinone compounds and their use
ZA9711092B (en) 1996-12-11 1999-07-22 Smithkline Beecham Corp Novel compounds.
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
US5929076A (en) 1997-01-10 1999-07-27 Smithkline Beecham Corporation Cycloalkyl substituted imidazoles
HUP0002842A3 (en) 1997-04-24 2002-01-28 Ortho Mcneil Pharm Inc Substituted imidazoles, process for producing them, pharmaceutical compositions containing them, their use and their intermediates
MA26487A1 (fr) 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .
NZ501112A (en) 1997-05-22 2002-10-25 G Substituted pyrazoles as p38 kinase inhibitors
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
US6087381A (en) 1997-05-22 2000-07-11 G. D. Searle & Company Pyrazole derivatives as p38 kinase inhibitors
US5932576A (en) 1997-05-22 1999-08-03 G. D. Searle & Company 3(5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
EP1019040B1 (de) 1997-05-23 2004-09-29 Bayer Corporation Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen
AU742293B2 (en) 1997-06-12 2001-12-20 Aventis Pharma Limited Imidazolyl-cyclic acetals
US20020156104A1 (en) 1997-06-13 2002-10-24 Jerry L. Adams Novel pyrazole and pyrazoline substituted compounds
JP2002505690A (ja) 1997-06-19 2002-02-19 スミスクライン・ビーチャム・コーポレイション 新規なアリールオキシピリミジン置換イミダゾール化合物
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
GB9713726D0 (en) 1997-06-30 1997-09-03 Ciba Geigy Ag Organic compounds
AU8757098A (en) 1997-06-30 1999-02-10 Ortho-Mcneil Pharmaceutical, Inc. 2-substituted imidazoles useful in the treatment of inflammatory diseases
US6251914B1 (en) 1997-07-02 2001-06-26 Smithkline Beecham Corporation Cycloalkyl substituted imidazoles
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
AR016294A1 (es) 1997-07-02 2001-07-04 Smithkline Beecham Corp Compuesto de imidazol sustituido, composicion farmaceutica que la contiene, su uso en la fabricacion de un medicamento y procedimiento para supreparacion
US6362193B1 (en) 1997-10-08 2002-03-26 Smithkline Beecham Corporation Cycloalkenyl substituted compounds
EP1021173A1 (de) 1997-10-10 2000-07-26 Imperial College Innovations Limited Verwendung von cytokin-unterdrückenden verbindungen (csaid) zur behandlung von gebärmutterkontraktionen
JP2002515891A (ja) * 1997-12-19 2002-05-28 スミスクライン・ビーチャム・コーポレイション 新規なピペリジン含有化合物
JP2001526230A (ja) 1997-12-19 2001-12-18 スミスクライン・ビーチャム・コーポレイション ヘテロアリール置換イミダゾール化合物、その医薬組成物および使用
IL136768A0 (en) 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
JP2002513562A (ja) 1998-05-04 2002-05-14 バーテックス ファーマシューティカルズ インコーポレイテッド 結晶化可能なｊｎｋ複合体
PL344004A1 (en) 1998-05-05 2001-09-10 Hoffmann La Roche Pyrazole derivatives as p-38 map kinase inhibitors
GB9809869D0 (en) 1998-05-09 1998-07-08 Medical Res Council Inhibition of protein kinases
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
WO1999058523A1 (en) 1998-05-14 1999-11-18 G.D. Searle & Co. 1,5-DIARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
IL139710A (en) 1998-05-15 2005-07-25 Astazeneca Ab Benzamide derivatives for the treatment of diseases mediated by cytokines
US6579872B1 (en) 1998-05-15 2003-06-17 Astrazeneca Ab Bezamide derivatives for the treatment of diseases mediated by cytokines
BR9910621A (pt) 1998-05-22 2001-01-30 Smithkline Beecham Corp Novos compostos de imidazol 2-alquil substituìdos
EP1080078B1 (de) 1998-05-22 2006-02-01 Scios Inc. Heterozyclische derivate für die behandlung von herzversagen und andere erkrankungen
CA2333157A1 (en) 1998-05-26 1999-12-02 Smithkline Beecham Corporation Novel substituted imidazole compounds
AU4429799A (en) * 1998-06-12 1999-12-30 Vertex Pharmaceuticals Incorporated Inhibitors of p38
AU4395399A (en) 1998-07-02 2000-01-24 Sankyo Company Limited Five-membered heteroaryl compounds
US6207687B1 (en) 1998-07-31 2001-03-27 Merck & Co., Inc. Substituted imidazoles having cytokine inhibitory activity
BR9912729A (pt) 1998-08-04 2001-05-02 Astrazeneca Ab Derivado de amida, processo para prepará-lo, e, uso do mesmo
ES2221426T3 (es) 1998-08-20 2004-12-16 Smithkline Beecham Corporation Nuevos compuestos de triazol sustituidos.
CA2342251A1 (en) 1998-08-28 2000-03-09 Scios Inc. Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
AU762245B2 (en) 1998-09-18 2003-06-19 Vertex Pharmaceuticals Incorporated Inhibitors of p38
ATE254105T1 (de) 1998-09-25 2003-11-15 Astrazeneca Ab Benzamid-derivate und ihre verwendung als cytokine inhibitoren
CN1158266C (zh) 1998-10-01 2004-07-21 阿斯特拉曾尼卡有限公司 化合物
WO2000019824A1 (en) 1998-10-07 2000-04-13 Smithkline Beecham Corporation Novel treatment for stroke management
EP1261334A1 (de) 1998-10-20 2002-12-04 Omeros Corporation Spüllösung enthaltend mapk hemmern und deren verwendung zur behandlung von schmerz und entzündung
PL347432A1 (en) 1998-10-23 2002-04-08 Hoffmann La Roche Bicyclic nitrogen heterocycles
WO2000026209A1 (en) 1998-11-03 2000-05-11 Novartis Ag Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles
US6548503B1 (en) 1998-11-04 2003-04-15 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
US6350744B1 (en) 1998-11-20 2002-02-26 Merck & Co., Inc. Compounds having cytokine inhibitory activity
EP1131318B1 (de) 1998-11-20 2004-03-24 G.D. Searle LLC Verfahren zur herstellung 5-substituierter pyrazole unter verwendung von dithietane
EP1140916B1 (de) 1998-12-16 2002-11-13 Aventis Pharma Limited Heteroaryl-zyklische acetale
KR100711538B1 (ko) 1998-12-25 2007-04-27 아스카 세이야쿠 가부시키가이샤 아미노피라졸 유도체
EP1140083A4 (de) 1999-01-08 2004-01-02 Smithkline Beecham Corp Neue verbindungen
EP2298311B1 (de) 1999-01-13 2012-05-09 Bayer HealthCare LLC Omega-carboxyarylsubstituierte-Diphenyl-Harnstoffe als p38-Kinasehemmer
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
JP2000281588A (ja) 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
CN1281604C (zh) 1999-06-03 2006-10-25 帝国脏器制药株式会社 取代吡唑化合物
WO2001000229A1 (en) 1999-06-24 2001-01-04 Pharmacia Corporation Combination of tumors necrocis factor (tnf) antagonists and cox-2 inhibitors for the treatment of inflammation
KR20020032591A (ko) 1999-09-17 2002-05-03 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 라이노바이러스 감염에서의 ｃｓａｉｄ의 용도
CA2395564A1 (en) 1999-11-22 2001-05-31 Smithkline Beecham Plc Novel compounds
DE60023025T2 (de) * 1999-11-23 2006-07-13 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
ES2230171T3 (es) 1999-11-23 2005-05-01 Smithkline Beecham Corporation Compuestos 3,4-dihidro-(1h)quinazolin-2-ona como inhibidores de csbp/p38 quinasa.
JP2003514900A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物
WO2001037837A1 (en) * 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)-QUINAZOLIN-2-ONES AND THEIR USE AS CSBP/p38 KINASE INHIBITORS
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
US6565880B2 (en) 2000-07-24 2003-05-20 Boehringer Ingelheim Pharmaceuticals, Inc. Oral dosage formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea
AU2002248269A1 (en) 2000-10-19 2002-08-12 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
EP1337250A2 (de) 2000-10-19 2003-08-27 SmithKline Beecham Corporation Verwendung von p38-hemmern zur behandlung von rauchinhalation
AU2002246855B2 (en) 2000-10-23 2005-12-22 Smithkline Beecham Corporation Novel compounds
ES2289004T3 (es) 2000-11-20 2008-02-01 Smithkline Beecham Corporation Nuevos compuestos.
JP2004521892A (ja) 2000-12-20 2004-07-22 メルク　エンド　カムパニー　インコーポレーテッド （ハロ−ベンゾカルボニル）複素環縮合フェニル系ｐ３８キナーゼ阻害剤
KR20040103972A (ko) 2002-04-19 2004-12-09 스미스클라인 비참 코포레이션 신규 화합물

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AU1783201A (en) 2001-06-04
EP1233951A4 (de) 2003-05-21
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