JP2003525295A - １，５−二置換−３，４−ジヒドロ−１ｈ−ピリミド［４，５−ｄ］ピリミジン−２−オン化合物およびｃｓｂｐ／ｐ３８キナーゼ介在疾患の治療におけるその使用 - Google Patents

１，５−二置換−３，４−ジヒドロ−１ｈ−ピリミド［４，５−ｄ］ピリミジン−２−オン化合物およびｃｓｂｐ／ｐ３８キナーゼ介在疾患の治療におけるその使用

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Publication number
JP2003525295A
JP2003525295A JP2001564176A JP2001564176A JP2003525295A JP 2003525295 A JP2003525295 A JP 2003525295A JP 2001564176 A JP2001564176 A JP 2001564176A JP 2001564176 A JP2001564176 A JP 2001564176A JP 2003525295 A JP2003525295 A JP 2003525295A
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Prior art keywords
alkyl
aryl
optionally substituted
dihydro
pyrimidin
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Pending
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JP2001564176A
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English (en)
Japanese (ja)
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JP2003525295A5 (enExample
Inventor
ジェリー・エル・アダムズ
ジェフリー・シー・ボーム
ラルフ・エフ・ホール
ジョン・ジェイ・タガート
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SmithKline Beecham Corp
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SmithKline Beecham Corp
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Publication date
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Publication of JP2003525295A publication Critical patent/JP2003525295A/ja
Publication of JP2003525295A5 publication Critical patent/JP2003525295A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
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    • 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
    • A61P27/02—Ophthalmic agents
    • 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
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
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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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • 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
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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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Toxicology (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
JP2001564176A 2000-03-02 2001-03-02 １，５−二置換−３，４−ジヒドロ−１ｈ−ピリミド［４，５−ｄ］ピリミジン−２−オン化合物およびｃｓｂｐ／ｐ３８キナーゼ介在疾患の治療におけるその使用 Pending JP2003525295A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US18641900P 2000-03-02 2000-03-02
US60/186,419 2000-03-02
PCT/US2001/006688 WO2001064679A1 (en) 2000-03-02 2001-03-02 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

Publications (2)

Publication Number Publication Date
JP2003525295A true JP2003525295A (ja) 2003-08-26
JP2003525295A5 JP2003525295A5 (enExample) 2008-04-03

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Country Status (25)

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EP (1) EP1265900B1 (enExample)
JP (1) JP2003525295A (enExample)
KR (1) KR100806978B1 (enExample)
CN (1) CN100482664C (enExample)
AR (2) AR030053A1 (enExample)
AT (1) ATE362473T1 (enExample)
AU (2) AU3999201A (enExample)
BR (1) BR0108715A (enExample)
CA (1) CA2402092C (enExample)
CY (1) CY1106816T1 (enExample)
CZ (1) CZ20022933A3 (enExample)
DE (1) DE60128457T2 (enExample)
DK (1) DK1265900T3 (enExample)
ES (1) ES2287107T3 (enExample)
HU (1) HUP0204431A3 (enExample)
IL (3) IL151426A0 (enExample)
MX (1) MXPA02008588A (enExample)
MY (1) MY141144A (enExample)
NO (1) NO326409B1 (enExample)
NZ (1) NZ520914A (enExample)
PL (1) PL358280A1 (enExample)
PT (1) PT1265900E (enExample)
TW (1) TWI290926B (enExample)
WO (1) WO2001064679A1 (enExample)
ZA (1) ZA200207017B (enExample)

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JP2004517922A (ja) * 2000-10-23 2004-06-17 スミスクライン・ビーチャム・コーポレイション 新規化合物
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
JP2005530838A (ja) * 2002-06-20 2005-10-13 セルテック アール アンド ディ リミテッド Ｐ３８キナーゼインヒビターとしてのアリールアミン置換二環式ヘテロ芳香族化合物
JP2005537300A (ja) * 2002-08-13 2005-12-08 セルテック アール アンド ディ リミテッド キナーゼ阻害剤としての二環式複素芳香族化合物
JP2007145828A (ja) * 2005-10-28 2007-06-14 Otsuka Pharmaceut Co Ltd 医薬組成物
JP2007517052A (ja) * 2003-12-23 2007-06-28 ノバルティス アクチエンゲゼルシャフト 二環式ヘテロ環式ｐ−３８キナーゼ阻害剤
JP2008523099A (ja) * 2004-12-13 2008-07-03 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
JP2009542818A (ja) * 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
JP2009542817A (ja) * 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
JP2016533372A (ja) * 2013-10-16 2016-10-27 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合複素環化合物、その調製方法、医薬組成物及びその使用

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DE69939168D1 (de) 1998-05-26 2008-09-04 Warner Lambert Co Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole 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
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
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
GB0124848D0 (en) * 2001-10-16 2001-12-05 Celltech R&D Ltd Chemical compounds
CN100369898C (zh) 2002-02-12 2008-02-20 史密丝克莱恩比彻姆公司 用作p38抑制剂的烟酰胺衍生物
CN1324015C (zh) 2002-02-13 2007-07-04 霍夫曼-拉罗奇有限公司 吡啶－和嘧啶－衍生物
KR20040103972A (ko) * 2002-04-19 2004-12-09 스미스클라인 비참 코포레이션 신규 화합물
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
US7084270B2 (en) * 2002-08-14 2006-08-01 Hoffman-La Roche Inc. Pyrimido compounds having antiproliferative activity
EP1539121A4 (en) 2002-08-29 2008-08-13 Scios Inc METHOD OF REQUESTING OSTEOGENESIS
US7129351B2 (en) 2002-11-04 2006-10-31 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
US7384937B2 (en) 2002-11-06 2008-06-10 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
CA2521124A1 (en) 2003-04-10 2004-10-21 F. Hoffmann-La Roche Ag Pyrimido compounds
US7244441B2 (en) 2003-09-25 2007-07-17 Scios, Inc. Stents and intra-luminal prostheses containing map kinase inhibitors
EP1676574A3 (en) 2004-12-30 2006-07-26 Johnson & Johnson Vision Care, Inc. Methods for promoting survival of transplanted tissues and cells
KR101040394B1 (ko) * 2010-05-18 2011-06-09 (주)이성산업 역화 방지 기능을 갖는 야외용 가스 히터
CN102816162B (zh) * 2011-06-10 2016-04-27 中国科学院广州生物医药与健康研究院 嘧啶并嘧啶酮类化合物及其药用组合物和应用
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
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
CN118434722A (zh) 2021-10-20 2024-08-02 英矽智能科技知识产权有限公司 甲硫氨酸腺苷转移酶2a(mat2a)抑制剂及其用途

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WO1999061444A2 (en) * 1998-05-26 1999-12-02 Warner-Lambert Company Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation
WO1999064400A1 (en) * 1998-06-12 1999-12-16 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
JP2000501116A (ja) * 1996-08-06 2000-02-02 ファイザー インク． 置換ピリド―またはピリミド―含有６，６―または６，７―二環式誘導体

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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
PL347432A1 (en) * 1998-10-23 2002-04-08 Hoffmann La Roche Bicyclic nitrogen heterocycles

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JP2000501116A (ja) * 1996-08-06 2000-02-02 ファイザー インク． 置換ピリド―またはピリミド―含有６，６―または６，７―二環式誘導体
WO1999061444A2 (en) * 1998-05-26 1999-12-02 Warner-Lambert Company Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation
WO1999064400A1 (en) * 1998-06-12 1999-12-16 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38

Cited By (12)

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EP1265900B1 (en) 2007-05-16
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