CN100358892C - 7-氧代吡啶并嘧啶 - Google Patents

7-氧代吡啶并嘧啶 Download PDF

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Publication number
CN100358892C
CN100358892C CNB018150276A CN01815027A CN100358892C CN 100358892 C CN100358892 C CN 100358892C CN B018150276 A CNB018150276 A CN B018150276A CN 01815027 A CN01815027 A CN 01815027A CN 100358892 C CN100358892 C CN 100358892C
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China
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compound
alkyl
formula
hydrogen
methyl
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Expired - Fee Related
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Chinese (zh)
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CN1451004A (zh
Inventor
温贝托·巴托洛梅·阿塞诺
陈健·吉弗瑞
詹姆斯·帕特里克·杜恩
大卫·迈克尔·戈尔茨坦
朱莉·安妮·利姆
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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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
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • 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
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • 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
    • A61P25/28—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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—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
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
CNB018150276A 2000-08-31 2001-08-22 7-氧代吡啶并嘧啶 Expired - Fee Related CN100358892C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22957700P 2000-08-31 2000-08-31
US60/229,577 2000-08-31

Related Child Applications (1)

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CNB2005100835295A Division CN1303072C (zh) 2000-08-31 2001-08-22 7－氧代吡啶并嘧啶

Publications (2)

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CN1451004A CN1451004A (zh) 2003-10-22
CN100358892C true CN100358892C (zh) 2008-01-02

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CNB2005100835295A Expired - Fee Related CN1303072C (zh) 2000-08-31 2001-08-22 7－氧代吡啶并嘧啶

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Country Status (18)

Country Link
EP (1) EP1315727B1 (https=)
JP (1) JP4146721B2 (https=)
KR (1) KR100582325B1 (https=)
CN (2) CN100358892C (https=)
AR (1) AR033996A1 (https=)
AT (1) ATE298751T1 (https=)
AU (2) AU1214702A (https=)
BR (1) BR0113590A (https=)
CA (1) CA2420122A1 (https=)
DE (1) DE60111752T2 (https=)
ES (1) ES2243568T3 (https=)
GT (1) GT200100190A (https=)
MX (1) MXPA03001733A (https=)
PA (1) PA8527401A1 (https=)
PE (1) PE20020524A1 (https=)
UY (1) UY26920A1 (https=)
WO (1) WO2002018379A2 (https=)
ZA (1) ZA200301078B (https=)

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KR20040103972A (ko) * 2002-04-19 2004-12-09 스미스클라인 비참 코포레이션 신규 화합물
EP2181704B1 (en) 2002-12-30 2015-05-06 Angiotech International Ag Drug delivery from rapid gelling polymer composition
DE602004024536D1 (de) * 2003-07-07 2010-01-21 Van Andel Res Inst Hemmung der tumor-angiogenese durch eine kombination von thrombospondin-1 und hemmern des vaskulären endothel-wachstumsfaktors
WO2005105097A2 (en) * 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
WO2005123718A2 (en) * 2004-06-15 2005-12-29 Pfizer Japan Inc. Benzimidazolone carboxylic acid derivatives
JP4968066B2 (ja) * 2005-04-25 2012-07-04 宇部興産株式会社 ４−アミノ−２−アルキルチオ−５−ピリミジンカルバルデヒドの製法
JP2006321749A (ja) * 2005-05-19 2006-11-30 Ube Ind Ltd ２−シアノマロンアルデヒドのアルカリ金属塩の製法
JP2009525292A (ja) 2006-01-31 2009-07-09 エフ．ホフマン−ラ ロシュ アーゲー ７ｈ−ピリド［３，４−ｄ］ピリミジン−８−オン、それらの製造及びプロテインキナーゼ阻害剤としての使用
JP2010509265A (ja) * 2006-11-09 2010-03-25 エフ．ホフマン−ラ ロシュ アーゲー キナーゼ阻害剤としての置換６−フェニル−ピリド［２，３−ｄ］ピリミジン−７−オン誘導体及びそれの使用方法
CA2690327A1 (en) 2007-06-15 2008-12-18 Thomas P. Cleary A novel process for the preparation of 3-amino-pentan-1,5-diol
JP2013507395A (ja) * 2009-10-09 2013-03-04 アフラクシス・インコーポレイテッド Ｃｎｓ障害治療用の８−エチル−６−（アリール）ピリド［２，３−ｄ］ピリミジン−７（８ｈ）−オン
US20120184542A1 (en) 2011-01-19 2012-07-19 Kevin Anderson Pyrido pyrimidines
EP2828259B1 (en) * 2012-03-22 2018-08-08 Oscotec, Inc. Substituted pyridopyrimidine compounds and their use as flt3 inhibitors
MY181020A (en) 2013-03-15 2020-12-16 Sanofi Sa Heteroaryl compounds and uses thereof
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
MA38393B1 (fr) 2014-03-13 2018-11-30 Sanofi Sa Composés hétéroaryle et utilisations associées
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
RU2771526C1 (ru) * 2018-09-14 2022-05-05 Аббиско Терапеутикс Ко., Лтд. Ингибитор fgfr, метод его получения и его применение
WO2022052924A1 (zh) * 2020-09-11 2022-03-17 上海凌达生物医药有限公司 一类含氮稠环类化合物的制备方法和用途

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WO1997044321A1 (en) * 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3－d]嘧啶
US5945422A (en) * 1997-02-05 1999-08-31 Warner-Lambert Company N-oxides of amino containing pyrido 2,3-D! pyrimidines

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JPS6183168A (ja) * 1984-09-28 1986-04-26 Ube Ind Ltd ２−メルカプト−４−アミノ−５−ホルミルピリミジンおよびその製法
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2002018380A1 (en) * 2000-08-31 2002-03-07 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines as inhibitors of a cellular proliferation

Patent Citations (3)

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CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3－d]嘧啶
WO1997044321A1 (en) * 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US5945422A (en) * 1997-02-05 1999-08-31 Warner-Lambert Company N-oxides of amino containing pyrido 2,3-D! pyrimidines

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JP4146721B2 (ja) 2008-09-10
ES2243568T3 (es) 2005-12-01
BR0113590A (pt) 2003-07-22
JP2004507540A (ja) 2004-03-11
CA2420122A1 (en) 2002-03-07
MXPA03001733A (es) 2003-05-27
KR100582325B1 (ko) 2006-05-22
AR033996A1 (es) 2004-01-21
DE60111752D1 (de) 2005-08-04
EP1315727A2 (en) 2003-06-04
PE20020524A1 (es) 2002-06-18
KR20030022423A (ko) 2003-03-15
DE60111752T2 (de) 2006-05-04
WO2002018379A3 (en) 2002-07-25
UY26920A1 (es) 2002-02-28
EP1315727B1 (en) 2005-06-29
AU1214702A (en) 2002-03-13
CN1451004A (zh) 2003-10-22
WO2002018379A2 (en) 2002-03-07
ZA200301078B (en) 2004-05-07
AU2002212147B2 (en) 2007-10-18
CN1303072C (zh) 2007-03-07
CN1721412A (zh) 2006-01-18
ATE298751T1 (de) 2005-07-15
PA8527401A1 (es) 2002-07-30
GT200100190A (es) 2002-05-23

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