CN1902193B - 可用作蛋白激酶抑制剂的喹喔啉 - Google Patents

可用作蛋白激酶抑制剂的喹喔啉 Download PDF

Info

Publication number
CN1902193B
CN1902193B CN2004800402644A CN200480040264A CN1902193B CN 1902193 B CN1902193 B CN 1902193B CN 2004800402644 A CN2004800402644 A CN 2004800402644A CN 200480040264 A CN200480040264 A CN 200480040264A CN 1902193 B CN1902193 B CN 1902193B
Authority
CN
China
Prior art keywords
compound
nitrogen
sulfur
oxygen
independently selected
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 - Fee Related
Application number
CN2004800402644A
Other languages
English (en)
Chinese (zh)
Other versions
CN1902193A (zh
Inventor
G·W·比米斯
J·P·迪菲
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CN1902193A publication Critical patent/CN1902193A/zh
Application granted granted Critical
Publication of CN1902193B publication Critical patent/CN1902193B/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P25/14Drugs 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
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • A61P27/00Drugs for disorders of the senses
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/44Benzopyrazines 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 carbon atoms of the hetero ring
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
CN2004800402644A 2003-12-04 2004-12-03 可用作蛋白激酶抑制剂的喹喔啉 Expired - Fee Related CN1902193B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US52684303P 2003-12-04 2003-12-04
US60/526,843 2003-12-04
PCT/US2004/040777 WO2005056547A2 (en) 2003-12-04 2004-12-03 Quinoxalines useful as inhibitors of protein kinases

Publications (2)

Publication Number Publication Date
CN1902193A CN1902193A (zh) 2007-01-24
CN1902193B true CN1902193B (zh) 2011-07-13

Family

ID=34676666

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2004800402644A Expired - Fee Related CN1902193B (zh) 2003-12-04 2004-12-03 可用作蛋白激酶抑制剂的喹喔啉

Country Status (7)

Country Link
US (2) US7592340B2 (https=)
EP (1) EP1694671A2 (https=)
JP (2) JP2007513184A (https=)
CN (1) CN1902193B (https=)
AU (1) AU2004297235A1 (https=)
CA (1) CA2548172A1 (https=)
WO (1) WO2005056547A2 (https=)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006283846B2 (en) * 2005-08-26 2012-04-05 Merck Serono Sa Pyrazine derivatives and use as PI3K inhibitors
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
AU2006313701B2 (en) 2005-11-11 2012-05-31 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
MX2009009304A (es) * 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
AR066879A1 (es) * 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
GEP20125502B (en) * 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
FR2933977B1 (fr) * 2008-07-18 2013-04-26 Centre Nat Rech Scient Derives heterocycliques utiles dans le traitement des maladies neurodegeneratives
MX2011002365A (es) 2008-09-02 2011-04-04 Novartis Ag Derivados de picolinamida como inhibidres de cinasa.
CA2752150A1 (en) * 2009-02-11 2010-08-19 Reaction Biology Corp. Selective kinase inhibitors
PH12012500382A1 (en) * 2009-09-03 2012-10-22 Bioenergenix Heterocyclic compounds for the inhibition of pask
EP2475667A1 (en) 2009-09-10 2012-07-18 F. Hoffmann-La Roche AG Inhibitors of jak
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
EP2508184A1 (en) 2011-04-06 2012-10-10 Æterna Zentaris GmbH Pyridopyrazine derivatives and their use
MX2013013090A (es) 2011-05-10 2013-12-16 Merck Sharp & Dohme Aminopirimidinas como inhibidores de tirosina cinaza del bazo.
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
EP2707357B1 (en) 2011-05-10 2017-01-18 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
WO2013052393A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
JP6378171B2 (ja) 2012-04-24 2018-08-22 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Vertex Pharmaceuticals Incorporated Dna−pk阻害剤
US9173883B2 (en) 2012-05-21 2015-11-03 Novartis Ag Ring-substituted N-pyridinyl amides as kinase inhibitors
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
RU2675270C2 (ru) 2013-10-17 2018-12-18 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
EP3083560B1 (en) 2013-12-20 2021-10-27 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
CN108472298B (zh) 2015-11-24 2021-04-20 深圳阿拉丁医疗科技有限公司 选择性激酶抑制剂
US10432056B2 (en) * 2016-04-26 2019-10-01 Ford Global Technologies, Llc Electric machine rotor endcap
RU2758669C2 (ru) 2016-09-27 2021-11-01 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
CN113943288A (zh) * 2020-07-17 2022-01-18 微境生物医药科技(上海)有限公司 5,6-二氢吡嗪并[2,3-c]异喹啉化合物

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US3935183A (en) * 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) * 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) * 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
JPS5476599A (en) * 1977-11-30 1979-06-19 Mitsubishi Yuka Yakuhin Kk Pyrimidoquinoxaline derivative*its manufacture and allergic asthma thrapeutic medicine
DOP1981004033A (es) * 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
SE8102194L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
JPS58124773A (ja) * 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc 5−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
WO1992011245A1 (en) * 1990-12-20 1992-07-09 Warner-Lambert Company 2-acylamido derivatives of 3,4-dihydro-3-oxo-quinoxaline having pharmaceutical activity
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
CA2079982A1 (en) * 1991-10-07 1993-04-08 Stephen E. De Laszlo Substituted pyrazino (2,3-d)-pyrimidinones as angiotensin ii antagonists
WO1996014843A2 (en) * 1994-11-10 1996-05-23 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
IL117659A (en) * 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
BR9713507A (pt) 1996-11-15 2000-02-29 Darwin Discovery Ltd Aril carboxamidas bicìclicas e seu uso terapêutico
EP1020453B1 (en) * 1997-09-01 2004-05-19 Kyorin Pharmaceutical Co., Ltd. 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives, addition salts thereof, and processes for the preparation of both
US6267952B1 (en) * 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
BR9908004A (pt) * 1998-02-17 2001-12-18 Tularik Inc Composto, composição e método para prevençãoou supressão de uma infecção viral
JP2002517486A (ja) 1998-06-12 2002-06-18 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 p38のインヒビター
CA2339188A1 (en) * 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6358953B1 (en) 1998-10-22 2002-03-19 Phillip B. B. Moheno Pterin antineoplastic agents
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
CA2355470C (en) 1999-01-13 2008-09-30 Warner-Lambert Company Benzoheterocycles and their use as mek inhibitors
CA2361561A1 (en) 1999-02-02 2000-08-10 K.U. Leuven Research & Development Immunosurpressive effects of pteridine derivatives
JP4622047B2 (ja) * 1999-06-09 2011-02-02 アステラス製薬株式会社 新規なヘテロ環カルボキサミド誘導体
WO2000076980A1 (en) 1999-06-10 2000-12-21 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
HUP0202332A2 (en) * 2000-02-05 2002-10-28 Vertex Pharma Pyrazole compositions useful as inhibitors of erk
EP1257546A1 (en) * 2000-02-17 2002-11-20 Amgen Inc. Kinase inhibitors
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
DE10013318A1 (de) * 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
GB0007934D0 (en) 2000-03-31 2000-05-17 Darwin Discovery Ltd Chemical compounds
EP1276739A2 (en) 2000-04-24 2003-01-22 Bristol-Myers Squibb Company Heterocycles that are inhibitors of impdh enzyme
CZ20023544A3 (cs) * 2000-04-28 2004-07-14 Baxter Healthcare Sa Deriváty 2-acylindolu a jejich použití jako protinádorové činidlo
ATE394102T1 (de) * 2000-06-28 2008-05-15 Astrazeneca Ab Substituierte chinazolin-derivate und deren verwendung als aurora-2-kinase inhibitoren
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE335737T1 (de) * 2000-09-15 2006-09-15 Vertex Pharma Isoxazole und ihre verwendung als erk-inhibitoren
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317450B1 (en) * 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6716851B2 (en) * 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) * 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
NZ526472A (en) * 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
US6849634B2 (en) 2000-12-21 2005-02-01 Icagen Potassium channel inhibitors
EP1357944B1 (en) 2001-01-30 2007-06-13 Altachem Pharma Ltd. Perylenequinones for use with immunotherapy agents
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
AR035230A1 (es) 2001-03-19 2004-05-05 Astrazeneca Ab Compuestos de bencimidazol, proceso para su preparacion, composicion farmaceutica, proceso para la preparacion de dicha composicion farmaceutica, y usos de estos compuestos para la elaboracion de medicamentos
EP1373257B9 (en) * 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
MXPA03009378A (es) * 2001-04-13 2004-01-29 Vertex Pharma Inhibidores de cinasas c-jun n-terminales (jnk) y otras proteinas cinasas.
US20030096813A1 (en) * 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
AU2002308748A1 (en) * 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
US6825190B2 (en) * 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
GB0115109D0 (en) * 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003000690A1 (en) 2001-06-25 2003-01-03 Aventis Pharmaceuticals Inc. Synthesis of heterocyclic compounds employing microwave technology
WO2003004492A1 (en) * 2001-07-03 2003-01-16 Vertex Pharmaceuticals Incorporated Isoxazolyl-pyrimidines as inhibitors of src and lck protein kinases
US20030114457A1 (en) 2001-07-09 2003-06-19 Axys Pharmaceuticals, Inc. 2- [5- (5-carbamimidoyl-1H-heteroaryl)-6-hydroxybiphenyl-3-yl]-succinic acid derivatives as factor viia inhibitors
FR2827599A1 (fr) * 2001-07-20 2003-01-24 Neuro3D Composes derives de quinoleine et quinoxaline,preparation et utilisations
US6698980B2 (en) * 2001-07-30 2004-03-02 Stewart Mining Products Inc. Rock stabilizing apparatus and method
JP5039268B2 (ja) 2001-10-26 2012-10-03 アベンティス・ファーマスーティカルズ・インコーポレイテツド ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
US6992087B2 (en) * 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
AU2002343557A1 (en) * 2001-11-21 2003-06-10 Pharmacia And Upjohn Company Substituted aryl 1,4-pyrazine derivatives
DE60236322D1 (de) * 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
TW200301251A (en) 2001-12-20 2003-07-01 Wyeth Corp Azaindolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands
AU2003215158A1 (en) 2002-02-13 2003-09-04 Axys Pharmaceuticals, Inc. 2-(5-(5-carbamimidoyl-1h-heteroaryl))-6-hydroxybiphenyl-3-yl derivatives as factor viia inhibitors
DE60327999D1 (de) * 2002-03-15 2009-07-30 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
EP1485100B1 (en) * 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles as inhibitors of protein kinases
WO2003078423A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions useful as inhibitors of protein kinases
AU2003218215A1 (en) * 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) * 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
CA2491895C (en) * 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
BR0312736A (pt) 2002-07-17 2005-04-26 Warner Lambert Co Associação de um inibidor carboxìlico alostérico da metaloproteinase-13 de matriz com celecoxib ou valdecoxib
JP2006503812A (ja) 2002-07-17 2006-02-02 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー アロステリックカルボキシルマトリックスメタロプロテイナーゼ−13阻害薬とセレコキシブまたはバルデコキシブではない選択的シクロオキシゲナーゼ−2阻害薬との組み合わせ
TW200403243A (en) 2002-07-18 2004-03-01 Wyeth Corp 1-Heterocyclylalkyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
TWI276631B (en) 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
US20040166137A1 (en) 2002-11-08 2004-08-26 Lackey John William Hetero-substituted benzimidazole compounds and antiviral uses thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ueda.reaction of lumichrome or 2-thiolumichrome with alkylamines.《j.heterocyclic chem》.1991,第28卷1485-1490. *
UEDA.synthesisi of diazepinoquinoxalines and imidazolobenzopterlidlines.《J.HETEROCYCLIC CHEM》.1996,第33卷169-172. *

Also Published As

Publication number Publication date
JP2008069178A (ja) 2008-03-27
HK1099764A1 (en) 2007-08-24
US7592340B2 (en) 2009-09-22
JP2007513184A (ja) 2007-05-24
EP1694671A2 (en) 2006-08-30
AU2004297235A1 (en) 2005-06-23
CN1902193A (zh) 2007-01-24
WO2005056547A3 (en) 2005-09-22
US20050234064A1 (en) 2005-10-20
CA2548172A1 (en) 2005-06-23
WO2005056547A2 (en) 2005-06-23
US20100081657A1 (en) 2010-04-01

Similar Documents

Publication Publication Date Title
CN1902193B (zh) 可用作蛋白激酶抑制剂的喹喔啉
JP2007513184A5 (https=)
EP1562938B1 (en) Heteroaryl-pyrimidine derivatives as jak inhibitors
EP1581526B1 (en) Benzisoxazole derivatives useful as inhibitors of protein kinases
JP2006508107A (ja) Jakおよび他のプロテインキナーゼのインヒビターとして有用な化合物
US20030236244A1 (en) Inhibitors of JAK and CDK2 protein kinases
US8653088B2 (en) Compositions useful as inhibitors of protein kinases
DE102010034699A1 (de) Pyrimidinderivate
WO2004072063A1 (en) Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
EP1697375A2 (en) Heterocyclic protein kinase inhibitors and uses thereof
CN101072556A (zh) 可用作蛋白激酶抑制剂的三唑
HK1099764B (en) Quinoxalines useful as inhibitors of protein kinases
JP2000154139A (ja) 縮環ピラジン誘導体
DE102008062825A1 (de) 3-(3-Pyrimidin-2-yl-benzyl)-[1,2,4]triazolo [4,3-b]pyridazin-derivate
CN101273032A (zh) 吡嗪激酶抑制剂
EP2243781A1 (en) Pyrazolopyridine derivatives as inhibitors of JAK and CDK2 protein kinases
HK1109567A (en) Triazoles useful as inhibitors of protein kinases

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1099764

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1099764

Country of ref document: HK

C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20110713

Termination date: 20121203