JP2007513184A - プロテインキナーゼのインヒビターとして有用なキノキサリン - Google Patents

プロテインキナーゼのインヒビターとして有用なキノキサリン Download PDF

Info

Publication number
JP2007513184A
JP2007513184A JP2006542853A JP2006542853A JP2007513184A JP 2007513184 A JP2007513184 A JP 2007513184A JP 2006542853 A JP2006542853 A JP 2006542853A JP 2006542853 A JP2006542853 A JP 2006542853A JP 2007513184 A JP2007513184 A JP 2007513184A
Authority
JP
Japan
Prior art keywords
compound
phenyl
compound according
membered
nitrogen
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.)
Pending
Application number
JP2006542853A
Other languages
English (en)
Japanese (ja)
Other versions
JP2007513184A5 (https=
Inventor
ガイ ダブリュー． ビーミス，
ジョン ピー． ダフィー，
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 JP2007513184A publication Critical patent/JP2007513184A/ja
Publication of JP2007513184A5 publication Critical patent/JP2007513184A5/ja
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic 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
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
JP2006542853A 2003-12-04 2004-12-03 プロテインキナーゼのインヒビターとして有用なキノキサリン Pending JP2007513184A (ja)

Applications Claiming Priority (2)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2007311671A Division JP2008069178A (ja) 2003-12-04 2007-11-30 プロテインキナーゼのインヒビターとして有用なキノキサリン

Publications (2)

Publication Number Publication Date
JP2007513184A true JP2007513184A (ja) 2007-05-24
JP2007513184A5 JP2007513184A5 (https=) 2008-01-31

Family

ID=34676666

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2006542853A Pending JP2007513184A (ja) 2003-12-04 2004-12-03 プロテインキナーゼのインヒビターとして有用なキノキサリン
JP2007311671A Pending JP2008069178A (ja) 2003-12-04 2007-11-30 プロテインキナーゼのインヒビターとして有用なキノキサリン

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2007311671A Pending JP2008069178A (ja) 2003-12-04 2007-11-30 プロテインキナーゼのインヒビターとして有用なキノキサリン

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=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011520941A (ja) * 2008-05-23 2011-07-21 ノバルティス アーゲー キノキサリン−およびキノリン−カルボキシアミド誘導体
JP2012517448A (ja) * 2009-02-11 2012-08-02 リアクション バイオロジー コープ． 選択的キナーゼ阻害剤
JP2013503896A (ja) * 2009-09-03 2013-02-04 バイオエナジェニックス Ｐａｓｋの阻害用複素環式化合物

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8071597B2 (en) * 2005-08-26 2011-12-06 Merck Serono Sa Pyrazine compounds and uses as PI3K inhibitors
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
WO2007054556A1 (de) 2005-11-11 2007-05-18 Æterna Zentaris Gmbh Neue pyridopyrazine und deren verwendung als modulatoren von kinasen
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
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
FR2933977B1 (fr) * 2008-07-18 2013-04-26 Centre Nat Rech Scient Derives heterocycliques utiles dans le traitement des maladies neurodegeneratives
PL2344474T3 (pl) 2008-09-02 2016-03-31 Novartis Ag Pochodne pikolinamidu jako inhibitory kinaz
JP5658756B2 (ja) 2009-09-10 2015-01-28 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｊａｋの阻害剤
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
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
US9216173B2 (en) 2011-10-05 2015-12-22 Merck Sharp & Dohme Corp. 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
EP2763975B1 (en) 2011-10-05 2016-04-06 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
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
MX371331B (es) 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).
US9173883B2 (en) 2012-05-21 2015-11-03 Novartis Ag Ring-substituted N-pyridinyl amides as kinase inhibitors
ME03336B (me) 2013-03-12 2019-10-20 Vertex Pharma Inhibitori dnk-pk
JP6408569B2 (ja) 2013-10-17 2018-10-17 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阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
WO2015095444A1 (en) 2013-12-20 2015-06-25 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
US10045981B2 (en) 2015-11-24 2018-08-14 Jakpharm, Llc Selective kinase inhibitors
US10432056B2 (en) * 2016-04-26 2019-10-01 Ford Global Technologies, Llc Electric machine rotor endcap
EP3518931A4 (en) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5476599A (en) * 1977-11-30 1979-06-19 Mitsubishi Yuka Yakuhin Kk Pyrimidoquinoxaline derivative*its manufacture and allergic asthma thrapeutic medicine
JPH061790A (ja) * 1991-10-07 1994-01-11 Merck & Co Inc アンギオテンシンｉｉのアンタゴニストとしての置換ピラジノ［２，３−ｄピリミジノン類
JP2001055378A (ja) * 1999-06-09 2001-02-27 Yamanouchi Pharmaceut Co Ltd 新規なヘテロ環カルボキサミド誘導体
WO2003045924A1 (en) * 2001-11-21 2003-06-05 Pharmacia & Upjohn Company Substituted aryl 1,4-pyrazine derivatives

Family Cites Families (81)

* 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
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
AU9049391A (en) 1990-12-20 1992-07-22 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
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
ES2200163T3 (es) 1996-11-15 2004-03-01 Darwin Discovery Limited Aril-carboxamidas biciclicas y su utilizacion terapeutica.
US6348461B1 (en) * 1997-09-01 2002-02-19 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
EA200000840A1 (ru) * 1998-02-17 2001-02-26 Туларик, Инк. Антивирусные производные пиримидина
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
EP1105394A1 (en) * 1998-08-21 2001-06-13 Du Pont 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
AU1223400A (en) 1998-10-22 2000-05-08 Phillip B. B. Moheno Novel pterin antineoplastic agents
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
IL144214A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
WO2000045800A2 (en) 1999-02-02 2000-08-10 K.U. Leuven Research & Development Immunosurpressive effects of pteridine derivatives
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
KR20010111298A (ko) * 2000-02-05 2001-12-17 버텍스 파마슈티칼스 인코포레이티드 Ｅｒｋ의 억제제로서 유용한 피라졸 조성물
AU3704101A (en) * 2000-02-17 2001-08-27 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
AU5553801A (en) 2000-04-24 2001-11-07 Bristol Myers Squibb Co Heterocycles that are inhibitors of impdh enzyme
CA2407677A1 (en) 2000-04-28 2002-10-28 Baxter Healthcare Sa 2-acyl indol derivatives and their use as anti-tumour agents
IL153246A0 (en) * 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
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
US6610677B2 (en) * 2000-09-15 2003-08-26 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
EP1317453B1 (en) * 2000-09-15 2006-08-09 Vertex Pharmaceuticals Incorporated Isoxazoles and their use as inhibitors of erk
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022605A1 (en) * 2000-09-15 2002-03-21 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)
US6989385B2 (en) * 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6849634B2 (en) 2000-12-21 2005-02-01 Icagen Potassium channel inhibitors
US20040110846A1 (en) 2001-01-30 2004-06-10 Beatrice Leveugle 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
CA2441733A1 (en) * 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
AU2002338642A1 (en) * 2001-04-13 2002-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1383771A1 (en) * 2001-04-20 2004-01-28 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
WO2002092573A2 (en) * 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
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
ATE337312T1 (de) * 2001-07-03 2006-09-15 Vertex Pharma Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
CA2452391A1 (en) 2001-07-09 2003-01-23 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
BR0213562A (pt) 2001-10-26 2004-08-31 Aventis Pharma Inc Benzimidazóis e análogos e seu uso como inibidores de cinases de proteìna
US6992087B2 (en) * 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
ATE466581T1 (de) * 2001-12-07 2010-05-15 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
JP2005523279A (ja) 2002-02-13 2005-08-04 アクシス ファーマシューティカルズ インコーポレイティッド 第ｖｉｉａ因子阻害剤としての２−［５−（５−カルバミミドイル−１ｈ−ヘテロアリール）］−６−ヒドロキシビフェニル−３−イル誘導体
US20040009981A1 (en) * 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
DE60332433D1 (de) * 2002-03-15 2010-06-17 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
US6846928B2 (en) * 2002-03-15 2005-01-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1485381B8 (en) * 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
US7304061B2 (en) * 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic 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
US7361665B2 (en) * 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
AU2003281169A1 (en) 2002-07-17 2004-02-02 Warner-Lambert Company Llc Combination of an allosteric carboxylic inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
EP1530475A2 (en) 2002-07-17 2005-05-18 Warner-Lambert Company LLC Pharmaceutical compositions comprising an allosteric carboxylic inhibitor of matrix metalloproteinase-13 and a selective inhibitor of cyclooxygenase-2
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
WO2004043913A2 (en) 2002-11-08 2004-05-27 Trimeris, Inc. Hetero-substituted benzimidazole compounds and antiviral uses thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5476599A (en) * 1977-11-30 1979-06-19 Mitsubishi Yuka Yakuhin Kk Pyrimidoquinoxaline derivative*its manufacture and allergic asthma thrapeutic medicine
JPH061790A (ja) * 1991-10-07 1994-01-11 Merck & Co Inc アンギオテンシンｉｉのアンタゴニストとしての置換ピラジノ［２，３−ｄピリミジノン類
JP2001055378A (ja) * 1999-06-09 2001-02-27 Yamanouchi Pharmaceut Co Ltd 新規なヘテロ環カルボキサミド誘導体
WO2003045924A1 (en) * 2001-11-21 2003-06-05 Pharmacia & Upjohn Company Substituted aryl 1,4-pyrazine derivatives

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
HELVETICA CHIMICA ACTA, vol. 69, no. 4, JPN6010072082, 1986, pages 793 - 802, ISSN: 0001804413 *
INDIAN JOURNAL OF CHEMISTRY, vol. 28, no. 12, JPN6010072085, 1989, pages 1026 - 1030, ISSN: 0001804416 *
JOURNAL OF THE CHEMICAL SOCIETY PERKIN TRANSACTIONS I, vol. 11, JPN6010072084, 1977, pages 1321 - 1325, ISSN: 0001804415 *
TETRAHEDRON LETTERS, JPN6010072083, 1972, pages 3359 - 3360, ISSN: 0001804414 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011520941A (ja) * 2008-05-23 2011-07-21 ノバルティス アーゲー キノキサリン−およびキノリン−カルボキシアミド誘導体
JP2012517448A (ja) * 2009-02-11 2012-08-02 リアクション バイオロジー コープ． 選択的キナーゼ阻害剤
JP2013503896A (ja) * 2009-09-03 2013-02-04 バイオエナジェニックス Ｐａｓｋの阻害用複素環式化合物

Also Published As

Publication number Publication date
US20100081657A1 (en) 2010-04-01
WO2005056547A3 (en) 2005-09-22
CA2548172A1 (en) 2005-06-23
EP1694671A2 (en) 2006-08-30
AU2004297235A1 (en) 2005-06-23
JP2008069178A (ja) 2008-03-27
HK1099764A1 (en) 2007-08-24
WO2005056547A2 (en) 2005-06-23
CN1902193A (zh) 2007-01-24
US7592340B2 (en) 2009-09-22
US20050234064A1 (en) 2005-10-20
CN1902193B (zh) 2011-07-13

Similar Documents

Publication Publication Date Title
JP2007513184A (ja) プロテインキナーゼのインヒビターとして有用なキノキサリン
JP2007513184A5 (https=)
JP4523271B2 (ja) プロテインキナーゼのインヒビターとして有用なチアゾール化合物
US7226919B2 (en) Compositions 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
US6846928B2 (en) Compositions useful as inhibitors of protein kinases
US8653088B2 (en) Compositions useful as inhibitors of protein kinases
EP1611125A1 (en) Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
JP5085330B2 (ja) プロテインキナーゼの阻害剤として有用なトリアゾール
JP2011006494A (ja) Ｊａｋキナーゼおよびｃｄｋ２プロテインキナーゼのインヒビター
JP2007512230A (ja) プロテインキナーゼ阻害剤として有用な（４−アミノ−１，２，５−オキサジアゾール−４−イル）−ヘテロ芳香族化合物
NZ531853A (en) Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors)
JP2007535551A (ja) Ｒｏｃｋおよび他のプロテインキナーゼの阻害剤として有用な組成物
EP1603886B1 (en) 4-substituted-5-cyano-1h-pyrimidin-6-(thi)ones as gsk-3 inhibitors
HK1099764B (en) Quinoxalines useful as inhibitors of protein kinases
CN101273032A (zh) 吡嗪激酶抑制剂
HK1109567A (en) Triazoles useful as inhibitors of protein kinases
HK1065033B (en) Thiazole compounds useful as inhibitors of protein kinases
EP2243781A1 (en) Pyrazolopyridine derivatives as inhibitors of JAK and CDK2 protein kinases

Legal Events

Date Code Title Description
A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20071130

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20071130

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20101208

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101215

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20110927