CN1845734B - 苯并咪唑衍生物及其作为蛋白激酶抑制剂的制药用途 - Google Patents

苯并咪唑衍生物及其作为蛋白激酶抑制剂的制药用途 Download PDF

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Publication number
CN1845734B
CN1845734B CN2004800249288A CN200480024928A CN1845734B CN 1845734 B CN1845734 B CN 1845734B CN 2004800249288 A CN2004800249288 A CN 2004800249288A CN 200480024928 A CN200480024928 A CN 200480024928A CN 1845734 B CN1845734 B CN 1845734B
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yuan
methyl
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compound
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Expired - Fee Related
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CN2004800249288A
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Chinese (zh)
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CN1845734A (zh
Inventor
V·贝尔迪尼
M·A·奥布里恩
M·G·卡尔
T·R·伊尔利
E·F·纳瓦罗
A·L·吉尔
S·霍瓦德
G·特雷沃塔
A·J·-A·沃尔福特
A·J·伍德赫德
P·怀亚特
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Astex Therapeutics Ltd
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Astex Therapeutics Ltd
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Priority claimed from GBGB0315657.7A external-priority patent/GB0315657D0/en
Priority claimed from GB0324919A external-priority patent/GB0324919D0/en
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Publication of CN1845734A publication Critical patent/CN1845734A/zh
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
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    • 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
    • C07D401/14—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 three or more hetero rings
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    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • 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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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2004800249288A 2003-07-03 2004-07-05 苯并咪唑衍生物及其作为蛋白激酶抑制剂的制药用途 Expired - Fee Related CN1845734B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US48468503P 2003-07-03 2003-07-03
GBGB0315657.7A GB0315657D0 (en) 2003-07-03 2003-07-03 Pharmaceutical compounds
US60/484,685 2003-07-03
GB0315657.7 2003-07-03
US51437403P 2003-10-24 2003-10-24
US60/514,374 2003-10-24
GB0324919A GB0324919D0 (en) 2003-10-24 2003-10-24 Pharmaceutical compounds
GB0324919.0 2003-10-24
PCT/GB2004/002824 WO2005002552A2 (en) 2003-07-03 2004-07-05 Benzimidazole derivatives and their use as protein kinases inhibitors

Publications (2)

Publication Number Publication Date
CN1845734A CN1845734A (zh) 2006-10-11
CN1845734B true CN1845734B (zh) 2011-06-22

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CN2004800249288A Expired - Fee Related CN1845734B (zh) 2003-07-03 2004-07-05 苯并咪唑衍生物及其作为蛋白激酶抑制剂的制药用途

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Country Link
US (3) US7977477B2 (https=)
EP (2) EP1648426B1 (https=)
JP (1) JP4833059B2 (https=)
CN (1) CN1845734B (https=)
AU (1) AU2004253338B2 (https=)
CA (1) CA2531050C (https=)
DK (2) DK2305250T3 (https=)
ES (2) ES2457466T3 (https=)
MX (1) MXPA05014223A (https=)
NZ (1) NZ543959A (https=)
PL (2) PL1648426T3 (https=)
PT (2) PT2305250E (https=)
SI (2) SI1648426T1 (https=)
TW (1) TWI372050B (https=)
WO (1) WO2005002552A2 (https=)

Families Citing this family (133)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
PL2256106T3 (pl) 2003-07-22 2015-08-31 Astex Therapeutics Ltd Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3)
WO2005061519A1 (en) 2003-12-19 2005-07-07 Takeda San Diego, Inc. Kinase inhibitors
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
BRPI0507278A (pt) * 2004-01-30 2007-06-26 Vertex Pharma moduladores dos transportadores do cassete de ligação ao atp
JP2008505167A (ja) * 2004-07-05 2008-02-21 アステックス、セラピューティックス、リミテッド 医薬組成物
EP1778669A2 (en) 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase inhibitors
ATE479687T1 (de) 2004-10-15 2010-09-15 Takeda Pharmaceutical Kinaseinhibitoren
EP1807074B1 (en) 2004-11-03 2013-10-23 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US20100160324A1 (en) * 2004-12-30 2010-06-24 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
WO2006070192A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases
EP1833819A1 (en) * 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
JP5475234B2 (ja) * 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド 医薬化合物
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
MX2007008781A (es) * 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
RU2436575C2 (ru) * 2005-01-21 2011-12-20 Астекс Терапьютикс Лимитед Соединения для использования в фармацевтике
AR052559A1 (es) * 2005-01-21 2007-03-21 Astex Therapeutics Ltd Derivados de pirazol para inhibir cdk's y gsk's
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
WO2006085685A1 (ja) * 2005-02-09 2006-08-17 Takeda Pharmaceutical Company Limited ピラゾール化合物
US7462639B2 (en) 2005-04-14 2008-12-09 Hoffmann-La Roche Inc. Aminopyrazole derivatives
EP1749523A1 (en) * 2005-07-29 2007-02-07 Neuropharma, S.A. GSK-3 inhibitors
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
EP1910385B1 (en) * 2005-08-04 2013-07-24 Sirtris Pharmaceuticals, Inc. Benzothiazoles and thiazolopyridines as sirtuin modulators
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP1928437A2 (en) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
AU2006322187A1 (en) * 2005-12-08 2007-06-14 Novartis Ag Pyrazolo[1,5-a]pyridine-3-carboxylic acids as EphB and VEGFR2 kinase inhibitors
US20090143375A1 (en) * 2005-12-15 2009-06-04 F. Hoffmann-La Roche Ag Tricyclic Lactam Derivatives, Their Manufacture and Use as Pharmaceutical Agents
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
EP1968579A1 (en) * 2005-12-30 2008-09-17 Astex Therapeutics Limited Pharmaceutical compounds
US20090170847A1 (en) * 2006-01-23 2009-07-02 Seung Chul Lee Imidazopyridine Derivatives Inhibiting Protein Kinase Activity, Method for the Preparation Thereof and Pharmaceutical Composition Containing Same
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2049119A2 (en) * 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
WO2008001101A2 (en) * 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
FR2903406B1 (fr) * 2006-07-04 2012-08-10 Aventis Pharma Sa Derives de pyrazolylbenzimidazole,compositions les contenant et utilisation
JP2010501567A (ja) * 2006-08-24 2010-01-21 ノバルティス アクチエンゲゼルシャフト 代謝系、心血管系および他の障害の処置のためのステアロイル−ＣｏＡ不飽和化酵素（ＳＣＤ）阻害剤としての２−（ピラジン−２−イル）−チアゾールおよび２−（１Ｈ−ピラゾール−３−イル）チアゾール誘導体ならびに関連化合物
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
KR20090053923A (ko) 2006-09-22 2009-05-28 노파르티스 아게 헤테로시클릭 유기 화합물
WO2008041767A1 (en) * 2006-10-05 2008-04-10 Banyu Pharmaceutical Co., Ltd. Gene/protein marker for prediction or diagnosis of pharmacological efficacy of aurora a inhibitor
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
JP5528807B2 (ja) * 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
CA2673368C (en) 2006-12-19 2014-10-28 The Board Of Trustees Of The University Of Illinois 3-benzofuranyl-4-indolyl maleimides as potent gsk3 inhibitors for neurogenerative disorders
CN101595105B (zh) 2006-12-20 2013-01-23 诺瓦提斯公司 作为scd抑制剂的2-取代的5元杂环化合物
DE102006060598A1 (de) * 2006-12-21 2008-06-26 Merck Patent Gmbh Tetrahydrobenzoisoxazole
TW200916472A (en) 2007-06-20 2009-04-16 Sirtris Pharmaceuticals Inc Sirtuin modulating compounds
CA2703978A1 (en) * 2007-10-29 2009-05-07 Schering Corporation Thiazole derivatives as protein kinase inhibitors
WO2009058730A1 (en) * 2007-10-29 2009-05-07 Schering Corporation Diamido thiazole derivatives as protein kinase inhibitors
BRPI0820171B8 (pt) 2007-11-16 2021-05-25 Rigel Pharmaceuticals Inc compostos de carboxamida, sulfonamida e amina para distúrbios metabólicos, composição farmacêutica, e, uso dos mesmos
CA2707047C (en) 2007-12-12 2017-11-28 Rigel Pharmaceuticals, Inc. Carboxamide, sulfonamide and amine compounds for metabolic disorders
DK2294065T3 (da) * 2008-01-22 2014-04-28 Vernalis R&D Ltd Indolyl-pyridonderivater med checkpoint kinase 1 inhibitorisk aktivitet
MX2010011288A (es) 2008-04-23 2010-11-09 Rigel Pharmaceuticals Inc Compuestos de carboxamida para el tratamiento de trastornos metabolicos.
EP2330894B8 (en) 2008-09-03 2017-04-19 BioMarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors
CN102271515B (zh) 2008-10-31 2014-07-02 健泰科生物技术公司 吡唑并嘧啶jak抑制剂化合物和方法
BRPI0920959A2 (pt) * 2008-11-20 2017-07-11 Oncotherapy Science Inc Inibidores de glicogênio sintase quinase-3 beta contendo derivados de 7-hidróxi-benzoimidazol-4-il-metanona
US8318928B2 (en) * 2008-12-15 2012-11-27 Glenmark Pharmaceuticals, S.A. Fused imidazole carboxamides as TRPV3 modulators
EP2376502B1 (en) 2008-12-19 2015-06-17 GlaxoSmithKline LLC Thiazolopyridine sirtuin modulating compounds
RU2535032C2 (ru) 2008-12-22 2014-12-10 Милленниум Фармасьютикалз, Инк. Сочетание ингибиторов аврора киназы и анти-cd 20 антител
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
UA103918C2 (en) * 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
JP2012531433A (ja) * 2009-06-25 2012-12-10 メドリューション リミテッド キナーゼ阻害剤としての置換複素環式化合物とその用法
UA110324C2 (en) * 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
CA2780031A1 (en) * 2009-11-12 2011-05-19 Selvita S.A. A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
JP5488807B2 (ja) 2010-01-25 2014-05-14 日立工機株式会社 遠心分離機及び遠心分離機用スイングロータ
CN101857589B (zh) * 2010-06-08 2013-12-18 东南大学 吡唑-苯并咪唑类衍生物及其应用
JP5985473B2 (ja) * 2010-07-13 2016-09-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US9540395B2 (en) 2011-02-28 2017-01-10 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
EP2766355B1 (en) 2011-10-11 2020-12-23 Dana-Farber Cancer Institute, Inc. Pyrazol-3-ones that activate pro-apoptotic bax
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
GB201211021D0 (en) * 2012-06-21 2012-08-01 Cancer Rec Tech Ltd Pharmaceutically active compounds
TW201406758A (zh) * 2012-06-28 2014-02-16 Daiichi Sankyo Co Ltd 三環性化合物
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
RU2015117950A (ru) * 2012-10-26 2016-12-20 Ф. Хоффманн-Ля Рош Аг 3,4-дизамещенный 1н-пиразол и 4,5-дизамещенный тиазол в качестве ингибиторов тирозинкиназы syk
WO2014143666A1 (en) 2013-03-15 2014-09-18 Biomarin Pharmaceutical Inc. Hdac inhibitors
CN104211692B (zh) * 2013-06-04 2019-05-24 广东东阳光药业有限公司 作为欧若拉激酶抑制剂的衍生物
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
CN104447701B (zh) * 2013-09-17 2019-03-22 广东东阳光药业有限公司 吡唑类衍生物及其用途
EP3076963A4 (en) 2013-12-06 2017-09-13 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-cd30 antibodies
ES2883289T3 (es) 2013-12-20 2021-12-07 Astex Therapeutics Ltd Compuestos heterocíclicos bicíclicos y sus usos en terapia
PE20211782A1 (es) * 2014-05-23 2021-09-08 Hoffmann La Roche Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
JOP20150177B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
JOP20150179B1 (ar) 2014-08-01 2021-08-17 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Ｂｔｋ抑制劑、ｐｉ３ｋ抑制劑、ｊａｋ－２抑制劑、及／或ｃｄｋ４／６抑制劑的治療組合物
MA40596B1 (fr) 2014-08-11 2021-12-31 Acerta Pharma Bv Combinaisons thérapeutiques d'un inhibiteur de btk et d'un inhibiteur de bcl-2
US20170239351A1 (en) 2014-08-11 2017-08-24 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, a PD-1 Inhibitor, and/or a PD-L1 Inhibitor
JP6861154B2 (ja) 2014-12-03 2021-04-21 ヤンセン ファーマシューティカ エヌ．ベー． 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド
AU2015357167B2 (en) 2014-12-03 2020-06-25 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo(1,5-alpha)pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
CN105801563B (zh) * 2015-01-15 2020-01-14 广东东阳光药业有限公司 吡唑类衍生物及其用途
EA039043B1 (ru) 2015-04-22 2021-11-25 Райджел Фармасьютикалз, Инк. Пиразольные соединения и способ получения и применения данных соединений
WO2016202758A1 (en) * 2015-06-18 2016-12-22 Bayer Pharma Aktiengesellschaft Substituted 2-(1h-pyrazol-1-yl)-1h-benzimidazole compounds
JP2018524292A (ja) 2015-07-21 2018-08-30 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． オーロラキナーゼインヒビターと化学療法剤の投与
BR112018009252A2 (pt) 2015-11-06 2018-11-06 Samumed Llc tratamento da osteoartrite
LT3389727T (lt) 2015-12-18 2020-10-12 Janssen Pharmaceutica Nv Radioaktyviai pažymėti mglur2/3 pet ligandai
EA037941B1 (ru) 2015-12-18 2021-06-09 Янссен Фармацевтика Нв ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ
US20170210741A1 (en) * 2016-01-27 2017-07-27 Southern Research Institute Benzimidazole Compounds, Use As Inhibitors of WNT Signaling Pathway in Cancers, and Methods for Preparation Thereof
LT3464285T (lt) 2016-06-01 2022-12-27 Biosplice Therapeutics, Inc. N-(5-(3-(7-(3-fluorfenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)- 3-metilbutanamido gamybos būdas
CN110494434B (zh) 2017-03-14 2022-05-24 豪夫迈·罗氏有限公司 吡唑并氯苯基化合物、其组合物及其使用方法
WO2018215389A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
US11874276B2 (en) 2018-04-05 2024-01-16 Dana-Farber Cancer Institute, Inc. STING levels as a biomarker for cancer immunotherapy
US20210236466A1 (en) * 2018-07-03 2021-08-05 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
EP3906026A4 (en) 2018-12-31 2022-10-19 Biomea Fusion, LLC IRREVERSIBLE INHIBITORS OF MENIN-MLL INTERACTION
TW202043205A (zh) 2018-12-31 2020-12-01 美商拜歐米富士恩有限公司 Menin-mll相互作用之抑制劑
US20230000842A1 (en) * 2019-01-17 2023-01-05 Samumed, Llc Methods of treating cartilage disorders through inhibition of clk and dyrk
JP2022528155A (ja) * 2019-03-25 2022-06-08 ザ・トラスティーズ・オブ・コロンビア・ユニバーシティ・イン・ザ・シティ・オブ・ニューヨーク 糖尿病ならびに膵臓機能障害に関連する他の病気の治療のための選択的ｆｏｘｏ阻害剤
MX2021013531A (es) 2019-05-05 2022-02-11 Qilu Regor Therapeutics Inc Inhibidores de cdk.
CN112047932B (zh) * 2019-06-05 2022-11-08 中国药科大学 吡唑类脾酪氨酸激酶抑制剂及其制备方法与用途
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
CN121159524A (zh) 2019-08-30 2025-12-19 里格尔药品股份有限公司 吡唑化合物，其配制品以及使用所述化合物和/或配制品的方法
CN111004221B (zh) * 2019-12-13 2021-02-02 长治学院 一种嘧啶/苯并咪唑杂合物、制备方法及医药用途
CN112592839B (zh) * 2021-01-08 2022-08-19 浙江工业大学 一株降解氨基甲酸乙酯的米根霉及其应用
CN113149978A (zh) * 2021-02-04 2021-07-23 中国药科大学 一种中间体化合物、制备方法及其用途
WO2022187303A1 (en) 2021-03-03 2022-09-09 Rigel Pharmaceuticals, Inc. A method for treating a disease or condition using a pyrazole compound or formulation thereof
CN113549038B (zh) * 2021-07-07 2023-05-23 常州大学 多取代异苯并呋喃化合物及其用途
AU2022325861A1 (en) 2021-08-11 2024-02-29 Biomea Fusion, Inc. Covalent inhibitors of menin-mll interaction for diabetes mellitus
IL310717A (en) 2021-08-20 2024-04-01 Biomea Fusion Inc Crystalline form of N-[4-[4-(4-morpholinyl)-7H-PYRROLO[2,3-D]PYRIMIDIN-6-YL]PHENYL]-4-[[3(R)-[(1-OXO ] -2-PROPEN-1-YL)AMINO]-1-PIPERIDINYL]METHYL]-2-PYRIDINECARBOXAMIDE, IRREVERSIBLE MENIN-MLL INHIBITOR FOR CANCER TREATMENT
JP2025513716A (ja) 2022-03-23 2025-04-30 ライジェル・ファーマシューティカルズ・インコーポレイテッド Ｉｒａｋ阻害剤としてのピリミド－２－イル－ピラゾール化合物
CN116178358B (zh) * 2022-11-04 2024-04-19 济南大学 一种靶向c-Src激酶SH3结构域的化合物及其应用
PY2389146A (es) * 2022-11-09 2025-06-23 Syngenta Crop Protection Ag Derivados de pirazol microbiocidas
WO2024155710A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6- yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2-pyridinecarboxamide as a covalent inhibitor of menin-mll interaction
CN116675714B (zh) * 2023-05-04 2025-08-29 西南医科大学 一种靶向光敏剂FA-BAT-NPs及其制备方法与应用
WO2025040140A1 (en) * 2023-08-22 2025-02-27 National Institute Of Biological Sciences, Beijing Substituted pyrazol-4-yl urea as kinase inhibitors
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers

Family Cites Families (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4431807A (en) 1980-06-12 1984-02-14 The United States Of America As Represented By The Secretary Of The Army 4-Methyl-5-(unsubstituted and substituted phenoxy)-6-methoxy-8-(aminoalkylamino)quinolines
US4619686A (en) 1984-07-17 1986-10-28 Eli Lilly And Company Pyridazinylurea compounds and methods of use as herbicides
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
EP0308020A3 (en) 1987-09-18 1990-12-05 Merck & Co. Inc. 5-(aryl and heteroaryl)-6-(aryl and heteroaryl)-1,2-dihydro-2-oxo 3-pyridinecarboxylic acids and derivatives thereof
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
US5451596A (en) 1992-12-29 1995-09-19 Rhone Poulenc Rorer Pharmaceuticals Inc. Cycloalkyl amine bis-aryl squalene synthase inhibitors
FR2707295A1 (fr) 1993-06-07 1995-01-13 Rhone Poulenc Agrochimie Fongicides pyrazoles substitués en position 3 par un hétérocycle.
US5852011A (en) 1994-05-31 1998-12-22 Mitsui Chemicals, Inc. Benzimidazole derivatives
EP0766676B1 (en) 1994-06-24 2002-05-22 Euroceltique S.A. Compounds for inhibiting phosphodiesterase iv
ATE251141T1 (de) 1995-03-10 2003-10-15 Berlex Lab Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
WO1997012613A1 (en) 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
AU706497B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5874452A (en) 1996-04-03 1999-02-23 Merck & Co., Inc. Biheteroaryl inhibitors of farnesyl-protein transferase
DK0906279T3 (da) 1996-05-30 2003-02-03 Hoffmann La Roche Pyrrolderivater
NZ503788A (en) 1997-10-27 2002-11-26 Agouron Pharma 4-aminothiazole derivatives and their use as inhibitors of cyclin-dependent kinases
AU2713799A (en) 1998-03-12 1999-09-27 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (ptpases)
ATE316961T1 (de) 1998-05-22 2006-02-15 Scios Inc Heterozyclische derivate für die behandlung von herzversagen und andere erkrankungen
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
WO2000059902A2 (en) 1999-04-02 2000-10-12 Du Pont Pharmaceuticals Company Aryl sulfonyls as factor xa inhibitors
PL215901B1 (pl) 1999-04-15 2014-02-28 Bristol Myers Squibb Co Cykliczny inhibitor bialkowych kinaz tyrozynowych, jego zastosowanie oraz kompozycja farmaceutyczna zawierajaca taki zwiazek
NZ515086A (en) 1999-04-28 2003-10-31 Aventis Pharma Gmbh Di-aryl acid derivatives as PPAR receptor ligands
DE19920936A1 (de) 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
SI1194425T1 (sl) 1999-06-23 2005-12-31 Sanofi Aventis Deutschland Substituirani benzimidazoli
JP4627356B2 (ja) 1999-06-30 2011-02-09 昭 松森 ウイルス性心筋炎の予防または治療薬剤
FR2795726A1 (fr) 1999-06-30 2001-01-05 Aventis Cropscience Sa Nouveaux pyrazoles fongicides
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
JP2003509412A (ja) 1999-09-17 2003-03-11 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子阻害剤
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
DE60040676D1 (de) 1999-09-17 2008-12-11 Millennium Pharm Inc BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa
YU54202A (sh) 2000-01-18 2006-01-16 Agouron Pharmaceuticals Inc. Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije
HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
HUP0202332A2 (en) 2000-02-05 2002-10-28 Vertex Pharma Pyrazole compositions useful as inhibitors of erk
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
US20040087798A1 (en) 2000-03-14 2004-05-06 Akira Yamada Novel amide compounds
EP1274705A1 (en) 2000-03-29 2003-01-15 Cyclacel Limited 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
JP2004501083A (ja) 2000-04-18 2004-01-15 アゴーロン・ファーマシューティカルズ・インコーポレイテッド プロテインキナーゼを阻害するためのピラゾール
EP1278749B1 (en) 2000-04-25 2005-01-26 Bristol-Myers Squibb Company USE OF 5-THIO-, SULFINYL- AND SULFONYLPYRAZOLO 3,4-b]-PYRIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS
US6414013B1 (en) 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
AU2001268711A1 (en) 2000-06-23 2002-01-08 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
EP1296982B1 (en) 2000-06-23 2007-09-19 Bristol-Myers Squibb Pharma Company 1-(heteroaryl-phenyl)-condensed pyrazol derivatives as factor xa inhibitors
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
CA2420164A1 (en) 2000-10-20 2002-05-02 Bristol-Myers Squibb Pharma Company Acylsemicarbazides and their use as cyclin dependent kinase (cdk) inhibitors
NZ526472A (en) 2000-12-21 2004-04-30 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors
DE10108480A1 (de) 2001-02-22 2002-09-05 Bayer Ag Pyrazolylpyrimidine
DE10110750A1 (de) 2001-03-07 2002-09-12 Bayer Ag Neuartige Aminodicarbonsäurederivate mit pharmazeutischen Eigenschaften
US6951848B2 (en) 2001-03-12 2005-10-04 Millennium Pharmaceuticals, Inc., Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
US6890915B2 (en) 2001-05-25 2005-05-10 Bristol-Myers Squibb Pharma Company Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
DE60206756T2 (de) 2001-06-29 2006-07-13 CV Therapeutics, Inc., Palo Alto Purin derivate als a2b adenosin rezeptor antagonisten
US7064215B2 (en) 2001-07-03 2006-06-20 Chiron Corporation Indazole benzimidazole compounds
WO2003006465A1 (en) 2001-07-13 2003-01-23 Cv Therapeutics, Inc. Partial and full agonist of a adenosine receptors
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
FR2831536A1 (fr) 2001-10-26 2003-05-02 Aventis Pharma Sa Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr
US6897208B2 (en) 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
AU2002349477A1 (en) 2001-11-26 2003-06-10 Takeda Chemical Industries, Ltd. Bicyclic derivative, process for producing the same, and use
AU2002357312A1 (en) 2001-12-20 2003-07-09 Bristol-Myers Squibb Company Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases
EP1472245A2 (en) 2002-02-06 2004-11-03 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
EP1581217A4 (en) 2002-11-01 2007-07-11 Merck & Co Inc CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ANDROGENIC RECEPTORS
AU2003285336B2 (en) 2002-12-04 2009-11-26 Sanofi-Aventis Deutschland Gmbh Imidazole-derivatives as factor Xa inhibitors
WO2004052371A2 (en) 2002-12-11 2004-06-24 7Tm Pharma A/S Cyclic quinoline compounds for use in mch receptor related disorders
EP1581527A4 (en) 2002-12-13 2006-11-22 Smithkline Beecham Corp MIMETICS OF THROMBOPOIETINE
JP4585448B2 (ja) 2002-12-23 2010-11-24 サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング 第Ｘａ因子阻害剤としてのピラゾール−誘導体
US20040242559A1 (en) 2003-04-25 2004-12-02 Aventis Pharma S.A. Novel indole derivatives, preparation thereof as medicinal products and pharmaceutical compositions, and especially as KDR inhibitors
FR2854159B1 (fr) * 2003-04-25 2008-01-11 Aventis Pharma Sa Nouveaux derives de l'indole, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de kdr
GB0315657D0 (en) 2003-07-03 2003-08-13 Astex Technology Ltd Pharmaceutical compounds
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
US20050032869A1 (en) 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
US8969372B2 (en) 2003-11-14 2015-03-03 Aptose Boisciences Inc. Aryl imidazoles and their use as anti-cancer agents
US7932281B2 (en) 2004-03-10 2011-04-26 Kureha Corporation Amine-based compound and use thereof
WO2006070192A1 (en) 2004-12-30 2006-07-06 Astex Therapeutics Limited Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases
EP1833819A1 (en) 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
EP1968579A1 (en) * 2005-12-30 2008-09-17 Astex Therapeutics Limited Pharmaceutical compounds
WO2008001101A2 (en) 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
EP2049119A2 (en) * 2006-06-29 2009-04-22 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea
JP5528807B2 (ja) * 2006-10-12 2014-06-25 アステックス、セラピューティックス、リミテッド 複合薬剤

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
638页31和32行
639页26行，424页（m）化合物，428页（x）和（y）化合物，420页（c）化合物，440页（b）化合物，439页（a）和（c）化合物.

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PL1648426T3 (pl) 2014-05-30
AU2004253338A1 (en) 2005-01-13
TWI372050B (en) 2012-09-11
EP2305250A1 (en) 2011-04-06
PT1648426E (pt) 2014-03-07
DK1648426T3 (da) 2014-02-10
SI2305250T1 (sl) 2014-06-30
PL2305250T3 (pl) 2014-07-31
CN1845734A (zh) 2006-10-11
TW200524598A (en) 2005-08-01
JP4833059B2 (ja) 2011-12-07
WO2005002552A3 (en) 2005-06-16
EP1648426A2 (en) 2006-04-26
US20070135477A1 (en) 2007-06-14
EP2305250B1 (en) 2014-03-26
SI1648426T1 (sl) 2014-04-30
EP1648426B1 (en) 2014-01-08
US20140010892A1 (en) 2014-01-09
NZ543959A (en) 2009-08-28
ES2457466T3 (es) 2014-04-25
CA2531050C (en) 2013-04-09
DK2305250T3 (da) 2014-04-22
ES2443995T3 (es) 2014-02-21
US20110224203A1 (en) 2011-09-15
WO2005002552A2 (en) 2005-01-13
AU2004253338B2 (en) 2010-02-18
US7977477B2 (en) 2011-07-12

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