CN101687885B - 作为激酶抑制剂的稠合噻唑衍生物 - Google Patents

作为激酶抑制剂的稠合噻唑衍生物 Download PDF

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Publication number
CN101687885B
CN101687885B CN200880024430XA CN200880024430A CN101687885B CN 101687885 B CN101687885 B CN 101687885B CN 200880024430X A CN200880024430X A CN 200880024430XA CN 200880024430 A CN200880024430 A CN 200880024430A CN 101687885 B CN101687885 B CN 101687885B
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Prior art keywords
methyl
dimethyl
morpholin
thiazolo
alkyl
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Chinese (zh)
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CN101687885A (zh
Inventor
R·P·亚历山大
P·S·奥吉拉
K·V·L·克雷佩
A·M·福雷
R·J·弗兰克林
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UCB SA
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UCB SA
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Priority claimed from GB0612644A external-priority patent/GB0612644D0/en
Priority claimed from GB0620062A external-priority patent/GB0620062D0/en
Application filed by UCB SA filed Critical UCB SA
Priority claimed from PCT/GB2008/002194 external-priority patent/WO2009001089A1/en
Publication of CN101687885A publication Critical patent/CN101687885A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/12Heterocyclic 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 three hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN200880024430XA 2006-06-26 2008-06-24 作为激酶抑制剂的稠合噻唑衍生物 Active CN101687885B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0612644A GB0612644D0 (en) 2006-06-26 2006-06-26 Therapeutic agents
GB0620062A GB0620062D0 (en) 2006-10-10 2006-10-10 Therapeutic agents
PCT/GB2007/002390 WO2008001076A1 (en) 2006-06-26 2007-06-26 Fused thiazole derivatives as kinase inhibitors
GBPCT/GB2007/002390 2007-06-26
PCT/GB2008/002194 WO2009001089A1 (en) 2007-06-26 2008-06-24 Fused thiazole derivatives as kinase inhibitors

Publications (2)

Publication Number Publication Date
CN101687885A CN101687885A (zh) 2010-03-31
CN101687885B true CN101687885B (zh) 2012-08-22

Family

ID=38671000

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880024430XA Active CN101687885B (zh) 2006-06-26 2008-06-24 作为激酶抑制剂的稠合噻唑衍生物

Country Status (20)

Country Link
US (3) US8242116B2 (cg-RX-API-DMAC10.html)
EP (2) EP2035436B1 (cg-RX-API-DMAC10.html)
CN (1) CN101687885B (cg-RX-API-DMAC10.html)
AT (1) ATE510840T1 (cg-RX-API-DMAC10.html)
AU (1) AU2008269577B2 (cg-RX-API-DMAC10.html)
CA (1) CA2692085C (cg-RX-API-DMAC10.html)
CO (1) CO6270229A2 (cg-RX-API-DMAC10.html)
CY (1) CY1114419T1 (cg-RX-API-DMAC10.html)
DK (1) DK2170906T3 (cg-RX-API-DMAC10.html)
EA (1) EA017187B1 (cg-RX-API-DMAC10.html)
ES (2) ES2365258T3 (cg-RX-API-DMAC10.html)
HR (1) HRP20130523T1 (cg-RX-API-DMAC10.html)
IL (1) IL202659A0 (cg-RX-API-DMAC10.html)
ME (1) ME01592B (cg-RX-API-DMAC10.html)
MX (1) MX2009013740A (cg-RX-API-DMAC10.html)
MY (1) MY148852A (cg-RX-API-DMAC10.html)
PL (1) PL2170906T3 (cg-RX-API-DMAC10.html)
PT (1) PT2170906E (cg-RX-API-DMAC10.html)
RS (1) RS52824B (cg-RX-API-DMAC10.html)
WO (1) WO2008001076A1 (cg-RX-API-DMAC10.html)

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WO2009071890A1 (en) * 2007-12-04 2009-06-11 Ucb Pharma S.A. Tricyclic kinase inhibitors
WO2009071895A1 (en) * 2007-12-04 2009-06-11 Ucb Pharma S.A. Fused thiazole and thiophene derivatives as kinase inhibitors
AU2008343932B2 (en) 2007-12-19 2013-08-15 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
ATE531372T1 (de) 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
JPWO2009130900A1 (ja) * 2008-04-24 2011-08-11 日本曹達株式会社 オキシム誘導体、中間体化合物および植物病害防除剤
US8603945B2 (en) * 2008-07-23 2013-12-10 The Regents Of The University Of California Methods and compositions for providing salicyclic acid-independent pathogen resistance in plants
EP2341052A4 (en) * 2008-09-05 2011-10-12 Shionogi & Co RING-CONDENSED MORPHOLINE DERIVATIVITY WITH PI3K-INHIBITING EFFECT
AU2010216219A1 (en) 2009-02-17 2011-09-01 Vertex Pharmaceuticals Incorporated Tetrahydrothiazolopyridine inhibitors of phosphatidylinositol 3-kinase
AR076126A1 (es) * 2009-03-18 2011-05-18 Schering Corp Compuestos biciclicos como inhibidores de diacilglicerol aciltransferasa
UY32582A (es) * 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
ES2638323T3 (es) * 2009-05-20 2017-10-19 Glaxosmithkline Llc Derivados de tiazolopirimidinona como inhibidores de PI3 quinasa
GB0912946D0 (en) 2009-07-24 2009-09-02 Addex Pharmaceuticals Sa New compounds 5
MX2012002059A (es) 2009-08-20 2012-04-19 Karus Therapeutics Ltd Compestos heterociclicos triciclicos como inhibidores de fosfoionositida 3-quinasa.
EA020010B1 (ru) * 2009-12-18 2014-07-30 Янссен Фармацевтика Нв БИЦИКЛИЧЕСКИЕ ТИАЗОЛЫ В КАЧЕСТВЕ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ mGluR5 РЕЦЕПТОРОВ
ES2431302T3 (es) 2009-12-18 2013-11-25 Janssen Pharmaceutica, N.V. Tiazoles bicíclicos como moduladores alostéricos de receptores mGluR5
EP2582693B1 (de) 2010-06-15 2016-03-30 Bayer Intellectual Property GmbH Neue ortho-substituierte arylamid-derivate
BR112013007056A2 (pt) 2010-10-01 2019-09-24 Basf Se compostos de imina
AU2011316016A1 (en) * 2010-10-13 2013-05-30 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
BR112013012961A2 (pt) * 2010-11-24 2019-09-24 Exelixis Inc benzoxazepinas como inhibidores de mtor e métodos de seu uso e fabricação
CN102649777B (zh) * 2011-02-25 2014-03-12 中国中化股份有限公司 一种制备1-芳基-3-羧基-5-吡唑啉酮类化合物的方法
WO2012129344A1 (en) 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
JO3398B1 (ar) 2011-12-22 2019-10-20 Novartis Ag مشتقات 2،3- ثانى هيدرو- بنزو[1,4] أوكسازين والمركبات المتعلقة بها كمثبطات كيناز فسفواينوسيتيد-3 (pi3k) لمعالجة على سبيل المثال التهاب المفاصل الروماتيدي
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20160039767A1 (en) 2013-03-14 2016-02-11 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153208A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
CA2903264A1 (en) 2013-03-14 2014-11-06 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
WO2015059049A1 (de) * 2013-10-21 2015-04-30 Umicore Ag & Co. Kg Monoarylierung aromatischer amine
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
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GB201514758D0 (en) 2015-08-19 2015-09-30 Karus Therapeutics Ltd Formulation
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CN108570043A (zh) * 2018-06-20 2018-09-25 王延娇 一种化合物及其作为选择性pi3k抑制剂在治疗肿瘤中的应用
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WO2006114606A1 (en) * 2005-04-26 2006-11-02 Ucb Pharma S.A. Fused thiazole derivatives as kinase inhibitors

Patent Citations (1)

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AU2008269577B2 (en) 2012-12-20
ATE510840T1 (de) 2011-06-15
CO6270229A2 (es) 2011-04-20
EA201000038A1 (ru) 2010-06-30
US8338592B2 (en) 2012-12-25
AU2008269577A1 (en) 2008-12-31
MY148852A (en) 2013-06-14
ME01592B (me) 2014-09-20
ES2416364T3 (es) 2013-07-31
EP2170906B1 (en) 2013-04-03
US20130079330A1 (en) 2013-03-28
PL2170906T3 (pl) 2013-08-30
US8710054B2 (en) 2014-04-29
EA017187B1 (ru) 2012-10-30
EP2035436A1 (en) 2009-03-18
IL202659A0 (en) 2010-06-30
CA2692085A1 (en) 2008-12-31
ES2365258T3 (es) 2011-09-27
EP2035436B1 (en) 2011-05-25
CN101687885A (zh) 2010-03-31
PT2170906E (pt) 2013-06-25
US8242116B2 (en) 2012-08-14
US20110003785A1 (en) 2011-01-06
CA2692085C (en) 2015-10-13
DK2170906T3 (da) 2013-06-24
HRP20130523T1 (en) 2013-07-31
MX2009013740A (es) 2010-02-01
EP2170906A1 (en) 2010-04-07
CY1114419T1 (el) 2016-08-31
US20100137302A1 (en) 2010-06-03
RS52824B (cg-RX-API-DMAC10.html) 2013-10-31
WO2008001076A1 (en) 2008-01-03

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