JP5498703B2 - プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド - Google Patents

プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド Download PDF

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Publication number
JP5498703B2
JP5498703B2 JP2008551474A JP2008551474A JP5498703B2 JP 5498703 B2 JP5498703 B2 JP 5498703B2 JP 2008551474 A JP2008551474 A JP 2008551474A JP 2008551474 A JP2008551474 A JP 2008551474A JP 5498703 B2 JP5498703 B2 JP 5498703B2
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compound
ring
formula
alkyl
alkenyl
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JP2009523822A5 (enExample
JP2009523822A (ja
Inventor
スティーブン デュラント,
ジャン−ダミアン シャリエ,
ロナルド ネグテル,
ガイ ブレンチリー,
デイビッド ケイ,
シャジア サディック,
シャーン ラマヤ,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P25/28Drugs 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
    • 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
    • A61P31/12Antivirals
    • 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
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
JP2008551474A 2006-01-23 2007-01-23 プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド Expired - Fee Related JP5498703B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US76109706P 2006-01-23 2006-01-23
US60/761,097 2006-01-23
PCT/US2007/001726 WO2007087283A2 (en) 2006-01-23 2007-01-23 Thiophene-carboxamides useful as inhibitors of protein kinases

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2012281195A Division JP2013056942A (ja) 2006-01-23 2012-12-25 プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド

Publications (3)

Publication Number Publication Date
JP2009523822A JP2009523822A (ja) 2009-06-25
JP2009523822A5 JP2009523822A5 (enExample) 2011-03-10
JP5498703B2 true JP5498703B2 (ja) 2014-05-21

Family

ID=38179584

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2008551474A Expired - Fee Related JP5498703B2 (ja) 2006-01-23 2007-01-23 プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド
JP2012281195A Pending JP2013056942A (ja) 2006-01-23 2012-12-25 プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド

Family Applications After (1)

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JP2012281195A Pending JP2013056942A (ja) 2006-01-23 2012-12-25 プロテインキナーゼのインヒビターとして有用なチオフェン−カルボキサミド

Country Status (7)

Country Link
US (3) US7915305B2 (enExample)
EP (2) EP1989205B1 (enExample)
JP (2) JP5498703B2 (enExample)
CN (1) CN101400678A (enExample)
AU (1) AU2007208358A1 (enExample)
CA (1) CA2637335A1 (enExample)
WO (1) WO2007087283A2 (enExample)

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AU2006287766B2 (en) 2005-09-06 2010-06-24 Smithkline Beecham Corporation Benzimidazole thiophene compounds as PLK inhibitors
EP1989205B1 (en) 2006-01-23 2012-06-13 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
EP2418210A1 (en) * 2006-04-13 2012-02-15 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
CN101484447A (zh) * 2006-05-23 2009-07-15 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的噻吩-甲酰胺类
JP2009538305A (ja) 2006-05-23 2009-11-05 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 プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド
PE20080710A1 (es) * 2006-06-02 2008-08-07 Smithkline Beecham Corp Compuestos de tiofeno de bencimidazol
US7615643B2 (en) 2006-06-02 2009-11-10 Smithkline Beecham Corporation Benzimidazole thiophene compounds
JP2010533736A (ja) 2007-07-19 2010-10-28 ハー・ルンドベック・アクチエゼルスカベット 5員複素環アミドおよび関連化合物
WO2010017046A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Pyrazolo[1,5-a]pyridines as mark inhibitors
AU2010311511B2 (en) 2009-10-30 2014-07-17 Janssen Pharmaceutica Nv Imidazo[1,2-b]pyridazine derivatives and their use as PDE10 inhibitors
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
US8933070B2 (en) 2010-07-02 2015-01-13 University Health Network Methods of targeting PTEN mutant diseases and compositions therefor
CN103619846B (zh) 2011-06-27 2016-08-17 詹森药业有限公司 1-芳基-4-甲基-[1,2,4]三唑[4,3-a]喹喔啉衍生物
JO3407B1 (ar) 2012-05-31 2019-10-20 Eisai R&D Man Co Ltd مركبات رباعي هيدرو بيرازولو بيريميدين
EP2863909B1 (en) 2012-06-26 2020-11-04 Janssen Pharmaceutica N.V. Combinations comprising 4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline compounds as pde 2 inhibitors and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders
ES2607184T3 (es) 2012-07-09 2017-03-29 Janssen Pharmaceutica, N.V. Inhibidores de la enzima fosfodiesterasa 10
CN108135916B (zh) * 2015-06-19 2022-01-28 北京科辉智药生物科技有限责任公司 手性特异性含硼化合物及其在治疗癌症或淀粉样变性中的应用
WO2018081719A1 (en) * 2016-10-31 2018-05-03 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of nek2 and uses thereof
CN116057045A (zh) 2020-06-05 2023-05-02 金耐特生物制药公司 成纤维细胞生长因子受体激酶抑制剂

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EP1989205B1 (en) 2006-01-23 2012-06-13 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
EP2418210A1 (en) 2006-04-13 2012-02-15 Vertex Pharmceuticals Incorporated Thiophene-carboxamides useful as inhibitors of protein kinases
CN101484447A (zh) 2006-05-23 2009-07-15 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的噻吩-甲酰胺类
JP2009538305A (ja) 2006-05-23 2009-11-05 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 プロテインキナーゼのインヒビターとして有用なチオフェンカルボキサミド

Also Published As

Publication number Publication date
CN101400678A (zh) 2009-04-01
US20110288095A1 (en) 2011-11-24
US8759389B1 (en) 2014-06-24
EP1989205A2 (en) 2008-11-12
EP2474546A1 (en) 2012-07-11
JP2013056942A (ja) 2013-03-28
EP1989205B1 (en) 2012-06-13
WO2007087283A2 (en) 2007-08-02
US8399478B2 (en) 2013-03-19
WO2007087283A3 (en) 2007-09-13
US7915305B2 (en) 2011-03-29
AU2007208358A1 (en) 2007-08-02
CA2637335A1 (en) 2007-08-02
JP2009523822A (ja) 2009-06-25
US20070219205A1 (en) 2007-09-20

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