JP2009536617A - タンパク質キナーゼの阻害剤として有用なチアゾール、イミダゾール、およびピラゾール - Google Patents

タンパク質キナーゼの阻害剤として有用なチアゾール、イミダゾール、およびピラゾール Download PDF

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Publication number
JP2009536617A
JP2009536617A JP2009505430A JP2009505430A JP2009536617A JP 2009536617 A JP2009536617 A JP 2009536617A JP 2009505430 A JP2009505430 A JP 2009505430A JP 2009505430 A JP2009505430 A JP 2009505430A JP 2009536617 A JP2009536617 A JP 2009536617A
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Prior art keywords
aliphatic
compound
disease
formula
halo
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JP2009505430A
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JP2009536617A5 (enExample
Inventor
ファン−ミゲル ヒメネス,
ロナルド ネグテル,
ダニエル ロビンソン,
フィリップ コリアー,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2009536617A publication Critical patent/JP2009536617A/ja
Publication of JP2009536617A5 publication Critical patent/JP2009536617A5/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/587—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with aliphatic hydrocarbon radicals substituted by 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, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
    • C07D277/593—Z being doubly bound oxygen or doubly bound nitrogen, which nitrogen is part of a possibly substituted oximino radical
    • A—HUMAN NECESSITIES
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A—HUMAN NECESSITIES
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    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

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  • Hematology (AREA)
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  • Oncology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
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JP2009505430A 2006-04-11 2007-04-11 タンパク質キナーゼの阻害剤として有用なチアゾール、イミダゾール、およびピラゾール Pending JP2009536617A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US79108306P 2006-04-11 2006-04-11
PCT/US2007/008819 WO2007117692A2 (en) 2006-04-11 2007-04-11 Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases

Publications (2)

Publication Number Publication Date
JP2009536617A true JP2009536617A (ja) 2009-10-15
JP2009536617A5 JP2009536617A5 (enExample) 2011-05-12

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JP2009505430A Pending JP2009536617A (ja) 2006-04-11 2007-04-11 タンパク質キナーゼの阻害剤として有用なチアゾール、イミダゾール、およびピラゾール

Country Status (9)

Country Link
US (3) US7589214B2 (enExample)
EP (1) EP2007732B1 (enExample)
JP (1) JP2009536617A (enExample)
CN (1) CN101460466B (enExample)
AT (1) ATE534632T1 (enExample)
AU (1) AU2007235237B2 (enExample)
CA (1) CA2648923A1 (enExample)
ES (1) ES2376765T3 (enExample)
WO (1) WO2007117692A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015524480A (ja) * 2012-08-10 2015-08-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ブルトン型チロシンキナーゼ(btk)阻害剤としてのヘテロ芳香族化合物
JP2017504634A (ja) * 2014-01-29 2017-02-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Btk阻害剤としてのピラゾール化合物
JP2017514914A (ja) * 2014-05-07 2017-06-08 北京▲賽▼林泰医▲藥▼技▲術▼有限公司 ブルートンチロシンキナーゼ阻害剤

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ATE534632T1 (de) * 2006-04-11 2011-12-15 Vertex Pharma Thiazole, imidazole und pyrazole als proteinkinasehemmer
AU2010240882B2 (en) * 2009-04-24 2014-10-23 Janssen Sciences Ireland Uc Diaryl ethers
AU2010331927B2 (en) 2009-12-17 2013-10-10 Merck Canada Inc. Aminopyrimidines as Syk inhibitors
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
WO2012154518A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
AU2012253885A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
MX340033B (es) 2011-12-28 2016-06-21 Janssen Sciences Ireland Uc Derivados heterobiciclicos como inhibidores del virus de la hepatitis c.
US20150291554A1 (en) 2012-11-02 2015-10-15 Pfizer Inc. Bruton's Tyrosine Kinase Inhibitors
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014151620A1 (en) * 2013-03-14 2014-09-25 Boehringer Ingelheim International Gmbh 5-thiazolecarboxamide dervatives and their use as btk inhibitors
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
RU2677884C2 (ru) * 2013-09-30 2019-01-22 Гуанчжоу Иннокэа Фарма Тек Ко., Лтд. Замещенные никотинимидные ингибиторы втк, их получение и применение в терапии раковых, воспалительных и аутоиммунных заболеваний
US9624201B2 (en) 2013-12-13 2017-04-18 Hoffmann-La Roche Inc. Inhibitors of bruton's tyrosine kinase
WO2016008411A1 (en) * 2014-07-18 2016-01-21 Beigene, Ltd. 5-amino-4-carbamoyl-pyrazole compounds as selective and irreversible t790m over wt-egfr kinase inhibitors and use thereof
HRP20211845T1 (hr) 2015-12-16 2022-03-04 Boehringer Ingelheim International Gmbh Derivati bipirazolila korisni za liječenje autoimunih bolesti
US10570118B2 (en) 2016-01-13 2020-02-25 Boehringer Ingelheim International Gmbh Isoquinolones as BTK inhibitors
SG11202109213RA (en) * 2019-02-25 2021-09-29 Beijing Innocare Pharma Tech Co Ltd Process for preparing 6- (1-acryloylpiperidin-4-yl) -2- (4-phenoxyphenyl) nicotinamide
WO2022012550A1 (en) * 2020-07-13 2022-01-20 Henan Normal University Substituted 1h-imidazo [1, 2-b] pyrazole-3-carboxamide as bruton's tyrosine kinase inhibitors

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JP2000509035A (ja) * 1996-04-24 2000-07-18 セルテック セラピューティックス リミテッド プロテインチロシンキナーゼp56ickの選択的インヒビターとして有用な5―アミノピラゾール化合物
WO2005123671A1 (ja) * 2004-06-22 2005-12-29 Taisho Pharmaceutical Co., Ltd. ピロール誘導体

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AU2001290912A1 (en) * 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
AU2002241966A1 (en) * 2001-01-26 2002-08-28 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
EP2256106B1 (en) 2003-07-22 2015-05-06 Astex Therapeutics Limited 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
FR2881426B1 (fr) * 2005-02-03 2007-03-30 Aventis Pharma Sa Pyrolles et imidazoles substitues, compositions les contenant, procede de frabrication et utilisation
ATE534632T1 (de) * 2006-04-11 2011-12-15 Vertex Pharma Thiazole, imidazole und pyrazole als proteinkinasehemmer

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US20130090479A1 (en) 2013-04-11
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US7589214B2 (en) 2009-09-15
WO2007117692A2 (en) 2007-10-18
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US8865751B2 (en) 2014-10-21
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