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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Japanese (ja)
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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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    • 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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    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
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    • 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
    • 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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  • Virology (AREA)
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  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
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  • Psychology (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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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7589214B2 (en) * 2006-04-11 2009-09-15 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
BRPI1016172A2 (pt) * 2009-04-24 2016-04-19 Tibotec Pharm Ltd éteres diarílicos
US8735417B2 (en) 2009-12-17 2014-05-27 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
US8759366B2 (en) 2009-12-17 2014-06-24 Merck Sharp & Dohme Corp. Aminopyrimidines as SYK inhibitors
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
JP6170944B2 (ja) 2011-12-28 2017-07-26 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｈｃｖ阻害剤としてのヘテロ−二環式誘導体
MD20150035A2 (ro) * 2012-11-02 2015-10-31 Pfizer Inc. Inhibitori de tirozinkinaza Bruton
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
JP6495886B2 (ja) 2013-03-15 2019-04-03 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阻害剤としての複素環式芳香族化合物
PL3052476T3 (pl) * 2013-09-30 2021-01-11 Guangzhou Innocare Pharma Tech Co., Ltd. Podstawione nikotynoimidowe inhibitory btk oraz sposób ich wytwarzania i zastosowanie w leczeniu raka, stanu zapalnego i chorób automunnologicznych
EP3080097B1 (en) 2013-12-13 2018-04-18 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
CN106687446B (zh) * 2014-07-18 2020-04-28 百济神州(北京)生物科技有限公司 作为t790m/wt-egfr的选择性和不可逆的激酶抑制剂的5-氨基-4-氨甲酰基-吡唑化合物及其用途
JP6976947B2 (ja) 2015-12-16 2021-12-08 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 自己免疫疾患の処置に有用なビピラゾリル誘導体
JP6916185B2 (ja) 2016-01-13 2021-08-11 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阻害剤としてのイソキノロン類
CN113454066B (zh) * 2019-02-25 2024-02-09 北京诺诚健华医药科技有限公司 制备6-(1-丙烯酰基哌啶-4-基)-2-(4-苯氧基苯基)尼克酰胺的工艺
CN116018138B (zh) * 2020-07-13 2025-08-15 河南知微生物医药有限公司 作为布鲁诺酪氨酸激酶抑制剂的取代的1H-咪唑并[1,2-b]吡唑-3-甲酰胺

Citations (2)

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Publication number Priority date Publication date Assignee Title
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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US7589214B2 (en) 2009-09-15
AU2007235237B2 (en) 2011-08-18
US8236832B2 (en) 2012-08-07
US20070298065A1 (en) 2007-12-27
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AU2007235237A1 (en) 2007-10-18
WO2007117692A3 (en) 2008-01-10
US20130090479A1 (en) 2013-04-11
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ATE534632T1 (de) 2011-12-15
US8865751B2 (en) 2014-10-21

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