JP6785302B2 - ビアリールキナーゼ阻害剤 - Google Patents

ビアリールキナーゼ阻害剤 Download PDF

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JP6785302B2
JP6785302B2 JP2018516713A JP2018516713A JP6785302B2 JP 6785302 B2 JP6785302 B2 JP 6785302B2 JP 2018516713 A JP2018516713 A JP 2018516713A JP 2018516713 A JP2018516713 A JP 2018516713A JP 6785302 B2 JP6785302 B2 JP 6785302B2
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oxy
amine
amino
methyl
dimethylpentyl
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Japanese (ja)
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JP2018537408A5 (enExample
JP2018537408A (ja
Inventor
ジョアン・ジェイ・ブロンソン
リン・チェン
ジョナサン・エル・ディッタ
キャロリン・ダイアン・ジアーバ
プラサダ・ラオ・ジャラガム
グアンリン・ルオ
ジョン・イー・マコー
タルン・クマール・メイシャル
スシール・ジェタナンド・ナラ
ラムクマール・ラジャマニ
ラメシュ・クマール・シストラ
スーダマニ・タンガベル
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
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    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/20—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hydrogen atoms and substituted hydrocarbon radicals directly attached to ring carbon atoms
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    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • 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
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KR102379518B1 (ko) 2014-04-02 2022-03-25 브리스톨-마이어스 스큅 컴퍼니 비아릴 키나제 억제제
ES2767776T3 (es) 2015-10-01 2020-06-18 Bristol Myers Squibb Co Inhibidores de biaril cinasa
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EP3555048B1 (en) 2016-12-19 2021-07-07 Novartis AG New picolinic acid derivatives and their use as intermediates
US11730723B2 (en) * 2020-04-21 2023-08-22 Lexicon Pharmaceuticals, Inc. Compounds and methods for treating viral infections
CN111995583A (zh) * 2020-08-18 2020-11-27 上海毕得医药科技有限公司 一种1,5-二甲基嘧啶-2(1h)-酮的合成方法
CN117715899A (zh) * 2021-07-15 2024-03-15 西藏海思科制药有限公司 Aak1抑制剂及其用途
US12344596B2 (en) 2022-03-01 2025-07-01 Lexicon Pharmaceuticals, Inc. Solid forms of (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and salts thereof
WO2023167806A1 (en) * 2022-03-01 2023-09-07 Lexicon Pharmaceuticals, Inc. Methods and compounds useful in the sythesis of an aak1 inhibitor
CN120202001A (zh) * 2022-11-10 2025-06-24 西藏海思科制药有限公司 一种含aak1抑制剂的药物组合物
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Family Cites Families (16)

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Publication number Priority date Publication date Assignee Title
AU2003286895A1 (en) 2002-11-05 2004-06-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
AR093195A1 (es) * 2012-02-29 2015-05-27 Meiji Seika Pharma Co Ltd Composicion para el control de plagas que incluye un derivado de iminopiridina
HUE036040T2 (hu) 2012-03-09 2018-06-28 Lexicon Pharmaceuticals Inc Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére
US8703953B2 (en) * 2012-03-09 2014-04-22 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
US8901305B2 (en) * 2012-07-31 2014-12-02 Bristol-Myers Squibb Company Aryl lactam kinase inhibitors
JP2016509066A (ja) 2013-02-22 2016-03-24 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アダプター関連キナーゼ１（ａａｋ１）の阻害剤としての５ｈ−クロメノ［３，４−ｃ］ピリジン
WO2015006100A1 (en) 2013-07-08 2015-01-15 Bristol-Myers Squibb Company Aryl amide kinase inhibitors
WO2015038112A1 (en) 2013-09-11 2015-03-19 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
EP3046919B1 (en) * 2013-09-19 2019-08-07 Basf Se N-acylimino heterocyclic compounds
EP3099300B1 (en) 2014-01-29 2018-09-05 Bristol-Myers Squibb Company Aryl lactam kinase inhibitors
ES2701903T3 (es) 2014-01-31 2019-02-26 Bristol Myers Squibb Co Inhibidores de cinasa a base de quinolina
KR102379518B1 (ko) * 2014-04-02 2022-03-25 브리스톨-마이어스 스큅 컴퍼니 비아릴 키나제 억제제
EP3200797A1 (en) 2014-09-30 2017-08-09 Bristol-Myers Squibb Company Quinazoline-based kinase inhibitors
EP3292124B1 (en) 2015-04-10 2019-05-22 Bristol-Myers Squibb Company 6h-isochromeno[3,4-c]pyridines and benzo[c][1,7]naphthyridin-6-(5h)-ones as adaptor associated kinase 1 (aak1) inhibitors
ES2767776T3 (es) 2015-10-01 2020-06-18 Bristol Myers Squibb Co Inhibidores de biaril cinasa
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