首页> 外国专利> New thiophenecarboxamido-substituted isoindole derivatives, useful as Factor XIa inhibitors for treatment or prophylaxis of, e.g. thromboembolic diseases, atherosclerosis, arthritis, Alzheimer's disease or cancer

New thiophenecarboxamido-substituted isoindole derivatives, useful as Factor XIa inhibitors for treatment or prophylaxis of, e.g. thromboembolic diseases, atherosclerosis, arthritis, Alzheimer's disease or cancer

机译：新的噻吩甲酰胺基取代的异吲哚衍生物，可用作因子XIa抑制剂，用于治疗或预防例如血栓栓塞性疾病，动脉粥样硬化，关节炎，阿尔茨海默氏病或癌症

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摘要

Thiophenecarboxamido-substituted isoindole derivatives (I) are new. Isoindole derivatives of formula (I) and their salts, hydrates, hydrated salts and solvates are new. R1 = H, OH or OT; R2 = H; or R1 + R2 = O; R3 = H, OH or OT; R4 = H; or R3 + R4 = O; R5 = halo, CF3 or Me; T = 1-4C alkyl; A = 1-4C alkanediyl (optionally substituted (os) by OH or OT); a, b = 0 or 1; B' = CO, COO, OCO, CONR6 or NR6CO; R6 = H or T; and D = 5-7 membered heterocyclyl (os by 1 or 2 of OH, CONH2, COT, 3-7C cycloalkyl, (3-7C) cycloalkylcarbonyl, 5-10 membered heterocyclyl, COOT, alkyl, (os by OH, CN, OT, mono- or dialkylamino, mono- or dialkylaminocarbonyl, 5-10 membered heterocyclyl, 5- or 6-membered heterocyclylcarbonyl or 5-10 membered heteroaryl), 6-10C aryl (os by halo, CF3, NO2, T or OT), 5-10 membered heteroaryl (os by CN, NH2 or T) or 5-10 membered heteroarylcarbonyl); alkyl (os by CN, mono- or dialkylamino, amidino, 5-10 membered heteroaryl, 5-10 membered heteroarylamino (os by halo), 5-10 membered heterocyclyl (os by 5-10 membered heteroaryl) or NHCOT) or 5-10 membered heteroaryl (os by halo or T). Alkyl moieties have 1-6C unless specified otherwise. An Independent claim is also included for the preparation of (I).

机译：噻吩甲酰胺基取代的异吲哚衍生物（I）是新的。式（I）的异吲哚衍生物及其盐，水合物，水合盐和溶剂化物是新的。 R1 = H，OH或OT; R2 = H;或R1 + R2 = O; R3 ＝ H，OH或OT; R4 = H;或R3 + R4 = O; R5 =卤素，CF3或Me; T = 1-4C烷基; A ＝ 1-4C链烷二基（任选被OH或OT取代（os））; a，b = 0或1; B'＝ CO，COO，OCO，CONR6或NR6CO; R6 ＝ H或T; D = 5-7元杂环基（由OH，CONH2，COT，3-7C环烷基，（3-7C）环烷基羰基中的1或2组成的os，5-10元杂环基，COOT，烷基，（由OH，CN， OT，单或二烷基氨基羰基，单或二烷基氨基羰基，5-10元杂环基，5或6元杂环羰基或5-10元杂芳基），6-10C芳基（通过卤素，CF3，NO2，T或OT制成），5-10元杂芳基（由CN，NH2或T所制）或5-10元杂芳基羰基）;烷基（CN生成的os，单或二烷基氨基，a基，5-10元杂芳基，5-10元杂芳基氨基（由卤素生成），5-10元杂环基（5-10元杂芳基由os生成）或NHCOT 10元杂芳基（由卤素或T表示）。除非另有说明，否则烷基部分具有1-6C。独立索赔也包括在准备（I）中。

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公开/公告号DE10137163A1

专利类型
公开/公告日2003-02-13

原文格式PDF
申请/专利权人 BAYER AG;
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申请/专利号DE20011037163
发明设计人 STRAUB ALEXANDER;LAMPE THOMAS;POHLMANN JENS;ROEHRIG SUSANNE;PERZBORN ELISABETH;SCHLEMMER KARL-HEINZ;
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申请日2001-07-30
分类号C07D409/14;C07D409/12;A61K31/40;
国家 DE
入库时间 2022-08-21 23:42:49

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