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Isothiazolopyridine-2-carboxamides and their use as pharmaceuticals

机译:异噻唑并吡啶-2-甲酰胺及其作为药物的用途

摘要

The present invention relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
机译:本发明涉及式I的取代的异噻唑并[5,4-b]吡啶-2-甲酰胺,其中R 1,R 2,R 3,R 10,R 11和X如权利要求中所定义。式I化合物是转谷氨酰胺酶,特别是转谷氨酰胺酶2(TGM2)的抑制剂,并且适用于治疗各种疾病,例如变性关节疾病,例如骨关节炎。本发明还涉及式I化合物的制备方法,其作为药物的用途以及包含它们的药物组合物。

著录项

  • 公开/公告号AU2012357864B2

    专利类型

  • 公开/公告日2017-03-02

    原文格式PDF

  • 申请/专利权人 SANOFI;

    申请/专利号AU20120357864

  • 发明设计人 SZILLAT HAUKE;LEEUW THOMAS;LORENZ MARTIN;

    申请日2012-12-18

  • 分类号C07D513/04;A61K31/4745;A61K31/496;A61K31/498;A61K31/53;A61K31/5377;A61P19;A61P25;A61P35;C07D513;

  • 国家 AU

  • 入库时间 2022-08-21 13:33:29

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