首页> 外国专利> Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives

Method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives

机译:取代的3-(2-苯胺基-1-环己基-1H-苯并咪唑-5-基)丙酸衍生物的制备方法

摘要

The present invention relates to a method for preparing substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives of the general formula (I) in which R1 represents a hydrogen atom or R1 represents a group selected from the series of C1-C3-alkyl-, C1-C3-alkoxy-, C1-C3-haloalkyl- and C1-C3-haloalkoxy-, R2 represents a hydrogen atom or a C1-C3-alkyl group, R3 represents a hydrogen atom or a C1-C3-alkyl group, R4 represents a cyclohexyl group, which is optionally singly or multiply substituted by a C1-C3-alkyl group, and R5 represents a hydrogen atom or a C1-C6-alkyl group; and also intermediates which may be used to prepare substituted 3-(2-anilino-1-cyclohexyl-1H-benzimidazol-5-yl)propanoic acid derivatives. The present invention also relates to a crystalline form of 3-(2-{[4-(trifluoromethoxy)phenyl]amino}-1-[(1R,5R)-3,3,5-trimethylcyclohexyl]-1H-benzimidazol-5-yl)propanoic acid, pharmaceutical compositions comprising this crystalline form, and also the use of this crystalline form for preparing a medicament for the treatment of a disease.; embedded image
机译:通式(I)的取代的3-(2-苯胺基-1-环己基-1H-苯并咪唑-5-基)丙酸衍生物的制备方法本发明涉及通式(I)的取代的3-(2-苯胺基-1-环己基-1H-苯并咪唑-5-基)丙酸衍生物的制备方法,其中R 1 代表氢原子或R 1 代表选自C 1 -C 3 -烷基-,C 1 -C 3 -烷氧基-,C 1 -C 3 -卤代烷基-和C 1 -C 3 -卤代烷氧基-,R 2 表示氢原子或C 1 -C 3 -烷基基,R 3 代表氢原子或C 1 -C 3 -烷基,R 4 代表任选被C 1 -C 3 -烷基单取代或多取代的环己基,R 5 表示氢原子或C 1 -C 6 -烷基;以及可用于制备取代的3-(2-苯胺基-1-环己基-1H-苯并咪唑-5-基)丙酸衍生物的中间体。本发明还涉及3-(2-{[4-(三氟甲氧基)苯基]氨基} -1-[(1R,5R)-3,3,5-三甲基环己基] -1H-苯并咪唑-5的结晶形式。 -基)丙酸,包含该晶体形式的药物组合物,以及该晶体形式在制备用于治疗疾病的药物中的用途; “嵌入式图像”

著录项

  • 公开/公告号US10703727B2

    专利类型

  • 公开/公告日2020-07-07

    原文格式PDF

  • 申请/专利权人 BAYER PHARMA AKTIENGESELLSCHAFT;

    申请/专利号US201615748027

  • 发明设计人 HEIKO SCHIRMER;

    申请日2016-07-25

  • 分类号C07D235/30;A61P35;

  • 国家 US

  • 入库时间 2022-08-21 11:29:52

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