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METHOD FOR PREPARING SUBSTITUTED 3-(2-ANILINO-1-CYCLOHEXYL-1H-BENZIMIDAZOL-5-YL)PROPANOIC ACID DERIVATIVES
专利权人:
发明人:
Heiko SCHIRMER
申请号:
US15748027
公开号:
US20180222871A1
申请日:
2016.07.25
申请国别(地区):
US
年份:
2018
代理人:
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.
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