Cycloalkyl-substituted imidazole derivative

摘要

A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

主权项

1. A compound of general formula (I): or a pharmacologically acceptable salt thereof, wherein: A is a C3 to C12 cycloalkyl group which may be substituted with one to three identical or different groups selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, an aryloxy group, and a heterocyclyloxy group; R1, R2, and R3 are independently selected from hydrogen, a fluoro group, and a C1 to C6 alkyl group; R4 is hydrogen or a prodrug group; and Y is selected from:
—CH2—CHR5—CH2—NHR6, wherein R5 is hydrogen, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 is hydrogen or a prodrug group;—O—CHR7—CH2—NHR8, wherein R7 is hydrogen, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R8 is hydrogen or a prodrug group; andwherein R9 is hydrogen or a prodrug group, and * is the position for substitution.