ACETIDINYLPROPYLPIPERIDINE DERIVATIVES, INTERMEDIATE COMPOUNDS AND THEIR APPLICATION AS TACHYQUININE ANTAGONISTS

摘要

The compounds and their pharmaceutically acceptable salts are useful as tachyquinine inhibitors which act in NK1, NK2 and NK3 receptors or a combination of two or more of them. They have the formula where A is CO, SO2 or CH2; Ar1 is phenyl, optionally substituted by one or more substituents selected from halogen, C1-6 alkoxy, optionally substituted by one of more halogen, and C1-6 alkyl, optionally substituted with one or more halogen, X1 is C3-7 cycloalkyl, aryl or C1-6 alkyl, the above C1-6 alkyl is, optionally, substituted with fluoro, CO2H, CO2(C1-4 alkyl), C3-7 cycloalkyl, adamamntyl, aryl or het, and the above C3-7 cycloalkyl is, optionally, substituted with one or two substituents each individually selected from C1-4 alkyl, C3-7 cycloalkyl, C1-4 alkoxy, OH, F, fluoro(C1-4 alkyl) and fluoro(C1-4 alkoxy); X is direct bond or NR1; R is SO2 aryl, SO2(C1-6 alkyl), optionally substituted by one or more halogen), (a) or (b). 38 claims