PIPERIDINE DERIVATIVES AS NK1 AND NK3 ANTAGONISTS.

摘要

The invention relates to compounds according to formula I exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising, same and a method of treatment for neurokinin-mediated conditions. Formula (I) or a pharmaceutically acceptable salt or solvate thereof wherein: m,=0 or 1; n =0 or 1; s=0 or 1; L is -O- or -N(R4 )-; R1 and R2 are each independently H, aryl, heteroaryl, -(C1-C6)atkylheterocyloalkyl, -(C1-C6)alkylheterocycloalkyl, -(C1-C6)alkylheteroaryl, -(C1-C6)alkyl-O-aryl, -(C1- C6)alkylaryl, and -CH2 N(R4)(R5), wherein each of said heterocyloalkyl, -(C1-C6)alkylheterocycloalkyl, -(C1-C6)alkylheteroaryl, -(C1-C6)alkyl-0-aryl, aryl, -(C1-C6)alkylaryl, heteroaryl, and -CH2N(R4)(R5), is optionally substituted with 1-3 moieties independently selected from X', Y' or Z'; R3 is H, CF3, OH, or-(C1-C6)alkyl; R4, and R5, are each independently selected from H, -(C1-C6)alkyl, or -(C1-C6)(C=0)R7; R7 is (C1-C6)alkyl, OH, -N(R4)(R), or -OR4; R8 and R9 are each independently (C1-C6)alkyl; X, Y, X', Y' and Z' are each independently selected from H, -(C1-C6)alkyl, -(C1-C6)alkyl-NR 4R5, CF3, OH, -O-(C1-C6)alkyl, -(C1-C6)alkyl-C(=0)R7, aryl, heteroaryl, cycloalkyl, -N02, -(C1-C6)alkylaryl, -0-aryl, halogen, CN, -CH3N(R4)(R5), -C(=O)R7, -C(=O)R7, -R6C(=0)R7 or -R6C(=O)NR4R5; and R6 is a bond, -CH2-, -0-, or -NR4-.