Piperidine derivatives as nk1 and nk3 antagonists

Details Piperidine derivatives as nk1 and nk3 antagonists Piperidine derivatives as nk1 and nk3 antagonists

C - Chemistry, Metallurgy

07

D

C07D 211/46 (2006.01) A61K 31/4468 (2006.01) A61K 31/45 (2006.01) C07D 211/36 (2006.01)

Patent

CA 2565953

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~.

La présente invention concerne des composés de formule (I), ou un sel ou solvate de ceux-ci, acceptable d'un point de vue pharmaceutique, ayant des propriétés d'inhibition de la neurokinine, une composition pharmaceutique les comprenant, et un procédé pour traiter des états pathologiques liés à la neurokinine. Dans la formule (I): m=0 ou 1; n =0 ou 1; s=0 ou 1; L est -O- ou -N(R?4¿ )-; R?1¿ et R?2¿ sont chacun indépendamment H, aryle, hétéroaryle, (C?1¿-C?6¿)alkyle, hétérocycloalkyle, (C¿1?-C¿6?) alkylhétérocycloalkyle, (C¿1-?C¿6?)alkylhétéroaryle, (C¿1-?C¿6?)alkyl-O-aryle, (C¿1- ?C¿6?)alkylaryle, et -CH¿2 ?N(R?4¿)(R?5¿), chacun des éléments hétérocycloalkyle, (C¿1?-C¿6?) alkylhétérocycloalkyle, (C¿1-?C¿6?)alkylhétéroaryle, (C¿1-?C¿6?)alkyl-O-aryle, (C¿1- ?C¿6?)alkylaryle, hétéroaryle et -CH¿2 ?N(R?4¿)(R?5¿) étant éventuellement substitué avec 1-3 fractions choisies indépendamment entre X', Y' ou Z'; R?3¿ est H, CF¿3?, OH, ou-(C¿1-?C¿6?)alkyle; R?4¿ et R?5¿ sont chacun indépendamment choisis entre H, -(C¿1-?C¿6?)alkyle, ou -(C¿1-?C¿6?)(C=O)R?7¿; R?7¿ est (C¿1-?C¿6?)alkyle, OH, -N(R?4¿)(R?5¿), ou -OR?4¿; R?8¿ et R?9¿ sont chacun indépendamment (C¿1-?C¿6?)alkyle; X, Y, X', Y' et Z' sont chacun choisis indépendamment entre H, -(C¿1-?C¿6?)alkyle, -(C¿1-?C¿6?)alkyl-NR?4¿R?5¿,? ¿CF¿3?, OH, -O-(C¿1-?C¿6?)alkyle, -(C¿1-?C¿6?)alkyl-C(=O)R?7¿, aryle, hétéroaryle, cycloalkyle, -NO¿2?, -(C¿1-?C¿6?)alkylaryle, -O-aryle, halogène, CN, -CH¿3?N(R?4¿)(R?5¿), -C(=O)R?7¿, -C(=O)R?7¿, -R?6¿C(=O)R?7¿ ou -R?6¿C(=O)NR?4¿R?5¿; et R?6¿ est une liaison, -CH¿2?-, -O-, ou -NR?4¿-.

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