4-Phenyl-pyridine derivatives

摘要

Compounds of the general formula
wherein
R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl;
R1 is hydrogen or halogen; or
R and R1 may be together -CH=CH-CH=CH-;
R2 and R2' are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or
R2 and R2' may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy;
R3 is hydrogen, lower alkyl or form a cycloalkyl group;
R4 is hydrogen, -N(R5)2, -N(R5)(CH2)nOH, -N(R5)S(O)2-lower alkyl, -N(R5)S(O)2-phenyl, -N=CH-N(R5)2, -N(R5)C(O)R5 or a cyclic tertiary amine of the group
R5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl;
R6 is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH Þ )nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group,
X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-;
n is 0 - 4; and
m is 1 or 2;
and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases, which relate to NK-1 receptor antagonists.