4-Phenylpyridinderivate und deren Verwendung als NK-1 Rezeptorantagonisten

摘要

The present invention relates to compounds of the general formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R<1> is hydrogen or halogen; or R and R<1> may be together -CH=CH-CH=CH-; R<2> and R<2'> are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R<2> and R<2'> may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R<3> is hydrogen, lower alkyl or form a cycloalkyl group; R<4> is hydrogen, -N(R<5>)2, -N(R<5>)(CH2)nOH, -N(R<5>)S(O)2-lower alkyl, -N(R<5>)S(O)2-phenyl, -N=CH-N(R<5>)2, -N(R<5>)C(O)R<5> or a cyclic tertiary amine of the group R<5> is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R<6> is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R<5>)CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R<5>)-, -(CH2)mO-, -(CH2)mN(R<5>)-, -N(R<5>)C(O)-, or -N(R<5>)(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.