3-PHENYLPYRIDINE DERIVATIVES AND THEIR USE AS NK-1 RECEPTOR ANTAGONISTS

摘要

The invention relates to compounds of formula (I) 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> is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R<3> is hydrogen, lower alkyl or form a cycloalkyl group; R<4> is hydrogen, -N(R<5>)2, -N(R<5>)S(O)2-lower alkyl, -N(R<5>)C(O)R<5> or a cyclic tertiary amine of the group (a); R<5> is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R<6> is hydrogen, hydroxy, lower alkyl, -N(R<5>)CO-lower alkyl, hydroxy-lower alkyl, cyano, -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. It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor.