4-PHENYL-PYRIMIDINE DERIVATIVES

摘要

The invention relates to compounds of formula (I) wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R?1 and R2¿ may be together with the two carbon atoms -CH=CH-CH=CH-; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4' are independently from each other hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, -(CH¿2?)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, -(CH2)n-morpholinyl, -(CH2)n-piperidinyl, -(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, -NH-(CH2)n+1N(R?4')¿2, -(CH2)n+1N(R4')2, -O-(CH2)n+1-morpholinyl, -O-(CH2)n+1-piperidinyl or -O-(CH2)n+1N(R4')2, wherein R4' is hydrogen or lower alkyl; and n is 0 - 2; X is -C(O)N(R4')- or -N(R4')C(O)-; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore be used for the treatment of diseases related to this receptor.