| 摘要 |
The invention provides compounds of the formulawhereinR1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R1 and R2 may together be -CH=CH-CH=CH-, wherein R1 and R2 together with the two carbon ring atoms to which they are attached form a fused ring; R3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4' are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, -(CH2)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(R4'')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; andn 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 used for the treatment of diseases related to this receptor. |
