| 摘要 |
The present invention relates to a compound of formula (I), wherein R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, benzyl, -C(0)-lower alkyl, -C(0)-CH2-lower alkoxy, -C(0)-C3-6-cycloalkyl, -(CH2)°-C(0)-NR,R', -(CH2)°S(0)2- lower alkyl or -S(0)2-NR,R'; o is 0 or 1; R,R' are independently from each other hydrogen or lower alkyl, or may form together with the N atom to which they are attached a 5 or 6 membered heterocycloalkyl ring; R2 is hydrogen or lower alkyl; R3 is halogen, lower alkoxy, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; and may be the same or different in case n is 2; n is 1 or 2; Ar is phenyl optionally substituted by one or two substituents selected from lower alkyl, halogen, lower alkoxy, lower alkyl substituted by hydroxy or cyano, or is a five or six membered heteroaryl group, selected from thiophenyl or pyridinyl which are optionally substituted by lower alkyl or halogen; or to a pharmaceutically active acid addition salt. It has surprisingly been found that the compounds of formula I show a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
|
