| 摘要 |
The present invention relates to a compounds of formula I wherein R1 is hydroxy or NR'R"; R' and R" are indepen-dently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a het-eroalkyl ring; R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O)2-Iower alkyl; R3 is lower alkyl, -(CH2)m-aryl, optionally substituted by halogen, or is -(CH2)m-cycloalkyl; R4 and R5 are independently from each other hydrogen or lower alkyl substituted by halogen, or are -(CR2)m-aryl or -(CR2)m-het-eroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substi-tuted by halogen, cyano, hydroxy, NR'R" or by lower alkoxy substituted by halogen, or are -(CR2)m-cycloalkyl, optionally substi-tuted by hydroxy or by aryl, or are a heteroalkyl ring, optionally substituted by =O or -(CR2)m-aryl, or R4 and R5 are together with the N-atom to which they are attached a heterocyclic ring system, optionally substituted by lower alkyl, aryl or halogen-substituted aryl, and R may be independently from each other hydrogen, lower alkyl or lower alkyl substituted by hydroxyl; n is 1 or 2; m is 0, 1 or 2; or to a pharmaceutically active salt, a racemic mixture, an enantiomer, an optical isomer or a tautomeric form thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD). |
