KNUST HENNER,LIMBERG ANJA,NETTEKOVEN MATTHIAS,RATNI HASANE,RIENER CLAUS,VIFIAN WALTER
申请号：
IN3214/CHENP/2011
公开号：
IN2011CN03214A
申请日:
2011.05.10
申请国别(地区):
IN
年份:
2012
代理人:
摘要：
The present invention relates to a compounds of formula I wherein R1 is hydroxy or NR"R" R" and R" are independently from each other hydrogen, lower alkyl, cycloalkyl, or may form together with the N-atom to which they are attached a heteroalkyl ring R2 is hydrogen, lower alkyl, lower alkoxy, halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano or S(O)2-lower 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-heteroaryl, wherein the rings may be substituted by one or more substituents, selected from halogen, lower alkyl, lower alkyl substituted by halogen, cyano, hydroxy, NR"R" or by lower alkoxy substituted by halogen, or are -(CR2)m-cycloalkyl, optionally substituted 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).
