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DERIVES DE PYRROLIDINE EN TANT QU'ANTAGONISTES DE NK3
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
KNUST, HENNER,NETTEKOVEN, MATTHIAS,RATNI, HASANE,VIFIAN, WALTER
申请号:
CA2821640
公开号:
CA2821640A1
申请日:
2012.01.03
申请国别(地区):
CA
年份:
2012
代理人:
摘要:
The invention relates to compounds of formula (I) wherein R1 is (A), or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by cyano, lower alkyl, halogen-substituted phenyl, lower alkyl-substituted [1,2,4]oxadiazol-3-yl or by 2-oxo-piperidin-1-yl; X is NR or O; R is C(O)-lower alkyl, -C(O)-cycloalkyl substituted by lower alkyl, cycloalkyl or is phenyl, pyridinyl or pyridazinyl, wherein phenyl, pyridinyl and pyridazinyl may optionally be substituted by lower alkyl, lower alkoxy, cyano, -C(O)-lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, halogen, cyano, lower alkyl or lower alkyl substituted by halogen; R4 is hydrogen or lower alkyl; wherein R2 and R4 are not simultaneously hydrogen or lower alkyl; R5 is lower alkyl; R6 halogen, hydroxy, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, S(O)2-lower alkyl or cyano; or to a pharmaceutically suitable acid addition salt 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).
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