发明名称 PYRROLIDINE DERIVATIVES AS NK3 ANTAGONISTS
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).
申请公布号 CA2821640(A1) 申请公布日期 2012.07.12
申请号 CA20122821640 申请日期 2012.01.03
申请人 F. HOFFMANN-LA ROCHE AG 发明人 KNUST, HENNER;NETTEKOVEN, MATTHIAS;RATNI, HASANE;VIFIAN, WALTER
分类号 C07D401/06;A61K31/4025;A61P25/00;C07D401/14;C07D403/06;C07D413/10 主分类号 C07D401/06
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