发明名称 2-oxo-2,3-dihydro-indoles for the treatment of CNS disorders
摘要 The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula; wherein ; is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; ; is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not;R2/R2′ are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring;R3 is lower alkyl, C3-6-cycloalkyl, CH2—C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by —O—, (CH2)3—O—C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3—S(O)2—C3-6-cycloalkyl or (CH2)2—S(O)2-lower alkyl;R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
申请公布号 US9221816(B2) 申请公布日期 2015.12.29
申请号 US201514645033 申请日期 2015.03.11
申请人 Hoffmann La-Roche Inc. 发明人 Brunner Daniela;Malberg Jessica;Shankar Bavani G.;Kolczewski Sabine;Limberg Anja;Prinssen Eric;Riemer Claus;Stoll Theodor
分类号 C07D471/04;C07D401/12;C07D403/12;C07D405/14;A61K31/506;A61K31/4439;A61K31/444;A61K45/06 主分类号 C07D471/04
代理机构 代理人 Buckwalter Brian
主权项 1. A compound of formulawhereinis phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl;is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not; R2/R2′ are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring; R3 is lower alkyl, C3-6-cycloalkyl, CH2—C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by —O—, (CH2)3—O—C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3—S(O)2—C3-6-cycloalkyl or (CH2)2—S(O)2-lower alkyl; R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not;as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
地址 Little Falls NJ US