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公开(公告)号：US09221816B2
公开(公告)日：2015-12-29
申请号：US14645033
申请日：2015-03-11
发明人： Daniela Brunner , Jessica Malberg , Bavani G. Shankar , Sabine Kolczewski , Anja Limberg , Eric Prinssen , Claus Riemer , Theodor Stoll
IPC分类号： C07D471/04 , C07D401/12 , C07D403/12 , C07D405/14 , A61K31/506 , A61K31/4439 , A61K31/444 , A61K45/06
CPC分类号： C07D471/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D209/34 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14
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.
摘要翻译： 本发明涉及通式的2-氧代-2,3-二氢 - 吲哚，其中是苯基或杂芳基，其选自吡啶基，嘧啶基，咪唑基，异恶唑基或吡唑基; 是苯基或吡啶基，其中吡啶基中的N原子可以在所有的自由位上; R1是氢，低级烷基，被卤素取代的低级烷基，低级烷氧基或卤素; n为1或2; 如果n为2，则R1可以相同或不相同; R2 / R2'彼此独立地为低级烷基，或与它们所连接的碳原子一起形成C 3-6 - 环烷基环; R3是低级烷基，C3-6-环烷基，CH2-C3-6环烷基，C3-6-环烷基，其中一个环 - 碳原子被-O - ，（CH2）3-O-C3-6-环烷基取代， 被羟基取代的低级烷基，被卤素取代的低级烷基，（CH 2）3 -S（O）2 -C 3-6 - 环烷基或（CH 2）2 -S（O） R4是氢，卤素或低级烷基; m为1或2; 如果m为2，则R4可以相同或不相同; 以及其药学上可接受的盐，与外消旋混合物或其相应的对映异构体和/或其光学异构体和/或立体异构体。
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