申请人:Rhone-Poulenc Sante
公开号:US05102890A1
公开(公告)日:1992-04-07
This invention relates to pyrrole derivatives of formula: ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system and Hetis naphthyridinyl, pyridyl or quinolyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3 and R=(3 to 10 C) straight- or branched-chain alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, (in which the amino portion is optionally substituted with alkyl), 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, pyrrolidinyl, 1-azetidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, (1-pyrrolidinyl)carbonyl, phenyl, pyridyl, 1-imidazolyl, or alternatively R=2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl, on the understanding that the alkyl radicals are straight- or branched-chain radicals and contain, except where specifically stated, 1 to 10 C, and that the piperazinyl, piperidino, piperidyl, pyrrolidinyl and azetidinyl radicals can be unsubstituted or substituted at any position with alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and, where they exist, their pharmaceutically acceptable salts and optical isomers, are useful as anxiolytics.
这项发明涉及以下化学式的吡咯衍生物:##STR1## 其中A与吡咯环形成异吲哚、6,7-二氢-5H-吡咯并[3,4-b]吡嗪、2,3,6,7-四氢-5H-[1,4]噁硫氮[2,3-c]吡咯或2,3,6,7-四氢-5H-[1,4]二硫氮[2,3-c]吡咯环系统,Het为萘啉基、吡啉基或喹啉基,未取代或取代有卤素、(1至4碳)烷基、(1至4碳)烷氧基、(1至4碳)烷硫基或CF.sub.3,R=(3至10碳)直链或支链烯基或烷基,未取代或取代有烷氧基、烷硫基、(3至6碳)环烷基、NH.sub.2、烷基氨基、二烷基氨基、烷基羰基氨基(其中氨基部分可选择性地取代烷基)、1-或2-哌嗪基、哌啶基、哌啶基、吗啉基、吡咯啉基、1-氮杂环丙基、氨甲酰基、烷基氨甲酰基、二烷基氨甲酰基、(1-哌嗪基)羰基、哌啶羰基、(1-吡咯啉基)羰基、苯基、吡啉基、1-咪唑基,或者R=2-或3-吡咯啉基、2-、3-或4-哌啶基,其中烷基基团为直链或支链基团,除非特别说明,含有1至10碳,哌嗪基、哌啶基、哌啶基、吡咯啉基和氮杂环丙基基团可以未取代或在任何位置取代烷基、烷基羰基、苄基或羟基烷基,或者可以与环的氮原子形成内酰胺基团,存在时,它们的药学上可接受的盐和光学异构体,可用作抗焦虑药物。