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首页> 外国专利> N-(1,8-NAPHTHYRIDIN-2-YL)ISOINDOLIN-2-ONES AND N-(1,8- NAPHTHYRIDIN-2-YL) PYRROLO(3,4-B)PYRAZINES

N-(1,8-NAPHTHYRIDIN-2-YL)ISOINDOLIN-2-ONES AND N-(1,8- NAPHTHYRIDIN-2-YL) PYRROLO(3,4-B)PYRAZINES

机译：N-（1,8-萘啶-2-基）异吲哚啉-2-酮和N-（1,8-萘啶-2-基）吡咯并（3,4-B）吡嗪

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摘要

Derivatives of formula (I), 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-oxathiinno[1,4][2,3C]pyrrole or 2,3,6,7-tetrahydro-5H- dithiinno[1,4][2,3C]pyrrole nucleus and Het = naphthyridinyl, pyridyl or quinolyl which are unsubstituted or substituted by a halogen, alkyl (1-4 C), alkoxy (1-4 C), alkylthio (1-4 C) or CF3, and R = alkenyl (3- 10 C) with a straight or branched chain or alkyl which is unsubstituted or substituted by alkoxy, alkylthio, cycloalkyl (3-6 C), NH2, alkylamino, dialkylamino, alkylcarbonylamino (in which the amino part is optionally alkyl-substituted), 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 else R = 2- or 3-pyrrolidinyl or 2-,3- or 4-piperidyl, it being understood that the alkyl radicals form a straight or branched chain and, unless specially mentioned, contain 1 to 10 C and that the piperazinyl, piperidino, piperidyl, pyrrolidinyl and azetidinyl radicals may be unsubstituted or substituted in any position by alkyl, alkylcarbonyl, benzyl or hydroxyalkyl or else may form a lactam functional group with the nitrogen atom of the ring, and, when they exist, their pharmaceutically acceptable salts and the optical isomers of the products of formula (I). IMAGE The products of formula (I) are useful as anxiolytics.
机译：式（I）的衍生物，其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6,7-四氢-5H-氧杂噻吩并[ 1,4] [2,3C]吡咯或2,3,6,7-四氢-5H-二噻吩并[1,4] [2,3C]吡咯核，Het =未取代或取代的萘啶基，吡啶基或喹啉基卤素，烷基（1-4 C），烷氧基（1-4 C），烷硫基（1-4 C）或CF3，R =带有直链或支链的烯基（3-10 C）或未取代的烷基或被烷氧基，烷硫基，环烷基（3-6 C），NH 2，烷基氨基，二烷基氨基，烷基羰基氨基（其中氨基部分任选被烷基取代），1-或2-哌嗪基，哌啶基，哌啶子基，吗啉代，吡咯烷基， 1-氮杂环丁烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，（1-吡咯烷基）羰基，苯基，吡啶基，1-咪唑基，或者R ＝ 2-或3-吡咯烷基或2-，3-或4-哌啶基，应理解为烷基形成直链或除非另外提及，否则含有1至10 C且哌嗪基，哌啶子基，哌啶基，吡咯烷基和氮杂环丁烷基基团可以未被取代或在任何位置被烷基，烷基羰基，苄基或羟烷基取代，或者可以形成内酰胺官能团基团具有环的氮原子，以及当它们存在时，它们的药学上可接受的盐和式（I）产物的旋光异构体。 <图像>式（I）的产物可用作抗焦虑药。

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