发明名称 N-(1,8-NAPHTHYRIDIN-2-YL)ISOINDOLIN-2-ONES AND N-(1,8- NAPHTHYRIDIN-2-YL) PYRROLO(3,4-B)PYRAZINES
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.
申请公布号 AU8193687(A) 申请公布日期 1988.06.02
申请号 AU19870081936 申请日期 1987.11.30
申请人 RHONE-POULENC SANTE, 发明人 JEAN-DOMINIQUE BOURZAT;MARC CAPET;CLAUDE COTREL;RICHARD LABAUDINIERE;PHILIPPE PITCHEN;GERARD ROUSSEL
分类号 C07D209/46;A61K31/435;A61K31/44;A61K31/4427;A61K31/47;A61P21/02;A61P25/08;A61P25/20;C07D209/48;C07D221/06;C07D401/04;C07D401/14;C07D403/02;C07D471/04;C07D487/04;C07D495/04;C07D497/04;C07D519/00 主分类号 C07D209/46
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