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    • 7. 发明授权
    • Oxabicycloheptane derivatives
    • 氧杂双环庚烷衍生物
    • US4713453A
    • 1987-12-15
    • US19973
    • 1987-02-27
    • Toshio TatsuokaKenji SuzukiKayoko ImaoFumio SatohSeiji MiyanoKunihiro Sumoto
    • Toshio TatsuokaKenji SuzukiKayoko ImaoFumio SatohSeiji MiyanoKunihiro Sumoto
    • C07D333/00A61K31/00A61K31/35A61K31/352A61K31/40A61K31/4025A61K31/435A61K31/443A61K31/4433A61K31/445A61K31/495A61K31/535A61K31/54A61P9/00A61P25/18A61P25/28C07D311/94C07D405/04C07D405/12C07D407/04C07D409/04C07D487/04C07D417/00C07D401/00C07D405/00C07D413/00
    • C07D405/04C07D311/94C07D405/12C07D409/04C07D487/04
    • The present invention relates to a novel oxabicycloheptane derivative of the following formula and a pharmaceutically acceptable salt thereof: ##STR1## where D is a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group, an arylalkoxy group, an acyloxy group, a dialkylcarbamoyloxy group or an amidoalkyloxy group; B is a substituted or unsubstituted phenyl, thienyl or furyl group; A is the group ##STR2## (where l is 0 or 1; m and n are each 1 or more, provided that m+n is an interger of 2-8; R.sup.1 is an alkylamino group, a dialkylamino group, an arylalkylamino group, a morpholino group, a thiomorpholino group, a 1-pyrrolidinyl group, a piperidino group, an N-alkylpiperazinyl group, an N-hydroxyalkylpiperazinyl or a pyrrolizidinyl group; and R.sup.2 is a lower alkyl group or a hydroxl group), or the group ##STR3## (where l, m, n, R.sup.1 and R.sup.2 are each the same as defined above), or the group ##STR4## (where R.sup.3 and R.sup.4 which may be the same or different each represents a hydrogen atom, a lower alkyl group, an alkoxycarbonyl group or an acyl group), or the group ##STR5## (where m, l, n, R.sup.1 and R.sup.2 are each the same as defined above). The oxabicycloheptane derivative having the formula defined above and pharmaceutically acceptable salts thereof are effective in ameliorating or eliminating the symptoms that appear either as a result of organic disorders in the brain or on account of pathergasia. These compouds also have antidepressant effects and the useful as psychopharmaceuticals.
    • 本发明涉及下式的新型氧杂双环庚烷衍生物及其药学上可接受的盐:其中D是氢原子,卤素原子,羟基,烷氧基,芳基烷氧基,酰氧基, 二烷基氨基甲酰氧基或酰氨基烷氧基; B是取代或未取代的苯基,噻吩基或呋喃基; A是组(其中l是0或1; m和n各自为1或更多,条件是m + n是2-8的整数; R1是烷基氨基,二烷基氨基,芳基烷基氨基 吗啉基,硫代吗啉基,1-吡咯烷基,哌啶子基,N-烷基哌嗪基,N-羟基烷基哌嗪基或吡咯烷基; R2为低级烷基或羟基),或该基团 < IMAGE>(其中l,m,n,R 1和R 2各自与上述相同)或基团(其中可以相同或不同的R 3和R 4各自表示氢原子,低级烷基 基团,烷氧基羰基或酰基)或基团(其中m,l,n,R 1和R 2各自与上述定义相同)。 具有上述定义的式的氧杂双环庚烷衍生物及其药学上可接受的盐在改善或消除由于脑中有机疾病或由于麻醉引起的症状而有效。 这些药物也具有抗抑郁作用,作为心理药物有用。