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1. 发明授权

US4045570A Heterocyclic S-imino-S-oxides 失效
标题翻译：杂环S-亚氨基-S-氧化物
公开(公告)号：US4045570A
公开(公告)日：1977-08-30
申请号：US575319
申请日：1975-05-07
申请人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
发明人： Gunther Dorhofer , Roland Heckendorn , Erich Schmid , Angelo Storni , Armin Zust
IPC分类号： C07D337/14 , C07D495/04
CPC分类号： C07D495/04 , C07D337/14
摘要： The invention relates to new heterocyclic S-imino-S-oxides of the formula I ##STR1## in which one of the symbols X.sub.1 and X.sub.2 denotes a direct bond and the other denotes the vinylene group --CH=CH-- or the epithio radical --S--, Y.sub.1 and Y.sub.2 conjointly denote an additional bond or one of the symbols denotes hydrogen and the other denotes hydrogen or, conjointly with the symbol R.sub.1 or R.sub.2, which is present on the same carbon atom, denotes the oxo radical, one of the symbols R.sub.1 and R.sub.2 denotes hydrogen or lower alkyl and the other denotes hydrogen or lower alkyl or, conjointly with the symbol Y.sub.1 or Y.sub.2, which is present on the same carbon atom, denotes the oxo radical, or, if Y.sub.1 and Y.sub.2 conjointly denote an additional bond, also denotes lower alkoxy, and R.sub.3 and R.sub.4 independently of one another denote hydrogen, halogen up to atomic number 35, lower alkyl, lower alkoxy or trifluoromethyl and R.sub.5 denotes hydrogen or lower alkyl, and to their acid addition salts in particular the pharmaceutically with inorganic and organic acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anticonvulsive activity and are useful for the treatment of epilepsy and of states of tension and states of agitation.
摘要翻译：本发明涉及式I（I）的新的杂环S-亚氨基-S-氧化物，其中符号X1和X2之一表示直接键，而另一个表示亚乙烯基-CH = CH-或环氧基-S-，Y1和Y2共同表示另外的键，或者一个符号表示氢，另一个表示氢，或与存在于同一碳原子上的符号R 1或R 2结合表示氧代基，符号R1和R2中的一个表示氢或低级烷基，另一个表示氢或低级烷基，或与存在于同一碳原子上的符号Y1或Y2结合表示氧代基，或者如果Y1和Y2 并且表示低级烷氧基，R3和R4彼此独立地表示氢，卤素直至原子数为35，低级烷基，低级烷氧基或三氟甲基，R5表示氢或低级烷基，并且表示其酸加成盐特别是药物中含有的有机和有机可接受的酸加成盐。这些新化合物具有宝贵的药理学特性。特别是它们具有抗惊厥活性，并且可用于治疗癫痫和张力状态和搅动状态。

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