申请人:Richter Gedeon Vegyeszeti Gyar Rt.
公开号:US05157038A1
公开(公告)日:1992-10-20
The invention relates to novel 2-oxo-1-oxa-8-azaspiro[4,5]decane derivatives of the formula (I), ##STR1## wherein X means oxygen or an >NR group, wherein R stands for hydrogen; a C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.1-4 alkyl group, the two latter two substituents optionally substituted on their aromatic moiety by one or more, same or different halogen, one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trihalomethyl group; or a tosyl group; R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group wherein R is as defined above, one of R.sup.1 and R.sup.2 m may represent a hydroxyl group and the other one is a methyl group; and R.sup.3 means hydrogen, benzyl, (C.sub.1-4 alkoxy)carbonyl, phenoxycarbonyl, benzyloxycarbonyl, formyl, piperidin-1-ylcarbonyl, morpholin-4-ylcarbonyl, 4-methylpiperazin-1-ylcarbonyl, 4-(2-hydroxethyl)piperazin-1-ylcarbonyl, 2-chloro-3-nicotinoylcarbamoyl or C.sub.1-6 alkylcarbamoyl group, as well as their acid addition and quaternary ammonium salts.
本发明涉及一种新型2-氧代-1-氧杂-8-氮杂螺[4,5]癸烷衍生物,其化学式为(I):##STR1## 其中,X代表氧或一个>NR基团,其中R代表氢;C.sub.1-12烷基;C.sub.3-6环烷基;碳环C.sub.6-10芳基或碳环C.sub.6-10芳基-C.sub.1-4烷基,后两个取代基在其芳香基上可以选择一个或多个,相同或不同的卤素,一个或多个C.sub.1-4烷基,C.sub.1-4烷氧基或三卤甲基基团;或对甲苯磺酰基;R.sup.1和R.sup.2一起代表一个亚甲基基团或当X代表>NR基团且R如上定义时,R.sup.1和R.sup.2中的一个可以代表一个羟基,另一个是甲基;R.sup.3代表氢,苄基,(C.sub.1-4烷氧基)羰基,苯氧羰基,苄氧羰基,甲酰基,哌啶-1-基羰基,吗啉-4-基羰基,4-甲基哌嗪-1-基羰基,4-(2-羟乙基)哌嗪-1-基羰基,2-氯-3-烟酰胺基甲酰基或C.sub.1-6烷基甲酰基团,以及它们的酸加合物和季铵盐。