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1. 发明授权

US4367239A Nitrosourea derivatives, pharmaceutical compositions thereof and method of preparation 失效
标题翻译：亚硝基脲衍生物，其药物组合物及其制备方法
公开(公告)号：US4367239A
公开(公告)日：1983-01-04
申请号：US191910
申请日：1980-09-29
申请人： Peter Bregnedal , Jorn Buus
发明人： Peter Bregnedal , Jorn Buus
IPC分类号： C07C275/68 , C07C127/17 , A61K31/17
CPC分类号： C07C275/68
摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。本发明的新化合物可以由下式表示：其中X和Y相同或不同，并且选自苯基和环己基，所述苯基和环己基任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代，一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

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