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1. 发明授权

US5219861A 6 .beta.-Thiomorphine derivatives 失效
标题翻译： 6β-吗啡衍生物
公开(公告)号：US5219861A
公开(公告)日：1993-06-15
申请号：US712760
申请日：1991-06-10
申请人： Ken Kanematsu , Issei Takayanagi , Mitsutaka Yoshida
发明人： Ken Kanematsu , Issei Takayanagi , Mitsutaka Yoshida
IPC分类号： C07D489/00
CPC分类号： C07D489/00
摘要： A novel morphine derivative represented by the following general formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group;R.sub.2 represents a hydrogen atom, a lower alkylthio group, an aryl group, a lower alkoxycarbonylalkyl group, a lower alkyl group or a lower alkanoyl group;R.sub.3 represents a lower cycloalkylmethyl group or an allyl group,and a pharmaceutically acceptable acid addition salt thereof. The compound of the above general formula shows an analgesic activity 5 or more times as high as that of morphine and a narcotic antagonist action. Further, it exhibits an extremely low drug dependence. These properties make it highly useful as an active ingredient of drugs such as analgesics or anesthetics.
摘要翻译：由以下通式表示的新颖的吗啡衍生物：其中R 1表示氢原子，低级烷基或低级烷酰基; R2表示氢原子，低级烷硫基，芳基，低级烷氧基羰基烷基，低级烷基或低级烷酰基; R3表示低级环烷基甲基或烯丙基，及其药学上可接受的酸加成盐。上述通式的化合物显示5倍或更多倍于吗啡和麻醉拮抗作用的镇痛活性。此外，它表现出极低的药物依赖性。这些性质使其作为药物如止痛剂或麻醉剂的活性成分非常有用。

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