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1. 发明公开

EP0064040A1 Therapeutically active disulphide compounds and their use 失效
标题翻译： Therapeutisch aktive Disulfidverbindungen und ihre Verwendung。
公开(公告)号：EP0064040A1
公开(公告)日：1982-11-03
申请号：EP82850071.0
申请日：1982-04-05
申请人： PHARMACIA AKTIEBOLAG
发明人： Carlsson, Jan Per Erik , Axen, Rolf Erik Axel Verner
IPC分类号： C07H15/24 , C07D499/50 , A61K31/43 , A61K31/70
CPC分类号： C07D213/71 , C07D213/89 , C07D277/78 , C07D499/00 , C07H15/252
摘要： Therapeutically active organic compound exhibiting at least one group comprising a structure -S'-S"-R, wherein the group -S"-R is defined by R being an organic group comprised in a physiologically acceptable compound H-S"-R obtainable by the splitting of the disulfide bridge -S'-S"- in said structure, in which compound H-S"-R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H-S"-R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure -S'-S"-R, consisting of a residue of a therapeutically active organic base compound of non-poly-peptide structure bound to S'.
The invention also relates to a method of modifying a therapeutically active organic compound of non-polypeptide structure by introducing a structure -S'-S"-R according to above; a method of treating diseases by administration of a compound according to the invention and also to a pharmaceutical composition containing at least one compound according to the invention.
摘要翻译：表现出至少一个包含结构-Smin -Ssec -R的基团的治疗活性有机化合物，其中基团-Ssec -R由R是由生理学上可接受的化合物HS sec -R中包含的有机基团所述结构中的二硫键-Smin -Ssec的分解，其中化合物HSsec-R硫原子S sec与R中的杂环芳环中的碳原子结合，其结构使得化合物HS 秒-R，同时保持生理可接受性，通过互变异构或包含与R结合的硫原子的共振的共振来稳定，以便主要排除在涉及硫醇二硫化物交换的反应之外; S min与脂肪族碳原子结合; 和所述化合物，除了包含结构-Smin -Ssec-R的基团或基团，由与S min结合的非多肽结构的治疗活性有机碱性化合物的残基组成。本发明还涉及通过引入上述结构-Smin -Ssec -R来修饰非多肽结构的治疗活性有机化合物的方法; 通过施用根据本发明的化合物治疗疾病的方法，还涉及含有至少一种本发明化合物的药物组合物。

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