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    • 3. 发明授权
    • 6,8-dimercaptooctanoic acid derivatives substituted at the 6-S and/or
8-S position with the (3-methylthiopropanoyl) radical and
pharmaceutical compositions intended for the treatment of cancerous
tumors
    • 在6-S和/或8-S位置用(3-甲硫基丙酰基)基取代的6,8-二巯基辛酸衍生物和用于治疗癌性肿瘤的药物组合物
    • US6117902A
    • 2000-09-12
    • US281654
    • 1999-03-30
    • Gerard Anthony QuashJacques GoreGuy Fournet
    • Gerard Anthony QuashJacques GoreGuy Fournet
    • C07D295/18A61K31/00A61K31/20A61K31/23A61K31/495A61P35/00A61P43/00C07C327/32C07D295/185A61K31/225C07C327/04C07C327/18
    • C07D295/185C07C327/32
    • The present invention provides 6,8-Dimercaptooctanoic acid derivatives substituted at the 6-S and/or 8-S position with the (3-methylthiopropanoyl) radical, wherein they correspond to the following formula (I): ##STR1## in which: R represents OR.sub.3 or ##STR2## R.sub.3 representing a hydrogen atom, a linear or branched alkyl radical, or a radical of the formula ##STR3## n being an integer from 1 to 10 and r' and r", which are identical or different, representing a hydrogen atom, a linear or branched alkyl radical or, taken together, form with the nitrogen atom, a nitrogen-containing heterocycle optionally substituted with an optionally substituted oxygen or nitrogen atom,R.sub.5 and R.sub.4, identical or different, represent a hydrogen atom or a linear or branched alkyl radical,R.sub.1 and R.sub.2, which are identical or different, represent a hydrogen atom, a radical --COCH.sub.3 or a radical of formula:--CO(CH.sub.2).sub.2 SCH.sub.3 (II)with the proviso that at least one of the radicals R.sub.1 or R.sub.2 represents a radical of formula (II) and the R and S enantiomers and their racemate as well as the salts of the said compounds of formula (I). The present invention also provides pharmaceutical compositions, and method of treatment and prevention of cancerous tumours.
    • 本发明提供在6-S和/或8-S位置与(3-甲硫基丙酰基)基取代的6,8-二巯基辛酸衍生物,其中它们对应于下式(I):其中:R表示OR 3 或R3表示氢原子,直链或支链烷基或式n的基团为1至10的整数,r'和r“可相同或不同,表示氢原子,直链或支链烷基 支链烷基或与氮原子一起形成,任选被任选取代的氧或氮原子取代的含氮杂环,相同或不同的R 5和R 4表示氢原子或直链或支链烷基, R 1和R 2相同或不同,表示氢原子,基团-COCH 3或式-CO-CH(CH 2)2 SCH 3(II)的基团,条件是基团R 1或R 2中的至少一个表示基团 的式(II)和R和S对映异构体 和它们的外消旋物以及所述式(I)化合物的盐。 本发明还提供药物组合物以及治疗和预防癌性肿瘤的方法。