申请人:Ashcroft Gillian
公开号:US20100035796A1
公开(公告)日:2010-02-11
The invention relates to 17α-(5-hydroxy-C
5
-hydrocarbyl)-1,3,5(10)-estratrien-3,17β-diol derivatives having cicatrising activity, preferably for topical use on wounds, without significant systemic effects, and to pharmaceutical compositions containing them. In particular, the invention relates to estradiol 17α-(5-hydroxypentyn-1-yl)derivatives and 3-esters, 5′-esters and 3,5′-diesters thereof and to a process for the preparation thereof by reaction of 3-OR-protected estrone with an alkali metal derivative of OR-protected 5-pentynol, followed by 3-, 5-′ or 3,5′-esterification.
该发明涉及具有愈合活性的17α-(5-羟基-C5-烷基)-1,3,5(10)-雌三烯-3,17β-二醇衍生物,优选用于局部用于伤口,不产生显著的全身作用,并且含有它们的药物组合物。具体而言,该发明涉及雌二醇17α-(5-羟基戊炔基)衍生物和其3-酯、5'-酯和3,5'-二酯,以及通过将3-OR保护的雌酮与5-戊炔醇的OR保护的碱金属衍生物反应,然后进行3-、5'-或3,5'-酯化制备它们的方法。