17-ALPHA-SUBSTITUTED DERIVATIVES OF ESTRADIOL WITH WOUND-HEALING ACTIVITY

摘要

The invention relates to 17a-(5-hydroxy-C₅-hydrocarbyl)-l,3,5(10)-estratrien-3,17ß-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 17a-(5-hydroxypentyn-l-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'-esterifÊcation.