The invention relates to 17alpha -(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17beta -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 17alpha -(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.
17-ALPHA-SUBSTITUTED DERIVATIVES OF ESTRADIOL WITH WOUND-HEALING ACTIVITY / G. Ashcroft, M. Brufani, F. Ceccacci, P.M. Farina, L. Filocamo, B. Garofalo, R. Joudioux, A. Maggi, R. Marini Bettolo, M.L. Migneco.
17-ALPHA-SUBSTITUTED DERIVATIVES OF ESTRADIOL WITH WOUND-HEALING ACTIVITY
A. Maggi;
2008
Abstract
The invention relates to 17alpha -(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17beta -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 17alpha -(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.
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