The invention relates to 17a-(5-hydroxy-Cs-hydrocarbyl)-1,3,5 (10)-estratrien-3,1 7 ~-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-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 / Ashcroft, G., Brufani, M., Ceccacci, F., Farina, P.M., Filocamo, L., Garofalo, B., Joudioux, R., Maggi, A., Marini Bettolo, R., Migneco, L.M.. - (2006).
17-alpha-substituted derivatives of estradiol with wound-healing activity
Brufani, Mario;Ceccacci, Francesca;Filocamo, Luigi;Marini Bettolo, Rinaldo;Migneco, Luisa Maria
2006
Abstract
The invention relates to 17a-(5-hydroxy-Cs-hydrocarbyl)-1,3,5 (10)-estratrien-3,1 7 ~-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-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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
