17-alpha-substituted derivatives of estradiol with wound-healing activity

US8357675B2 · kind B2 · utility

Assignee

• EUTICALS SPA · IT

Inventors

• Gillian Ashcroft · Manchester, GB
• Mario Brufani · Roma, IT
• Francesca Ceccacci · Roma, IT
• Paolo Farina · Milano, IT
• Luigi Filocamo · Roma, IT
• Barbara Garofalo · Roma, IT
• Roberta Joudioux · Roma, IT
• Adriana Maggi · Milano, IT
• Rinaldo Marini Bettolo · Roma, IT
• Luisa Maria Migneco · Roma, IT

Key dates

• Filing date: Jul 28, 2006
• Grant date: Jan 22, 2013
• Expiry date: Jun 1, 2028

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07J1/0096
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to 17α-(5-hydroxy-C5-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′-esterifÊcation.