发明授权
US08357675B2 17-alpha-substituted derivatives of estradiol with wound-healing activity
有权
17-α-取代的雌二醇衍生物具有伤口愈合活性
- 专利标题： 17-alpha-substituted derivatives of estradiol with wound-healing activity
- 专利标题（中）： 17-α-取代的雌二醇衍生物具有伤口愈合活性
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申请号： US11989807申请日： 2006-07-28
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公开(公告)号： US08357675B2公开(公告)日： 2013-01-22
- 发明人: Gillian Ashcroft , Mario Brufani , Francesca Ceccacci , Paolo Maria Farina , Luigi Filocamo , Barbara Garofalo , Roberta Joudioux , Adriana Maggi , Rinaldo Marini Bettolo , Luisa Maria Migneco
- 申请人： Gillian Ashcroft , Mario Brufani , Francesca Ceccacci , Paolo Maria Farina , Luigi Filocamo , Barbara Garofalo , Roberta Joudioux , Adriana Maggi , Rinaldo Marini Bettolo , Luisa Maria Migneco
- 申请人地址： IT
- 专利权人： Euticals S.p.A.
- 当前专利权人： Euticals S.p.A.
- 当前专利权人地址： IT
- 代理机构： Lerner, David, Littenberg, Krumholz & Mentlik, LLP
- 优先权： ITMI05A1516 20050802
- 国际申请： PCT/EP2006/007488 WO 20060728
- 国际公布： WO2007/014711 WO 20070208
- 主分类号： A61K31/567
- IPC分类号： A61K31/567 ; C07J1/00
摘要：
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.