发明授权
US08153781B2 Dendrimer conjugates of agonists and antagonists of the GPCR superfamily
失效
GPCR超家族的激动剂和拮抗剂的树枝状结合物缀合物
- 专利标题： Dendrimer conjugates of agonists and antagonists of the GPCR superfamily
- 专利标题（中）： GPCR超家族的激动剂和拮抗剂的树枝状结合物缀合物
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申请号： US12143451申请日： 2008-06-20
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公开(公告)号： US08153781B2公开(公告)日： 2012-04-10
- 发明人: Kenneth A. Jacobson , Yoonkyung Kim , Athena Klutz , Beatrice Hechler , Christian Gachet
- 申请人： Kenneth A. Jacobson , Yoonkyung Kim , Athena Klutz , Beatrice Hechler , Christian Gachet
- 申请人地址： US DC Washington FR Paris
- 专利权人： The United States of America as represented by the Secretary, Department of Health and Human Services,Inserm
- 当前专利权人： The United States of America as represented by the Secretary, Department of Health and Human Services,Inserm
- 当前专利权人地址： US DC Washington FR Paris
- 代理机构： Leydig, Voit & Mayer, Ltd.
- 主分类号： C07H19/22
- IPC分类号： C07H19/22
摘要：
Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1 adenosine receptor agonist having a purine nucleoside moiety and a functional group at the N6 position of the purine nucleoside moiety, wherein the functional group has the formula (I):N6H—Ar1—CH2—C(═O)NH—R1 (I), wherein Ar1 and R1 as defined herein. Also disclosed are pharmaceutical compositions, methods of treating various diseases, and a diagnostic method employing such conjugates.