AMP DERIVATIVES FOR TREATING CARDIAC
DISEASES
申请(专利)号： EP20110713395
专利号： EP2539352A2 主分类号： C07F9/6561 申请权利人： UNIVERSITY OF
CONNECTICUT; THE UNITED STATES OF AMERICA, AS REPRESENTED BY
THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES 公开国代码： EP 优先权国家： US
摘 要：
Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogs of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the CP bond. When administered to calsequestrin-overexpressing mice (a genetic model of
申请日： 2011-02-22 公开公告日： 2013-01-02
分类号： C07F9/6561 发明设计人： LIANG, BRUCE;
JACOBSON, KENNETH A.; JOSHI,
BHALCHANDRA V.; KUMAR,
THATIKONDA SANTOSH
申请国代码： EP
优先权： 20100222 US
306687 P
摘 要 附 图：
heart failure) via a mini-osmotic pump (Alzet), some analogs significantly
increased intact heart contractile function in vivo, as assessed by
echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogs for treatment of heart failure has been expanded. 主权项：
1. A phosphonate or phosphinate N-methanocarba derivative of AMP comprising, /n 权 利 要 求 说 明 书 【AMP DERIVATIVES FOR TREATING CARDIAC DISEASES】的权利说明书内容是......请下载后查看
AMP DERIVATIVES FOR TREATING CARDIAC DISEASES
