发明名称 CARBAMATE ANALOGS OF THIAPHYSOVENINE, PHARMACEUTICAL COMPOSITIONS, AND METHOD FOR INHIBITING CHOLINESTERASES
摘要 Substituted carbamates of tricyclic compounds which have a cyclic sulfer atom, having the formula: (See formula I) wherein R1 is H or a linear or branched chain C1- C10 alkyl group; and R2 is selected from the group consisting of a linear or branched chain -C1-C10 alkyl group, and (See formula I) wherein R3 and R4 are independently selected from the group consisting of H and a linear or branched chain C1-C10 -alkyl group; and with the proviso that when one of R1 or R2 is a H or a methyl group the other of R1 or R2 is not H and optical isomers of the 3aS series, provide highly potent and selective cholinergic agonist and blocking activity and are useful as pharmaceutical agents. Cholinergic disease are treated with these compounds such as glaucom a, Myasthenia Gravis, Alzheimer's disease. Methods for inhibiting esterase s, acetylcholinesterase and butyryl-cholinesterase are also provided.
申请公布号 CA2119782(C) 申请公布日期 2005.08.23
申请号 CA19922119782 申请日期 1992.09.26
申请人 THE GOVERNMENT OF THE UNITED STATES OF AMERICA REPRESENTED BY THE SECRETARY 发明人 BRZOSTOWSKA, MALGARZOTA;BROSSI, ARNOLD;HE, XIAO-SHU;RAPOPORT, STANLEY I.;GREIG, NIGEL H.
分类号 A61K31/40;A61K31/407;A61P21/00;A61P21/04;A61P25/02;A61P25/28;A61P27/02;A61P27/06;A61P43/00;C07D495/04;(IPC1-7):C07D495/04 主分类号 A61K31/40
代理机构 代理人
主权项
地址