申请人:Glaxo Wellcome Inc.
公开号:US06177445B1
公开(公告)日:2001-01-23
Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X1 and X2 are independently halogen; ha and hb are independenity from 0 to 2; Z1 and Z2 are indepentdently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl with the proviso that Z1 and Z2 are not both hydrogen; Y1, Y2, and Y3 and Y4 are independently hydrogen, halogen or C1-3 alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if ha and hb are both 0, then r is 0 and n is 0 to 2; R1 to R14 are independently hydrogen, halogen, C1-3 alkoxy, or R2 and R3 together with the carbon atoms to which they are bonded, R5 and R6 together with the carbon atoms to which they are bonded, R9 and R10 together with the carbon atoms to which they are bonded, R12 and R13 together with the carbon atoms to which they are bonded, may independently form a methylenedioxy or ethylenedioxy moiety contained in five- or six-membered ring; W1 and W2 are carbon; and A is a pharmaceutically acceptable anion.
本发明涉及公式(I)的超短作用神经肌肉松弛剂,其在紧急插管、常规手术和术后情况下作为骨骼肌松弛剂非常有用,其中q和t独立地为0到4;X1和X2独立地为卤素;ha和hb独立地为0到2;Z1和Z2独立地为氢、C1-6烷基、C2-6烯基或C2-6炔基,但须满足Z1和Z2不同时为氢;Y1、Y2、Y3和Y4独立地为氢、卤素或C1-3烷氧基;m和p独立地为1到6;n和r独立地为0到4;但须满足如果ha和hb都为0,则r为0且n为0到2;R1到R14独立地为氢、卤素、C1-3烷氧基,或者R2和R3与它们所结合的碳原子、R5和R6与它们所结合的碳原子、R9和R10与它们所结合的碳原子、R12和R13与它们所结合的碳原子可以独立地形成包含在五元或六元环中的亚甲二氧基或乙撑二氧基基团;W1和W2为碳;A是一种药学上可接受的阴离子。