Treatment or prevention of cardiovascular events via the administration of a colchicine derivative
申请人:Murray and Poole Enterprises, LTD.
公开号:US11026901B2
公开(公告)日:2021-06-08
A method for the treatment or prevention of a cardiovascular event in a subject with atherosclerotic vascular disease comprising the step of:
b) administering a therapeutically effective amount of a compound of formula (I), a known colchicine derivative and/or a salt thereof
wherein:
R1, R2, R3, R4, R9, R10, R11 and R12 independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, C1-4 alkyl or dialkylamino, hydroxyl, C1-4 alkoxy, C1-4 alkylthio, a group of the formula —SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl, C1-4 acyloxy, or optionally substituted phenyl, optionally substituted phenoxy;
R7 and R8 independently represent hydrogen, C1-4 alkyl or C1-4 acyl; and
R5′, R5″, R6′ and R6″ independently represent hydrogen, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, halogen, C1-4 haloalkyl, nitro, amino, C2-4 acylamino, hydroxyl, C1-4 alkoxy or C1-4 alkylthio a group of the formula —SO2N(Rx)2 or SO2Rx where Rx is C1-4 alkyl, C1-4 acyloxy, or optionally substituted phenyl.
一种治疗或预防动脉粥样硬化性血管疾病患者心血管事件的方法,包括以下步骤
b) 给药治疗有效量的式(I)化合物、已知的
秋水仙碱衍
生物和/或其盐
其中:
R1、R2、R3、R4、R9、R10、R11 和 R12 独立地代表氢、C1-4 烷基、C2-4 烯基、C3-6 环烷基、卤素、C1-4 卤代烷基、硝基、
氨基、C2-4 乙酰
氨基、C1-4 烷基或二烷基
氨基、羟基、C1-4 烷氧基、C1-4 烷
硫基、式 -SO2N(Rx)2 或 SO2Rx 的基团(其中 Rx 是 C1-4 烷基、C1-4 乙酰氧基或任选取代的苯基、任选取代的苯氧基);
R7 和 R8 独立地代表氢、C1-4 烷基或 C1-4 乙酰基;以及
R5′、R5″、R6′和 R6″ 独立地代表氢、C1-4 烷基、C2-4 烯基、C3-6 环烷基、卤素、C1-4 卤烷基、硝基、
氨基、C2-4 乙酰
氨基、羟基、C1-4 烷氧基或 C1-4 烷
硫基,其中 Rx 是 C1-4 烷基、C1-4 乙酰氧基或任选取代的苯基。