| 摘要 |
本发明系关于新颖式I甲醯胺化合物，及其关于药剂制造之用途。该甲醯胺化合物为钙蛋白 (钙依赖性半胱胺酸蛋白 )抑制剂之前体药物。本发明因此亦关于利用此等甲醯胺化合物以治疗与高钙蛋白 活性有关联之病症。#P 097151007P01.bmpR#sP!1#eP!为C#sB!1#eB!-C#sB!l0#eB!-烷基、C#sB!2#eB!-C#sB!10#eB!-烯基、C#sB!2#eB!-C#sB!10#eB!-炔基、C#sB!3#eB!-C#sB!7#eB!-环烷基、C#sB!3#eB!-C#sB!7#eB!-环烷基-C#sB!1#eB!-C#sB!4#eB!-烷基、芳基、杂芳基、芳基-C#sB!l#eB!-C#sB!6#eB!-烷基、芳基-C#sB!2#eB!-C#sB!6#eB!-烯基、杂芳基-C#sB!1#eB!-C#sB!4#eB!-烷基或杂芳基-C#sB!2#eB!-C#sB!6#eB!-烯基，R#sP!2#eP!为C#sB!3#eB!-C#sB!7#eB!-环烷基、C#sB!3#eB!-C#sB!7#eB!-环烷基-C#sB!1#eB!-C#sB!4#eB!-烷基、芳基、O-芳基、O-CH#sB!2#eB!-芳基、杂芳基、芳基-C#sB!1#eB!-C#sB!6#eB!-烷基、芳基-C#sB!2#eB!-C#sB!6#eB!-烯基、杂芳基-C#sB!l#eB!-C#sB!4#eB!-烷基或杂芳基-C#sB!2#eB!-C#sB!6#eB!-烯基，R#sP!3a#eP!与R#sP!3b#eP!一起形成部份基团S-Alk-S、O-Alk-S或O-Alk-O，其中Alk为线性C#sB!2#eB!-C#sB!5#eB!-烷二基，其可为未经取代或被1,2,3或4个选自C#sB!1#eB!-C#sB!4#eB!-烷基或卤素之基团取代；X为式C(=O)-O-R#sP!x1#eP!、C(=O)-NR#sP!x2#eP!R#sP!x3#eP!、C(=O)-N(R#sP!x4#eP!)-(C#sB!l#eB!-C#sB!6#eB!-伸烷基)-NR#sP!x2#eP!R#sP!x3#eP!或C(=O)-N(R#sP!x4#eP!)NR#sP!x2#eP!R#sP!x3#eP!之基团，n为0,1或2，变数Y#sP!1#eP!, Y#sP!2#eP!, Y#sP!3#eP!或Y#sP!4#eP!之一为氮原子，而其余变数Y#sP!1#eP!, Y#sP!2#eP!, Y#sP!3#eP!或Y#sP!4#eP!为CH；R#sP!y#eP!为例如OH、SH、卤素、NO#sB!2#eB!、NH#sB!2#eB!、CN、CF#sB!3#eB!、CHF#sB!2#eB!、CH#sB!2#eB!F、O-CF#sB!3#eB!、O-CHF#sB!2#eB!、O-CH#sB!2#eB!F、COOH、OCH#sB!2#eB!COOH、C#sB!1#eB!-C#sB!6#eB!-烷基、C#sB!l#eB!-C#sB!6#eB!-烷氧基、C#sB!l#eB!-C#sB!6#eB!-烷氧基-C#sB!l#eB!-C#sB!4#eB!-烷基、C#sB!1#eB!-C#sB!6#eB!-烷硫基等；W为式Wl或W2基团，其系经由氮连结：#P 097151007P02.bmp其中*系意谓对6-员杂芳族环之链结，而#系意谓对R#sP!2#eP!之链结，m为0, 1或2，及R#sP!w#eP!为例如OH、SH、卤素、NO#sB!2#eB!、NH#sB!2#eB!、CN、CF#sB!3#eB!、CHF#sB!2#eB!、CH#sB!2#eB!F、O-CF#sB!3#eB!、O-CHF#sB!2#eB!、O-CH#sB!2#eB!F、COOH、OCH#sB!2#eB!COOH。 |
