| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain the subject new compound having potent and sustainably excellent cell adhesion inhibitory activity and GPIIb/IIIa antagonism, and safely usable at low doses as a preventive/therapeutic agent for transient cerebral ischemia attack, unstable angina pectoris and the like. SOLUTION: This new compound (salt) is represented by formula I [R1 is a basic 5- to 7-membered N-contg. heterocyclic ring or an aryl carbonyl having a proton-accepting group or a group convertible thereto; R2 is H or a hydrocarbon; X is a lone pair or group of the formula X1-CH2CO (X1 is a lone pair, O or the like); Y is NH or O; Z is an alkylene; R5 is carboxyl], e.g. (2S)-3- 2-[(9 aR)-2-piperidin-4-ylmethyloctahydropyrido[1,2-a]pyrazin-8- yl]acetylamino}-2-(toluene-4-sulfonylamino)propionic acid. The compound of formula I is obtained using a compound of formula II as starting material and then through respective compounds of formula III and formula IV (R15 is a carboxyl-protecting group; denotes an asymmetric center), or the like.</p> |
