| 摘要 |
A compound of formula (I) where: R1 is C3-C7 cycloalkyl, substituted with one or more basic groups such as amino, amidino and or guanidine; aromatic heterocyclyl containing at least one nitrogen atom, and substituted with one or more basic groups such as amino, amidino and or guanidine; aliphatic heterocyclyl, containing at least one hetero atom selected from S or O, and substituted with one or more basic groups such as amino, amidino and or guanidine. R2 is H, C1-3 alkyl, amino, halogen, hydroxy; R3 is COOR5 R4 is SH, S-CO-C1-6 alkyl or S-CO-aryl; R5 is H, C1-6 alkyl or aryl; X is C(Z)2 Y is C(Z)2; Z is independently H, C1-6 alkyl or phenyl(C1-6 alkyl); where alkyl, cycloalkyl, aryl, alkylcarbamoyl, alkylthio, alkoxy, aroyl, aroylamino, aryloxy, arylthio, amidino, amino, aryl, carbamoyl, carboxy, cyano,cycloalkyl, formyl, guanidine, halogen, heterocyclyl, hydroxy, oxo, nitro, thiol, Z2N-CO-O-, ZO-CO-NZ or Z2CO-NZ. A process for the preparation of compounds of formula (I) is also disclosed. A pharmaceutical composition containing a compound of formula (I) for the inhibition of carboxypeptidase U. Also, a combined pharmaceutical composition comprising: a) a compound of formula (I), and b) one or more antithrombotic agent such as an antiplatelet agent, thromboxane receptor inhibitor, synthetase inhibitor, fibrinogen receptor antagonist, prostacyclin mimetic, phosphodiesterase inhibitor or ADP-receptor (P2T) antagonist.
|
