| 摘要 |
<p>THE PRESENT INVENTION RELATES TO A NOVEL SELECTIVE THROMBIN INHIBITOR HAVING THE FOLLOWING FORMULA (I), WHICH IS ALSO EFFECTIVE BY ORAL ADMINISTRATION: IN WHICH R1 REPRESENTS ACETYL SUBSTITUTED WITH ARYL OR ARYLOXY, OR REPRESENTS SULFONYL SUBSTITUTED WITH SUBSTITUTED OR UNSUBSTITUTED ARYL OR N-CONTAINING HETEROCYCLIC GROUP,X REPRESENTS A GROUP OF FORMULA -NOR -N N-R5 R2 AND R3 INDEPENDENTLY OF ONE ANOTHER REPRESENT HYDROGEN; CYCLOALKYL SUBSTITUTED OR UNSUBSTITUTED WITH CARBOXYL OR ALKOXYCARBONYL; ARYLALKYLOXY; HYDROXY; OR LOWER ALKYL SUBSTITUTED OR UNSUBSTITUTED WITH CARBOXYL, ALKOXYCARBONYL OR HYDROXY, OR R2 AND R3 TOGETHER WITH NITROGEN ATOM TO WHICH THEY ARE ATTACHED CAN FORM A PIPERIDINE GROUP SUBSTITUTED WITH CARBOXYL OR ALKOXYCARBONYL, R4 REPRESENTS HYDROGEN, LOWER ALKYL OR LOWER ALKOXY, R5 REPRESENTS ALKANESULFONYL; ALKOXYCARBONYL; ALKYLCARBONYL; FORMYL; LOWER ALKYL; ARYL SUBSTITUTED OR UNSUBSTITUTED WITH ALKOXY OR HALOALKYL; OR HYDROXY-SUBSTITUTED LOWER ALKYL, AND R6 AND R7 INDEPENDENTLY OF ONE ANOTHER REPRESENT HYDROGEN, LOWER ALKYL OR AMINO, AND TO A PROCESS FOR PREPARATION THEREOF AND A PHARMACEUTICAL COMPOSITION FOR THROMBIN INHIBITION WHICH COMPRISES THE COMPOUND OF FORMULA (I) AS AN ACTIVE INGREDIENT.</p> |
