| 摘要 |
PURPOSE: Provided are proline derivatives, their stereoisomers or their pharmaceutically acceptable salts which are characterized by showing an excellent antithrombin activity, thus being useful as drugs such as antithrombotic agents, being available in oral administration and showing little side effect. CONSTITUTION: Proline derivatives are represented by general formula(1), wherein R1 represents formula(2) or (3), wherein A represents(a), (b) or (c); R2 represents hydrogen or lower alkyl; R3 represents optionally substituted lower alkyl, optionally substituted aryl or optionally substituted lower alkoxy; R4 represents hydrogen, optionally substituted lower alkyl, optionally substituted lower alkylcarbonyl, optionally substituted lower alkylsulfonyl or optionally substituted lower alkoxycarbonyl; R0 represents hydrogen or lower alkyl; B represents CH2 or S; and n is an integer of from 1 to 3.
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