发明授权
US06344466B2 Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors
有权
苯甲酰胺和磺酰胺取代的氨基胍和烷氧基胍作为蛋白酶抑制剂
- 专利标题: Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors
- 专利标题(中): 苯甲酰胺和磺酰胺取代的氨基胍和烷氧基胍作为蛋白酶抑制剂
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申请号: US09796319申请日: 2001-02-28
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公开(公告)号: US06344466B2公开(公告)日: 2002-02-05
- 发明人: Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
- 申请人: Richard M. Soll , Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan , Colleen Siedem
- 主分类号: A61K31445
- IPC分类号: A61K31445
摘要:
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage.