公开(公告)号：US07550474B2

公开(公告)日：2009-06-23

申请号：US10816544

申请日：2004-04-01

Applicant: Kevin D. Kreutter ,  Lily Lee ,  Tianbao Lu ,  Venkatraman Mohan ,  Sharmila Patel ,  Hui Huang ,  Guozhang Xu ,  Mark Fitzgerald

Inventor： Kevin D. Kreutter ,  Lily Lee ,  Tianbao Lu ,  Venkatraman Mohan ,  Sharmila Patel ,  Hui Huang ,  Guozhang Xu ,  Mark Fitzgerald

IPC: A61K31/435 ,  C07D221/02 ,  C07D335/00 ,  C07D309/00 ,  C07C321/00

CPC classification number: C07D213/73 ,  C07C279/00 ,  C07C291/04 ,  C07D213/26 ,  C07D213/89 ,  C07D215/12 ,  C07D413/12 ,  C07D487/04

Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. 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, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.

Abstract translation: 描述了苯基乙酰胺化合物，包括式I化合物或其溶剂合物，水合物或其药学上可接受的盐; 其中R3-R6，R11，B，Y和W在说明书中列出。 本发明的化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样的丝氨酸蛋白酶，如凝血酶和因子Xa。 描述了抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制栓塞形成的组合物。 本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂， 血线和支架。 另外，化合物可以被可检测地标记并用于血栓的体内成像。