Invention Grant
US08497245B2 Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
有权
胰蛋白酶样丝氨酸蛋白酶抑制剂,它们的制备和用作凝血因子IIa和Xa的选择性抑制剂
- Patent Title: Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors IIa and Xa
- Patent Title (中): 胰蛋白酶样丝氨酸蛋白酶抑制剂,它们的制备和用作凝血因子IIa和Xa的选择性抑制剂
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Application No.: US13332900Application Date: 2011-12-21
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Publication No.: US08497245B2Publication Date: 2013-07-30
- Inventor: Peter Herold , Stjepan Jelakovic , Mohammed Daghish , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz , Friedrich-Alexander Ludwig , Adel Rafai Far , Ting Kang
- Applicant: Peter Herold , Stjepan Jelakovic , Mohammed Daghish , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz , Friedrich-Alexander Ludwig , Adel Rafai Far , Ting Kang
- Applicant Address: DE Leipzig
- Assignee: The Medicines Company (Leipzig) GmbH
- Current Assignee: The Medicines Company (Leipzig) GmbH
- Current Assignee Address: DE Leipzig
- Agency: Clark & Elbing LLP
- Main IPC: A61K38/05
- IPC: A61K38/05

Abstract:
The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.
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