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US 9,434,760 B2Granted
Prolinamide derivatives as thrombin inhibitors, preparation method and application thereof
AssigneeShanghai Institute of Pharmaceutical Industry
InventorsMin Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
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Abstract
Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
Claims2
A compound of formula (I), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug thereof:
- wherein:
- A represents —SO2R1, —COR1, —R2COR1, or —R2CO2R1;
- wherein:
- R1 represents cycloalkyl, aryl, —R3-cycloalkyl, —R3-aryl, or —NR4R5;
- wherein cycloalkyl and aryl are substituted with 1 or 2 substituents selected from the group consisting of hydroxyl, carboxyl, halogen, C1-4 alkyl, C1-4 alkoxy, acyl, sulfonyl, sulfhydryl, alkylthio, cycloalkyl, heterocycloalkyl, amino, alkylamino, dialkylamino, cyano, ester group, trifluoromethyl, and CONH2;
- R2 and R3 represent unsubstituted C1˜6 alkyl;
- R4 and R5 represent independently H or unsubstituted C1˜6 alkyl;
- D represents
- F represents —NH—(CH2)m—R6;
- wherein:
- m represents 1;
- R6 represents unsubstituted
- G represents
- wherein:
- n represents 0;
- and
- R7 represents H.
14 more elements
Dependencies are inferred from the claim text.