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US 2013/0296245 A1Published application
Prolinamiade derivatives as thrombin inhibitor, prepraration 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.
Claims17
A compound of formula (I), pharmaceutically acceptable salt and pharmaceutically acceptable prodrug thereof:
- wherein:
- A represents C1-6 alkyl, cycloalkyl, heterocycloalkyl, aryl, —SO2R1, —SO3R1, —COR1, —CO2R1, —PO(OR1)2, —R2-cycloalkyl, —R2-heterocycloalkyl, —R2-aryl, —R2SO2R1, —R2SO3R1, —R2COR1, —R2CO2R1, or —R2PO(OR1)2;
- wherein:
- R1 represents H, C1-6 alkyl, cycloalkyl, heterocycloalkyl, aryl, —R3-cycloalkyl, —R3-heterocycloalkyl, —R3-aryl, alkenyl or —NR4R5;
- R2 and R3 represent C1-6 alkyl;
- R4 and R5 represent independently H, C1-6 alkyl, cycloalkyl or heterocycloalkyl;
- B represents H;
- D represents
- E represents
- which are substituted or unsubstituted on the ring;
- wherein substituents on the ring are selected from carboxyl, halogen, alkyl, alkoxy, acyl, sulfonyl, sulfhydryl, alkylthio, cycloalkyl, heterocycloalkyl, amino, alkylamino, dialkylamino, cyano, ester group, trifluoromethyl or C1-4 alkyl carrying the above groups;
- F represents —NH—(CH2)m—R6;
- wherein:
- m represents 0-3;
- R6 represents unsubstituted
- wherein:
- X, Y and Z represent independently S, O or N;
- G represents
- wherein:
- n represents 0-3;
- p represents 1-8;
- R7 represents H or C1-6 alkyl.
19 more elements
Dependencies are inferred from the claim text.