Thrombin inhibitors
View Patent ↗Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof.
1. A compound of the general formula
and pharmaceutically acceptable salts thereof, wherein
n is 0, 1, 2 or 3;
X is hydrogen, halogen or C 1-4 alkyl;
Y is a bond or —CH(R)—;
W is a bond or —(C(R 4 )(R 5 )) 1-5 -;
R and R 1 are independently selected from the group consisting of hydrogen, C 1-4 alkyl, cycloC 3-7 alkyl, aryl or a 5- to 7-membered heterocycle; and
R 2 , R 3 , R 4 , and R 5 , in each occurrence, are independently selected from the group consisting of hydrogen and C 1-4 alkyl.
2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, where n is 1.
3. A compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein R 1 is cyclohexyl, pyridyl, methyl or phenyl, and R is hydrogen, phenyl or cyclohexyl.
4. A compound of claim 3 , or a pharmaceutically acceptable salt thereof, wherein X is Cl.
5. A compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein R 2 and R 3 are independently selected rom the group consisting of hydrogen, —CH 3 and —CH 2 CH 3 .
6. A compound of claim 5 , or a pharmaceutically acceptable salt thereof, selected from the group consisting of
7. A composition for inhibiting thrombus formation in blood comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
8. A method for inhibiting thrombus formation in a patient comprising administering to the patient a compound of claim 1 .
9. A method for inhibiting formation of blood platelet aggregates in a patient comprising administering to the patient a compound of claim 1 .