Benzamides and related inhibitors of factor Xa
View Patent ↗Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
1. A compound having the following structure:
wherein:
R 1a is H or F;
R 1d1 is H or —OMe;
A-Q is a member selected from the group consisting of:
or a pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.
2. A compound of claim 1 , wherein R 1a is H.
3. A compound of claim 1 , wherein R 1a is F.
4. A compound of claim 1 , wherein R 1d1 is H.
5. A compound of claim 1 , wherein R 1d1 is —OMe.
6. A compound of claim 1 selected from the group consisting of:
or a pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives thereof.
7. A pharmaceutical composition for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising a phannaceutically acceptable carrier and a pharmaceutically effective amount of a compound of claim 1 .
8. A method for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising administering to said mammal a therapeutically effective amount of a compound of claim 1 .
9. The method of claim 8 , wherein the condition is selected from the group consisting of:
acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, occlusive coronary thrombus occurring post-thrombolytic therapy or post-coronary angioplasty, a thrombotically mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, transient ischemic attacks, venous thrombosis, deep venous thrombosis, pulmonary embolus, coagulopathy, disseminated intravascular coagulation, thrombotic thrombocytopenic purpura, thromboangiitis obliterans, thrombotic disease associated with heparin-induced thrombocytopenia, thrombotic complications associated with extracorporeal circulation, thrombotic complications associated with instrumentation, and thrombotic complications associated with the fitting of prosthetic devices.
10. A method for inhibiting the coagulation of a biological sample, comprising the step of administering a compound of claim 1 .