Pyrazinone COMPOUNDS, PHARMACEUTICAL COMPOSITION (VARIANTS) AND DOSAGE FORM, PROCESS PROTEASE INHIBITION AND A METHOD OF REDUCING SURFACE thrombogenic CAPACITY, METHOD FOR TREATING THROMBOSIS AND PROTEOLYSIS Abuse, associated with various diseases, METHOD OF REDUCING BLOOD COAGULATION AND METHOD FOR DETERMINING THE THROMBIN IN MAMMALS

摘要

Pyrazinone compounds are described, including compounds of formula (I), where X is O, NR, or CH = N, R — R, R, R, R, W, m, and n are defined in the specification, as well as their hydrates, solvates, or pharmaceutically acceptable salts. The compounds of the present invention are effective protease inhibitors, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Some compounds exhibit antithrombotic activity due to direct selective inhibition of thrombin. Compositions are also described for inhibiting the loss of blood platelets, inhibiting the aggregation of thrombocytes, inhibiting the formation of fibrin, inhibiting the formation of blood clots and inhibiting the formation of an embolus. Another field of application of the compounds of the invention is their use as anticoagulants, either incorporated into materials or physically related to materials used to manufacture blood collection devices, artificial blood circulation and blood storage, such as catheters, blood dialysis machines, syringes tubes for blood collection, circulatory system and stents. In addition, the compounds may contain a detectable label and be used to obtain an image of blood clots in vivo. The international application was published along with an international search report.