Compound N - (4 - amidino - 2.6 - difluorobenzil) - 1 - (2 - (3 - Chloro - 5 - (Difluoromethoxy) phenyl) - 2 - hidroxiacetil). - 2 - carboxamide derivative and Pharmaceutical composition comprising the same, and its use in preparation of Medicine and Synthetic routes for its production

摘要

A compound N - (4 - amidino - 2.6 - difluorobenzil) - 1 - (2 - (3 - Chloro - 5 - (Difluoromethoxy) phenyl) - 2 - hidroxialcetil). - 2 - carboxamide which responds to the formula (1) or a derivative thereof, including acceptable for pharmaceutical use of prodrugs the formula (1) wherein R1 represents OR2 or C (OR) OR3, R2 is H, alkyl, C1 - 10Alkylaryl C1 - 3 or alquiloxiarilo c1-3 alkyl (parties whose last two groups are optionally interrupted by one or more Oxygen ATOMS, and the parties whose last two aryl groups are optionally substituted by one or more substituents selected from Halogen, phenyl Methyl or methoxy,,The last three groups are optionally substituted by one or more substituents); R3 represents alkyl and Halogen C1 - 10 (whose last groups are optionally interrupted by one or more Oxygen Atoms), or alkylaryl C1 - 3 or alquiloxiarilo c1-3 alkyl cuy (Parties I last two groups are optionally interrupted by one or more Oxygen Atoms.And the parties whose last two aryl groups are optionally substituted by one or more substituents selected from Halogen, phenyl methyl or methoxy groups, of which the last three are also optionally substituted by one or more substituents) or an acceptable Pair Halogen derivative Pharmaceutical Use of the same.It also describes the pharmaceutical composition that comprises and the use of said compound in the manufacture of medicines.Such compounds and their Derivatives are useful as competitive inhibitors of Trypsin like proteases, such as thrombin, or are useful as prodrugs of and therefore are particularly useful for the treatment of conditions which require the inhibition of Thrombin ( For example, thrombosis) or as anticoagulants.