New forms of specific substituted thiophene carboxamide (rivaroxaban), useful for prevention and treatment of thromboembolic disease, have higher solubility than known modifications

摘要

Modification II and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) (I), are new. Modification II and the amorphous form of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide (rivaroxaban) of formula (I), are new. Independent claims are also included for: (1) method for preparing modification II by either: (a) dissolving modification I in inert solvent, then precipitating; (b) dissolving modification I in inert solvent and storing the solution at elevated temperature until all solvent has evaporated; or (c) suspending amorphous (I) in anhydrous, inert solvent and stirring or shaking the suspension until quantitative conversion to modification II has occurred; and (2) method for preparing amorphous (I) by melting crystalline (I) then cooling rapidly. [Image] ACTIVITY : Thrombolytic; Anticoagulant; Cardiant; Antianginal; Vasotropic; Cerebroprotective; Antiarteriosclerotic; Antiinflammatory; Antirheumatic; Nootropic; Neuroprotective; Cytostatic; Ophthalmological. No biological data given. MECHANISM OF ACTION : Inhibition of blood coagulation factor Xa. No biological data given.