DERIVATIVES OF PHENOXY-N-[4-(1,1-DIOXOTHIAZOLIDIN-2-YL)PHENYL]-VALERAMIDE AND OTHER COMPOUNDS AS COAGULATION FACTOR Xa INHIBITORS IN TREATMENT OF THROMBEMBOLIC DISEASE AND TUMOR Russian patent published in 2007 - IPC C07D275/02 C07D417/12 A61K31/425 A61K31/54 A61P7/00 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of phenoxy-N-[4-(1,1-dioxoisothiazolidin-2-yl)-valeramide and describes compounds of the formula (I): wherein E represents phenyl or isoquinoline each of that is monosubstituted with group R¹ wherein R¹ represents -CN, amidino-group, halogen atom, -NH₂, -CH₂NH₂ or compound of the formula: W represents -OCHAr', -OCHA, -NHCHAr', -NHCHA, -NHCOOCHAr', -NHCONHCHAr' or piperidine-1,2-diyl; Ar' represents unsubstituted phenyl or mono- or disubstituted phenyl, Hal, A or -CF₃; A represents alkyl with 1, 2, 3, 4, 5, 6 or 7 C-atoms; X represents -CONH; Y represents Ar-diyl; T represents group -(CH₂)₃; Ar represents unsubstituted phenyl or mono- or disubstituted phenyl, Hal, A or -CF₃; Hal represents fluorine (F), chlorine (Cl), bromine (Br) or iodine (J) atoms. These compounds are the coagulation factor Xa inhibitors. Also, invention relates to a method for synthesis of compounds of the formula (I), a medicinal agent containing these compounds and using compounds of the formula (I) for preparing a drug used in treatment of thrombosis, myocardium infarction, arteriosclerosis, inflammation, apoplexy, stenocardia, restenosis after plastic surgery in vessels, intermittent lameness, migraine, tumors, tumor diseases and/or tumor metastasis and a kit (set). Also, invention relates to intermediate compounds of the formula (I-1): wherein R¹ represents -NO₂ or -NH₂; R represents methyl, chlorine atom or trifluoromethyl and their salts. Invention provides synthesis of novel compounds possessing valuable biological properties.

EFFECT: valuable medicinal properties of compounds.

9 cl, 1 tbl, 14 ex