| abstract |
Benzamidine derivatives of formula (I) wherein R1 represents -C (= NH) -NH2 which may also be substituted with -COA, -CO- [C (R5) 2] m-Ar, COOA, -OHo a conventional amino protecting group, of the formula (II); R2 represents H, A, OR5, N (R5) 2, NO2, CN, Hal, NR5COA, NHCOAr, NHSO2A, NHSO2Ar, COOR5, CON (R5) 2CONHAr, COR5, COAr, S (O) nA or S (O) nAr, R3 represents R5 or - [C (R5) 2] m-COOR5, R3 and X also represent together -CO-N forming a 5-member ring, R3 -C = O and X being equal to N, R4 represents A, cycloalkyl, - [C (R5) 2m] Ar, - [C (R5) 2] m-Het or -CR5 = CR5-Ar, R5 represents H, A or benzyl, X represents O, NR5, or CH2, Y represents O, NR5, N [c (R5) 2] m-Ar, N [C (R5) 2] m-Het, N [C (R5) 2] m-COOR5, of the formula (III) N [C (R5) 2] m-CON (R5) sub index2, N [C (R5) sub index2] m-CONR5Ar or N [C (R5) 2] m-CONAr sub index2, W represents a link, - SO sub.index2, -CO-, COO- or CONR5-, A represents alkyl of 1 to 20 carbon atoms in which one or two groups of CH2 may be replaced by atoms of O or S or by groups of -CR5 = CR5 and / or 1 to 7 atoms of H may be replaced by F, Ar represents phenyl or unsubstituted or mono, di or trisubstituted with R, A, Ar, OR5, N (R5) 2 NO2, CN, Hal, NHCOA, NHCOA r, NHSO2A, NHSO2Ar, COOR5, CON (R5) 2, CONHAr, COR5, COAr S (O) nA or S (O) nAr, Ar represents phenyl, or naphthyl, unsubstituted or mono, di or trisubstituted with R1, A , OR5, N (R5) 2, NO2, CN, Hal, NHCOA, COOR5, CON (R5) 2, COR5 or S (O) nA, Hetrepresents a mono or bicyclic heterocyclic system, saturated or unsaturated, containing one, two , three, or four same or different heteroatoms such as comonitrogen, oxygen and sulfur, and which is unsubstituted or mono or polysubstituted with Hal, A, Ar, OR5, COOR5, CN, N (R5) sub-index 2, NHCOA, NHCOAry / or carbonyloxy, Hal represents F, Cl, Br or I, m is 0, 1, 2, 3 or 4, n is 0, 1 or 2, and its salts. The compounds are inhibitors of the coagulation factor Xa.Procedure to prepare these compounds, their use for the prophylaxis and / or therapy of thromboembolic diseases, compositions |