| abstract |
The compounds of the formula (1) wherein R is H, A, A-CO-, Hal, -C ::: C-H, -C ::: C-A or -C ::: C-C (= O) -A; R1 is H, = O, Hal, A, OH, OA, A-COO-, Ph- (CH2) n-COO-, cycloalkyl- (CH2) n-COO-, A-CONH-, A-CONA-, Ph -CONA-, N3, NH2, NO2, CN, COOH, COOA, CO-NH2, CONHA, CON (A) 2, O-allyl, O-propargyl, O-benzyl, = N-OH, = N-OA or = CF2; Ph is unsubstituted or mono, di or trisubstituted phenyl with A, OA or Hal; R2 is H, Hal or A; R3n is a saturated, unsaturated or aromatic monocyclic heterocycle with 1 to 4 atoms of N, O and / or S, which may be unsubstituted or mono, di or trisubstituted with Hal, A, OA, CN, (CH2) nOH, (CH2 ) nHal, NR4R5, = NH, = N-OH, = N-OA and / or O of carbonyl (= O), or CONR4R5; R4, R5 are, independently of each other, H or A, R4 and R5 are also together an alkylene chain with 3, 4 or 5 C atoms that can also be substituted with A, Hal, OA and / or O carbonyl (= CO); A is unbranched, branched or cyclic alkyl with 1-10 C atoms, where 1-7 H atoms can also be replaced by F and / or Cl; Hal is F, Cl, Br or I; n is 0, 1, 2, 3, or 4; as well as its derivatives, salts, solvates and stereoisomers of pharmaceutical utility, including mixtures in all proportions. They are inhibitors of coagulation factor Xa and can be used for the prophylaxis and / or therapy of thromboembolic diseases and for the treatment of tumors. |