| abstract |
Semicarbazide derivatives of the formula (1) where: R is C (= NH) -NH2, which may also be monosubstituted by OH, OCOOA, OCOO (CH2) nN (A) 2, OCOO (CH2) m-Het, COO (CH2) nN (A) 2, COO (CH2) m-Het, COC (A) 2-R4, COOA, COSA, COOAr, COOAr ', CH2NH2, a remainder of formula (2) or (3); R1 is X, Ar or Ar '; R2 is phenyl monosubstituted by S (O) pA, S (O) pNHA, CF3, COOA or CH2NHA, R3 is H or Hal; R4 is -CHal3, O (C = O) A or a remainder of formula (4); Ar is unsubstituted or mono, bi or trisubstituted phenyl by A, OH, OA, NH2, NHA, NA2, NO2, CF3, CN, Hal, COA, NHCOA, COOA, CONH2, CONHA, CONA2, S (O) pA, S (O) pNH2, S (O) pNHA, S (O) pNA2; Ar 'is - (CH2) n-Ar, A is H, unbranched, branched or C1-20 cyclic alkyl; X is C1-20 unbranched or branched alkyl, where one or two CH2 groups may be replaced by O or S atoms and / or 1-7 H atoms may be replaced by F; Het is a saturated, unsaturated or aromatic mono or bicyclic heterocycle with 1 to 4 atoms of N, O and / or S, which may be unsubstituted or mono or disubstituted by A; Hal is F, Cl, Br or I; n is 1, 2, 3, 4, 5 or 6; m is 1, 2, 3, 4, 5, or 6; p is 0, 1 or 2; as well as its derivatives, solvates and stereoisomers for pharmaceutical use, including mixtures in all proportions. These compounds are inhibitors of coagulation factor Xa and can be applied for the prophylaxis and / or therapy of thromboembolic conditions and for the treatment of tumors. |