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US 2003/0199698 A1Published application
Carbamic acid esters as inhibitors of factor xa
OwnerHorst Juraszyk, Dieter Dorsch +4inventors
InventorsHorst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
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Abstract
Novel compounds of the formula I 1 in which R, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic illnesses.
Claims18
Compounds of the formula I
- 20
- in which
- R is —CO—N═C(NH2)2, —NH—C(═NH)—NH2 or —C(═NH)—NH2, which may also be monosubstituted by OH, —OCOOA, —OCOO(CH2)nNAA′, —COO(CH2)NAA′, —OCOO(CH2)m-Het, —COO(CH2)m-Het, —CO—CAA′-R3, —COO—CAA′-R3, COOA, COSA, COOAr or COOAr′ or by a conventional amino-protecting group,
- 21
- R′ is unbranched, branched or cyclic alkyl having 1-20 carbon atoms, in which one or two CH2 groups may be replaced by O or S atoms, or is Ar, Ar′ or X,
- R2 is phenyl which is monosubstituted by S(O)pA, S(O)pNHA, CF3, COOA, CH2NHA, CN or OA,
- R3 is —C(Hal)3, —O(C═O)A or
- 22
- Ar is phenyl or naphthyl which is unsubstituted or monosubstituted, disubstituted or trisubstituted by A, OA, NAA′, NO2, CF3, CN, Hal, NHCOA, COOA, CONAA′, S(O)pA or S(O)pNAA′,
- Ar′ is —(CH2)n-Ar,
- A and A′ are each, independently of one another, H or unbranched, branched or cyclic alkyl having 1-20 carbon atoms,
- Het is a monocyclic or bicyclic, saturated, unsaturated or aromatic heterocyclic radical having 1 to 4 N, O and/or S atoms, bonded via N or C, which may be unsubstituted or substituted by A,
- X is —(CH2)n—Y,
- Y is COOA or
- 23
- Hal is F, Cl, Br or 1,
- m is 0 or 1,
- n is 1, 2, 3, 4, 5 or 6, and
- p 0, 1 or 2,
- and their pharmaceutically tolerated salts and solvates.
17 more elements
Dependencies are inferred from the claim text.