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US 2004/0171658 A1Published application
Carbohydrate derivatives
OwnerPeter Raddatz, Dieter Dorsch +4inventors
InventorsPeter Raddatz, Dieter Dorsch, Johannes Gleitz, Chistopher Barnes, Ulrich Koert, Marko Vogler
Life of this patent
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Abstract
Novel compounds of the formula I in which Y, T, W, 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 diseases and for the treatment of tumours. 1
Claims22
Compounds of the formula I
- 15
- in which
- R1 is CN, CON(R3)2, [C(R4)2]nN(R3)2, C(═NH)—NH2, which may also be monosubstituted by —COR3, —COOR3, OR3, OCOR2, OCOOR3or by a conventional amino-protecting group, or is
- 16
- R2 is H, Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3 )2, [C(R4)2]n—Ar, [C(R4)2]n-Het or [C(R4)2]ncycloalkyl,
- R3 is H, A, [C(R4)2]n—Ar, [C(R4)2]n-Het or [C(R4)2]ncycloalkyl,
- R4 is H or A,
- W is —[C(R4)2]n—,
- T is —[C(R4)2]n— or CONR3,
- Y is Het or
- phenyl, naphthyl or biphenyl, each of which is unsubstituted or monosubstituted, disubstituted or trisubstituted by Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2N(R4)2, S(O)mA, R1, Het, CO-Het1, NR4COHet1 or SO2Het1,
- Ar is phenyl, naphthyl or biphenyl, each of which is unsubstituted or monosubstituted, disubstituted or trisubstituted by Hal, A, OR4, N(R4)2, NO2, CN, COOR4, CON(R4)2, NR4COA, NR4CON(R4)2, NR4SO2A, COR4, SO2N(R4)2 or S(O)mA,
- Het is a monocyclic or bicyclic saturated, unsaturated or aromatic heterocyclic radical having from 1 to 4 N, O and/or S atoms, which may be unsubstituted or monosubstituted, disubstituted or trisubstituted by carbonyl oxygen, Hal, A, [C(R4)2]n—Ar, [C(R4)2]n-Het2, [C(R4)2]ncycloalkyl, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 and/or S(O)nA,
- Het1 is a monocyclic 3-7-membered, saturated heterocyclic radical having 1 to 2 N, O and/or S atoms,
- Het2 is a monocyclic or bicyclic saturated, unsaturated or aromatic heterocyclic radical having 1 to 2 N, O and/or S atoms, which may be unsubstituted or monosubstituted or disubstituted by carbonyl oxygen, Hal, A, OR3, N(R3 )2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 and/or S(O)nA,
- A is unbranched or branched alkyl having 1-6 carbon atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups and/or in addition 1-7 H atoms may be replaced by F,
- Hal is F, Cl, Br or I,
- n is 0, 1 or 2,
- m is 0, 1 or 2,
- and pharmaceutically usable derivatives, solvates and stereoisomers thereof, including mixtures thereof in all ratios.
17 more elements
Dependencies are inferred from the claim text.