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US 2006/0052376 A1Published application
Carboxamides
AssigneeMerck Patent GmbH
InventorsDieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Hanns Wurziger, Johannes Gleitz, Christoph Van Amsterdam
Life of this patent
Estimating the term…
Abstract
Novel compounds of the formula (I), in which D, W, X, Y, T, m and R1 have the meaning indicated 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.
Claims24
Compounds of the formula I
- in which
- D denotes aromatic carbo- or heterocycle having 0 to 4 N, O and/or S atoms which is unsubstituted or mono- or polysubstituted by Hal, A, OR2, N(R2)2, NO2, CN, COOR2 or CON(R2)2,
- X denotes —C═O or C(R3)2,
- W denotes —[C(R3)2]n—,
- R1 denotes H or A, which may be substituted by OR3, S(O)nR3, N(R3)2, CN, COOR3, CON(R3)2, OCON(R3)2, N(R3)COOR3, N(R3)CON(R3)2,
- N(R3)SO2R3, SO2N(R3)2 or —C≡C—,
- R2 denotes H, A, —[C(R3)2]n—Ar′, —[C(R3)2]n-Het′, —[C(R3)2]n-cycloalkyl, —[C(R3)2]—N(R3)2 or —[C(R3)2]n—OR3,
- R3 denotes H or A,
- Y denotes alkylene, cycloalkylene, Het-diyl or Ar-diyl,
- T denotes a mono- or bicyclic saturated, unsaturated or aromatic carbo- or heterocycle having 0 to 4 N, O and/or S atoms which is mono- or disubstituted by ═O, ═S, ═NR2, ═N—CN, ═N—NO2, ═NOR2, ═NCOR2, ═NCOOR2, ═NOCOR2 and may furthermore be mono-, di- or trisubstituted by R2, Hal, A, —[C(R3)2]n—Ar, —[C(R3)2]n-Het, —[C(R3)2]n-cycloalkyl, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2 and/or S(O)nA,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups and/or also 1-7H atoms may be replaced by F,
- Ar denotes phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2N(R2)2, S(O)nA,
- —[C(R3)2]n—COOR2 or —O—[C(R3)2]o—COOR2,
- Ar′ denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)nA, —[C(R3)2]n—COOR3 or —O—[C(R3)2]o—COOR3,
- Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, ═S, ═N(R2)2, Hal, A, —[C(R3)2]n—Ar,
- —[C(R3)2]n-Het′, —[C(R3)2]n-cycloalkyl, —[C(R3)2]n, —OR2,
- —[C(R3)2]n—N(R3)2, NO2, CN, —[C(R3)2]n—COOR2′
- —[C(R3)2]n—CON(R2)2, —[C(R3)2]n—NR2COA, NR2CON(R2)2,
- —[C(R3)2]n—NR2SO2A, COR2, SO2NR2 and/or S(O)nA,
- Het′ denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by carbonyl oxygen, ═S, ═N(R3)2, Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR3 and/or S(O)nA,
- Hal denotes F, Cl, Br or I,
- m denotes 1 or 2,
- n denotes 0, 1 or 2,
- o denotes 1, 2 or 3,
- and pharmaceutically usable derivatives, solvates and stereoisomers thereof, including mixtures thereof in all ratios.
22 more elements
Dependencies are inferred from the claim text.