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US 2006/0135515 A1Published application
Heterocyclic amides and their use treating thromboembolic diseases and tumors
OwnerDieter Dorsch, Bertram Cezanne +4inventors
InventorsDieter Dorsch, Bertram Cezanne, Werner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Abstract
Novel compounds of the formula (I), in which D, W, X, Y, T 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
Claims23
Compounds of the formula I
- in which
- D denotes an aromatic five-membered heterocyclic ring having 1 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 NR3 or O,
- R1 denotes H, Ar, Het, cycloalkyl or A, which may be substituted by OR2, SR2, N(R2)2, Ar, Het, cycloalkyl, CN, COOR2 or CON(R2)2,
- R2 denotes H, A, —[C(R3)2]n—Ar, —[C(R3)2]n-Het, —[C(R3)2]n-cycloalkyl, —[C(R3)2]n—N(R3)2 or —[C(R3)2]n—OR3,
- R3 denotes H or A,
- W denotes —[C(R3)2]n—,
- Y denotes alkylene, cycloalkylene, Het-diyl or Ar-diyl,
- T denotes a mono- or bicyclic saturated, unsaturated or aromatic carbo- or heterocyclic ring having 0 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by Hal, A, —[C(R3)2]n—Ar, —[C(R3)2]n-Het, —[C(R3)2]n-cycloalkyl, OR3, N(R3)2, NO2, CN, COOR2 CON(R2)2, NR2COA, NR2CON(R2)2, NR2SO2A, COR2, SO2NR2 and/or S(O)mA and/or carbonyl oxygen,
- or N(R2)2
- and, if Y=piperidine-1,4-diyl, also R2 or cycloalkyl,
- 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, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)mA, —[C(R3)2]n—COOR2′ or —O—[C(R3)2]0—COOR2′,
- R2′ denotes H A, —[C(R3)2]n—Ar′, —[C(R3)2]n-Het′, —[C(R3)2]n-cycloalkyl, [C(R3)2]n—N(R3)2 or —[C(R3)2]n—OR3,
- R2″ denotes H, A, —[C(R3)2]n—Ar′ or —[C(R3)2]n-cycloalkyl, —[C(R3)2]n—N(R3)2 or —[C(R3)2]n—OR3,
- Ar′ denotes phenyl or benzyl, each of which is unsubstituted or mono- or disubstituted by Hal or A,
- Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocyclic ring having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, ═S, ═N(R3)2, Hal, A, —[C(R3)2]n—Ar, —[C(R3)2]n-Het1, —[C(R3)2]n-cycloalkyl, —[C(R3)2]n—OR2′, —[C(R3)2]n—N(R2′)2, NO2, CN, —[C(R3)2]n—COOR2′, —[C(R3)2]n—CON(R2′)2, —[C(R3)2]n—NR2′COA, NR2 CON(R2′)2, —[C(R3)2]n—NR2′SO2A, COR2′, SO2NR2′ and/or S(O)mA,
- Het1 denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocyclic ring having 1 to 2 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by carbonyl oxygen, ═S, ═N(R3)2, Hal, A, OR2″, N(R2″)2, NO2, CN, COOR2″, CON(R2″)2, NR2″COA, NR2″CON(R2″)2, NR2″SO2A, COR2″, SO2NR2″ and/or S(O)mA,
- Hal denotes F, Cl, Br or I,
- n denotes 0, 1 or 2,
- m 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.
20 more elements
Dependencies are inferred from the claim text.