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US 2007/0185189 A1Published application
Prolinylarylacetamides
AssigneeMerck Patent GmbH
InventorsWerner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz
Life of this patent
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Abstract
Novel compounds of the formula (I), in which R, R1, R2, R3, X, X′ and Y 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
- R denotes Hal, —C≡C—H, —C≡C-A or OA,
- R1 denotes H, ═O, Hal, A, OH, OA, A-COO—, Ph-(CH2)n—COO—, cycloalkyl-(CH2)n—COO—, A-CONH—, A-CONA-, Ph-CONA-, N3, NH2, NO2, CN, COOH, COOA, CONH2, CONHA, CON(A)2, O-allyl, O-propargyl, O-benzyl, ═N—OH, ═N—OA or ═CF2,
- X, X′ each, independently of one another, denote CH, CHal or N,
- Y denotes R4 or Hal,
- Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, OA, OH or Hal,
- R2 denotes H, Hal or A,
- R3 denotes H or A,
- R4 denotes OH, OA, A-COO—, NHA, NHAr, NAA′, Het or —NH—CHR5—COOR,
- R5 denotes H, A, —CHR3—OH, (CH2)n-Ph, (CH2)n—COOH, (CH2)n—CONH2, (CH2)p—NH2, (CH2)n—NH(═NH)NH2, (CH2)n-Het1 or (CH2)n—SR3,
- 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 A, OH, OA, CN, COOH, COOA and/or carbonyl oxygen (═O),
- Het1 denotes a mono- or bicyclic aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di- or trisubstituted by A, OH, OA and/or CN,
- A, A′ each, independently of one another, denote unbranched, branched or cyclic alkyl having 1-12 C atoms, in which, in addition, 1-7 H atoms may be replaced by F and/or chlorine,
- Ar denotes naphthyl, biphenyl, or 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]p—COOR3,
- Hal denotes F, Cl, Br or I,
- n denotes 0, 1, 2 or 3,
- p denotes 1, 2, 3, 4 or 5,
- and pharmaceutically usable derivatives, solvates, salts and stereoisomers thereof, including mixtures thereof in all ratios.
15 more elements
Dependencies are inferred from the claim text.