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US 2013/0158005 A1Published application
Pyrimidine derivatives as fak inhibitors
AssigneeMerck Patent GmbH
InventorsTimo Heinrich, Christina Esdar, Hartmut Greiner
Life of this patent
Estimating the term…
Abstract
Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
Claims12
Compounds of the formula I
- in which
- R1 denotes (CH2)nAr1 or (CH2)nHet1,
- R2 denotes Ar2 or Het2,
- R3 denotes H, Hal, A, Het4 or CN,
- Ar1 denotes phenyl which is unsubstituted or mono-, di-, tri-, tetra or pentasubstituted by Hal, A, (CH2)nOH, (CH2)nOA, (CH2)nCN, NO2, SO2A, COOH, COOA, NH2, NHA, NA2, NHCH2Ar1, CHO, COA, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, Het3, NHCOHet3, SO2NH2, SO2NHA and/or NHCOA,
- Ar2 denotes phenyl which is unsubstituted or mono-, di-, tri-, tetra or pentasubstituted by Hal, A, (CH2)nOH, (CH2)nOA, (CH2)nCN, NO2, SO2A, COOH, COOA, NH2, NHA, NA2, NHCH2Ar1, CHO, COA, (CH2)nCONH2, (CH2)nCONHA, (CH2)nCONA2, SO2NH2, NHSO2A, SO2NHA, NA′SO2A, C(R4R5)CN and/or NHCOA,
- Het1 denotes a mono- or bicyclic aromatic, unsaturated or saturated heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di-, tri- or tetrasubstituted by Hal, A, NH2, NHA, NA2, COOH, CN, NHCOA, CN, NHCOA, COA, OAr, COOA, CONH2, CONHA, CONA2, CONHAr and/or ═O,
- Het2 denotes a mono- or bicyclic aromatic heterocycle having 1 to 4 N, O and/or S atoms, which may be unsubstituted or mono-, di-, tri- or tetrasubstituted by Hal, A, NH2, NHA, NA2, COOH, COA, COOA, CONH2, CONHA, CONA2, CONHAr, C(R4R5)CN, NHSO2A, NASO2A, NHCOA, NA′COA, NACHO, NH(CH2)pNHCHO and/or ═O,
- Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal and/or A,
- R4, R5 each, independently of one another, denote H or A,
- R4 and R5 together also denote alkylene having 2-5 C atoms, in which one CH2 group may be replaced by NH, NA', O or S,
- Het3 denotes a mono- or bicyclic aromatic, unsaturated or saturated heterocycle having 1 to 3 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by A, NH2 and/or ═O,
- Het4 denotes a monocyclic aromatic heterocycle having 1 to 3 N, O and/or S atoms, which may be unsubstituted or mono- or disubstituted by A,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7H atoms may be replaced by F and/or in which one or two non-adjacent CH and/or CH2 groups may be replaced by O, NH, NA′, S, SO, SO2 and/or by CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- A′ denotes unbranched or branched alkyl having 1-6 C atoms,
- Hal denotes F, Cl, Br or I,
- n denotes 0, 1, 2, 3 or 4,
- p denotes 1, 2, 3 or 4,
- and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
18 more elements
Dependencies are inferred from the claim text.