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US 2011/0257172 A1Published application
3-(3-Pyrimidine-2-yl-benzyl)-[1,2,4] triazolo[4,3-b]pyrimidine derivatives
AssigneeMerck Patent GmbH
InventorsOliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I, in which R1, R2, R3, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Claims22
Compounds of the formula I
- in which
- R1 denotes Ar, Het, A, CONHA, CONA2, OA, OHet, OAr, N(R5)2, NR5[C(R5)2]nHet, NR5[C(R5)2]nAr, COHet, SO2NHA or SO2NA2,
- R2 denotes H, A, Hal, OR5, N(R5)2, N═CR5N(R5)2, SR5, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2, S(O)mA, Het, [C(R5)2]nN(R5)2, [C(R5)2]nHet, O[C(R5)2]nN(R5)2, O[C(R5)2]nHet, S[C(R5)2]nN(R5)2, S[C(R5)2]nHet, —NR5[C(R5)2]nN(R5)2, —NR5[C(R5)2]nHet, NHCON(R5)2, NHCONH[C(R5)2]nN(R5)2, NHCONH[C(R5)2]n-Het, NHCO[C(R5)2]nN(R5)2, NHCO[C(R5)2]nHet, CON(R5)2, CONR5[C(R5)2]nN(R5)2, CONR5[C(R5)2]nHet, COHet, COA, O[C(R5)2]nNR5COZ, O[C(R5)2]nNR5COHet1, O[C(R5)2]nCyc[C(R5)2]nN(R5)2, O[C(R5)2]nCyc[C(R5)2]nOR5, O[C(R5)2]nCyc[C(R5)2]nHet1,
- O[C(R5)2]nCR5(NR5)2COOR5, O[C(R5)2]nNR5CO[C(R5)2]nNR5COA, O[C(R5)2]nNR5COOA, O[C(R5)2]nCO—NR5-A, O[C(R5)2]nCO—NR5—[C(R5)2]nHet1, O[C(R5)2]nCONH2,. O[C(R5)2]nCONHA, [C(R5)2]nCONA2 or O[C(R5)2]nCO—NR5—[C(R5)2]nN(R5)2
- Z denotes CR5(NR5)2CR5(OR5)A,
- Cyc denotes cycloalkylene having 3-7 C atoms,
- R3, R3′ each, independently of one another, denote H, F or A, together also denote alkylene having 2-5 C atoms,
- R4 denotes H, A or Hal,
- R5 denotes H or A,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which 1-7 H atoms may be replaced by OH, F, Cl and/or Br, and/or in which one or two CH2 groups may be replaced by O, NH, S, SO, SO2 and/or CH═CH groups,
- or
- cyclic alkyl having 3-7 C atoms,
- Ar denotes phenyl, naphthyl or biphenyl, each of which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR5, N(R5)2, SR5, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2 and/or S(O)mA,
- Het denotes a mono-, bi- or tricyclic 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 Hal, A, OR5, N(R5)2, SR5, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2, S(O)mA, CO-Het1, Het1, [C(R5)2]n-N(R5)2, [C(R5)2]nHet1, O[C(R5)2]nN(R5)2, O[C(R5)2]nHet1, NHCOOA, NHCON(R5)2, NHCOO[C(R5)2]nN(R5)2, NHCOO[C(R5)2]nHet1, NHCONH[C(R5)2]nN(R5)2, NHCONH[C(R5)2]nHet1, OCONH[C(R5)2]nN(R5)2, OCONH[C(R5)2]nHet1, CO-Het1, CHO, COA, ═S, ═NH, ═NA and/or ═O (carbonyl oxygen),
- Het1 denotes a monocyclic saturated heterocycle having 1 to 2 N and/or O atoms, which may be mono- or disubstituted by A, OA, OH, Hal and/or ═O (carbonyl oxygen),
- Hal denotes F, Cl, Br or I,
- m denotes 0, 1 or 2,
- n denotes 1, 2, 3 or 4,
- and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
16 more elements
Dependencies are inferred from the claim text.