Back to results
US 2011/0218198 A1Published application
Pyrrolopyridinylpyrimidin-2-ylamine derivatives
AssigneeMerck Patent Gesellschaft
InventorsMargarita Wucherer-Plietker, David Bruce, Dirk Finsinger, Ulrich Graedler, Dieter Dorsch, Christina Esdar
Life of this patent
Estimating the term…
Abstract
Compounds of the formula I in which X, R1, R2, R3, R4 and R6 have the meanings indicated in Claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.
Claims21
Compounds of the formula I
- in which
- R1 denotes H or A,
- R2 denotes A, Hal, CN, (CH2)nCONH(CH2)pAr, —C(OH)R5—Ar, —[C(R)2]n—Ar, —[C(R5)2]n-Het, —[C(R5)2]n-cycloalkyl, —NR5A, —NR5Ar, NR5Het, —[C(R5)2]mN(R5)2, 1-hydroxycyclopentan-1-yl or 1-hydroxycyclohexan-1-yl,
- R3 denotes H, R5, —[C(R5)2]n—Ar, —[C(R5)2]n-Het, —[C(R5)2]n-cycloalkyl,
- R4 denotes H, Het-, Ar—, —R5, —OR5, —[C(R6)2]C(O)N(R6)2, CO-Het or O(CH2)pHet1,
- R5 denotes H, A or cycloalkyl,
- R6 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 F,
- cycloalkyl denotes cyclic alkyl having 3-7 C atoms, which may additionally be substituted by alkyl having 1-6 C atoms,
- A denotes unbranched or branched alkyl having 1-10 C atoms, in which one or two CH and/or CH2 groups may be replaced by N, O, S atoms and/or by —CH═CH— groups and/or in addition 1-7 H atoms may be replaced by F,
- X denotes NH, O, S or SO2,
- Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR5, N(R5)2, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, COR5, SO2N(R)2 and/or S(O)pA,
- Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, and/or O and/or S atoms which is unsubstituted or mono- or disubstituted by Hal, A, OR5, (CH2)pN(R5)2, NO2, CN, (CH2)pCOOR5, (CH2)pCON(R5)2, NR5COA, (CH2)pHet1, (CH2)pCOHet1, NR5SO2A, COR5, SO2NR5 and/or S(O)pA,
- Het1 denotes a saturated heterocycle having 1 to 4 N, O, and or S atoms which is unsubstituted or mono- or disubstituted by A, S(O)pA and/or COA,
- Hal denotes F, Cl, Br or I,
- m denotes 1, 2, 3 or 4,
- n denotes 0, 1, 2, 3 or 4,
- p denotes 0, 1 or 2,
- and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
16 more elements
Dependencies are inferred from the claim text.