Back to results
US 8,541,584 B2Granted
3-(1,2,3-triazol-4-yl) pyrrolo [2,3-b] pyridine derivatives
AssigneeMerck Patent GmbH
InventorsDieter Dorsch, Margarita Wucherer-Plietker, Thomas J. J. Mueller, Eugen Merkul
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 inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
Claims16
A compound of formula I
- in which
- R1 denotes A, —[C(R3)(R4)]nAr, —[C(R3)(R4)]nHet or —[C(R3)(R4)]nCyc,
- R2 denotes H, A, Hal, CN, —[C(R3)2]n—Ar′, —[C(R3)2]n—Het′, —[C(R3)2]n—Cyc, OR3 or N(R3)2,
- R3 denotes H or A,
- R4 denotes H, A, —[C(R3)2]nOR3, —[C(R3)2]nCOOR3, —[C(R3)2]nN(R3)2 or —[C(R3)2]nHet,
- A denotes unbranched or branched alkyl having 1-6 C atoms, in which one or two CH2 groups are each optionally replaced by O, N or S atoms or —CH═CH— groups and/or 1-7 H atoms are each optionally replaced by F,
- Cyc denotes cycloalkyl having 3, 4, 5, 6 or 7 C atoms,
- Ar denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, —[C(R3)2]nOR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2N(R3)2 and/or S(O)nA,
- Ar′ denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, CO—Het1, Het1, [C(R3)2]nN(R3)2, [C(R3)2]nHet1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]n—N(R3)2, OCONH[C(R3)2]nHet1, CO—Het1, CHO and/or COA,
- 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, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3 and/or S(O)nA,
- Het′ denotes a mono-, bi- or tricyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms which is unsubstituted or may be mono- or disubstituted by Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, CO—Het1, Het1, [C(R3)2]nN(R3)2, [C(R3)2]nHet1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]n—Het1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO—Het1, CHO, COA, ═S, ═NH, ═NA and/or ═O,
- Het1 denotes a monocyclic saturated heterocycle having 1 to 2 N and/or O atoms, which is unsubstituted or mono- or disubstituted by A, OA, OH, Hal and/or ═O,
- Hal denotes F, Cl, Br or I
- N denotes 0, 1 or 2,
- or a pharmaceutically usable salt, tautomer or stereoisomer thereof, including mixtures thereof in all ratios.
12 more elements
Dependencies are inferred from the claim text.