Substituted imidazo[1,2-a]pyrimidines and —pyridines

摘要

Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.;

主权项

1. A compound of formula (I) in which R1 is hydrogen, hydroxy, halogen, cyano, CO-(1-6C-alkyl), C(O)OR10, CO(NR8R9), NR8R9, NH—C(O)NR8R9, NH—C(O)R11, 2-6C-alkinyl, or
a group selected from 1-6C-alkyl, 2-6C-alkenyl, 1-6C-alkoxy, 3-7C-cycloalkyl, aryl, heteroaryl, -(1-6C-alkylen)-aryl, -(1-6C-alkylen)-heteroaryl, —O-(3-7C-cycloalkyl), —O-aryl, —O-(3-7C-heterocyclyl), —O-heteroaryl, —O-(1-6C-alkylen)-(3-7C-cycloalkyl), —O-(1-6C-alkylen)-aryl, —O-(1-6C-alkylen)-(3-7C-heterocyclyl), —O-(1-6C-alkylen)-heteroaryl,
wherein said group is optionally substituted independently with one or more substituents selected from:hydroxy, halogen, 1-6C-alkyl, 1-4C-haloalkyl, 1-6C-alkoxy, —NR8R9, cyano, (═O), —C(O)NR8R9, —C(O)OR10, —NHC(O)R11, —NHS(O)2R11, heteroaryl,
wherein said substituent can be optionally substituted with 1-6C-alkoxy, R2 is hydrogen, hydroxy, halogen, cyano, CO-(1-6C-alkyl),C(O)OR10, CO(NR8R9), NR8R9, —NH—C(O)R11, —NH—C(O)NR8R9, —NHS(O)2R11 or
a group selected from 1-6C-alkyl, 2-6C-alkenyl, 1-6C-alkoxy, 3-7C-cycloalkyl, aryl, heteroaryl,
wherein said group is optionally substituted independently with one or more substituents selected from:hydroxy, halogen, 1-6C-alkyl, 1-4C-haloalkyl, 1-6C-alkoxy, —NR8R9, cyano, —C(O)NR8R9, —C(O)OR10, —NHC(O)R11, —NHS(O)2R11, NH-(1-6C-alkyl)-O-(1-6C-alkyl), R3 is hydrogen, 1-6C-alkyl, R4 is phenyl optionally substituted by 1-6C-alkyl, halogen, cyano, R5 is hydrogen, halogen, R6 is hydrogen, 1-6C-alkyl, A is N, C(R7), R7 is hydrogen, hydroxy, halogen, cyano, C(O)OR10, CO(NR8R9), 3-7C-cycloalkyl, or
a group selected from 1-6C-alkyl, 2-6C-alkenyl, 1-6C-alkoxy, aryl, heteroaryl,
wherein said group is optionally substituted independently with one or more substituents selected from:hydroxy, halogen, 1-6C-alkyl, 1-4C-haloalkyl, 1-6C-alkoxy, —NR8R9, cyano, —C(O)NR8R9, —C(O)OR10, —NHC(O)R11, —NHS(O)2R11, X is —CH2—, Y is —CH2—, —CH(OH)—, R8, R9 which can be the same or different, is hydrogen, hydroxy, 3-7C-cycloalkyl or
a group selected from 1-4C-alkyl, 1-6C-alkoxy, wherein said group is optionally substituted, independently with one or more substituents selected from:
halogen, hydroxy, mono- or di-(1-4C-alkylamino), 1-4C-alkoxy, or 3-7C-cycloalkyl or,R8 and R9 together with the nitrogen to which they are attached may also form a saturated or unsaturated 3-6C-heterocyclic ring,
which is optionally substituted by (═O) R10 is hydrogen, 1-6C-alkyl, R11 is 1-4C-alkyl (optionally substituted independently with one or more halogen or hydroxyl groups) or 3-7C-cycloalkyl, or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer.