| 摘要 |
FIELD: medicine.SUBSTANCE: invention refers to new heteroaryl compounds of general formula (I) and their pharmaceutically acceptable salts possessing the properties of protein kinase inhibitor, such as mTOR, IKK-2, Tyk2, Syk-kinase. In formula (I)Rrepresents substituted or unsubstituted Calkyl, substituted or unsubstituted aryl, specified in phenyl, substituted or unsubstituted 5-6-member heteroaryl with 1-3 nitrogen atoms in a cycle specified in pyridine, pyrazole, indole, indazole, triazole, benzimidazole, 2-(1H-imidazo-[4,5-b]pyridine, substituted or unsubstituted 5-7- member cycloalkyl or substituted or unsubstituted heterocycloalkyl specified in pyrrolidinyl; -X-A-B-Y- taken together form -N(R)CHC(O)NH-, -N(R)C(O)CHNH-, -N(R)C(O)NH-, -N(R)C=N- or -C(R)=CHNH-; L represents a direct bond, NH or O; Rrepresents substituted or unsubstituted Calkyl, substituted or unsubstituted aryl specified in phenyl, tetrahydronaphthalene, unsubstituted 5-7- member mono- or 8- member bicycloalkyl; and Rand Rindependently represent H or Calkyl. The substitutes in the substituted groups are specified in one or more halogen, Calkyl, hydroxyl, amino, nitro, thiol, Calkyl thioether, cyano, carboxyl, Calkyl ester, halogen alkyl, Ccycloalkyl or heteroaryl specified in pyridyl, triazole, O-lower alkyl, aryl specified in phenyl, phenyl-lower alkyl, COCH, CONH, OCHF, CFor OCFgroups wherein CONHgroup may be substituted by cyclohexyl.EFFECT: compounds can find application for treating or preventing cancer, inflammatory pathological conditions, metabolic pathological conditions.24 cl, 8 dwg, 2 tbl, 169 ex |
