| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: present invention refers to new compounds of formula 1a:, wherein Q1 and Q2, each separately and independently is specified in a group consisting of N and C-Z6, provided both Q1 and Q2 are not C-Z6 simultaneously; E1 represents phenyl, and wherein the cycle E1 is substituted by one or more residues R16, and wherein the cycle E1 is substituted by one or more residues R18; wherein A is specified in a group consisting of phenyl or pyrazolyl; G1 means pyrazolyl; the cycle A is substituted in any substituted position by one residue A1, wherein A1 is specified in a group consisting of A2 and A3; A2 and A3 are those as specified in cl.1 of the patent claim, the cycle A is optionally substituted by one or more residues R2; X2 represents a direct bond wherein E1 is independently bound to the group NR3 in formula 1a; X3 represents -O-; V and V2 represent H2, and VI is independently specified in a group consisting of Hor O; each Z2 is independently and separately specified in a group consisting of hydrogen, C1-C6-alkyl; each Z3 is independently and separately specified in a group consisting of H, C1-C6-alkyl, branched C3-C7-alkyl and - (CH2)N(R4); each Z4 represents H; each Z6 is independently and separately specified in a group consisting of H, C1-C6-alkyl, branched C3-C7-alkyl, hydroxyl, hydroxy-C3-C6-alkyl, branched hydroxy-C2-C6-alkyl-, (R3)N-, (R4)N-, -N(R3)C(O)R8, C(O)N(R4), halogen, -(CH)G1 and -R17; each R2 is specified in a group consisting of C1-C6-alkyl and branched C3-C8-alkyl; each R3 represents H; each R4 represents H, C1-C6-alkyl or branched C3-C7-alkyl; each R8 is independently and separately specified in a group consisting of C1-C6-alkyl and branched C3-C7-alkyl; each R16 is independently and separately specified in a group consisting of C1-C6-alkyl, branched C3-C7-alkyl, halogen and a cyano group; each R17 represents pyrazolyl; wherein R17 may be additionally substituted by one or more residues Z2 or Z3; R18 represents hydrogen; and n is equal to 0-6; p is equal to 1-4; q is equal to 2-6; r is equal to 0 or 1; t is equal to 1-3, v is equal to 1 or 2. Besides, the invention describes a method for modulation of wild-type kinase activity, a pharmaceutical composition for treating hyperproliferative diseases in cancer in mammals; there are also described methods of treating cancer in a patient.EFFECT: there are prepared and described new compounds which can find the application in modulation of kinase activity.20 cl, 56 ex, 2 tbl |
