| 摘要 |
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to new pyrimidine derivatives and their pharmaceutically acceptable salts possessing the properties of a mTOR kinase inhibitor. In formula (I):A represents a 6-8-member mono- or bicyclic heterocyclic ring containing 1 to 2 heteroatoms optionally specified in N and O as apexes of the ring and having 0-2 double bonds; and wherein the ring A is additionally substituted by 0 to 2 substitutes Rspecified in a group consisting of -OR, -Rand -(CH)-ORwherein Ris optionally specified in hydrogen and Calkyl; Rrepresents Calkyl; G is specified in a group consisting of -C(O)-, -OC(O)-, -NHC(O)- and -S(O)-; B is specified in a group consisting of phenylene and 5-6-member heteroarylene consisting 1-2 nitrogen heteroatom as apexes of the ring, and substituted by 0 to 1 substitutes Rspecified in F, Cl, Br, I and R; wherein Rrepresents Calkyl; D is specified in a group consisting of -NRC(O)NRR, -NRR, C(O)NRR, -NRC(=N-CN)NRR, -NRC(O)R, -NRC(O)ORand -NRS(O)R, and wherein the group D and a substitute placed on an adjoining atom in the ring B, optionally combined to form a 5-6-member heterocyclic or heteroaryl ring containing 1 to 3 heteroatoms specified in N, O and S, as apexes of the ring and substituted by the substitute 0-1 R. The R-Rradical values are presented in the patent claim.EFFECT: invention also refers to a pharmaceutical composition containing said compounds, and to the use of the compounds for preparing a drug for treating a malignant tumour mediated by mTOR kinase activity.33 cl, 13 dwg, 4 tbl, 498 ex |
