PYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE Russian patent published in 2013 - IPC C07D403/14 C07D413/14 C07D405/14 C07D401/14 C07D417/14 C07D471/02 C07D471/12 A61K31/519 A61P35/00 

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 R^A specified in a group consisting of -OR^a, -R^c and -(CH₂)_1-4-OR^a wherein R^a is optionally specified in hydrogen and C_1-6alkyl; R^c represents C_1-6alkyl; G is specified in a group consisting of -C(O)-, -OC(O)-, -NHC(O)- and -S(O)_0-2-; 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 R^B specified in F, Cl, Br, I and R^p; wherein R^p represents C_1-6 alkyl; D is specified in a group consisting of -NR³C(O)NR⁴R⁵, -NR⁴R⁵, C(O)NR⁴R⁵, -NR³C(=N-CN)NR⁴R⁵, -NR³C(O)R⁴, -NR³C(O)OR⁴ and -NR³S(O)₂R⁴, 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^D. The R¹-R⁵ radical 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