PYRIDINO[1,2-A]PYRIMIDONE ANALOGUE USED AS AN MTOR/PI3K INHIBITOR Russian patent published in 2018 - IPC C07D471/04 C07D487/04 C07D491/147 

FIELD: chemistry.

SUBSTANCE: invention relates to a new compound of formula (I) or its pharmaceutically acceptable salt possessing the properties of inhibitor mTOR/PI3K. Action of the double inhibitor allows simultaneously blocking multiple signal transduction sites and more efficient prevention of signal transduction, thereby overcoming or delaying the drug resistance, and has a longer and more effective effect in the cancer treatment. In the compound of formula (I) structural unit can be replaced by or ; E is selected from the group consisting of C_3-6 cycloalkyl or C_1-6 alkyl substituted with R₃, and number R₃ is 0, 1, 2 or 3, or E is selected from the group consisting of and , or E is selected from the group consisting of and optionally substituted with 1, 2 or 3 R₃; where zero, one, two or three of G_1~5 are selected from N, and the remaining ones are selected from C(R₃); G₆ is selected from the group consisting of -C(R₃)(R₃)-, -C(=O)N(R₃)-, -N(R₃)-, -C(=NR₃)-, -S(=O)₂N(R₃)-, -S(=O)N(R₃)-, -O-, -S-, -C(=O)O-, -C(=O)-, -C(=S)-, -S(=O)-, -S(=O)₂- and -N(R₃)C(=O)N(R₃)-; zero, one or two of G_7~9 are selected from N, and the remaining ones are selected from C(R₃); zero, one, two, three or four of G_10~16 are selected from N, and the remaining ones are selected from C(R₃); G₁₇ is selected from N or C(R₃); zero, one, two or three of G_18~22 are selected from the group consisting of -C(=O)N(R₃)-, -N(R₃)-, -C(=NR₃)-, -S(=O)₂N(R₃)-, -S(=O)N(R₃)-, -O-, -S-, -C(=O)O-, -C(=O)-, -C(=S)-, -S(=O)-, -S(=O)₂- and -N(R₃)C(=O)N(R₃)-, and the remaining ones are selected from -C(R₃)(R₃)-; one of L and Q is -S(=O)₂NH- and the other is a single bond; or one of L and Q is -S(=O)₂- and the other is CH₂; A and T are independently selected from N or CH; one of X and Y is selected from N and the other is selected from C(R₃); and Z is selected from CH, or X and Y is selected from C(R₃) and Z is selected from CH; B is selected from the group consisting of -N(R_a)-; heteroatom or heteroatom group are independently selected from the group consisting of -C(=O)N(R_a)-, -N(R_a)-, -C(=NR_a)-, -S(=O)₂N(R_a)-, -S(=O)N(R_a)-, -O-, -S-, -C(=O)O-, -C(=O)-, -C(=S)-, -S(=O)-, -S(=O)₂- and -N(R_a)C(=O)N(R_a)-; each m₁ is independently selected from 0, 1, 2 or 3; R₁ is independently selected from the group consisting of H, F, Cl, Br, I, OR_a, N(R_b)(R_c), C_1-3 alkyl, R₂ and R₃ are independently selected from the group consisting of H, F, Cl, Br, I, CN, OR_a, N(R_b)(R_c), C_1-3 alkyl optionally substituted with R_d, D₁ is selected from the group consisting of a single bond, -C(R_e)(R_e)-, -C(=O)N(R_a)-, -N(R_a)-, -C(=NR_a)-, -S(=O)₂N(R_a)-, -S(=O)N(R_a)-, -O- and -S-; D₂ is selected from -C(R_a)(R_a)-; n is selected from 1, 2, 3, 4, 5 or 6; R_a, R_b and R_c are independently selected from the group consisting of H, C_3-6 cycloalkyl or C_1-6 alkyl optionally substituted with R_d; R_e is selected from the group consisting of H, C_1-6 alkyl or alkoxy optionally substituted with R_d, C_3-6 cycloalkyl optionally substituted with R_d; R_d is selected from the group consisting of F, Cl, Br, I, CN, OH, CHO, COOH, CH₃, CF₃, CH₃O and CH₃CH₂O, and number R_d is selected from 0, 1, 2, or 3; optionally, R_a and R_a in the same D₂, two D₂, or R_a and one D₂ together with the same carbon atom or oxygen atom, to which they are both attached, form one 3-, 4-, 5- or 6-membered carbocyclic ring or an oxygen-containing heterocyclic ring, wherein the number of oxygen atoms is 1 or 2.

EFFECT: compounds can be used for treating cancer.

8 cl, 3 dwg, 4 tbl, 241 ex