PYRIMIDINE DERIVATIVE THAT SUPPRESSES CANCER CELL GROWTH AND MEDICAL APPLICATION THEREOF Russian patent published in 2023 - IPC C07D239/48 C07D239/42 C07D401/12 C07D403/12 C07D495/04 A61K31/505 A61K31/506 A61K31/519 A61P35/00 

Abstract RU 2792849 C1

FIELD: oncology.

SUBSTANCE: invention relates to a compound with formula 1 or a pharmaceutically acceptable salt thereof, as well as a pharmaceutical composition for the treatment or prevention of lung cancer expressing a mutation in the epidermal growth factor receptor. In general formula 1, A, B, D, E and G are combinations of A=N, B=C, D=C, E=C and G=N or combinations of A=N, B=C, D=N, E =C and G=C, W is oxygen or NH, X and Y are each independently CH, oxygen or nitrogen, Z1 and Z2 are each independently C1-C 4 alkyl or each independently consists of a carbon atom and linked to each other to form a 6-membered heterocyclic ring containing 1 N together with X and Y provided that when X is oxygen then Z1 is absent and when Y is oxygen then Z2 is absent, R1 is C1-C4 alkyl, R2 is hydrogen or C1-C4 alkyl, R3 and R4 are each independently hydrogen, halogen, OH, OMe, OEt, CN, CF3, C1-C4-alkyl or linked to each other with the formation of a 5- or 6-membered heteroaryl ring, which contains at least one heteroatom selected from the group consisting of N, O and S, R5 represents hydrogen, halogen, OH, OMe, OEt, CN, CF3 or C1-C4-alkyl, R6 and R7 are each independently hydrogen, halogen, OH, OMe, OEt, CN, CF3, COOH, COO-C1-C4-alkyl, COO-C1-5-cycloalkyl, C1 -C4 -alkyl or connected to each other to form a 5- or 6-membered heteroaryl ring, R8 is hydrogen, halogen, OH, OMe, OEt, CN, CF3 or C1-C4-alkyl, R9 represents -C(O)-CH=CH2 or C1-C4-alkyl, and R10 is absent, represents hydrogen, halogen, C1-C4-alkyl, OH, OMe, OEt, CN, CF3, NMe2, piperazine substituted with C1-C3 alkyl piperazine, morpholine or morpholine substituted with C1-C3 alkyl.

EFFECT: providing compounds suitable for the treatment of lung cancer expressing a mutation in the epidermal growth factor receptor.

5 cl, 1 tbl, 1 ex

1

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RU 2 792 849 C1

Authors

Ryu, Hyung-Chul

Kim, Jae-Sun

Kim, Sung-Eun

Lee, Sun-Ho

Lee, Yong-Hyub

Dates

2023-03-27Published

2020-06-19Filed