HETEROCYCLIC COMPOUND OF PYRIMIDIN-4(3H)-ONE, METHOD FOR PRODUCTION THEREOF AND PHARMACEUTICAL USE THEREOF Russian patent published in 2025 - IPC C07D401/14 C07D471/04 C07D491/107 C07D519/00 A61K31/506 A61K31/513 A61K45/06 A61P35/00 A61P43/00 

Abstract RU 2839367 C1

FIELD: medicine.

SUBSTANCE: invention relates to a compound of general formula (II) or pharmaceutically acceptable salts, stereoisomers, stable isotopic derivatives and mixtures thereof, which can be used to treat and/or prevent diseases associated with abnormal SHP2 activity. In formula (II), ring A is selected from the group consisting of a phenyl ring and 6-member heteroaryl ring containing one heteroatom selected from N; ring B is selected from the group consisting of 5-member heteroaryl ring fused with ring A, where 5-member heteroaryl ring contains one or two heteroatoms selected from N; and wherein the phenyl ring and the heteroaryl ring are optionally substituted with one or more substituents selected from the group consisting of D, halogen, cyano, C1-6 alkyl, -ORa and -NRaRb; R1 is selected from a group consisting of H, D, cyano, C1-2 alkyl and -NRaRb; R2 is selected from a group consisting of H and C1-2 alkyl, where one or more hydrogen atoms of the alkyl are optionally substituted with one or more substitutes selected from the group consisting of D and fluorine; R4a and R4b each is independently selected from a group consisting of C1-6 alkyl, where alkyl is optionally substituted with one or more substitutes selected from the group consisting of D or -NRaRb; R4a and R4b optionally together with the carbon atom to which the R4a and R4b, form C3-7 carbocyclic ring or 4–7 membered heterocyclic ring containing one oxygen; Ra and Rb each independently represents H. Invention also relates to a compound of general formula (IV), in which X is selected from the group consisting of -O- and -CH2-; R7 is selected from a group consisting of H, D and C1-2 alkyl, where one or more hydrogen atoms of the alkyl are optionally substituted with one or more substitutes selected from the group consisting of D and fluorine; values A, B, R1 and R2 are defined above. Invention also relates to specific compounds, a pharmaceutical composition containing said compounds and use thereof to produce a medicinal agent.

EFFECT: treatment and/or prevention of diseases associated with abnormal activity of SHP2, and treatment and/or prevention of diseases associated with SHP2, wherein the diseases are cancer selected from leukaemia, Noonan syndrome, leopard syndrome, neuroblastoma, melanoma, lung cancer, breast cancer, oesophagus cancer, colon cancer, head and neck cancer and stomach cancer.

6 cl, 3 tbl, 19 ex

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RU 2 839 367 C1

Authors

Chen, Syanyan

Gao, Insyan

Dates

2025-04-30Published

2021-01-13Filed