PYRIDOPYRIMIDINE COMPOUNDS ACTING AS DOUBLE INHIBITORS OF mTORC 1/2 Russian patent published in 2022 - IPC C07D471/04 C07D519/00 A61K31/5377 A61K31/5383 A61K31/5386 A61P35/00 A61P35/02 

Abstract RU 2771201 C2

FIELD: pharmaceutics.

SUBSTANCE: invention relates to the field of organic compounds. A compound of the formula (IV), its pharmaceutically acceptable salt, or its stereoisomer is proposed, where R1 is H; R2 is Me; alternatively, R1, R2 and N atom in morpholine ring form 5-6-element heterocycloalkyl; R3 is selected from NH2, 5-6-element heteroaryl and n is selected from 1 and 2; ring A is selected from phenyl, 9- and 10-element heteroaryl; R4 and R5 are H; alternatively, R4 and R5 are joined together to form 5-6-element heterocycloalkyl; D1, D2, D3 and D4 are respectively selected from a single bond, -CH2-, -CH2CH2- and -O-, and at least one of D1, D2, D3 and D4 is not a single bond, where -CH2- or -CH2CH2- is optionally substituted with R, and R is equal to 1; D5, D6, D7 and D8 are respectively selected from a single bond, -CH2-, -O- and -NH-, and at least one of D5, D6, D7 and D8 is not a single bond, where -CH2- is optionally substituted with R, and R is equal to 1 or 2, -NH- is optionally substituted with R; T1 is selected from CH and N; T2 is selected from -CH2-, -NH-, -O-, -S- and -C(=O)NH-, where -CH2 is optionally substituted with R, and R is equal to 1 or 2, -NH is optionally substituted with R; where R is respectively selected from CF3, F, OH, C1-3alkyl and C1-3alkoxy; 5-6-element heteroaryl, 9-element heteroaryl and 10-element heteroaryl respectively contain 1, 2 or 3 heteroatoms or heteroatomic groups independently selected from -O-, -NH- and N. Specific compounds, a pharmaceutical composition, and the use of a compound of the formula (IV) for the preparation of a drug for the treatment of breast cancer are also proposed.

EFFECT: production of pyridopyrimidine compounds that have a double inhibitory activity against mTOR1/2.

17 cl, 9 tbl, 56 ex

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RU 2 771 201 C2

Authors

Chen, Kevin X

Chen, Zhaoguo

Zhang, Li

Yu, Yanxin

Zhou, Kai

Hu, Boyu

Wang, Xiaofei

Hu, Guoping

Li, Jian

Chen, Shuhui

Dates

2022-04-28Published

2018-11-02Filed