MACROCYCLIC COMPOUND WITH FUNCTIONS OF WEE1 INHIBITOR AND ITS APPLICATION OPTIONS Russian patent published in 2022 - IPC C07D487/22 C07D519/00 A61K31/519 A61K31/5377 A61K31/551 A61P35/00 

Abstract RU 2783243 C2

FIELD: pharmaceutical chemistry.

SUBSTANCE: group of inventions relates to pharmaceutical chemistry and includes a compound of the formula (II), specific macrocyclic compounds specified in the claims, their stereoisomers and pharmaceutically acceptable salts, as well as their use in the manufacture of a drug. In the formula (II), R1 is selected from H and C1-3alkyl; R5 is selected from H and C1-3alkyl, where C1-3alkyl is optionally substituted with R, R6 is such as specified in the claims; r and m are equal to 1 or 2; D is selected from -N(R2)- and -C(R3)(R4)-; R2 is selected from H and C1-3alkyl; R3 and R4 are independently selected from H, F, Cl, Br, I, NH2, and C1-3alkyl, where NH2 is optionally substituted with R, while R is equal to 1,2, or 3; alternatively, R3 and R4, together with a carbon atom, to which they are attached, form 5-6-element heterocycloalkyl, which contains N as a heteroatom, a number of heteroatoms is equal to one or two, where 5-6-element heterocycloalkyl is optionally substituted with R, while R is equal to 1,2, or 3; R6 is selected from H, F, Cl, Br, I, C1-3alkoxy, and -O-C3-6cycloalkyl, where C1-3alkoxy is optionally substituted with R, while R is equal to 1, 2, or 3; R7 is selected from H, F, Cl, Br, I, C1-3alkyl, C1-3alkoxy, and 5-6-element heterocycloalkyl, which contains N as a heteroatom, a number of heteroatoms is equal to one or two, where C1-3alkyl, C1-3alkoxy, and 5-6-element heterocycloalkyl are optionally substituted with R, while R is equal to 1, 2, or 3; alternatively, R6 and R7, together with ring atoms, to which they are attached, form a ring A, while the ring A is 5-6-element heterocycloalkyl, which contains N as a heteroatom, a number of heteroatoms is equal to one or two, which optionally substituted with R, and R is equal to 1, 2, or 3; R is independently selected from OH, C1-3alkyl, C1-3alkoxy, and C1-3dialkylamino.

EFFECT: macrocyclic compounds showing inhibitory activity relatively to Wee1 kinase.

20 cl, 8 tbl, 42 ex

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RU 2 783 243 C2

Authors

Qian, Wenyuan

Yang, Chundao

Li, Zhengwei

Li, Jie

Li, Jian

Chen, Shuhui

Dates

2022-11-10Published

2018-10-31Filed