BENZAZEPINE COMPOUNDS, CONJUGATES AND THEIR USE Russian patent published in 2022 - IPC C07D403/12 C07D223/16 A61K31/55 A61P35/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound represented by a structure of the formula (IIA) or to its pharmaceutically acceptable salt, where is a double bond, L¹⁰ is selected from -C(O)- and -C(O)N(R¹⁰)-*, where * is a place of bond of L¹⁰ with R⁵, L² is -C(O)-, each of R¹ and R² is hydrogen, R⁴ is -N(R¹⁰)₂, R⁵ is selected from C_9-10 bicyclic carbocycle and 9-10-element condensed 5-6 or condensed 6-6 bicyclic heterocycle containing 1 or 2 heteroatoms independently selected from nitrogen, oxygen, and boron, where R⁵ is optionally substituted, and where substitutes are independently selected in each case from: -OR¹⁰, -N(R¹⁰)₂, -C(O)OR¹⁰, =O, and -CH₃ optionally substituted with -N(R¹⁰)₂ or phenyl optionally substituted with -C(O)N(R¹⁰)₂, and R¹⁰ is independently selected in each case from hydrogen, -C(O)OCH₂C₆H₅ and C_1-6 alkyl optionally substituted with halogen, -NH₂, -NHC(O)OCH₂C₆H₅ or phenyl. The invention also relates to conjugates with a structure based on an antibody and pharmaceutical compositions having TLR8 agonist activity based on the compound of the formula (IIA).

EFFECT: new compounds, conjugates, and a pharmaceutical composition based on them are obtained, which can be used in medicine for the treatment of cancer.

41 cl, 10 dwg, 6 tbl, 16 ex