NEW BENZODIAZEPINE DERIVATIVES Russian patent published in 2019 - IPC C07D519/00 C07D487/14 A61K31/55 A61K31/5513 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (III) and formula (VI):

(III), or pharmaceutically acceptable salts, cytotoxic dimers, conjugates of monomers and dimers thereof, where: double line between N and C is a double bond, X is absent, and Y is H; W is C=O; R₅ is OR, SH or NHR; optional R₅ is a linking group or is selected from a polypyrrole, polyindolyl, polyimidazolyl, polypyrrole-imidazolyl, polypyrrole-indolyl or polyimidazole-indolyl link, optionally bearing a linking group; R₆ is OR; R is H or linear or branched alkyl having from 1 to 3 carbon atoms; X' is CH₂; Y' is O; and Z' is CH₂; each A and A' is O; each D and D′ is linear alkyl having from 1 to 10 carbon atoms; L is absent or is a phenyl group, which is optionally substituted, where the substituent is a linking group that binds to the cell-binding agent through a covalent bond, or is selected from OR₇, NR₈R₉ and OCOR₁₁; R is H or linear or branched alkyl having from 1 to 3 carbon atoms; every R₇, R₈, R₉, and R₁₁ independently is H, linear or branched alkyl having from 1 to 10 carbon atoms, or a polyethylene glycol fragment -(OCH₂CH₂)_n, where n is an integer from 1 to 10.

EFFECT: invention also relates to methods of using the compounds or conjugates for in vitro, in situ and in vivo diagnosis or treatment of mammalian cells or associated pathological conditions.

18 cl, 59 dwg, 7 tbl, 40 ex