NOVEL BENZODIAZEPINE DERIVATIVES Russian patent published in 2015 - IPC C07D519/00 C07D487/00 A61K31/55 A61K31/5513 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula:

double line between N and C represents double bond, X is absent, a Y stands for H; W stands for C=O; each of R₁, R₂, R₃, R₄ stands for H; R₅ is selected from groups OR₁₅, where R₁₅ has the same determination as R; optionally R₅ stands for binding group or is selected from groups: polypyrrole, polyindolyl, polyimidazolyle, polypyrrole-imidazolyle, polypyrrole-indolyl or polyimidazole-indolyl unit, optionally bound to binding groups; R₆ stands for OR or optionally, R₆ stands for binding group; Z is selected from groups (CH₂)_n, where n stands for 1, 2 or 3, CR₁₅R₁₆, where each of R₁₅ and R₁₆ independently stands for H or linear alkyl, having from 1 to 10 carbon atoms; R stands for H or linear or branched alkyl, having from 1 to 3 carbon atoms, optionally substituted with group -COR₁₁; R₁₁ stands for H or -OR₁₄; and R₁₄ stands for H or linear or branched alkyl, having from 1 to 3 carbon atoms; each of R₁, R₂, R₃, R₄, R₁', R₂', R₃' and R₄' stands for H, optionally any of R₁, R₂, R₃, R₄, R₁', R₂', R₃' or R₄' stands for binding group, Z is selected from groups (CH₂)_n, where n stands for 1, 2 or 3; R₆ stands for OR, or optionally R₆ stands for binding group; A and A′ stand for O, D and D', similar or different, and independently represent linear or branched alkyls, having from 1 to 10 carbon atoms; L is absent or stands for phenyl group, where said phenyl group representing L, is optionally substituted, where substituent is represented by binding group or is selected from OR₇, NR₈R₉, NRCOR' or OCOR₁₁; R and R' independently represent H or linear or branched alkyl, having from 1 to 10 carbon atoms, optionally substituted with halogen or group -COR₇; R₇, R₈, R₉ and R₁₁ independently represent H or linear or branched alkyl, having from 1 to 10 carbon atoms, or polyethylene glycol unit (-OCH₂CH₂)_n, where n stands for integer number from 1 to 10; on condition that said compound has not more than one binding group, which provides bond with cell-binding agent due to covalent bond, which possess anti-proliferative activity.

EFFECT: obtaining novel compounds.

24 cl, 59 dwg, 9 tbl, 40 ex