ANTIBODY DRUG CONJUGATES Russian patent published in 2018 - IPC C07D309/32 A61K47/68 A61P35/00 

FIELD: medicine.

SUBSTANCE: invention relates to conjugates of a medication of formula [D-(X)_b-(AA)_w-(L)-]_n-Ab, wherein D is a group that is a drug of formula (Ia) or (Ib), or a pharmaceutically acceptable salt or stereoisomer thereof, where the wavy lines of formulas (Ia) and (Ib) indicate the place of covalent attachment to (X)_b, if this is the case, or (AA)_w, if this is the case, or to the L linker group; each of R₁, R₂ and R₃ is independently selected from hydrogen and OR_a; each of R₄, R₅, R₆, R₇, R₈, R₉, R₁₀ and R₁₂ is independently selected from the group consisting of hydrogen and unsubstituted C₁-C₁₂ alkyl; R₁₁ is hydrogen; R₁₃ is hydrogen; each of R₁₅, R₁₆, R₁₇, R_17’, R_18’, R₂₄, R_24’, R₂₅ and R₂₆ is independently selected from the group consisting of hydrogen and unsubstituted C₁-C₁₂ alkyl; R₁₈ is hydrogen; R₂₇ is selected from hydrogen, unsubstituted C₁-C₁₂ alkyl and halogen; each R_a is unsubstituted C₁-C₁₂ alkyl; and each dashed line represents an optional additional bond, but when there is a triple bond between the C atom to which R₂₅ is attached, and the C atom to which R₂₆ and R₂₇ are attached, then R₂₅ and either R₂₆, or R₂₇ are absent; L is a linker group, (AA)_w is an amino acid unit, X is an extending group, Ab is a component comprising at least one antigen-binding site, n is the group's ratio [D-(X)_b-(AA)_w-(L)-] to the Ab component containing at least one antigen-binding site, and is in the range of 1 to 20. (Ia), (Ib). A: .

EFFECT: conjugates are intended for the treatment of cancer.

36 cl, 40 dwg, 71 tbl, 22 ex