FIELD: pharmaceuticals.
SUBSTANCE: invention discloses antibody-drug conjugates containing an antibody conjugated with a drug pyrrolobenzodiazepine component through a disulphide linker,
,
where X 
Y is C(=O)-NH or CH2-NH; A is a pyrrole optionally substituted with a =C(R)2 group, in which R is independently selected from H and C1-C6-alkyl; R1 and R2 are independently selected from H or C1-C6-alkyl or R1 and R2 form cyclopropyl; p equals integer from 1 to 8; and Ab is an antibody which is selected from a group consisting of anti-HER2, anti-CD22, anti-CD33, anti-Napi2b and anti-CLL-1, as well as pyrrolobenzodiazepine intermediate linker compounds, pharmaceutical compositions and methods of using antibody-drug conjugates for treating hyperproliferative diseases.
EFFECT: disclosed are antibody-drug conjugates of pyrrolobenzodiazepine conjugates and methods of using them.
56 cl, 15 dwg, 9 tbl, 15 ex
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