PYRROLOBENZODIAZEPINE CONJUGATES Russian patent published in 2021 - IPC A61K31/5517 A61K47/68 C07D519/00 A61P35/00 

Abstract RU 2744200 C2

FIELD: biotechnology; medicine.

SUBSTANCE: group of inventions refers to pyrrolobenzodiazepine antibody-drug conjugates and use thereof. Disclosed is a conjugate of formula I:

,

where L is an antibody or its antigen-binding fragment to a tumor-associated antigen, DL is a link of formula II:

,

where either R10 and R11 form a double nitrogen-carbon bond between the nitrogen and carbon atoms with which they are bonded, or R11 is OH and R10 is:

,

p = 1–20.

EFFECT: said conjugates can be used for treating a proliferative disease; conjugates are well tolerated in toxicity studies in various animal species, which provides a high therapeutic index of such conjugates.

20 cl, 4 dwg, 4 tbl, 8 ex

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RU 2 744 200 C2

Authors

Khovard Filip Uilson

Danni Elizabet

Masterson Lyuk

Dates

2021-03-03Published

2017-02-10Filed