CONJUGATES OF ENGINEERED ANTIBODIES WITH CYSTEINE SUBSTITUTES Russian patent published in 2020 - IPC C07D487/04 C07D519/00 A61K47/68 C07K16/28 A61P35/00 

Abstract RU 2733740 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to novel conjugates of a cell-binding agent with a cytotoxic agent in which a cell-binding agent (CBA) is covalently bound to a cytotoxic agent through the engineered Cys, such as the engineered Cys in the heavy chain CH3 domain, at the position corresponding to position 442 (or C442) according to the EU/OU numbering system in the CBA antibody. Present invention also discloses methods of producing conjugates of the invention. Additionally disclosed are a pharmaceutical composition and methods, suitable for inhibiting abnormal cell growth or treating proliferative disorder in a mammal using conjugates of the invention.

EFFECT: disclosed are conjugates of constructed antibodies with cysteine substitutes.

33 cl, 8 dwg, 3 tbl, 7 ex

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RU 2 733 740 C2

Authors

Yoder Nicholas C.

Bai Chen

Miller Michael Louis

Dates

2020-10-06Published

2016-06-28Filed