PYRIDAZINEDIONE-BASED HETEROBICYCLIC COVALENT LINKERS AND METHODS AND APPLICATIONS THEREOF
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United States of America
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Dec 26, 2024
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Oct 21, 2022
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Oct 21, 2022
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Abstract
Pyridazinedione-based heterobicyclic covalent linkers useful for formation of protein-drug conjugates, protein-protein conjugates, or the like, preparation methods thereof, and applications of the linkers in formation of various protein conjugates are disclosed. The present disclosure provides a new class of linkers to overcome the limitations of the existing pyridazinedione-based linkers. These linkers can be synthesized from commercially available starting materials in 1-3 steps and are highly reactive toward the thiols derived from the reduction of disulfide bridges in proteins.
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