CD206 targeted drug delivery vehicles carrying novel bisphosphonate drug payloads via a degradable linker
AssigneeNavidea Biopharmaceuticals, Inc.
InventorsDavid A. Ralph, Jeffrey Scott Arnold
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AssigneeNavidea Biopharmaceuticals, Inc.
InventorsDavid A. Ralph, Jeffrey Scott Arnold
Estimating the term…
Provided are novel compounds containing a polymeric carbohydrate backbone, one or more mannose-binding C-type lectin receptor targeting moieties, and a nitrogenous bisphosphonate compound coupled to the backbone via a thiol-maleimide conjugation, in addition to pharmaceutical compositions, methods of synthesizing, and methods of use. The thiol-maleimide conjugation of a bisphosphonate to a polymeric carbohydrate backbone provides for methods of using the compounds and compositions thereof for releasing the therapeutic payload when internalized into a mannose-binding C-type lectin receptor-expressing cell, such as tumor associated macrophages (TAMs) for the treatment of various diseases, including, cancer, autoimmune diseases, and inflammatory disorders.
A compound comprising:
A method of repolarizing a tumor associated macrophage (TAM) from an immunosuppressive (M2-like) phenotype to a proinflammatory (M1-like) phenotype, comprising:
The method of 25, wherein the compound comprises a subunit as shown in Formula (I):
Dependencies are inferred from the claim text.