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filingDate 2021-08-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_16e6dda3c5598f4759f26e9087f0ccc0
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publicationDate 2022-02-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2022031057-A1
titleOfInvention Conjugate of functional drug and toll-like receptor 7 or 8 agonist of which active site is temporarily inactivated and use thereof
abstract The present invention relates to: a toll-like receptor 7 or 8 agonist-drug conjugate material in which a functional drug and a toll-like receptor 7 or 8 agonist are linked by a chemical bond containing a cleavable site; and use thereof, in which, by using the synergistic effect of the functional drug and the toll-like receptor 7 or 8 agonist material, and using the properties of the temporarily inactivated state, the side effects of the toll-like receptor 7 or 8 agonist can be reduced. In particular, the conjugate material is designed such that the immunostimulatory function of the toll-like receptor 7 or 8 agonist is inhibited due to the chemical bond, while the immunostimulatory function is recovered at an injection site or in a tumor microenvironment or target immune cells, thus exhibiting kinetic properties in which immunostimulatory efficacy can be controlled over time, and minimizing the induction of nonspecific immune responses. In addition, since various functions can be combined with a drug, the inactivated toll-like receptor 7 or 8 agonist-functional drug conjugate can be widely used in pharmaceutical compositions for various applications, which are capable of controlling cancer cell death, the activation of therapeutic immune cells, and immunosuppressive cells and environments, at an injection site or in a tumor microenvironment.
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