http://rdf.ncbi.nlm.nih.gov/pubchem/patent/BR-112019027880-A2

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_40adb9e4a934268c05df31da6e3f6138
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filingDate 2018-06-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9ca32d12fcbafd91f88f751db603349f
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bab605fde4524df7785559de5826d509
publicationDate 2020-07-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber BR-112019027880-A2
titleOfInvention drug loading cell penetration molecule, methods to facilitate the absorption of a biologically active compound, to improve the bioavailability of a biologically active drug or compound, to introduce a biologically active drug or compound into a site, to treat an individual, and, composition
abstract the invention relates to improvements in drug delivery and the use of cell-penetrating agents (cpas) or cell-penetrating peptides (cpps) that have been stabilized, for example: i) stapling two amino acids to form stapled cpps (staps) or ii) sewing three or more amino acids to form stitched cpp (stips). more particularly a drug loading cell penetration molecule (dccpm) is provided which comprises: a biologically active compound (bac), and a cell penetrating agent (cpa), in which bac and cpa are linked directly or through of a bifunctional ligand (bfl). cpa is a stabilized peptide (cpp) that has an imposed conformation when being stapled to form a stapled peptide (stap) or when being sewn to form a stitched peptide (stip). the stip or stap comprises a crosslink or bridge between at least two amino acids of the peptide and the crosslink or bridge provides a cyclization between at least two amino acids that are not formed by an olefin metathesis. cyclization can be achieved by one or more of: condensation of an aldehyde or ketone with a protected hydrazine or hydrazine; a michael addition of thiol-ene; a disulfide formation; a 1.3 dipolar cyloadload of huisgen; a reaction between an amine and carboxylic acid; a singlet or triplet carbine reaction; or a suzuki or sonogashira coupling.
priorityDate 2017-06-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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