http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AU-2018203194-A1

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-195
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K19-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-704
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00
filingDate 2018-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_61fe10dccac06b04bebf83edaa84df7c
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_901030ca2ca54955f0172bfe2cd1c78c
publicationDate 2018-05-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AU-2018203194-A1
titleOfInvention Legumain activated doxorubicin derivative as well as preparation method and application thereof
abstract The present invention discloses doxorubicin derivatives for targeted activation by legumain, its preparation method and use. The doxorubicin derivatives are obtained by 5 condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: r H H 0 0 OH ,N--R3-An--& 4-Rs-R - "OH compounds A and B have the following structures, respectively: OCHS) OH 0 ,NH 2 R3-Asn-R4-R5-R6 "OH 10 Compound A Compound B wherein R3 in compound B is Leu or absent; R4 is any one amino acid selected from the group consisting of Ala and Thr; R5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R6 is 0 , wherein n=1-20; or 0 , wherein R7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1 -C20 fatty 15 hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be use to prepare an anti-tumor drug.
priorityDate 2012-12-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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