http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2021128592-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ff81a650b70e913d3b2524b45e4c7320 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-704 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K9-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-704 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-08 |
| filingDate | 2020-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e31fc128e9f5ae31786b268e0fe4f20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9e337f2f247e2bd23c812a43a02310dd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_197642442a7137a42d9fdcac47588924 |
| publicationDate | 2021-05-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2021128592-A1 |
| titleOfInvention | REVERSING THE UNDESIRABLE pH-PROFILE OF DOXORUBICIN VIA ACTIVATION OF A DISUBSTITUTED MALEAMIC ACID PRODRUG AT TUMOR ACIDITY |
| abstract | A pre-prodrug, comprising a drug, e.g., doxorubicin, which has off-target toxicity (e.g., cardiotoxicity) with respect to its antineoplastic activity, and an amine functionality of the drug incorporated into a disubstituted maleimide (DMI). The pre-prodrug may be linked to a targeting or de-targeting agent or a polar modulator, e.g., charged ligand, amino acid, peptide, etc., to increase therapeutic index. The pre-prodrug is hydrolyzed to the prodrug, having a disubstituted maleamic acid (DMA). A polar modulator such as glutamic acid prevents cellular uptake of the prodrug, but not the doxorubicin drug released from the prodrug after dissociation. The prodrug is pH sensitive, and below pH 7.0, tends to cleave to form free drug and cyclized maleic anhydride. Tumor environments tend to be more acidic, e.g., pH 6.8, than cardiac tissue, e.g., pH 7.4, and therefore the heart is spared while the drug is selectively released within a tumor. |
| priorityDate | 2019-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 276.