http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111909155-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 2020-08-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2022-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2022-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-111909155-B |
| titleOfInvention | Proteolytic targeting of chimeras, prodrug molecules for improving their oral bioavailability and their applications |
| abstract | The invention provides a proteolytic targeting chimera, a prodrug molecule for improving its oral bioavailability and its application. This technical solution developed a novel PROTAC degrader compound based on ribociclib derivatives and CRBN ligands. Small molecules can simultaneously and effectively degrade CDK2/4/6 and their complexes in malignant melanoma; they can also rapidly reset the cell cycle and induce apoptosis of various cancer cells, especially melanoma cells. The mechanism should be explained that CDK 2/4/6 deficiency may lead to synthetic lethal effects in malignant melanoma in the presence of this compound. These results suggest that CDK2/4/6 binding holds promise as a kinase target for the treatment of solid tumors. In addition, the present invention also develops a prodrug with high oral bioavailability for the first time, which is convenient for oral administration in animal experiments. It provides a general solution for oral administration of PROTAC molecules with CRBN ligands. |
| priorityDate | 2020-08-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 239.