| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d21cbff64022f95c237c0bd3ec8656ca |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-44
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-44 |
| filingDate |
2014-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate |
2019-01-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c588532fb775d32c02264113309f8837
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d0ec42f3d7cb7bd8f375b3481d549e46
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d97892b4a421798c57acfb70af2d7e4b
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8cf60cad6e67af6c2d833af2a657c2d1
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6bcaf05836c1340b7f2a14f1d43ce06d
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9e604238fc0c600dc01fac7ab3dae633
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac9cf4f4a4681c65986ae645e2ba0b59
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_01dc83cbc2bf6745b0a2a2767e00d3d6 |
| publicationDate |
2019-01-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
US-10167258-B2 |
| titleOfInvention |
Inhibitors of mitochondrial pyruvate dehydrogenase kinase isoforms 1-4 and uses thereof |
| abstract |
The present disclosure relates to the identification of PDK inhibitors and their use in the treatment of diseases such as diabetes, cardiovascular disease and cancer. The invention relates to the development of robust PDK inhibitors that can be used to improve glucose metabolism and correct metabolic dysfunction in vivo. Based on the unique structural features present in the ATP-binding pocket of PDK2, a single functional-group change was made in a known Hsp90 inhibitor that binds to the corresponding pocket of the latter protein from the GHKL family. This approach efficiently converted the Hsp90 inhibitor to a highly specific inhibitor for all PDK isoforms. These final PDK inhibitors of this series robustly augments PDC activity with reduced phosphorylation in tissues. |
| isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11746090-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11780811-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11376330-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11530184-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2020247213-A1 |
| priorityDate |
2013-12-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |