| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ad87ce8da37c0281d2a09374e26c5a05
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_207f994e3b86b8833ec15f106d3fb502
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_e73522660e7503cc08bde172f67e3767
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_904e057cb1af189e62db0907d6b0dca2
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a2f2c5972365172d35633c3e715a4137 |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D235-18
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4545
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 |
| filingDate |
2010-05-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e326281b7641c985a8484ab643385ab6
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_27fcaf88f51e5c4e42fa18fc332f4a62
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dd0f85b2e5f2870a28ba4422d5a4cfff
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_067f8f3056223b16dfe34a0e48d7ee99 |
| publicationDate |
2012-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
US-2012059003-A1 |
| titleOfInvention |
Inhibitors of inv(16) leukemia |
| abstract |
This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. |
| isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2017223260-A1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-10774049-B2
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9446048-B2 |
| priorityDate |
2009-05-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |