http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113272294-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_e19ad3b2bfb8a9a6a21f7c929731e7ae http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_9a53a8a8d2f141e57eb88c209d9d4c1a http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a48a6221448d4a86bf6e59a258704e26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8aeee144da3e54b8869ad70eec8b095c http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_45fdf96a3628013575e9adc0e72e99c3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_92f3b088742cbcd6faf0b6ec55f9b7d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4a89dde72a64f6a441cac8978163ae78 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-90 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-81 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-81 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 |
| filingDate | 2019-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f2543812d3100bd4b74ade1c23889cf3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0484f9611de57aa6a7fe95ee054347ee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9631ee888b3a2b603738ff046fb623ff http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0d686e37fcace35d24868c819be162b6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_76abec09fe44da82375c54a3e98ccaad |
| publicationDate | 2021-08-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-113272294-A |
| titleOfInvention | 2, 6-bis (((1H-benzo [ D ] imidazol-2-yl) thio) methyl) pyridine and N2, N6-dibenzylpyridine-2, 6-dicarboxamide derivatives and related compounds as phosphoinositide 3-kinase (PI3K) inhibitors for the treatment of cancer |
| abstract | 2, 6-bis (((1H-benzo [ d ] imidazol-2-yl) thio) methyl) pyridine and N2, N6-dibenzylpyridine-2, 6-dicarboxamide derivatives and related compounds are useful as phosphoinositide 3-kinase (PI3K) inhibitors for the treatment of cancer. The present invention relates to pharmaceutically active 2, 6-bis (((1H-benzo [ d ] imidazol-2-yl) thio) methyl) pyridine, N2, N6-dibenzylpyridine-2, 6-dicarboxamide and N2, N6-bis (3-hydroxyphenyl) pyridine-2, 6-dicarboxamide, as well as derivatives thereof, and to structurally related compounds. These compounds are phosphoinositide 3-kinase inhibitors (PI3K) and are useful for treating or preventing cancerous diseases. The invention further relates to processes for the preparation of such compounds as well as pharmaceutical compositions and formulations comprising such compounds and optionally together with other pharmaceutically active compounds. The invention further relates to a method of determining the activity of a PI3K a or PI3K a mutant, the method comprising: a) providing a solid phase which is functionalized by immobilizing GST-GRP1 molecules thereon, b) performing an enzymatic reaction catalyzed by PI3K α or PI3K α mutants to convert PIP2 to PIP3, c) adding a competitor PIP3 carrying a detectable label or reporter molecule, and d) determining the enzymatic activity based on the amount of PIP3 obtained in step b) that competes with the competitor PIP3 for binding to the functionalized solid phase. |
| priorityDate | 2018-08-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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