Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_18d92c46f60af8af24e262b67381d7eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1167e9abc558332ee75993087c77c498 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 |
filingDate |
2015-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_28d2f8159bdf83a04d5a7bb4658873f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_157ba28c2865196c3a19e177be058cb6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2b4a3917f9f38f049a3f510ab8e91eb4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cadcef888f5356277cf8df96ffdb0141 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a725c821eff49c97b5810746d0609f2 |
publicationDate |
2017-01-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
EP-3119781-A1 |
titleOfInvention |
Compounds which inhibit rna polymerase, compositions including such compounds, and their use |
abstract |
RNA polymerase I (Pol I) is a dedicated polymerase for the transcription of the 47S ribosomal RNA precursor subsequently processed into the mature 5.8S, 18S and 28S ribosomal RNAs and assembled into ribosomes in the nucleolus. Pol I activity is commonly deregulated in human cancers. Based on the discovery of lead molecule BMH-21, a series of pyridoquinazolinecarboxamides were synthesized as inhibitors of Pol I and activators of the destruction of RPA194, the Pol I large catalytic subunit protein. The present invention identifies a set of bioactive compounds, including purified stereoisomers, that potently cause RPA194 degradation that function in a tightly constrained chemical space. Pharmaceutical compositions comprising these compounds and their uses in cancer and other Pol I related diseases is also provided. |
priorityDate |
2014-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |