http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3119781-A1

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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

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