Design, Synthesis and Structure-activity Relationships of Pyridoquinazolinecarboxamides as RNA Polymerase I Inhibitors

Case ID:

C12897

This invention describes a set of novel small molecules that inhibit RNA polymerase I. RNA polymerase I (Pol I) governs the transcription of ribosomal RNAs, which are needed for building and function of the ribosomes. These ribosynthetic activities are greatly increased in cancer cells, and Pol I transcription rate is commonly deregulated in human cancers. The small molecules described here inhibit Pol I and cause degradation of RPA194, the catalytic subunit driving the Pol I activity. The molecules inhibit the growth of cancer cells and hold promise as new anticancer agents.

Patent Information:

Title	App Type	Country	Serial No.	Patent No.	File Date	Issued Date	Expire Date	Patent Status
Design, Synthesis and Structure-activity Relationships of Pyridoquinazolinecarboxamides as RNA Polymerase I Inhibitors	PCT: Patent Cooperation Treaty	European Patent Office	15765295.9	3119781	3/20/2015	9/16/2020	3/20/2035	Granted
Design, Synthesis and Structure-activity Relationships of Pyridoquinazolinecarboxamides as RNA Polymerase I Inhibitors	PCT: Patent Cooperation Treaty	France	15765295.9	3119781	3/20/2015	9/16/2020	3/20/2035	Granted
Design, Synthesis and Structure-activity Relationships of Pyridoquinazolinecarboxamides as RNA Polymerase I Inhibitors	PCT: Patent Cooperation Treaty	Germany	15765295.9	3119781	3/20/2015	9/16/2020	3/20/2035	Granted
Design, Synthesis and Structure-activity Relationships of Pyridoquinazolinecarboxamides as RNA Polymerase I Inhibitors	PCT: Patent Cooperation Treaty	United Kingdom	15765295.9	3119781	3/20/2015	9/16/2020	3/20/2035	Granted
COMPOUNDS WHICH INHIBIT RNA POLYMERASE, COMPOSITIONS INCLUDING SUCH COMPOUNDS, AND THEIR USE	PCT: Patent Cooperation Treaty	United States	15/126,588	11,001,581	9/16/2016	5/11/2021	3/20/2035	Granted
COMPOUNDS WHICH INHIBIT RNA POLYMERASE, COMPOSITIONS INCLUDING SUCH COMPOUNDS, AND THEIR USE	DIV: Divisional	United States	17/195,149		3/8/2021			Pending

Direct Link:

https://jhu.technologypublisher.com/technology/47101

Inventors:

Category(s):

Clinical and Disease Specializations, Clinical and Disease Specializations > Oncology, Technology Classifications > Therapeutic Modalities > Small Molecules, Technology Classifications > Therapeutic Modalities,

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For Information, Contact:

Jeanine Pennington

jpennin5@jhmi.edu

410-614-0300

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