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

Case ID:
C12897
Disclosure Date:
2/6/2014
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 Canada 2,943,022 2943022 3/20/2015 1/16/2024 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 Ireland 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 Italy 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 Spain 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
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For Information, Contact:
Jeanine Pennington
jpennin5@jhmi.edu
410-614-0300
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