Substituted Pyridines as Inhibitors of DNMT1

N. David Adams (Inventor), Andrew Benowitz (Inventor), Maria Lourdes (Inventor), Karen Evans (Inventor), David T Fosbenner (Inventor), Bryan King (Inventor), Mei Li (Inventor), Juan Luengo (Inventor), William Miller (Inventor), Alexander Reif (Inventor), Stuart Romeril (Inventor), Stanley Schmidt (Inventor), Roger Butlin (Inventor), Kristin Goldberg (Inventor), Allan Jordan (Inventor), Christopher Kershaw (Inventor), Ali Raoof (Inventor), Bohdan Waszkowycz (Inventor)

Research output: Patent


The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Original languageEnglish
Patent numberWO2017216727
Priority date21/12/17
Publication statusPublished - 21 Dec 2017

Research Beacons, Institutes and Platforms

  • Manchester Cancer Research Centre


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