Patent number: 10975056
Abstract: The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (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.
Type:
Grant
Filed:
June 13, 2017
Date of Patent:
April 13, 2021
Assignees:
GlaxoSmithKline Intellectual Property Development Limited, Cancer Research Technology Ltd.
Inventors:
Nicholas David Adams, Andrew B. Benowitz, María Lourdes Rueda Benede, Karen Anderson Evans, David T Fosbenner, Bryan Wayne King, Mei Li, Juan Ignacio Luengo, William Henry Miller, Alexander Joseph Reif, Stuart Paul Romeril, Stanley J. Schmidt, Roger J. Butlin, Kristin M. Goldberg, Allan M. Jordan, Christopher S. Kershaw, Ali Raoof, Bohdan Waszkowycz
Patent number: 10961200
Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
Type:
Grant
Filed:
June 28, 2019
Date of Patent:
March 30, 2021
Assignees:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
Inventors:
David J. Maloney, Alex Gregory Waterson, Ganesh Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor Darley-Usmar, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, Jennifer L. Kouznetsova, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang