1082041-85-7Relevant articles and documents
Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes
Zhang, Xuqing,Zhu, Bin,Guo, Lili,Bakaj, Ivona,Rankin, Matthew,Ho, George,Kauffman, Jack,Lee, Seunghun P.,Norquay, Lisa,MacIelag, Mark J.
supporting information, p. 451 - 458 (2021/04/06)
A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK profiling led to multiple compounds with good physical properties, excellent oral bioavailability, and a clean in vitro safety profile. Compound 13 was identified as a lead compound as evidenced by the reversal of sulprostone-induced suppression of glucose-stimulated insulin secretion in INS 1E β-cells in vitro and in a rat ivGTT model in vivo. A glutathione adduction liability was eliminated by replacing the naphthalene of structure 13 with the indazole ring of structure 43.
COMPOUNDS FOR USE IN THE TREATMENT OF FASCIOLIASIS
-
Page/Page column 29, (2020/02/22)
The present invention relates to compounds of formula (1a), (1b), (1c), (1d) or (1e) and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
PYRIDIN-2-ONE DERIVATIVES OF FORMULA (III) USEFUL AS EP3 RECEPTOR ANTAGONISTS
-
Paragraph 0661-0662, (2019/02/24)
The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.