864757-75-5Relevant academic research and scientific papers
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists
Haga, Yuji,Mizutani, Sayaka,Naya, Akira,Kishino, Hiroyuki,Iwaasa, Hisashi,Ito, Masahiko,Ito, Junko,Moriya, Minoru,Sato, Nagaaki,Takenaga, Norihiro,Ishihara, Akane,Tokita, Shigeru,Kanatani, Akio,Ohtake, Norikazu
experimental part, p. 883 - 893 (2011/03/19)
The design, synthesis and structure-activity relationships of a novel class of N-phenylpyridone MCH1R antagonists are described. The core part of the N-phenylpyridone structure was newly designed and the side chain moieties that were attached to the core part were extensively explored. As a result of optimization of the N-phenylpyridone leads, we successfully developed the orally available, and brain-penetrable MCH1R selective antagonist 7c, exhibiting excellent anti-obese effect in diet-induced obese (DIO) mice.
PYRIDONE DERIVATIVE
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Page/Page column 65-66, (2010/11/25)
The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R 1 and R 2 may be same or different and stands for H, etc., or R 1 and R 2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X 1 -X 3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X 4 -X 7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y 1 and Y 3 may be same or different and stand for single bond, -0-, -NR-, -S-, etc ; Y 2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z 1 and Z 2 may be same or different and stand for single bond or lower alkylene; or R 1 , L and Z 2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R 1 binds; and Ar stands for aromatic carbocyclic group, etc.].
