927892-94-2Relevant academic research and scientific papers
Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists
Ando, Makoto,Sekino, Etsuko,Haga, Yuji,Moriya, Minoru,Ito, Masahiko,Ito, Junko,Iwaasa, Hisashi,Ishihara, Akane,Kanatani, Akio,Ohtake, Norikazu
scheme or table, p. 5186 - 5190 (2010/03/24)
Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.
PHENYLPYRIDONE DERIVATIVE
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Page/Page column 35-36, (2008/12/05)
A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
