93022-07-2Relevant academic research and scientific papers
Identification of a novel benzimidazole derivative as a highly potent NPY Y5 receptor antagonist with an anti-obesity profile
Tamura, Yuusuke,Hayashi, Kyouhei,Omori, Naoki,Nishiura, Yuji,Watanabe, Kana,Tanaka, Nobuyuki,Fujioka, Masahiko,Kouyama, Naoki,Yukimasa, Akira,Tanaka, Yukari,Chiba, Takeshi,Tanioka, Hideki,Nambu, Hirohide,Yukioka, Hideo,Sato, Hiroki,Okuno, Takayuki
, p. 90 - 95 (2013/02/25)
Optimization of HTS hit 1 for NPY Y5 receptor binding affinity, CYP450 inhibition, solubility and metabolic stability led to the identification of some orally available oxygen-linker derivatives for in vivo study. Among them, derivative 4i inhibited food intake induced by the NPY Y5 selective agonist, and chronic oral administration of 4i in DIO mice caused a dose-dependent reduction of body weight gain.
POLYCYCLIC LPA1 ANTAGONIST AND USES THEREOF
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Page/Page column 88, (2012/06/30)
Described herein is the LPA1 antagonist 1- {4'-[3-methyl-4-((R)- l-phenyl-ethoxycarbonylamino)- isoxazol-5-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing t
POLYCYCLIC ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS
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Page/Page column 43, (2010/12/29)
Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
