166895-10-9Relevant academic research and scientific papers
Substituted imidazoles as glucagon receptor antagonists
Chang, Linda L.,Sidler, Kelly L.,Cascieri, Margaret A.,De Laszlo, Stephen,Koch, Greg,Li, Bing,MacCoss, Malcolm,Mantlo, Nathan,O'Keefe, Stephen,Pang, Margaret,Rolando, Anna,Hagmann, William K.
, p. 2549 - 2553 (2007/10/03)
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC50 = 0.053 μM) and selectivity (> 1000 ×) over p38 MAP kinase in this class of compounds.
Oxazoles for treating cytokine mediated diseases
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, (2008/06/13)
This invention relates to the novel oxazole compounds of Formula (I) and novel pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable diluent or carrier. This invention also relates to a method of inhibiting cytokines and the treatment of cytokine mediated diseases, in mammals, thereby by administration of an effective amount of a compound according to Formula (I).
