- Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro-2H-pyran-4-yl) methyl]-4-(trifluoromethyl)-5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain
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Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified a pyrimidine ester as a partial agonist at the CB2 receptor with micromolar potency. Subsequent lead optimization identified 35, GW842166X, as the optimal compound in the series. 35 has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and was selected as a clinical candidate for this indication.
- Giblin, Gerard M. P.,O'Shaughnessy, Celestine T.,Naylor, Alan,Mitchell, William L.,Eatherton, Andrew J.,Slingsby, Brian P.,Rawlings, D. Anthony,Goldsmith, Paul,Brown, Andrew J.,Haslam, Carl P.,Clayton, Nick M.,Wilson, Alex W.,Chessell, Iain P.,Wittington, Andrew R.,Green, Richard
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p. 2597 - 2600
(2008/02/03)
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- RENIN INHIBITORS
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The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
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Page/Page column 47
(2008/06/13)
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- Indole-2-carboxamide derivatives useful as beta-2 agonists
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The invention relates to indole derivatives of general formula: and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions. In particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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