- Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements
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Dual orexin receptor antagonists (DORAs), or orexin 1 (OX1) and orexin 2 (OX2) receptor antagonists, have demonstrated clinical utility for the treatment of insomnia. Medicinal chemistry efforts focused on the reduction of bioactivat
- Roecker, Anthony J.,Mercer, Swati P.,Bergman, Jeffrey M.,Gilbert, Kevin F.,Kuduk, Scott D.,Harrell, C. Meacham,Garson, Susan L.,Fox, Steven V.,Gotter, Anthony L.,Tannenbaum, Pamela L.,Prueksaritanont, Thomayant,Cabalu, Tamara D.,Cui, Donghui,Lemaire, Wei,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
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p. 4992 - 4999
(2015/03/05)
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- DISUBSTITUTED OCTAHY-DROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS
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Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
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Page/Page column 81
(2012/11/07)
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- FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS
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Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
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Page/Page column 57
(2011/05/06)
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- AMINOPYRIMIDINES AS SYK INHIBITORS
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The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
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Page/Page column 58
(2011/07/07)
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- FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS
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Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
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Page/Page column 88
(2011/05/06)
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- DISUBSTITUTED OCTAHY - DROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS
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Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
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Page/Page column 81
(2011/05/06)
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- SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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Page/Page column 80-81
(2009/12/02)
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