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Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Wilson, David M; Apps, James; Bailey, Nicholas; Bamford, Mark J; Beresford, Isabel J; Brackenborough, Kim; Briggs, Michael A; Brough, Stephen; Calver, Andrew R; Crook, Barry; Davis, Rebecca K; Davis, Robert P; Davis, Susannah; Dean, David K; Harris, Leanne; Heslop, Teresa; Holland, Vicky; Jeffrey, Phillip; Panchal, Terrance A; Parr, Christopher A; Quashie, Nigel; Schogger, Joanne; Sehmi, Sanjeet S; Stean, Tania O; Steadman, Jon G A; Trail, Brenda; Wald, Jeffrey; Worby, Angela; Takle, Andrew K; Witherington, Jason; Medhurst, Andrew D.
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  • Wilson DM; GlaxoSmithKline R&D, Neurology Centre of Excellence for Drug Discovery, Harlow, Essex CM19 5AW, United Kingdom. Electronic address: David.M.Wilson@astrazeneca.com.
Bioorg Med Chem Lett ; 23(24): 6890-6, 2013 Dec 15.
Article en En | MEDLINE | ID: mdl-24269482
This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists as novel therapies for the treatment of Alzheimer's disease and other dementias. By carefully controlling the physicochemical properties of the benzazepine series and through the implementation of an aggressive and innovative screening strategy that employed high throughput in vivo assays to efficiently triage compounds, the medicinal chemistry effort was able to rapidly progress the benzazepine class of H3 antagonists through to the identification of clinical candidates with robust in vivo efficacy and excellent developability properties.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzazepinas / Receptores Histamínicos H3 / Antagonistas de los Receptores Histamínicos H3 Tipo de estudio: Diagnostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2013 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Benzazepinas / Receptores Histamínicos H3 / Antagonistas de los Receptores Histamínicos H3 Tipo de estudio: Diagnostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2013 Tipo del documento: Article Pais de publicación: Reino Unido