401631-70-7Relevant academic research and scientific papers
Tricyclic aminopyrimidine histamine H4 receptor antagonists
Savall, Brad M.,Gomez, Laurent,Chavez, Frank,Curtis, Michael,Meduna, Steven P.,Kearney, Aaron,Dunford, Paul,Cowden, Jeffery,Thurmond, Robin L.,Grice, Cheryl,Edwards, James P.
scheme or table, p. 6577 - 6581 (2011/12/04)
This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists
Cramp, Sue,Dyke, Hazel J.,Higgs, Christopher,Clark, David E.,Gill, Matthew,Savy, Pascal,Jennings, Neil,Price, Steve,Lockey, Peter M.,Norman, Dennis,Porres, Soraya,Wilson, Francis,Jones, Alison,Ramsden, Nigel,Mangano, Raffaella,Leggate, Dan,Andersson, Marie,Hale, Richard
scheme or table, p. 2516 - 2519 (2010/06/20)
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H4 receptor inverse agonists is described. The initial hit, 3A (IC50 19 nM) was identified by means of a ligand-based virtual screening approach. Subsequent medicinal chemistry exploration yielded 18I which possessed increased potency (R-enantiomer IC50 1 nM) as well as enhanced microsomal stability.
Benzofuro- and benzothienopyrimidine modulators of the histamine H4 receptor
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Page/Page column 13, (2008/06/13)
Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions media
Pyrimidine compounds as histamine modulators
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, (2008/06/13)
The present invention relates to novel pyrimidine compounds, for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compoun
Pyrimidine compounds for the treatment of inflammatory disorders
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Page/Page column 12, (2010/11/26)
The present invention relates to novel pyrimidine compounds, for the modulation of the histamine H4 receptor and the treatment or prevention of conditions mediated by the histamine H4 receptor. The invention also relates to the preparation of such compoun
