328277-09-4Relevant articles and documents
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.
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 12-13, (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