857273-77-9Relevant articles and documents
Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity
Peters, Jens-Uwe,Kühne, Holger,Dehmlow, Henrietta,Grether, Uwe,Conte, Aurelia,Hainzl, Dominik,Hertel, Cornelia,Kratochwil, Nicole A.,Otteneder, Michael,Narquizian, Robert,Panousis, Constantinos G.,Ricklin, Fabienne,R?ver, Stephan
scheme or table, p. 5426 - 5430 (2010/12/25)
Pyrido pyrimidinones are selective agonists of the human high affinity niacin receptor GPR109A (HM74A). They show no activity on the highly homologous low affinity receptor GPR109B (HM74). Starting from a high throughput screening hit the in vitro activity of the pyrido pyrimidinones was significantly improved providing lead compounds suitable for further optimization.
ORGANIC COMPOUNDS
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Page/Page column 56, (2008/06/13)
Novel substituted piperidines of the general formulae (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent.