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.
The present invention provides dialkyl ether compounds and pharmaceutically acceptable salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same.
Novel substituted piperidines of the general formulae (I)
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.
Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: Optimization of in vitro activity
作者:Jens-Uwe Peters、Holger Kühne、Henrietta Dehmlow、Uwe Grether、Aurelia Conte、Dominik Hainzl、Cornelia Hertel、Nicole A. Kratochwil、Michael Otteneder、Robert Narquizian、Constantinos G. Panousis、Fabienne Ricklin、Stephan Röver
DOI:10.1016/j.bmcl.2010.07.108
日期:2010.9
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. (c) 2010 Elsevier Ltd. All rights reserved.