81228-07-1Relevant academic research and scientific papers
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.
DIALKYL ETHER DELIVERY AGENTS
-
Page/Page column 24, (2008/06/13)
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.
SUBSTITUTED PHENOXY-AMINOPROPANOLS
-
, (2008/06/13)
Substituted phenoxy-aminopropanols of the formula STR1 wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R 1 is hydrogen, halogen or lower alkyl and R 2 and R 3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective β-adrenergic blocking activity and antihypertensive activity.
β1-Selective Adrenoceptor Antagonists. 2. 4-Ether-Linked Phenoxypropanolamines
Machin, Peter J.,Hurst, David N.,Bradshaw, Rachel M.,Blaber, Leslie C.,Burden, David T.,et al.
, p. 1570 - 1576 (2007/10/02)
A series of 4-substituted phenoxypropanolamines was prepared and examined for β-adrenoceptor activity.Some of the compounds, especially the oxy>ethoxy>phenoxy>propanolamines (14, 15, and 24), showed potent β1-blo
