92536-05-5Relevant academic research and scientific papers
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase
Keith, John M.,Hawryluk, Natalie,Apodaca, Richard L.,Chambers, Allison,Pierce, Joan M.,Seierstad, Mark,Palmer, James A.,Webb, Michael,Karbarz, Mark J.,Scott, Brian P.,Wilson, Sandy J.,Luo, Lin,Wennerholm, Michelle L.,Chang, Leon,Rizzolio, Michele,Chaplan, Sandra R.,Breitenbucher, J. Guy
, p. 1280 - 1284 (2014/03/21)
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase
Wittman, Mark D.,Balasubramanian, Balu,Stoffan, Karen,Velaparthi, Upender,Liu, Pieying,Krishnanathan, Subramaniam,Carboni, Joan,Li, Aixin,Greer, Ann,Attar, Ricardo,Gottardis, Marco,Chang, Chiehying,Jacobson, Bruce,Sun, Yax,Hansel, Steven,Zoeckler, Mary,Vyas, Dolatrai M.
, p. 974 - 977 (2007/10/03)
A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency.
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route
Blagg, Julian,Allerton, Charlotte M.N.,Batchelor, David V.J.,Baxter, Andrew D.,Burring, Denise J.,Carr, Christopher L.,Cook, Andrew S.,Nichols, Carly L.,Phipps, Joanne,Sanderson, Vivienne G.,Verrier, Hugh,Wong, Stephen
, p. 6691 - 6696 (2008/03/14)
This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has >1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route.
3' Cyanophenylalkanolamines: a contribution to the search for selective β adrenomimetic compounds
Pratesi,Grana,Villa
, p. 753 - 765 (2007/10/06)
Some derivatives of 1 (3' cyanophenyl) 2 aminoethanol have been synthesized in which OH is substituted at the nucleus, methyl or ethyl at the α carbon atom and isopropyl or t butyl at the nitrogen atom. The pharmacological research has shown that by combi
