Affiliation: Arena Pharmaceuticals
- Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomniaYIFENG XIONG
Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
Bioorg Med Chem Lett 22:1870-3. 2012..Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation...
- Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosisYIFENG XIONG
Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
J Med Chem 53:4412-21. 2010..10k was orally bioavailable in rats, dogs, and monkeys and had an acceptable safety profile. As a result, 10k was selected further evaluation and advanced into clinical development as a potential treatment for arterial thrombosis...
- Synthesis and in vivo evaluation of phenethylpiperazine amides: selective 5-hydroxytryptamine(2A) receptor antagonists for the treatment of insomniaYIFENG XIONG
Arena Pharmaceuticals, San Diego, California 92121, USA
J Med Chem 53:5696-706. 2010..In vivo, these two compounds showed dose-dependent, statistically significant improvements on deep sleep (delta power) and sleep consolidation at doses as low as 0.1 mg/kg...
- Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose controlGraeme Semple
Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
Bioorg Med Chem Lett 21:3134-41. 2011..As a result of these and other data described here, 3k (APD668, JNJ-28630368) was the first compound with this mechanism of action to be progressed into clinical development for the treatment of diabetes...
- APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biologyJohn W Adams
Arena Pharmaceuticals, Inc, San Diego, CA 92121, USA
J Pharmacol Exp Ther 331:96-103. 2009..These results demonstrate that APD791 is an orally available, high-affinity 5-HT(2A) receptor antagonist with potent activity on platelets and vascular smooth muscle...
- Solubilized phenyl-pyrazole ureas as potent, selective 5-HT(2A) inverse-agonists and their application as antiplatelet agentsPeter I Dosa
Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, United States
Bioorg Med Chem Lett 19:5486-9. 2009..Optimization of this series resulted in selective compounds that proved effective in modulating 5HT-induced amplification of ADP-stimulated human platelet aggregation...
- Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonistsSangdon Han
Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA Electronic address
Bioorg Med Chem Lett 25:322-6. 2015..It also demonstrated robust in vivo efficacy mediated via CB2 activation in the rodent models of inflammatory and osteoarthritis pain after oral administration. ..
- 5-HT(2A) inverse-agonists for the treatment of insomniaBradley R Teegarden
Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA
Curr Top Med Chem 8:969-76. 2008....
- Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119Graeme Semple
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6166 Nancy Ridge Drive, San Diego, California 92121, USA
J Med Chem 51:5172-5. 2008..Compound 8g showed in vivo activity in rodents and was active in an oral glucose tolerance test in mice following oral administration...