188345-71-3Relevant articles and documents
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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, (2015/05/26)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists
Coleman, Paul J.,Schreier, John D.,McGaughey, Georgia B.,Bogusky, Michael J.,Cox, Christopher D.,Hartman, George D.,Ball, Richard G.,Harrell, C. Meacham,Reiss, Duane R.,Prueksaritanont, Thomayant,Winrow, Christopher J.,Renger, John J.
scheme or table, p. 2311 - 2315 (2010/09/08)
Orexins are neuropeptides that regulate wakefulness and arousal. Small molecule antagonists of orexin receptors may provide a novel therapy for the treatment of insomnia and other sleep disorders. In this Letter we describe the design and synthesis of con
Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)- bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors
Bunnelle, William H.,Daanen, Jerome F.,Ryther, Keith B.,Schrimpf, Michael R.,Dart, Michael J.,Gelain, Arianna,Meyer, Michael D.,Frost, Jennifer M.,Anderson, David J.,Buckley, Michael,Curzon, Peter,Cao, Ying-Jun,Puttfarcken, Pamela,Searle, Xenia,Ji, Anguo,Putman, C. Brent,Surowy, Carol,Toma, Lucio,Barlocco, Daniela
, p. 3627 - 3644 (2008/02/11)
A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors (nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of bridged bicyclic diamines exhibit double-digit-picomolar binding affinities for the α4β2 subtype, placing them with epibatidine among the most potent nAChR ligands described to date. Structure-activity studies have revealed that substitutions, particularly hydrophilic groups in the pyridine 5-position, differentially modulate the agonist activity at ganglionic vs central nAChR subtypes, so that improved subtype selectivity can be demonstrated in vitro. Analgesic efficacy has been achieved across a broad range of pain states, including rodent models of acute thermal nociception, persistent pain, and neuropathic allodynia. Unfortunately, the hydrophilic pyridine substituents that were shown to enhance agonist selectivity for central nAChRs in vitro tend to limit CNS penetration in vivo, so that analgesic efficacy with an improved therapeutic window was not realized with those compounds.
