Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation
Utilization of Theravance's multivalent approach to drug discovery towards 5-HT4 receptor agonists with a focus on identification of neutral (non-charged at physiological pH) secondary binding groups is described. Optimization of a quinolone-tr
Long, Daniel D.,Armstrong, Scott R.,Beattie, David T.,Choi, Seok-Ki,Fatheree, Paul R.,Gendron, Roland A.L.,Genov, Daniel,Goldblum, Adam A.,Humphrey, Patrick P.,Jiang, Lan,Marquess, Daniel G.,Shaw, Jeng-Pyng,Smith, Jacqueline A.M.,Turner, S. Derek,Vickery, Ross G.
p. 6048 - 6052
(2012/10/29)
Prokinetic agent for bowel preparation
The invention provides methods of bowel preparation before a diagnostic, surgical or therapeutic procedure, in particular, bowel preparation before a colonoscopy procedure, using a 5-HT4 receptor agonist as a prokinetic agent.
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(2008/12/09)
Crystalline form of a quinolinone-carboxamide compound
The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
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Page/Page column 10
(2010/11/24)
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