Search Results - "Harper, Bart"
-
1
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder
Published in Journal of medicinal chemistry (28-01-2016)“…The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical…”
Get full text
Journal Article -
2
Investigation of piperazine benzamides as human β3 adrenergic receptor agonists for the treatment of overactive bladder
Published in Bioorganic & medicinal chemistry letters (15-02-2017)“…[Display omitted] The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β3-adrenergic receptor for the treatment of…”
Get full text
Journal Article -
3
Investigation of piperazine benzamides as human β 3 adrenergic receptor agonists for the treatment of overactive bladder
Published in Bioorganic & medicinal chemistry letters (15-02-2017)“…The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β -adrenergic receptor for the treatment of overactive bladder…”
Get full text
Journal Article -
4
Design, Synthesis, and Evaluation of Conformationally Restricted Acetanilides as Potent and Selective β3 Adrenergic Receptor Agonists for the Treatment of Overactive Bladder
Published in Journal of medicinal chemistry (27-02-2014)“…A series of conformationally restricted acetanilides were synthesized and evaluated as β3-adrenergic receptor agonists (β3-AR) for the treatment of overactive…”
Get full text
Journal Article -
5
Rapid development of two factor IXa inhibitors from hit to lead
Published in Bioorganic & medicinal chemistry letters (01-06-2015)“…[Display omitted] Two high-throughput screening hits were investigated for SAR against human factor IXa. Both hits feature a benzamide linked to a…”
Get full text
Journal Article -
6
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide: A Selective α-Amino Amide Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Published in Journal of medicinal chemistry (15-06-2006)“…A series of β-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type…”
Get full text
Journal Article -
7
Discovery of Vibegron: A Potent and Selective β 3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder
Published in Journal of medicinal chemistry (28-01-2016)Get full text
Journal Article -
8
-
9
2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity
Published in Bioorganic & medicinal chemistry (01-09-2008)“…The synthesis and biological profile of imidazole carboxamides of general structure 6 as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are…”
Get full text
Journal Article -
10
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
Published in Bioorganic & medicinal chemistry letters (15-08-2007)“…Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases…”
Get full text
Journal Article -
11
-
12
Heterocyclic acetamide and benzamide derivatives as potent and selective b sub(3)-adrenergic receptor agonists with improved rodent pharmacokinetic profiles
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…A series of amide derived b sub(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from…”
Get full text
Journal Article -
13
Heterocyclic acetamide and benzamide derivatives as potent and selective β 3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles
Published in Bioorganic & medicinal chemistry letters (2010)“…A series of amide derived β 3-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is…”
Get full text
Journal Article -
14
Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles
Published in Bioorganic & medicinal chemistry letters (15-03-2010)“…A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1,…”
Get full text
Journal Article