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Article Title

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Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.

National Institute Of Diabetes And Digestive And Kidney Diseases

Investigation of piperazine benzamides as humanß

Merck

Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.

Merck Research Laboratories

Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.

Asahi Kasei Pharma

Discovery of TD-4306, a long-actingß2-agonist for the treatment of asthma and COPD.

Theravance

Multivalent design of long-actingß(2)-adrenoceptor agonists incorporating biarylamines.

Theravance

Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.

Glaxosmithkline

Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selectiveß3 adrenergic receptor agonists for the treatment of overactive bladder.

Merck And

Synthesis and in vitro and in vivo characterization of highlyß1-selectiveß-adrenoceptor partial agonists.

University Of Nottingham

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for humanß-adrenoceptors.

University Of Nottingham

Synthesis and evaluation of potent and selective beta(3) adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres.

Glaxosmithkline

2-(Dimethylaminomethyl)-tetrahydroisoxazolopyridobenzazepine derivatives. Synthesis of a new 5-HT(2C) antagonist with potential anxiolytic properties.

Janssen-Cilag

The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating a urea group.

Glaxosmithkline

The discovery of long-acting saligeninß2 adrenergic receptor agonists incorporating hydantoin or uracil rings.

Glaxosmithkline

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.

Glaxosmithkline

Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups.

Glaxosmithkline

QSAR analysis of thiazole benzenesulfonamide substituted 3-pyridylethanolamines as beta3-adrenergic receptor agonist.

S.G.S.I.T.S.

Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.

National Institute Of Mental Health

Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.

TBA

Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.

National Institute Of Mental Health

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles.

Merck Research Laboratories

Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.

Hunter College And The Graduate Center Of The City University Of New York

Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and molecular modeling based on the solved X-ray structure of the beta2-adrenergic receptor: part 6.

Astellas Pharma

Discovery of novel thiourea derivatives as potent and selective beta3-adrenergic receptor agonists.

Astellas Pharma

Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.

Astellas Pharma

Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.

Astellas Pharma

Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.

Universit£

Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I.

Astellas Pharma

Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.

Fujisawa Pharmaceutical

Relationship between stereochemistry and the beta3-adrenoceptor agonistic activity of 4'-hydroxynorephedrine derivative as an agent for treatment of frequent urination and urinary incontinence.

Kissei Pharmaceutical

(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.

Wyeth-Ayerst Research

Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.

Pfizer

Beta 3 agonists. Part 1: evolution from inception to BMS-194449.

Bristol-Myers Squibb Pharmaceutical Research Institute

 

A simplified template approach towards the synthesis of a potent beta-3 adrenoceptor agonist at the human receptor

TBA

Progress in structure based drug design for G protein-coupled receptors.

Heptares Therapeutics

Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective humanß3 adrenergic receptor agonists.

Merck Research Laboratories

Thienopyrimidines asß3-adrenoceptor agonists: hit-to-lead optimization.

4Sc

Spiroindolones, a potent compound class for the treatment of malaria.

Swiss Tropical And Public Health Institute

A vHTS approach for the identification of beta-adrenoceptor ligands.

4Sc

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.

Merck Research Laboratories

Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.

University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj

 

Carboxyl-promoted enhancement of selectivity for the β₃ adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β₃ binding selectivity

TBA

 

BMS-187257, a potent, selective, and novel heterocyclic β₃ adrenergic receptor agonist

TBA

Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.

Glaxosmithkline

Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.

Astellas Pharma

Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.

Astellas Pharma

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.

Institute Of Nuclear Chemistry Johannes Gutenberg-University Mainz

Substituted 1,2,3,4-tetrahydroquinolin-6-yloxypropanes as beta3-adrenergic receptor agonists: design, synthesis, biological evaluation and pharmacophore modeling.

Central Drug Research Institute

Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.

Astellas Pharma

Highly functionalized 7-azaindoles as selective PPAR gamma modulators.

Merck Research Laboratories

Discovery of a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.

Astellas Pharma

Potent oxindole based human beta3 adrenergic receptor agonists.

Eli Lilly

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Pfizer

Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.

Bristol-Myers Squibb Pharmaceutical Research Institute

Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.

Università

Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.

Eli Lilly

Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.

Columbia University College Of Physicians And Surgeons

Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.

Dainippon Pharmaceutical

Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.

Dainippon Pharmaceutical

Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.

Dainippon Pharmaceutical

Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y

National Institute Of Diabetes And Digestive And Kidney Diseases

BMS-201620: a selective beta 3 agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute

Structure-Activity Relationship of Heterocyclic P2Y

National Institute Of Diabetes And Digestive And Kidney Diseases

Development of 3D-QSAR models in cyclic ureidobenzenesulfonamides: human beta3-adrenergic receptor agonist.

Central Drug Research Institute

Cyclic amine sulfonamides as linkers in the design and synthesis of novel human beta(3) adrenergic receptor agonists.

Wyeth Research

Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.

Dainippon Pharmaceutical

Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.

Wyeth Research

Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.

Wyeth Research

4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor.

Wyeth-Ayerst Research

BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

Bristol-Myers Squibb Pharmaceutical Research Institute

New oxadiazolidinedione derivatives as potent and selective human beta3 agonists.

Wyeth-Ayerst Research

2,4-Thiazolidinediones as potent and selective human beta3 agonists.

Wyeth-Ayerst Research

Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.

Merck Research Laboratories

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.

Merck Research Laboratories

Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.

Merck Research Laboratories

Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.

Merck Research Laboratories

Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore.

Merck Research Laboratories

Substituted oxazole benzenesulfonamides as potent human beta3 adrenergic receptor agonists.

Merck Research Laboratories

Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective beta3 adrenergic receptor agonist antiobesity agents.

Merck Research Laboratories

Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.

Merck Research Laboratories

Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D

National Institute Of Neurological Disorders And Stroke

Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.

Merck Research Laboratories

L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.

Merck Research Laboratories

Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.

Merck Research Laboratories

Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.

Merck Research Laboratories

Pharmacological treatment of obesity: therapeutic strategies.

The R. W. Johnson Pharmaceutical Research Institute

3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.

Merck Research Laboratories

Design and in Vivo Characterization of A

Medical College Of Wisconsin

3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.

Merck Research Laboratories

Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.

Merck Research Laboratories

Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.

Merck Research Laboratories

3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT

University Of Minnesota Twin Cities

Discovery of benzamides as potent human ?3 adrenergic receptor agonists.

Merck And

Comparative 3D QSAR study on ?(1)-, ?(2)-, and ?(3)-adrenoceptor agonists.

National Institute Of Pharmaceutical Education And Research

Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.

Drug Discovery Laboratory

Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.

Glaxosmithkline

2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.

University Of Tennessee

Synthesis and biological evaluation of ?

Shenyang Pharmaceutical University

Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.

Texas Tech University Health Sciences Center

Design and synthesis of aryloxypropanolamine as ?

East China Normal University

Structure-Guided Modification of Heterocyclic Antagonists of the P2Y

National Institute Of Diabetes And Digestive And Kidney Diseases

Discovery of Novel Indazole Derivatives as Orally Available?

Asahi Kasei Pharma

Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.

Case Western Reserve University

Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.

UniversitÄT WÜRzburg

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

Pharmacological characterization of KUR-1246, a selective uterine relaxant.

Kissei Pharmaceutical

The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.

University Of Nottingham