PMID

Data

Article Title

Organization

Discovery of phenyl acetamides as potent and selective GPR119 agonists.

Merck

Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents.

Institute of Materia Medica

Novel 5-nitropyrimidine derivatives bearing endo-azabicyclic alcohols/amines as potent GPR119 agonists.

Jiangxi University of Traditional Chinese Medicine

Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists.

East China Normal University

Design and synthesis of 1H-pyrazolo[3,4-c]pyridine derivatives as a novel structural class of potent GPR119 agonists.

Taisho Pharmaceutical

G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges.

Sanofi-Aventis Deutschland

Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists.

Merck Research Laboratory

Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.

Merck Research Laboratories

Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.

Arena Pharmaceuticals

Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.

Astrazeneca

Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists.

Korea Research Institute of Chemical Technology

Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists.

Arena Pharmaceuticals

Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.

Genomics Institute of The Novartis Research Foundation

Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.

Departments of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical and Translational Research, and Pharmaceutical Candi

Synthesis and structure-activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists.

Bristol-Myers Squibb

Discovery of structurally novel, potent and orally efficacious GPR119 agonists.

Genomics Institute of The Novartis Research Foundation

Discovery and optimization of 5-(2-((1-(phenylsulfonyl)-1,2,3,4-tetrahydroquinolin-7-yl)oxy)pyridin-4-yl)-1,2,4-oxadiazoles as novel gpr119 agonists.

Amgen

Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists.

Takeda Pharmaceutical

Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists.

Amgen

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.

Amgen

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.

Astrazeneca

Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists.

Kangwon National University

Novel acylethanolamide derivatives that modulate body weight through enhancement of hypothalamic pro-opiomelanocortin (POMC) and/or decreased neuropeptide Y (NPY).

Hebrew University of Jerusalem

Synthesis and biological evaluation of 5-nitropyrimidine analogs with azabicyclic substituents as GPR119 agonists.

College of Pharmacy of Kangwon National University

Modulators of the GPR119 Receptor for the Treatment of Metabolic Syndrome.

Dart Neuroscience

Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Pfizer

From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.

Pfizer

Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.

Astrazeneca

GPR119 Modulators for the Treatment of Diabetes, Obesity, and Related Diseases: Patent Highlight.

TBA

Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.

Glaxosmithkline

Identification of new potent GPR119 agonists by combining virtual screening and combinatorial chemistry.

Boehringer Ingelheim Pharma

Mitigating heterocycle metabolism in drug discovery.

Amgen

Synthesis and SAR studies of bicyclic amine series GPR119 agonists.

Sanwa Kagaku Kenkyusho

Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.

Astrazeneca

Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists.

Astellas Pharma

Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.

Arena Pharmaceuticals

Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.

Merck Research Laboratories

Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.

Arena Pharmaceuticals

Design of potent and selective GPR119 agonists for type II diabetes.

Merck

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

Pfizer

Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.

Pfizer

2,5-Disubstituted pyridines as potent GPR119 agonists.

Glaxosmithkline

Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.

Arena Pharmaceuticals

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

Discovery of a novel series of GPR119 agonists: Design, synthesis, and biological evaluation of N-(Piperidin-4-yl)-N-(trifluoromethyl)pyrimidin-4-amine derivatives.

Takeda Pharmaceutical

Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes.

M. S. University of Baroda

Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach.

Takeda Pharmaceutical

The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.

Chinese Academy of Medical Sciences&Peking Union Medical College

Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a log

Astrazeneca

Anti-diabetic drugs recent approaches and advancements.

Mizoram University

Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists.

Sichuan University

Effective Application of Metabolite Profiling in Drug Design and Discovery.

Pfizer

One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.

Koneru Lakshmaiah Education Foundation

Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists.

Japan Tobacco

Treatment of Diabetes, Obesity, Dyslipidemia, and Related Disorders with GPR119 Agonists.

Therachem Research Medilab

Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity.

University of Florida

Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure.

Japan Tobacco

Discovery of novel spiro[chromane-2,4'-piperidine] derivatives as potent and orally bioavailable G-protein-coupled receptor 119 agonists.

Kowa

Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.

Chinese Academy of Sciences

Design and synthesis of novel pyrimido[5,4-d]pyrimidine derivatives as GPR119 agonist for treatment of type 2 diabetes.

Jiangxi University of Traditional Chinese Medicine

Practical application of ligand efficiency metrics in lead optimisation.

Astrazeneca

Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists.

Taisho Pharmaceutical

Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure.

Japan Tobacco

Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists.

Sogang University

Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.

Merck

Design, synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists.

Korea Research Institute of Chemical Technology

Novel 3H-[1,2,3]triazolo[4,5-c]pyridine derivatives as GPR119 agonists: Synthesis and structure-activity/solubility relationships.

Taisho Pharmaceutical

Optimization of a novel series of potent and orally bioavailable GPR119 agonists.

Kowa

Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist.

Jiangxi University of Traditional Chinese Medicine