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Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein-Protein Interaction.

Janssen Research and Development
Evaluation of anti-diabetic effect and gall bladder function with 2-thio-5-thiomethyl substituted imidazoles as TGR5 receptor agonists.

Janssen Research and Development
Discovery of Orally Efficacious Tetrahydrobenzimidazoles as TGR5 Agonists for Type 2 Diabetes.

Janssen Research and Development
Tetrahydropyrazolo[4,3-c]pyridine derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.

Janssen Research and Development
Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.

Janssen Research and Development
The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.

Janssen Research and Development
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Janssen Research and Development
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.

Janssen Research and Development
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.

Janssen Research and Development
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.

Janssen Research and Development
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.

Janssen Research and Development
Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.

Janssen Research and Development
Elements and modulation of functional dynamics.

Janssen Research and Development
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.

Janssen Research and Development
The discovery and SAR of cyclopenta[b]furans as inhibitors of CCR2.

Janssen Research and Development
Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists.

Janssen Research and Development
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs.

Janssen Research and Development
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.

Janssen Research and Development
Inhibition of hypoxia-inducible factor prolyl hydroxylase domain oxygen sensors: tricking the body into mounting orchestrated survival and repair responses.

Janssen Research and Development
Discovery and SAR of 5-aminooctahydrocyclopentapyrrole-3a-carboxamides as potent CCR2 antagonists.

Janssen Research and Development
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.

Janssen Research and Development
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.

Janssen Research and Development
The discovery of potent selective NPY Y(2) antagonists.

Janssen Research and Development
A thiocarbamate inhibitor of endothelial lipase raises HDL cholesterol levels in mice.

Janssen Research and Development
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists.

Janssen Research and Development
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.

Janssen Research and Development
Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.

Janssen Research and Development
A novel series of N-(azetidin-3-yl)-2-(heteroarylamino)acetamide CCR2 antagonists.

Janssen Research and Development
Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.

Janssen Research and Development
Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.

Janssen Research and Development
Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.

Janssen Research and Development
Azabenzthiazole inhibitors of leukotriene A4 hydrolase.

Janssen Research and Development
Design and characterization of optimized adenosine A2A/A1 receptor antagonists for the treatment of Parkinson's disease.

Janssen Research and Development
Identification of a duald OR antagonist/µ OR agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d).

Janssen Research and Development
Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions.

Janssen Research and Development
Discovery of Acyl-Indole Derivatives as Pan-Serotype Dengue Virus NS4B Inhibitors.

Janssen Research and Development
-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.

Janssen Research and Development
Diazepinone HBV capsid assembly modulators.

Janssen Research and Development
Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer.

Janssen Research and Development
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

Janssen Research and Development
Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.

Janssen Research and Development
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.

Janssen Research and Development
3-Substituted Quinolines as RORγt Inverse Agonists.

Janssen Research and Development
Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.

Janssen Research and Development
Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.

Janssen Research and Development
6-Substituted quinolines as RORγt inverse agonists.

Janssen Research and Development
Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.

Janssen Research and Development
Indazole-based ligands for estrogen-related receptor α as potential anti-diabetic agents.

Janssen Research and Development
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.

Janssen Research and Development
Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists.

Janssen Research and Development
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Janssen Research and Development
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Janssen Research and Development