J. Hynes

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Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.

A B Smith, C. Strader, M. Cichy-Knight, 1996, Journal of medicinal chemistry.

Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.

A B Smith, M. Cichy-Knight, W. Shakespeare, 1998, Journal of medicinal chemistry.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

James Lin, K. McIntyre, D. Shuster, 2015, Journal of medicinal chemistry.

Small molecule p38 inhibitors: novel structural features and advances from 2002-2005.

J. Hynes, Katerina Leftheri, 2005, Current topics in medicinal chemistry.

Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.

D. Shuster, J. Macor, J. Yanchunas, 2020, Journal of medicinal chemistry.

DBS sampling can be used to stabilize prodrugs in drug discovery rodent studies without the addition of esterase inhibitors.

T. Olah, L. Cornelius, J. Santella, 2010, Bioanalysis.

Design and synthesis of novel scaffolds for drug discovery: hybrids of beta-D-glucose with 1,2,3,4-tetrahydrobenzo[e][1,4]diazepin-5-one, the corresponding 1-oxazepine, and 2- and 4-pyridyldiazepines.

R. Hirschmann, A. Smith, J. Hynes, 2001, Organic letters.

The discovery of BMS-457, a potent and selective CCR1 antagonist.

W. Guo, C. Cavallaro, A. Tebben, 2013, Bioorganic & medicinal chemistry letters.

Study on the mechanisms of glucocorticoid-induced hypertension: glucocorticoids increase transmembrane Ca2+ influx in vascular smooth muscle in vivo.

J. Hynes, L. Kornel, N. Kanamarlapudi, 1995, Endocrine research.

Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

J. Barrish, C. Cavallaro, A. Tebben, 2014, Journal of medicinal chemistry.

Discovery of highly potent, selective, covalent inhibitors of JAK3.

S. Spergel, G. Schieven, J. Barrish, 2017, Bioorganic & medicinal chemistry letters.

Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity

K. McIntyre, Wen-pin Yang, S. Ruepp, 2017, The Journal of Immunology.

This information is current as Demonstrates Steroid Sparing Activity Disease in Murine Lupus Models and Selective IRAK 4 Inhibition Attenuates

K. McIntyre, Wen-pin Yang, S. Ruepp, 2016 .

Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.

J. Barrish, D. Xie, N. Murugesan, 2020, ACS medicinal chemistry letters.

N-aryl pyrazoles, indazoles and azaindazoles as antagonists of CC chemokine receptor 1: patent cooperation treaty applications WO2010/036632, WO2009/134666 and WO2009/137338

P. Carter, J. Hynes, 2010, Expert opinion on therapeutic patents.

Tricyclic Sulfones as Potent, Selective and Efficacious RORγt Inverse Agonists - Exploring C6 and C8 SAR Using Late-Stage Functionalization.

Michael G. Yang, D. Shuster, C. Weigelt, 2020, Bioorganic & medicinal chemistry letters.

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

David S. Nirschl, David S Nirschl, Sidney Pitt, 2014, Bioorganic & medicinal chemistry letters.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

A. Doweyko, James Lin, J. Wityak, 2010, Journal of medicinal chemistry.

Identification of highly potent and selective PI3Kδ inhibitors.

G. Schieven, C. Weigelt, M. Poss, 2017, Bioorganic & medicinal chemistry letters.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

K. McIntyre, Sidney Pitt, G. Schieven, 2017, Journal of medicinal chemistry.

Assessing the risk of drug crystallization in vivo.

E. Janovitz, D. Drexler, S. Ruepp, 2019, Journal of pharmacological and toxicological methods.

C-3 Amido-indole cannabinoid receptor modulators.

Ping Chen, Derek J. Norris, K. McIntyre, 2002, Bioorganic & medicinal chemistry letters.

Synthesis and characterization of tritium labeled N-((R)-1-((S)-4-(4-chlorophenyl)-4-hydroxy-3,3-dimethylpiperidin-1-yl)-3-methyl-1-oxobutan-2-yl)-3-sulfamoylbenzamide.

J. Hynes, S. Bonacorsi, Balu N Balasubramanian, 2015, Journal of labelled compounds & radiopharmaceuticals.

Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.

J. Chen, S. Mandlekar, C. Cavallaro, 2012, Journal of medicinal chemistry.

Development of a Practical Synthesis of a p38 Kinase Inhibitor via a Safe and Robust Amination

S. Tummala, Paul C. Lobben, S. Leung, 2012 .

A General Large Scale Synthesis of 2-Alkyl-7-methoxyindoles

K. Leftheris, A. P. Skoumbourdis, J. Hynes, 2001 .

Novel chimeric scaffolds to extend the exploration of receptor space: hybrid beta-D-glucose-benzoheterodiazepine structures for broad screening. Effect of amide alkylation on the course of cyclization reactions.

R. Hirschmann, Amos B. Smith, J. Hynes, 2004, The Journal of organic chemistry.

N-Amination of pyrrole and indole heterocycles with monochloramine (NH2Cl).

K. Leftheris, J. Hynes, A. Dyckman, 2004, The Journal of organic chemistry.

Development of a Scalable Synthesis for the Potent Kinase Inhibitor BMS-986236; 1-(5-(4-(3-Hydroxy-3-methylbutyl)-1H-1,2,3-triazol-1-yl)-4-(isopropylamino)pyridin-2-yl)-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile

A. Mathur, A. Gupta, P. Carter, 2019, Organic Process Research & Development.

Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.

Ping Chen, Derek J. Norris, S. Spergel, 2003, Journal of medicinal chemistry.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

John Dodd, John S Tokarski, Arthur M Doweyko, 2008, Journal of medicinal chemistry.

Copper-catalyzed chlorination of functionalized arylboronic acids.

J. Hynes, Hong-ru Wu, 2010, Organic letters.

Cyclic derivatives as modulators of chemokine receptor

Michael G. Yang, A. Srivastava, P. Carter, 2004 .

Developing Adnectins that target SRC co-activator binding to PXR: a structural approach toward understanding promiscuity of PXR.

Eric T Baldwin, Martin C. Wright, Andrew J Tebben, 2015, Journal of molecular biology.

A Review of Clinical Trials Assessing the Efficacy and Safety of Newer Antiarrhythmic Drugs in Atrial Fibrillation

G. Naccarelli, S. Samii, J. Luck, 2003, Journal of Interventional Cardiac Electrophysiology.

Old and new antiarrhythmic drugs for converting and maintaining sinus rhythm in atrial fibrillation: comparative efficacy and results of trials.

G. Naccarelli, S. Samii, J. Luck, 2003, The American journal of cardiology.

Maintaining stability of sinus rhythm in atrial fibrillation: Antiarrhythmic drugs versus ablation

G. Naccarelli, J. Luck, J. Hynes, 2002, Current cardiology reports.

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Wei Li, Gulzar Ahmed, John Dodd, 2004, Journal of medicinal chemistry.

Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.

A. Doweyko, Sidney Pitt, G. Schieven, 2010, Bioorganic & medicinal chemistry letters.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

K. McIntyre, Sidney Pitt, G. Schieven, 2017, Bioorganic & medicinal chemistry letters.

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt ‒ Identification of a Potent, Selective Series with Biologic-Like In Vivo Efficacy.

K. McIntyre, D. Shuster, J. Macor, 2019, Journal of medicinal chemistry.

Chapter Nine - Advances in the Discovery of Small-Molecule IRAK4 Inhibitors

J. Hynes, S. Nair, 2014 .

Annulation Reaction Enables the identification of an Exocyclic Amide Tricyclic Chemotype as Retinoic Acid Receptor-Related Orphan Receptor Gamma (RORγ/RORc) Inverse Agonists.

Michael A. Galella, C. Weigelt, M. Cvijic, 2020, Bioorganic & medicinal chemistry letters.

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

A. Doweyko, K. McIntyre, D. Shuster, 2008, Bioorganic & medicinal chemistry letters.

Amination of heterocyclic compounds with o-benzoylhydroxylamine derivatives.

L. Parlanti, J. Hynes, Michael M. Miller, 2007, Organic letters.

Copper-catalyzed chlorination of functionalized arylboronic acids.

J. Hynes, Hong-ru Wu, 2010, Organic Letters.