Publications by authors named "Sidney Pitt"

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Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Steven H Spergel, Michael E Mertzman, James Kempson, Junqing Guo, Sylwia Stachura, Sidney Pitt, William J Pitts

ACS Med Chem Lett· March 2019

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
John Hynes, Hong Wu, James Kempson, James J-W Duan, Zhonghui Lu, Sidney Pitt, William J Pitts

Bioorg Med Chem Lett· July 2017

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Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Qingjie Liu, Qing Shi, David Marcoux, Douglas G Batt, Lyndon Cornelius, Sidney Pitt

J Med Chem· June 2017

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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
James J-W Duan, Zhonghui Lu, Bin Jiang, Bingwei V Yang, Lidia M Doweyko, Sidney Pitt, William J Pitts

Bioorg Med Chem Lett· December 2014

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The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Stephen T Wrobleski, Shuqun Lin, T G Murali Dhar, Alaric J Dyckman, Tianle Li, Sidney Pitt

Bioorg Med Chem Lett· July 2013

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Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.
Alaric J Dyckman, Tianle Li, Sidney Pitt, Rosemary Zhang, Ding Ren Shen

Bioorg Med Chem Lett· August 2011

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5-amino-pyrazoles as potent and selective p38α inhibitors.
Jagabandhu Das, Robert V Moquin, Alaric J Dyckman, Tianle Li, Sidney Pitt

Bioorg Med Chem Lett· December 2010

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Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.
Shuqun Lin, Stephen T Wrobleski, John Hynes, Sidney Pitt, Rosemary Zhang

Bioorg Med Chem Lett· October 2010

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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.
Chunjian Liu, James Lin, Stephen T Wrobleski, Shuqun Lin, John Hynes, Sidney Pitt

J Med Chem· September 2010

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Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Jagabandhu Das, Robert V Moquin, Sidney Pitt, Rosemary Zhang, Ding Ren Shen

Bioorg Med Chem Lett· April 2008

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Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Stephen T Wrobleski, Shuqun Lin, John Hynes, Hong Wu, Sidney Pitt

Bioorg Med Chem Lett· April 2008

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Benzothiazole based inhibitors of p38alpha MAP kinase.
Chunjian Liu, James Lin, Sidney Pitt, Rosemary F Zhang, John S Sack

Bioorg Med Chem Lett· March 2008

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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.
John Hynes, Hong Wu, Sidney Pitt, Ding Ren Shen, Rosemary Zhang

Bioorg Med Chem Lett· March 2008

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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 Hynes, Alaric J Dyckman, Shuqun Lin, Stephen T Wrobleski, Hong Wu, Sidney Pitt

J Med Chem· January 2008

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Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
T G Murali Dhar, Stephen T Wrobleski, Shuqun Lin, Joseph A Furch, David S Nirschl, Sidney Pitt

Bioorg Med Chem Lett· September 2007

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2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Jagabandhu Das, Ping Chen, Derek Norris, Ramesh Padmanabha, James Lin, Sidney Pitt

J Med Chem· November 2006

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5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.
Chunjian Liu, Stephen T Wrobleski, James Lin, Gulzar Ahmed, Axel Metzger, Sidney Pitt

J Med Chem· October 2005

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Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Ping Chen, Derek Norris, Jagabandhu Das, Steven H Spergel, John Wityak, Sidney Pitt

Bioorg Med Chem Lett· December 2004

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The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Katerina Leftheris, Gulzar Ahmed, Ran Chan, Alaric J Dyckman, Zahid Hussain, Sidney Pitt

J Med Chem· December 2004

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Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Louis J Lombardo, Francis Y Lee, Ping Chen, Derek Norris, Joel C Barrish, Sidney Pitt

J Med Chem· December 2004

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Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).
John Wityak, Jagabandhu Das, Robert V Moquin, Zhongqi Shen, James Lin, Sidney Pitt

Bioorg Med Chem Lett· November 2003

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Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.
Jagabandhu Das, Robert V Moquin, James Lin, Chunjian Liu, Arthur M Doweyko, Sidney Pitt

Bioorg Med Chem Lett· August 2003

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Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.
Jagabandhu Das, James Lin, Robert V Moquin, Zhongqi Shen, Steven H Spergel, Sidney Pitt

Bioorg Med Chem Lett· July 2003

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Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).
Ping Chen, Derek Norris, Edwin J Iwanowicz, Steven H Spergel, James Lin, Sidney Pitt

Bioorg Med Chem Lett· May 2002

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