Publications by authors named "Rajeev Bhide"

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Discovery of BMS-986308: A Renal Outer Medullary Potassium Channel Inhibitor for the Treatment of Heart Failure.
Jeremy M Richter, Prashantha Gunaga, Navnath Yadav, Rajesh Onkardas Bora, Rajeev Bhide

J Med Chem· June 2024

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Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.
Satheesh Nair, Sreekantha Ratna Kumar, Venkatram Reddy Paidi, Ramesh Sistla, Durgarao Kantheti, Rajeev S Bhide

ACS Med Chem Lett· July 2020

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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors.
Rajeev S Bhide, Alec Keon, Carolyn Weigelt, John S Sack, Robert J Schmidt

Bioorg Med Chem Lett· November 2017

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Identification of highly potent and selective PI3Kδ inhibitors.
David Marcoux, Lan-Ying Qin, Zheming Ruan, Qing Shi, Qian Ruan, Rajeev Bhide

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, Rajeev S Bhide

J Med Chem· June 2017

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Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Lan-Ying Qin, Zheming Ruan, Robert J Cherney, T G Murali Dhar, James Neels, Rajeev S Bhide

Bioorg Med Chem Lett· February 2017

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Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.
Rajeev S Bhide, James Neels, Lan-Ying Qin, Zheming Ruan, Sylwia Stachura

Bioorg Med Chem Lett· September 2016

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Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: observation of extensive dynamics in an enzyme/inhibitor complex.
Soong-Hoon Kim, Keith L Constantine, Gerald J Duke, Valentina Goldfarb, John T Hunt, Rajeev S Bhide

Bioorg Med Chem Lett· July 2013

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The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases.
Rajeev S Bhide, Louis J Lombardo, John T Hunt, Zhen-Wei Cai, Joel C Barrish

Mol Cancer Ther· February 2010

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Preclinical pharmacokinetics and in vitro metabolism of brivanib (BMS-540215), a potent VEGFR2 inhibitor and its alanine ester prodrug brivanib alaninate.
Punit H Marathe, Amrita V Kamath, Yueping Zhang, Celia D'Arienzo, Rajeev Bhide

Cancer Chemother Pharmacol· December 2009

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Metabolism of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737): identification of an unusual N-acetylglucosamine conjugate in the cynomolgus monkey.
Benjamin M Johnson, Amrita V Kamath, John E Leet, Xiaohong Liu, Rajeev S Bhide

Drug Metab Dispos· December 2008

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Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Réjean Ruel, Carl Thibeault, Alexandre L'Heureux, Alain Martel, Zhen-Wei Cai, Rajeev S Bhide

Bioorg Med Chem Lett· May 2008

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Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Zhen-wei Cai, Yongzheng Zhang, Robert M Borzilleri, Ligang Qian, Stephanie Barbosa, Rajeev S Bhide

J Med Chem· March 2008

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Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.
Zhen-Wei Cai, Donna Wei, Robert M Borzilleri, Ligang Qian, Amrita Kamath, Rajeev S Bhide

Bioorg Med Chem Lett· February 2008

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Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.
Kyoung Soon Kim, Songfeng Lu, Lyndon A Cornelius, Louis J Lombardo, Robert M Borzilleri, Rajeev S Bhide

Bioorg Med Chem Lett· August 2006

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Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Robert M Borzilleri, Rajeev S Bhide, Joel C Barrish, Celia J D'Arienzo, George M Derbin

J Med Chem· June 2006

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Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Rajeev S Bhide, Zhen-Wei Cai, Yong-Zheng Zhang, Ligang Qian, Donna Wei

J Med Chem· April 2006

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Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Robert M Borzilleri, Xiaoping Zheng, Ligang Qian, Christopher Ellis, Zhen-wei Cai, Rajeev S Bhide

J Med Chem· June 2005

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Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Louis J Lombardo, Amy Camuso, John Clark, Krista Fager, Johnni Gullo-Brown, Rajeev S Bhide

Bioorg Med Chem Lett· April 2005

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Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.
Robert M Borzilleri, Zhen-Wei Cai, Christopher Ellis, Joseph Fargnoli, Aberra Fura, Rajeev S Bhide

Bioorg Med Chem Lett· March 2005

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Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.
John T Hunt, Toomas Mitt, Robert Borzilleri, Johnni Gullo-Brown, Joseph Fargnoli, Rajeev Bhide

J Med Chem· July 2004

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Concise and efficient synthesis of 4-fluoro-1H-pyrrolo[2,3-b]pyridine.
Carl Thibault, Alexandre L'Heureux, Rajeev S Bhide, Réjean Ruel

Org Lett· December 2003

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