Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with …

W Albrecht, A Unger, SM Bauer, SA Laufer - 2017 - ACS Publications
The anti-inflammatory potential of p38 mitogen-activated protein kinase (MAPK) inhibitors
was coincidentally expanded to a dual inhibition of p38α MAPK and phosphodiesterase 4 …

KR-003048, a potent, orally active inhibitor of p38 mitogen-activated protein kinase

AG Montalban, E Boman, CD Chang, SC Ceide… - European journal of …, 2010 - Elsevier
The tumor necrosis factor-α (TNF-α) cytokine, secreted by activated monocytes/
macrophages and T lymphocytes, is implicated in several diseases, including rheumatoid …

Discovery of 6-(2, 4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl) propylamino]-8-methyl-8 H-pyrido [2, 3-d] pyrimidin-7-one (Pamapimod) and 6-(2, 4 …

DM Goldstein, M Soth, T Gabriel… - Journal of Medicinal …, 2011 - ACS Publications
The development of a new series of p38α inhibitors resulted in the identification of two
clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid …

Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation

HR Hope, GD Anderson, BL Burnette… - … of Pharmacology and …, 2009 - ASPET
Signal transduction through the p38 mitogen-activated protein (MAP) kinase pathway is
central to the transcriptional and translational control of cytokine and inflammatory mediator …

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy) …

C Liu, J Lin, J Hynes, H Wu, ST Wrobleski… - Journal of Medicinal …, 2015 - ACS Publications
In search for prodrugs to address the issue of pH-dependent solubility and exposure
associated with 1 (BMS-582949), a previously disclosed phase II clinical p38α MAP kinase …

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 …

C Liu, J Lin, ST Wrobleski, S Lin… - Journal of medicinal …, 2010 - ACS Publications
The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP
kinase inhibitor that is currently in phase II clinical trials for the treatment of rheumatoid …

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors

B Devadas, SR Selness, L Xing, HM Madsen… - Bioorganic & medicinal …, 2011 - Elsevier
A novel series of highly potent and selective p38 MAP kinase inhibitors was developed
originating from a substituted N-aryl-6-pyrimidinone scaffold. SAR studies coupled with in …

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase

NJ Liverton, JW Butcher, CF Claiborne… - Journal of medicinal …, 1999 - ACS Publications
Novel potent and selective diarylimidazole inhibitors of p38 MAP (mitogen-activated protein)
kinase are described which have activity in both cell-based assays of tumor necrosis factor-α …

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl) phenyl) thiazole-5-carboxamide (BMS-640994)—A potent and efficacious p38α MAP kinase …

J Hynes Jr, H Wu, S Pitt, DR Shen, R Zhang… - Bioorganic & medicinal …, 2008 - Elsevier
A novel structural class of p38α MAP kinase inhibitors has been identified via iterative SAR
studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS …

3-Amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38α mitogen-activated protein kinase

LH Pettus, S Xu, GQ Cao, PP Chakrabarti… - Journal of medicinal …, 2008 - ACS Publications
The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many
proinflammatory pathways, regulating the cellular response to a multitude of external stimuli …