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18 results

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Page 1
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: chmait s. J Med Chem. 2010 Apr 8;53(7):2973-85. doi: 10.1021/jm100095x. J Med Chem. 2010. PMID: 20218619
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Xu S, Henkle B, Sherman L, Plant M, Miner K, McBride H, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: chmait s. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4724-8. doi: 10.1016/j.bmcl.2009.06.058. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19574047
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Henkle B, Sherman L, Plant M, Miner K, McBride HJ, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: chmait s. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1680-4. doi: 10.1016/j.bmcl.2010.01.059. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138761
Identification of triazolopyridazinones as potent p38α inhibitors.
Herberich B, Jackson C, Wurz RP, Pettus LH, Sherman L, Liu Q, Henkle B, Saris CJ, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Herberich B, et al. Among authors: chmait s. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1226-9. doi: 10.1016/j.bmcl.2011.11.067. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22196117
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Hu E, Kunz RK, Chen N, Rumfelt S, Siegmund A, Andrews K, Chmait S, Zhao S, Davis C, Chen H, Lester-Zeiner D, Ma J, Biorn C, Shi J, Porter A, Treanor J, Allen JR. Hu E, et al. Among authors: chmait s. J Med Chem. 2013 Nov 14;56(21):8781-92. doi: 10.1021/jm401234w. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24102193
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR. Hu E, et al. Among authors: chmait s. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJS, Allen JR. Rzasa RM, et al. Among authors: chmait s. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.
Tamayo NA, Norman MH, Bartberger MD, Hong FT, Bo Y, Liu L, Nishimura N, Yang KC, Tadesse S, Fotsch C, Chen J, Chmait S, Cupples R, Hale C, Jordan SR, Lloyd DJ, Sivits G, Van G, St Jean DJ Jr. Tamayo NA, et al. Among authors: chmait s. J Med Chem. 2015 Jun 11;58(11):4462-82. doi: 10.1021/jm5018175. Epub 2015 Jun 1. J Med Chem. 2015. PMID: 25914941
18 results