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Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine.
Horne DB, Biswas K, Brown J, Bartberger MD, Clarine J, Davis CD, Gore VK, Harried S, Horner M, Kaller MR, Lehto SG, Liu Q, Ma VV, Monenschein H, Nguyen TT, Yuan CC, Youngblood BD, Zhang M, Zhong W, Allen JR, Chen JJ, Gavva NR. Horne DB, et al. Among authors: allen jr. J Med Chem. 2018 Sep 27;61(18):8186-8201. doi: 10.1021/acs.jmedchem.8b00518. Epub 2018 Sep 10. J Med Chem. 2018. PMID: 30148953
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Lanman BA, Allen JR, Allen JG, Amegadzie AK, Ashton KS, Booker SK, Chen JJ, Chen N, Frohn MJ, Goodman G, Kopecky DJ, Liu L, Lopez P, Low JD, Ma V, Minatti AE, Nguyen TT, Nishimura N, Pickrell AJ, Reed AB, Shin Y, Siegmund AC, Tamayo NA, Tegley CM, Walton MC, Wang HL, Wurz RP, Xue M, Yang KC, Achanta P, Bartberger MD, Canon J, Hollis LS, McCarter JD, Mohr C, Rex K, Saiki AY, San Miguel T, Volak LP, Wang KH, Whittington DA, Zech SG, Lipford JR, Cee VJ. Lanman BA, et al. Among authors: allen jg, allen jr. J Med Chem. 2020 Jan 9;63(1):52-65. doi: 10.1021/acs.jmedchem.9b01180. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820981
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: allen jr. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
Chromenones as potent bradykinin B1 antagonists.
Bryan MC, Biswas K, Peterkin TA, Rzasa RM, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR. Bryan MC, et al. Among authors: allen jr. Bioorg Med Chem Lett. 2012 Jan 1;22(1):619-22. doi: 10.1016/j.bmcl.2011.10.068. Epub 2011 Oct 28. Bioorg Med Chem Lett. 2012. PMID: 22088753
Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease.
Chen JJ, Qian W, Biswas K, Yuan C, Amegadzie A, Liu Q, Nixey T, Zhu J, Ncube M, Rzasa RM, Chavez F Jr, Chen N, DeMorin F, Rumfelt S, Tegley CM, Allen JR, Hitchcock S, Hungate R, Bartberger MD, Zalameda L, Liu Y, McCarter JD, Zhang J, Zhu L, Babu-Khan S, Luo Y, Bradley J, Wen PH, Reid DL, Koegler F, Dean C Jr, Hickman D, Correll TL, Williamson T, Wood S. Chen JJ, et al. Among authors: allen jr. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6447-54. doi: 10.1016/j.bmcl.2013.09.041. Epub 2013 Sep 29. Bioorg Med Chem Lett. 2013. PMID: 24139583
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: allen jr. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A, Siegmund AC, Wen PH, Whittington DA, Allen JR, Wood S. Pettus LH, et al. Among authors: allen jr. J Med Chem. 2020 Mar 12;63(5):2263-2281. doi: 10.1021/acs.jmedchem.9b01034. Epub 2019 Oct 18. J Med Chem. 2020. PMID: 31589043
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Tamayo NA, Bourbeau MP, Allen JR, Ashton KS, Chen JJ, Kaller MR, Nguyen TT, Nishimura N, Pettus LH, Walton M, Belmontes B, Moriguchi J, Chen K, McCarter JD, Hanestad K, Chung G, Ninniri MSS, Sun J, Poppe L, Spahr C, Hui J, Jia L, Wu T, Dahal UP, Edson KZ, Payton M. Tamayo NA, et al. Among authors: allen jr. J Med Chem. 2022 Mar 24;65(6):4972-4990. doi: 10.1021/acs.jmedchem.1c02030. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35286090
1,702 results