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Page 1
3-Phenyl-5-isothiazole carboxamides with potent mGluR1 antagonist activity.
Fisher MJ, Backer RT, Barth VN, Garbison KE, Gruber JM, Heinz BA, Iyengar S, Hollinshead SP, Kingston A, Kuklish SL, Li L, Nisenbaum ES, Peters SC, Phebus L, Simmons RM, van der Aar E. Fisher MJ, et al. Among authors: simmons rm. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2514-7. doi: 10.1016/j.bmcl.2012.02.003. Epub 2012 Feb 9. Bioorg Med Chem Lett. 2012. PMID: 22386665
Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.
Hao J, Dehlinger V, Fivush AM, Rudyk HC, Britton TC, Hollinshead SP, Vokits BP, Clark BP, Henry SS, Massey SM, Peng L, Dressman BA, Heinz BA, Roberts EF, Bracey-Walker MR, Swanson S, Catlow JT, Love PL, Tepool AD, Peters SC, Simmons RM, Iyengar S, McKinzie DL, Monn JA. Hao J, et al. Among authors: simmons rm. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1249-52. doi: 10.1016/j.bmcl.2013.01.009. Epub 2013 Jan 12. Bioorg Med Chem Lett. 2013. PMID: 23374867
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Dominguez E, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Buckmaster JL, Castano AM, Del Prado M, Escribano A, Filla SA, Ho KH, Hudziak KJ, Jones CK, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Dominguez E, et al. Among authors: simmons rm. J Med Chem. 2005 Jun 30;48(13):4200-3. doi: 10.1021/jm0491952. J Med Chem. 2005. PMID: 15974569
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Dreyfus N, Myers JK, Badescu VO, de Frutos O, de la Puente ML, Ding C, Filla SA, Fynboe K, Gernert DL, Heinz BA, Hemrick-Luecke SK, Johnson KW, Johnson MP, López P, Love PL, Martin LJ, Masquelin T, McCoy MJ, Mendiola J, Morrow D, Muhlhauser M, Pascual G, Perun TJ, Pfeifer LA, Phebus LA, Richards SJ, Rincón JA, Seest EP, Shah J, Shaojuan J, Simmons RM, Stephenson GA, Tromiczak EG, Thompson LK, Walter MW, Weber WW, Zarrinmayeh H, Thomas CE, Joshi E, Iyengar S, Johansson AM. Dreyfus N, et al. Among authors: simmons rm. ACS Med Chem Lett. 2013 May 7;4(6):560-4. doi: 10.1021/ml400049p. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900709 Free PMC article.
GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: simmons rm. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6459-62. doi: 10.1016/j.bmcl.2013.09.046. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24119554
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: simmons rm. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. Epub 2013 Sep 24. Bioorg Med Chem Lett. 2013. PMID: 24140446
Modulation of TARP γ8-Containing AMPA Receptors as a Novel Therapeutic Approach for Chronic Pain.
Knopp KL, Simmons RMA, Guo W, Adams BL, Gardinier KM, Gernert DL, Ornstein PL, Porter W, Reel J, Ding C, Wang H, Qian Y, Burris KD, Need A, Barth V, Swanson S, Catlow J, Witkin JM, Zwart R, Sher E, Choong KC, Wall TM, Schober D, Felder CC, Kato AS, Bredt DS, Nisenbaum ES. Knopp KL, et al. Among authors: simmons rma. J Pharmacol Exp Ther. 2019 Jun;369(3):345-363. doi: 10.1124/jpet.118.250126. Epub 2019 Mar 25. J Pharmacol Exp Ther. 2019. PMID: 30910921
138 results