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Page 1
Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.
Shipe WD, Sharik SS, Barrow JC, McGaughey GB, Theberge CR, Uslaner JM, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD. Shipe WD, et al. Among authors: theberge cr. J Med Chem. 2015 Oct 8;58(19):7888-94. doi: 10.1021/acs.jmedchem.5b00983. Epub 2015 Sep 25. J Med Chem. 2015. PMID: 26378882
Identification of potent, highly constrained CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hershey JC, Jelley R, Kreatsoulas C, Moore EL, Mosser SD, Quigley AG, Roller SA, Salvatore CA, Sharik SS, Theberge CR, Zartman CB, Kane SA, Graham SL, Selnick HG, Vacca JP, Williams TM. Stump CA, et al. Among authors: theberge cr. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2572-6. doi: 10.1016/j.bmcl.2010.02.086. Epub 2010 Feb 25. Bioorg Med Chem Lett. 2010. PMID: 20299218
NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ. McCauley JA, et al. Among authors: theberge cr. J Med Chem. 2004 Apr 8;47(8):2089-96. doi: 10.1021/jm030483s. J Med Chem. 2004. PMID: 15056006
Potent benzimidazolone-based CGRP receptor antagonists.
Theberge CR, Bednar RA, Bell IM, Corcoran HA, Fay JF, Hershey JC, Johnston VK, Kane SA, Mosser S, Salvatore CA, Williams TM, Zartman CB, Zhang XF, Graham SL, Vacca JP. Theberge CR, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6122-5. doi: 10.1016/j.bmcl.2008.10.019. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18947992
The discovery of highly potent CGRP receptor antagonists.
Stump CA, Bell IM, Bednar RA, Bruno JG, Fay JF, Gallicchio SN, Johnston VK, Moore EL, Mosser SD, Quigley AG, Salvatore CA, Theberge CR, Blair Zartman C, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Stump CA, et al. Among authors: theberge cr. Bioorg Med Chem Lett. 2009 Jan 1;19(1):214-7. doi: 10.1016/j.bmcl.2008.10.106. Epub 2008 Oct 31. Bioorg Med Chem Lett. 2009. PMID: 19010673
Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.
Bell IM, Bednar RA, Fay JF, Gallicchio SN, Hochman JH, McMasters DR, Miller-Stein C, Moore EL, Mosser SD, Pudvah NT, Quigley AG, Salvatore CA, Stump CA, Theberge CR, Wong BK, Zartman CB, Zhang XF, Kane SA, Graham SL, Vacca JP, Williams TM. Bell IM, et al. Among authors: theberge cr. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6165-9. doi: 10.1016/j.bmcl.2006.09.045. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2006. PMID: 17027263
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
Bell IM, Bednar RA, Corcoran HA, Fay JF, Gallicchio SN, Johnston VK, Hershey JC, Miller-Stein CM, Moore EL, Mosser SD, Roller SA, Salvatore CA, Theberge CR, Wong BK, Blair Zartman C, Kane SA, Williams TM, Graham SL, Vacca JP. Bell IM, et al. Among authors: theberge cr. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4740-2. doi: 10.1016/j.bmcl.2009.06.057. Epub 2009 Jun 17. Bioorg Med Chem Lett. 2009. PMID: 19577468
16 results