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Page 1
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: heasley se. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R. Vazquez ML, et al. Among authors: heasley se. J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23. J Med Chem. 2018. PMID: 29298069
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, Macinnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JL, Curtiss SW, Fobian YM, Heasley SE, Cubbage JW, Moon JB, Brown DL, Acker BA, Maddux TM, Tollefson MB, Mischke BV, Owen DR, Freskos JN, Molyneaux JM, Benson AG, Blevis-Bal RM. Hughes RO, et al. Among authors: heasley se. J Med Chem. 2010 Mar 25;53(6):2656-60. doi: 10.1021/jm901781q. J Med Chem. 2010. PMID: 20196613
Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: use of a conformation-based hypothesis to facilitate compound design.
Walker DP, Arhancet GB, Lu HF, Heasley SE, Metz S, Kablaoui NM, Franco FM, Hanau CE, Scholten JA, Springer JR, Fobian YM, Carter JS, Xing L, Yang S, Shaffer AF, Jerome GM, Baratta MT, Moore WM, Vazquez ML. Walker DP, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1120-6. doi: 10.1016/j.bmcl.2012.11.107. Epub 2012 Dec 12. Bioorg Med Chem Lett. 2013. PMID: 23298810
Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation.
Arhancet GB, Walker DP, Metz S, Fobian YM, Heasley SE, Carter JS, Springer JR, Jones DE, Hayes MJ, Shaffer AF, Jerome GM, Baratta MT, Zweifel B, Moore WM, Masferrer JL, Vazquez ML. Arhancet GB, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. doi: 10.1016/j.bmcl.2012.11.109. Epub 2012 Dec 6. Bioorg Med Chem Lett. 2013. PMID: 23260349
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Hughes RO, Walker JK, Cubbage JW, Fobian YM, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Owen DR, Jacobsen EJ, Freskos JN, Molyneaux JM, Brown DL, Stallings WC, Acker BA, Maddux TM, Tollefson MB, Williams JM, Moon JB, Mischke BV, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4092-6. doi: 10.1016/j.bmcl.2009.06.004. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19539468
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Hughes RO, Walker JK, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Jacobsen EJ, Cubbage JW, Fobian YM, Owen DR, Freskos JN, Molyneaux JM, Brown DL, Acker BA, Maddux TM, Tollefson MB, Moon JB, Mischke BV, Rumsey JM, Zheng Y, MacInnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5209-13. doi: 10.1016/j.bmcl.2009.07.019. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19631533
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Owen DR, Walker JK, Jon Jacobsen E, Freskos JN, Hughes RO, Brown DL, Bell AS, Brown DG, Phillips C, Mischke BV, Molyneaux JM, Fobian YM, Heasley SE, Moon JB, Stallings WC, Joseph Rogier D, Fox DN, Palmer MJ, Ringer T, Rodriquez-Lens M, Cubbage JW, Blevis-Bal RM, Benson AG, Acker BA, Maddux TM, Tollefson MB, Bond BR, Macinnes A, Yu Y. Owen DR, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4088-91. doi: 10.1016/j.bmcl.2009.06.012. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19540112 Free article.
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
Nieman JA, Nair SK, Heasley SE, Schultz BL, Zerth HM, Nugent RA, Chen K, Stephanski KJ, Hopkins TA, Knechtel ML, Oien NL, Wieber JL, Wathen MW. Nieman JA, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2010 May 15;20(10):3039-42. doi: 10.1016/j.bmcl.2010.03.115. Epub 2010 Apr 3. Bioorg Med Chem Lett. 2010. PMID: 20403696
Acidic triazoles as soluble guanylate cyclase stimulators.
Roberts LR, Bradley PA, Bunnage ME, England KS, Fairman D, Fobian YM, Fox DN, Gymer GE, Heasley SE, Molette J, Smith GL, Schmidt MA, Tones MA, Dack KN. Roberts LR, et al. Among authors: heasley se. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6515-8. doi: 10.1016/j.bmcl.2011.08.071. Epub 2011 Aug 28. Bioorg Med Chem Lett. 2011. PMID: 21924901