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Page 1
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Srivastava AS, Ko S, Watterson SH, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Yip S, Li P, Sun D, Wu DR, Dai J, Wang C, Zhang Y, Wang B, Pawluczyk J, Kempson J, Zhao R, Hou X, Rampulla R, Mathur A, Galella MA, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Srivastava AS, et al. Among authors: watterson sh. ACS Med Chem Lett. 2020 Sep 16;11(11):2195-2203. doi: 10.1021/acsmedchemlett.0c00335. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214829 Free PMC article.
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Watterson SH, et al. J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10. J Med Chem. 2016. PMID: 26924461
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ. Gilmore JL, et al. Among authors: watterson sh. J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27309907
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29. J Med Chem. 2019. PMID: 30893553
Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419).
Watterson SH, Chen P, Zhao Y, Gu HH, Dhar TG, Xiao Z, Ballentine SK, Shen Z, Fleener CA, Rouleau KA, Obermeier M, Yang Z, McIntyre KW, Shuster DJ, Witmer M, Dambach D, Chao S, Mathur A, Chen BC, Barrish JC, Robl JA, Townsend R, Iwanowicz EJ. Watterson SH, et al. J Med Chem. 2007 Jul 26;50(15):3730-42. doi: 10.1021/jm070299x. Epub 2007 Jun 22. J Med Chem. 2007. PMID: 17585753
Novel tricyclic inhibitors of IkappaB kinase.
Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: watterson sh. J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816. J Med Chem. 2009. PMID: 19267461
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.
Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: watterson sh. Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19376699
Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis.
Gillooly KM, Pattoli MA, Taylor TL, Chen L, Cheng L, Gregor KR, Whitney GS, Susulic V, Watterson SH, Kempson J, Pitts WJ, Booth-Lute H, Yang G, Davies P, Kukral DW, Strnad J, McIntyre KW, Darienzo CJ, Salter-Cid L, Yang Z, Wang-Iverson DB, Burke JR. Gillooly KM, et al. Among authors: watterson sh. J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. doi: 10.1124/jpet.109.156018. Epub 2009 Aug 3. J Pharmacol Exp Ther. 2009. PMID: 19652024
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Dyckman AJ, et al. Among authors: watterson sh. Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21087862
32 results