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Page 1
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG. Watterson SH, et al. Among authors: balimane p. J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u. J Med Chem. 2010. PMID: 20405922
Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.
Potin D, Launay M, Monatlik F, Malabre P, Fabreguettes M, Fouquet A, Maillet M, Nicolai E, Dorgeret L, Chevallier F, Besse D, Dufort M, Caussade F, Ahmad SZ, Stetsko DK, Skala S, Davis PM, Balimane P, Patel K, Yang Z, Marathe P, Postelneck J, Townsend RM, Goldfarb V, Sheriff S, Einspahr H, Kish K, Malley MF, DiMarco JD, Gougoutas JZ, Kadiyala P, Cheney DL, Tejwani RW, Murphy DK, Mcintyre KW, Yang X, Chao S, Leith L, Xiao Z, Mathur A, Chen BC, Wu DR, Traeger SC, McKinnon M, Barrish JC, Robl JA, Iwanowicz EJ, Suchard SJ, Dhar TG. Potin D, et al. Among authors: balimane p. J Med Chem. 2006 Nov 30;49(24):6946-9. doi: 10.1021/jm0610806. J Med Chem. 2006. PMID: 17125246
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. Among authors: balimane p. 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
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, 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, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Guo J, et al. Among authors: balimane p. Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1. Bioorg Med Chem Lett. 2016. PMID: 27055941
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: balimane p. 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 and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D. Velaparthi U, et al. Among authors: balimane p. J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3. J Med Chem. 2008. PMID: 18763755
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. Among authors: balimane p. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.
Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ. Dhar TG, et al. Among authors: balimane p. ACS Med Chem Lett. 2016 Jan 19;7(3):283-8. doi: 10.1021/acsmedchemlett.5b00448. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985316 Free PMC article.
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.
Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ. Yang MG, et al. Among authors: balimane p. J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7. J Med Chem. 2016. PMID: 28002964
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.
Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG. Xiao HY, et al. Among authors: balimane pv. J Med Chem. 2016 Nov 10;59(21):9837-9854. doi: 10.1021/acs.jmedchem.6b01099. Epub 2016 Oct 20. J Med Chem. 2016. PMID: 27726358
44 results