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Page 1
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. Wittman M, et al. Among authors: balimane p. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Saulnier MG, Frennesson DB, Wittman MD, Zimmermann K, Velaparthi U, Langley DR, Struzynski C, Sang X, Carboni J, Li A, Greer A, Yang Z, Balimane P, Gottardis M, Attar R, Vyas D. Saulnier MG, et al. Among authors: balimane p. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1702-7. doi: 10.1016/j.bmcl.2008.01.049. Epub 2008 Jan 18. Bioorg Med Chem Lett. 2008. PMID: 18258427
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Langley DR, Sang X, Frennesson D, Carboni J, Li A, Greer A, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Vyas D. Zimmermann K, et al. Among authors: balimane p. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4075-80. doi: 10.1016/j.bmcl.2008.05.104. Epub 2008 Jun 21. Bioorg Med Chem Lett. 2008. PMID: 18572407
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
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. Zimmermann K, et al. Among authors: balimane p. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20153189
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
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 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.
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
44 results