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Page 1
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).
Li J, Kennedy LJ, Shi Y, Tao S, Ye XY, Chen SY, Wang Y, Hernández AS, Wang W, Devasthale PV, Chen S, Lai Z, Zhang H, Wu S, Smirk RA, Bolton SA, Ryono DE, Zhang H, Lim NK, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Kadiyala P, Hosagrahara V, Zhang L, Xu C, Li YX, Muckelbauer JK, Chang C, An Y, Krystek SR, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA. Li J, et al. Among authors: tino ja. J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812. J Med Chem. 2010. PMID: 20218621
Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.
Mukherjee R, Locke KT, Miao B, Meyers D, Monshizadegan H, Zhang R, Search D, Grimm D, Flynn M, O'Malley KM, Zhang L, Li J, Shi Y, Kennedy LJ, Blanar M, Cheng PT, Tino J, Srivastava RA. Mukherjee R, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):716-26. doi: 10.1124/jpet.108.143271. Epub 2008 Sep 17. J Pharmacol Exp Ther. 2008. PMID: 18799592
Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).
Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA. Li J, et al. Among authors: tino ja. J Med Chem. 2007 Nov 29;50(24):5890-3. doi: 10.1021/jm7010595. Epub 2007 Oct 31. J Med Chem. 2007. PMID: 17973363
Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.
Ye XY, Chen S, Zhang H, Locke KT, O'Malley K, Zhang L, Srivastava R, Miao B, Meyers D, Monshizadegan H, Search D, Grimm D, Zhang R, Lippy J, Twamley C, Muckelbauer JK, Chang C, An Y, Hosagrahara V, Zhang L, Yang TJ, Mukherjee R, Cheng PT, Tino JA. Ye XY, et al. Among authors: tino ja. Bioorg Med Chem Lett. 2010 May 1;20(9):2933-7. doi: 10.1016/j.bmcl.2010.03.019. Epub 2010 Mar 7. Bioorg Med Chem Lett. 2010. PMID: 20356736
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist.
Shi Y, Li J, Kennedy LJ, Tao S, Hernández AS, Lai Z, Chen S, Wong H, Zhu J, Trehan A, Lim NK, Zhang H, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Muckelbauer J, Chang C, Krystek SR, Li YX, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA. Shi Y, et al. Among authors: tino ja. ACS Med Chem Lett. 2016 Apr 4;7(6):590-4. doi: 10.1021/acsmedchemlett.6b00033. eCollection 2016 Jun 9. ACS Med Chem Lett. 2016. PMID: 27326332 Free PMC article.
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1H-pyrazol-1-yl)methyl)phosphonate (BMS-820132).
Shi Y, Wang Y, Meng W, Brigance RP, Ryono DE, Bolton S, Zhang H, Chen S, Smirk R, Tao S, Tino JA, Williams KN, Sulsky R, Nielsen L, Ellsworth B, Wong MKY, Sun JH, Leith LW, Sun D, Wu DR, Gupta A, Rampulla R, Mathur A, Chen BC, Wang A, Fuentes-Catanio HG, Kunselman L, Cap M, Zalaznick J, Ma X, Liu H, Taylor JR, Zebo R, Jones B, Kalinowski S, Swartz J, Staal A, O'Malley K, Kopcho L, Muckelbauer JK, Krystek SR Jr, Spronk SA, Marcinkeviciene J, Everlof G, Chen XQ, Xu C, Li YX, Langish RA, Yang Y, Wang Q, Behnia K, Fura A, Janovitz EB, Pannacciulli N, Griffen S, Zinker BA, Krupinski J, Kirby M, Whaley J, Zahler R, Barrish JC, Robl JA, Cheng PTW. Shi Y, et al. Among authors: tino ja. J Med Chem. 2022 Mar 10;65(5):4291-4317. doi: 10.1021/acs.jmedchem.1c02110. Epub 2022 Feb 18. J Med Chem. 2022. PMID: 35179904
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV. Shi Q, et al. Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. doi: 10.1016/j.bmcl.2014.02.075. Epub 2014 Mar 13. Bioorg Med Chem Lett. 2014. PMID: 24685542
Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.
Hernández AS, Cheng PT, Musial CM, Swartz SG, George RJ, Grover G, Slusarchyk D, Seethala RK, Smith M, Dickinson K, Giupponi L, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA. Hernández AS, et al. Among authors: tino ja. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5928-33. doi: 10.1016/j.bmcl.2007.07.099. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17869100
Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.
Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P, Slusarchyk D, Yan M, Humphreys WG, Zhang H, Ewing WR, Robl JA, Gordon D, Tino JA. Li J, et al. Among authors: tino ja. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1825-9. doi: 10.1016/j.bmcl.2008.02.021. Epub 2008 Feb 13. Bioorg Med Chem Lett. 2008. PMID: 18295486
Tetrazole based amides as growth hormone secretagogues.
Li JJ, Wang H, Li J, Qu F, Swartz SG, Hernández AS, Biller SA, Robl JA, Tino JA, Slusarchyk D, Seethala R, Sleph P, Yan M, Grover G, Flynn N, Murphy BJ, Gordon D. Li JJ, et al. Among authors: tino ja. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2536-9. doi: 10.1016/j.bmcl.2008.03.059. Epub 2008 Mar 22. Bioorg Med Chem Lett. 2008. PMID: 18378446
42 results