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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: cheng pt. 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. Among authors: cheng pt. 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 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: cheng ptw. 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
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R, Cheng L, Sleph P, Sun W, Tieman A, Wetterau JR, Doweyko A, Chandrasena G, Chang SY, Humphreys WG, Sasseville VG, Biller SA, Ryono DE, Selan F, Hariharan N, Cheng PT. Devasthale PV, et al. Among authors: cheng l, cheng pt. J Med Chem. 2005 Mar 24;48(6):2248-50. doi: 10.1021/jm0496436. J Med Chem. 2005. PMID: 15771468
Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Devasthale PV, Chen S, Jeon Y, Qu F, Ryono DE, Wang W, Zhang H, Cheng L, Farrelly D, Golla R, Grover G, Ma Z, Moore L, Seethala R, Sun W, Doweyko AM, Chandrasena G, Sleph P, Hariharan N, Cheng PT. Devasthale PV, et al. Among authors: cheng l, cheng pt. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2312-6. doi: 10.1016/j.bmcl.2007.01.060. Epub 2007 Jan 25. Bioorg Med Chem Lett. 2007. PMID: 17292606
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: cheng pt. J Med Chem. 2007 Nov 29;50(24):5890-3. doi: 10.1021/jm7010595. Epub 2007 Oct 31. J Med Chem. 2007. PMID: 17973363
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Wang W, Devasthale P, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Kunselman L, Morgan N, Ponticiello R, Zebo R, Zhang L, Locke K, Lippy J, O'Malley K, Hosagrahara V, Zhang L, Kadiyala P, Chang C, Muckelbauer J, Doweyko AM, Zahler R, Ryono D, Hariharan N, Cheng PT. Wang W, et al. Among authors: cheng pt. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1939-44. doi: 10.1016/j.bmcl.2008.01.126. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18291645
Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Ye XY, Li YX, Farrelly D, Flynn N, Gu L, Locke KT, Lippy J, O'Malley K, Twamley C, Zhang L, Ryono DE, Zahler R, Hariharan N, Cheng PT. Ye XY, et al. Among authors: cheng pt. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3545-50. doi: 10.1016/j.bmcl.2008.05.014. Epub 2008 May 6. Bioorg Med Chem Lett. 2008. PMID: 18511276
Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.
Zhang H, Ryono DE, Devasthale P, Wang W, O'Malley K, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Locke K, Zhang L, Lippy J, Kunselman L, Morgan N, Flynn N, Moore L, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Doweyko AM, Bell A, Chang C, Muckelbauer J, Zahler R, Hariharan N, Cheng PT. Zhang H, et al. Among authors: cheng pt. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19201606
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: cheng pt. 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
149 results