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Page 1
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: harrity t. J Med Chem. 2005 Mar 24;48(6):2248-50. doi: 10.1021/jm0496436. J Med Chem. 2005. PMID: 15771468
Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor activator, improves diabetes and other metabolic abnormalities and preserves beta-cell function in db/db mice.
Harrity T, Farrelly D, Tieman A, Chu C, Kunselman L, Gu L, Ponticiello R, Cap M, Qu F, Shao C, Wang W, Zhang H, Fenderson W, Chen S, Devasthale P, Jeon Y, Seethala R, Yang WP, Ren J, Zhou M, Ryono D, Biller S, Mookhtiar KA, Wetterau J, Gregg R, Cheng PT, Hariharan N. Harrity T, et al. Diabetes. 2006 Jan;55(1):240-8. Diabetes. 2006. PMID: 16380499
The dual peroxisome proliferator-activated receptor alpha/gamma activator muraglitazar prevents the natural progression of diabetes in db/db mice.
Tozzo E, Ponticiello R, Swartz J, Farrelly D, Zebo R, Welzel G, Egan D, Kunselman L, Peters A, Gu L, French M, Chen S, Devasthale P, Janovitz E, Staal A, Harrity T, Belder R, Cheng PT, Whaley J, Taylor S, Hariharan N. Tozzo E, et al. Among authors: harrity t. J Pharmacol Exp Ther. 2007 Apr;321(1):107-15. doi: 10.1124/jpet.106.115337. Epub 2007 Jan 26. J Pharmacol Exp Ther. 2007. PMID: 17259449
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: harrity t. 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 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: harrity t. 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
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: harrity t. J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812. J Med Chem. 2010. PMID: 20218621
Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.
Zhang H, Ding CZ, Lai Z, Chen SS, Devasthale P, Herpin T, Morton G, Qu F, Ryono D, Smirk R, Wang W, Wu S, Ye XX, Li YX, Apedo A, Farrelly D, Wang T, Gu L, Morgan N, Flynn N, Chu C, Kunselman L, Lippy J, Locke K, O'Malley K, Harrity T, Cap M, Zhang L, Hosagrahara V, Kadiyala P, Xu C, Doweyko AM, Zahler R, Hariharan N, Cheng PT. Zhang H, et al. Among authors: harrity t. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4. Bioorg Med Chem Lett. 2015. PMID: 25686852
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.
Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG. Wang W, et al. Among authors: harrity t. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6646-51. doi: 10.1016/j.bmcl.2011.09.074. Epub 2011 Sep 24. Bioorg Med Chem Lett. 2011. PMID: 21996520
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG. Devasthale P, et al. Among authors: harrity t. J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9. J Med Chem. 2013. PMID: 23964740
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
Li JJ, Wang H, Tino JA, Robl JA, Herpin TF, Lawrence RM, Biller S, Jamil H, Ponticiello R, Chen L, Chu CH, Flynn N, Cheng D, Zhao R, Chen B, Schnur D, Obermeier MT, Sasseville V, Padmanabha R, Pike K, Harrity T. Li JJ, et al. Among authors: harrity t. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. doi: 10.1016/j.bmcl.2007.03.017. Epub 2007 Mar 12. Bioorg Med Chem Lett. 2007. PMID: 17383874
39 results