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Items: 39

1.

Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).

Li J, Kennedy LJ, Walker SJ, Wang H, Li JJ, Hong Z, O'Connor SP, Ye XY, Chen S, Wu S, Yoon DS, Nayeem A, Camac DM, Ramamurthy V, Morin PE, Sheriff S, Wang M, Harper TW, Golla R, Seethala R, Harrity T, Ponticiello RP, Morgan NN, Taylor JR, Zebo R, Maxwell B, Moulin F, Gordon DA, Robl JA.

ACS Med Chem Lett. 2018 Nov 13;9(12):1170-1174. doi: 10.1021/acsmedchemlett.8b00307. eCollection 2018 Dec 13.

2.

PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor.

Hangeland JJ, Abell LM, Adam LP, Jiang J, Friends TJ, Haque LE, Neels J, Onorato JM, Chen AYA, Taylor DS, Yin X, Harrity TW, Basso MD, Yang R, Sleph PG, Gordon DA, Huang CS, Wexler RR, Finlay HJ, Lawrence RM.

ACS Med Chem Lett. 2018 Jun 15;9(7):673-678. doi: 10.1021/acsmedchemlett.8b00138. eCollection 2018 Jul 12.

3.

Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.

Ye XY, Chen SY, Wu S, Yoon DS, Wang H, Hong Z, O'Connor SP, Li J, Li JJ, Kennedy LJ, Walker SJ, Nayeem A, Sheriff S, Camac DM, Ramamurthy V, Morin PE, Zebo R, Taylor JR, Morgan NN, Ponticiello RP, Harrity T, Apedo A, Golla R, Seethala R, Wang M, Harper TW, Sleczka BG, He B, Kirby M, Leahy DK, Li J, Hanson RL, Guo Z, Li YX, DiMarco JD, Scaringe R, Maxwell B, Moulin F, Barrish JC, Gordon DA, Robl JA.

J Med Chem. 2017 Jun 22;60(12):4932-4948. doi: 10.1021/acs.jmedchem.7b00211. Epub 2017 Jun 5.

PMID:
28537398
4.

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.

ACS Med Chem Lett. 2016 Apr 4;7(6):590-4. doi: 10.1021/acsmedchemlett.6b00033. eCollection 2016 Jun 9.

5.

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.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4.

PMID:
25686852
6.

Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).

Li J, Kennedy LJ, Wang H, Li JJ, Walker SJ, Hong Z, O'Connor SP, Nayeem A, Camac DM, Morin PE, Sheriff S, Wang M, Harper T, Golla R, Seethala R, Harrity T, Ponticiello RP, Morgan NN, Taylor JR, Zebo R, Gordon DA, Robl JA.

ACS Med Chem Lett. 2014 May 22;5(7):803-8. doi: 10.1021/ml500144h. eCollection 2014 Jul 10.

7.

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.

J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9.

PMID:
23964740
8.

11β-hydroxysteroid dehydrogenase type 1 gene knockout attenuates atherosclerosis and in vivo foam cell formation in hyperlipidemic apoE⁻/⁻ mice.

García RA, Search DJ, Lupisella JA, Ostrowski J, Guan B, Chen J, Yang WP, Truong A, He A, Zhang R, Yan M, Hellings SE, Gargalovic PS, Ryan CS, Watson LM, Langish RA, Shipkova PA, Carson NL, Taylor JR, Yang R, Psaltis GC, Harrity TW, Robl JA, Gordon DA.

PLoS One. 2013;8(2):e53192. doi: 10.1371/journal.pone.0053192. Epub 2013 Feb 1.

9.

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.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6646-51. doi: 10.1016/j.bmcl.2011.09.074. Epub 2011 Sep 24.

PMID:
21996520
10.

Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1).

Wu SC, Yoon D, Chin J, van Kirk K, Seethala R, Golla R, He B, Harrity T, Kunselman LK, Morgan NN, Ponticiello RP, Taylor JR, Zebo R, Harper TW, Li W, Wang M, Zhang L, Sleczka BG, Nayeem A, Sheriff S, Camac DM, Morin PE, Everlof JG, Li YX, Ferraro CA, Kieltyka K, Shou W, Vath MB, Zvyaga TA, Gordon DA, Robl JA.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6693-8. doi: 10.1016/j.bmcl.2011.09.058. Epub 2011 Sep 21.

PMID:
21983444
11.

Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.

Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a.

PMID:
20684603
12.

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.

Brigance RP, Meng W, Fura A, Harrity T, Wang A, Zahler R, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4395-8. doi: 10.1016/j.bmcl.2010.06.063. Epub 2010 Jun 15.

PMID:
20598534
13.

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.

J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812.

PMID:
20218621
14.

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.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15.

PMID:
19201606
15.

(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.

Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA.

J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15.

PMID:
18412317
16.

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.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1939-44. doi: 10.1016/j.bmcl.2008.01.126. Epub 2008 Feb 7.

PMID:
18291645
17.

The Guinea pig as a preclinical model for demonstrating the efficacy and safety of statins.

Madsen CS, Janovitz E, Zhang R, Nguyen-Tran V, Ryan CS, Yin X, Monshizadegan H, Chang M, D'Arienzo C, Scheer S, Setters R, Search D, Chen X, Zhuang S, Kunselman L, Peters A, Harrity T, Apedo A, Huang C, Cuff CA, Kowala MC, Blanar MA, Sun CQ, Robl JA, Stein PD.

J Pharmacol Exp Ther. 2008 Feb;324(2):576-86. Epub 2007 Nov 6.

PMID:
17986646
18.

Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).

Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R, Harrity T, Stoffel R, Taylor DS, Lavoie TB, Kish K, Jacobson BL, Sheriff S, Adam LP, Ewing WR, Robl JA.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. Epub 2006 Dec 21.

PMID:
17502136
19.

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.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. Epub 2007 Mar 12.

PMID:
17383874
20.

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.

J Pharmacol Exp Ther. 2007 Apr;321(1):107-15. Epub 2007 Jan 26.

PMID:
17259449
21.

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.

Diabetes. 2006 Jan;55(1):240-8.

22.

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.

J Med Chem. 2005 Mar 24;48(6):2248-50.

PMID:
15771468
23.

5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.

Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.

PMID:
15380200
24.

Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.

Magnin DR, Biller SA, Wetterau J, Robl JA, Dickson JK Jr, Taunk P, Harrity TW, Lawrence RM, Sun CQ, Wang T, Logan J, Fryszman O, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1337-40.

PMID:
12657277
25.

The ability of statins to inhibit bone resorption is directly related to their inhibitory effect on HMG-CoA reductase activity.

Staal A, Frith JC, French MH, Swartz J, Güngör T, Harrity TW, Tamasi J, Rogers MJ, Feyen JH.

J Bone Miner Res. 2003 Jan;18(1):88-96.

26.

A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.

Robl JA, Sulsky R, Sun CQ, Simpkins LM, Wang T, Dickson JK Jr, Chen Y, Magnin DR, Taunk P, Slusarchyk WA, Biller SA, Lan SJ, Connolly F, Kunselman LK, Sabrah T, Jamil H, Gordon D, Harrity TW, Wetterau JR.

J Med Chem. 2001 Mar 15;44(6):851-6.

PMID:
11300866
27.

An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.

Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA.

Science. 1998 Oct 23;282(5389):751-4.

28.

An inhibitor of the microsomal triglyceride transfer protein inhibits apoB secretion from HepG2 cells.

Jamil H, Gordon DA, Eustice DC, Brooks CM, Dickson JK Jr, Chen Y, Ricci B, Chu CH, Harrity TW, Ciosek CP Jr, Biller SA, Gregg RE, Wetterau JR.

Proc Natl Acad Sci U S A. 1996 Oct 15;93(21):11991-5.

29.

Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.

Dickson JK Jr, Biller SA, Magnin DR, Petrillo EW Jr, Hillyer JW, Hsieh DC, Lan SJ, Rinehart JK, Gregg RE, Harrity TW, Jolibois KG, Kalinowski SS, Kunselman LK, Mookhtiar KA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):661-4. No abstract available.

PMID:
8576906
30.

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.

Magnin DR, Biller SA, Chen Y, Dickson JK Jr, Fryszman OM, Lawrence RM, Logan JV, Sieber-McMaster ES, Sulsky RB, Traeger SC, Hsieh DC, Lan SJ, Rinehart JK, Harrity TW, Jolibois KG, Kunselman LK, Rich LC, Slusarchyk DA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):657-60. No abstract available.

PMID:
8576905
31.

1,1-Bisphosphonate squalene synthase inhibitors: interplay between the isoprenoid subunit and the diphosphate surrogate.

Magnin DR, Biller SA, Dickson JK Jr, Logan JV, Lawrence RM, Chen Y, Sulsky RB, Ciosek CP Jr, Harrity TW, Jolibois KG, et al.

J Med Chem. 1995 Jul 7;38(14):2596-605.

PMID:
7629799
32.

Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo.

Ciosek CP Jr, Magnin DR, Harrity TW, Logan JV, Dickson JK Jr, Gordon EM, Hamilton KA, Jolibois KG, Kunselman LK, Lawrence RM, et al.

J Biol Chem. 1993 Nov 25;268(33):24832-7.

33.

Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety.

Robl JA, Duncan LA, Pluscec J, Karanewsky DS, Gordon EM, Ciosek CP Jr, Rich LC, Dehmel VC, Slusarchyk DA, Harrity TW, et al.

J Med Chem. 1991 Sep;34(9):2804-15.

PMID:
1895299
34.

Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.

Biller SA, Forster C, Gordon EM, Harrity T, Rich LC, Marretta J, Ciosek CP Jr.

J Med Chem. 1991 Jun;34(6):1912-4. No abstract available.

PMID:
2061928
35.

Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.

Karanewsky DS, Badia MC, Ciosek CP Jr, Robl JA, Sofia MJ, Simpkins LM, DeLange B, Harrity TW, Biller SA, Gordon EM.

J Med Chem. 1990 Nov;33(11):2952-6. No abstract available.

PMID:
2231594
36.

Isoprenoid (phosphinylmethyl)phosphonates as inhibitors of squalene synthetase.

Biller SA, Forster C, Gordon EM, Harrity T, Scott WA, Ciosek CP Jr.

J Med Chem. 1988 Oct;31(10):1869-71. No abstract available.

PMID:
3172121
37.

Cartilage-associated collagenolytic activity in rabbits with antigen-induced chronic synovitis.

Ciosek CP Jr, Harrity TW.

J Lab Clin Med. 1980 Sep;96(3):460-9.

PMID:
6249878
38.

Effects of antiinflammatory agents on the acute response of immune synovitis in rabbits.

Goldlust MB, Rich LC, Harrity TW.

Arthritis Rheum. 1977 May;20(4):937-46.

PMID:
871302
39.

Anti-complement effects of two anti-inflammatory agents. Niflumic and flufenamic acids.

Harrity TW, Goldlust MB.

Biochem Pharmacol. 1974 Nov 15;23(22):3107-20. No abstract available.

PMID:
4216354

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