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Items: 25

1.

Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Zhou G, Coburn CA, Zeng Q, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Ji T, Zan S, Chen L, Mazzola R, Kim JH, Sha D, Selyutin O, Rosenblum SB, Lavey B, Nair AG, Heon Kim S, Keertikar KM, Rokosz L, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4851-4856. doi: 10.1016/j.bmcl.2016.08.002. Epub 2016 Aug 2.

PMID:
27568086
2.

Matched and mixed cap derivatives in the tetracyclic indole class of HCV NS5A inhibitors.

Dwyer MP, Keertikar KM, Chen L, Tong L, Selyutin O, Nair AG, Yu W, Zhou G, Lavey BJ, Yang DY, Wong M, Kim SH, Coburn CA, Rosenblum SB, Zeng Q, Jiang Y, Shankar BB, Rizvi R, Nomeir AA, Liu R, Agrawal S, Xia E, Kong R, Zhai Y, Ingravallo P, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):4106-11. doi: 10.1016/j.bmcl.2016.06.063. Epub 2016 Jun 25.

PMID:
27423481
3.

Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14.

PMID:
27282742
4.

Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.

Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X.

ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13.

5.

Discovery and hit-to-lead optimization of 2,6-diaminopyrimidine inhibitors of interleukin-1 receptor-associated kinase 4.

McElroy WT, Michael Seganish W, Jason Herr R, Harding J, Yang J, Yet L, Komanduri V, Prakash KC, Lavey B, Tulshian D, Greenlee WJ, Sondey C, Fischmann TO, Niu X.

Bioorg Med Chem Lett. 2015 May 1;25(9):1836-41. doi: 10.1016/j.bmcl.2015.03.043. Epub 2015 Mar 28.

PMID:
25870132
6.

The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.

DeMong D, Dai X, Hwa J, Miller M, Lin SI, Kang L, Stamford A, Greenlee W, Yu W, Wong M, Lavey B, Kozlowski J, Zhou G, Yang DY, Patel B, Soriano A, Zhai Y, Sondey C, Zhang H, Lachowicz J, Grotz D, Cox K, Morrison R, Andreani T, Cao Y, Liang M, Meng T, McNamara P, Wong J, Bradley P, Feng KI, Belani J, Chen P, Dai P, Gauuan J, Lin P, Zhao H.

J Med Chem. 2014 Mar 27;57(6):2601-10. doi: 10.1021/jm401858f. Epub 2014 Feb 26.

PMID:
24527772
7.

2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.

Dai C, Li D, Popovici-Muller J, Zhao L, Girijavallabhan VM, Rosner KE, Lavey BJ, Rizvi R, Shankar BB, Wong MK, Guo Z, Orth P, Strickland CO, Sun J, Niu X, Chen S, Kozlowski JA, Lundell DJ, Piwinski JJ, Shih NY, Siddiqui MA.

Bioorg Med Chem Lett. 2011 May 15;21(10):3172-6. doi: 10.1016/j.bmcl.2011.01.002. Epub 2011 Jan 6.

PMID:
21458257
8.

Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.

Girijavallabhan VM, Chen L, Dai C, Feltz RJ, Firmansjah L, Li D, Kim SH, Kozlowski JA, Lavey BJ, Kosinski A, Piwinski JJ, Popovici-Muller J, Rizvi R, Rosner KE, Shankar BB, Shih NY, Siddiqui MA, Tong L, Wong MK, Yang DY, Yang L, Yu W, Zhou G, Guo Z, Orth P, Madison V, Bian H, Lundell D, Niu X, Shah H, Sun J, Umland S.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7283-7. doi: 10.1016/j.bmcl.2010.10.081. Epub 2010 Oct 23.

PMID:
21106451
9.

Biaryl substituted hydantoin compounds as TACE inhibitors.

Yu W, Tong L, Kim SH, Wong MK, Chen L, Yang DY, Shankar BB, Lavey BJ, Zhou G, Kosinski A, Rizvi R, Li D, Feltz RJ, Piwinski JJ, Rosner KE, Shih NY, Siddiqui MA, Guo Z, Orth P, Shah H, Sun J, Umland S, Lundell DJ, Niu X, Kozlowski JA.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5286-9. doi: 10.1016/j.bmcl.2010.06.134. Epub 2010 Jul 1.

PMID:
20663669
10.

Structure and activity relationships of tartrate-based TACE inhibitors.

Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25.

PMID:
20638281
11.

Discovery and SAR of hydantoin TACE inhibitors.

Yu W, Guo Z, Orth P, Madison V, Chen L, Dai C, Feltz RJ, Girijavallabhan VM, Kim SH, Kozlowski JA, Lavey BJ, Li D, Lundell D, Niu X, Piwinski JJ, Popovici-Muller J, Rizvi R, Rosner KE, Shankar BB, Shih NY, Siddiqui MA, Sun J, Tong L, Umland S, Wong MK, Yang DY, Zhou G.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1877-80. doi: 10.1016/j.bmcl.2010.01.148. Epub 2010 Feb 4.

PMID:
20172725
12.

The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.

Rosner KE, Guo Z, Orth P, Shipps GW Jr, Belanger DB, Chan TY, Curran PJ, Dai C, Deng Y, Girijavallabhan VM, Hong L, Lavey BJ, Lee JF, Li D, Liu Z, Popovici-Muller J, Ting PC, Vaccaro H, Wang L, Wang T, Yu W, Zhou G, Niu X, Sun J, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Arshad Siddiqui M, Strickland CO.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5.

PMID:
20022498
13.

Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors.

Gilbert EJ, Zhou G, Wong MK, Tong L, Shankar BB, Huang C, Kelly J, Lavey BJ, McCombie SW, Chen L, Rizvi R, Dong Y, Shu Y, Kozlowski JA, Shih NY, Hipkin RW, Gonsiorek W, Malikzay A, Lunn CA, Favreau L, Lundell DJ.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):608-11. doi: 10.1016/j.bmcl.2009.11.084. Epub 2009 Nov 22.

PMID:
20005710
14.

Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.

Guo Z, Orth P, Wong SC, Lavey BJ, Shih NY, Niu X, Lundell DJ, Madison V, Kozlowski JA.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):54-7. doi: 10.1016/j.bmcl.2008.11.034. Epub 2008 Nov 14.

PMID:
19054672
15.

Labelling and biological evaluation of [(11)C]methoxy-Sch225336: a radioligand for the cannabinoid-type 2 receptor.

Evens N, Bosier B, Lavey BJ, Kozlowski JA, Vermaelen P, Baudemprez L, Busson R, Lambert DM, Van Laere K, Verbruggen AM, Bormans GM.

Nucl Med Biol. 2008 Oct;35(7):793-800. doi: 10.1016/j.nucmedbio.2008.07.004.

PMID:
18848664
16.

Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.

Mazzola RD Jr, Zhu Z, Sinning L, McKittrick B, Lavey B, Spitler J, Kozlowski J, Neng-Yang S, Zhou G, Guo Z, Orth P, Madison V, Sun J, Lundell D, Niu X.

Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. doi: 10.1016/j.bmcl.2008.09.045. Epub 2008 Sep 13.

PMID:
18835710
17.

Cannabinoid CB(2)-selective inverse agonist protects against antigen-induced bone loss.

Lunn CA, Fine J, Rojas-Triana A, Jackson JV, Lavey B, Kozlowski JA, Hipkin RW, Lundell DJ, Bober L.

Immunopharmacol Immunotoxicol. 2007;29(3-4):387-401.

PMID:
18075852
18.

Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists.

Lunn CA, Reich EP, Fine JS, Lavey B, Kozlowski JA, Hipkin RW, Lundell DJ, Bober L.

Br J Pharmacol. 2008 Jan;153(2):226-39. Epub 2007 Oct 1. Review.

19.

Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.

Lavey BJ, Kozlowski JA, Shankar BB, Spitler JM, Zhou G, Yang DY, Shu Y, Wong MK, Wong SC, Shih NY, Wu J, McCombie SW, Rizvi R, Wolin RL, Lunn CA.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3760-4. Epub 2007 Apr 10.

PMID:
17466519
20.

Characterization of peripheral human cannabinoid receptor (hCB2) expression and pharmacology using a novel radioligand, [35S]Sch225336.

Gonsiorek W, Hesk D, Chen SC, Kinsley D, Fine JS, Jackson JV, Bober LA, Deno G, Bian H, Fossetta J, Lunn CA, Kozlowski JA, Lavey B, Piwinski J, Narula SK, Lundell DJ, Hipkin RW.

J Biol Chem. 2006 Sep 22;281(38):28143-51. Epub 2006 Jun 5.

21.

A novel cannabinoid peripheral cannabinoid receptor-selective inverse agonist blocks leukocyte recruitment in vivo.

Lunn CA, Fine JS, Rojas-Triana A, Jackson JV, Fan X, Kung TT, Gonsiorek W, Schwarz MA, Lavey B, Kozlowski JA, Narula SK, Lundell DJ, Hipkin RW, Bober LA.

J Pharmacol Exp Ther. 2006 Feb;316(2):780-8. Epub 2005 Oct 28.

PMID:
16258021
22.

Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.

Shankar BB, Lavey BJ, Zhou G, Spitler JA, Tong L, Rizvi R, Yang DY, Wolin R, Kozlowski JA, Shih NY, Wu J, Hipkin RW, Gonsiorek W, Lunn CA.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4417-20.

PMID:
16115769
23.

Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.

Lavey BJ, Kozlowski JA, Hipkin RW, Gonsiorek W, Lundell DJ, Piwinski JJ, Narula S, Lunn CA.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):783-6.

PMID:
15664857
24.

Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.

Fossetta J, Deno G, Gonsiorek W, Fan X, Lavey B, Das P, Lunn C, Zavodny PJ, Lundell D, Hipkin RW.

Br J Pharmacol. 2004 Jul;142(5):851-60. Epub 2004 Jun 14.

25.

Catalytic Antibody Mediated Hydrolysis of Paraoxon.

Lavey BJ, Janda KD.

J Org Chem. 1996 Oct 18;61(21):7633-7636. No abstract available.

PMID:
11667704

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