Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 12

1.

Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt.

Gauld S, Jacquet S, Gauvin D, Wallace C, Wang Y, McCarthy R, Goess C, Leys L, Huang S, Su Z, Edelmayer R, Wetter J, Salte K, McGaraughty S, Argiriadi M, Honore P, Luccarini JM, Bressac D, Desino K, Breinlinger E, Cusack K, Potin D, Kort M, Masson P.

J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046. doi: 10.1124/jpet.119.258046. [Epub ahead of print]

2.

Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.

Amaudrut J, Argiriadi MA, Barth M, Breinlinger EC, Bressac D, Broqua P, Calderwood DJ, Chatar M, Cusack KP, Gauld SB, Jacquet S, Kamath RV, Kort ME, Lepais V, Luccarini JM, Masson P, Montalbetti C, Mounier L, Potin D, Poupardin O, Rouaud S, Spitzer L, Wallace CD.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1799-1806. doi: 10.1016/j.bmcl.2019.05.015. Epub 2019 May 9.

PMID:
31101472
3.

Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit.

George DM, Breinlinger EC, Friedman M, Zhang Y, Wang J, Argiriadi M, Bansal-Pakala P, Barth M, Duignan DB, Honore P, Lang Q, Mittelstadt S, Potin D, Rundell L, Edmunds JJ.

J Med Chem. 2015 Jan 8;58(1):222-36. doi: 10.1021/jm500669m. Epub 2014 Jul 7.

PMID:
25000588
4.

Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.

Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Finlay W, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Arbuckle W, Anderson M, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Jones P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6237-41. doi: 10.1016/j.bmcl.2010.08.101. Epub 2010 Aug 24.

PMID:
20843687
5.

2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.

Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15.

PMID:
20594841
6.

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.

J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u.

PMID:
20405922
7.

An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis.

Suchard SJ, Stetsko DK, Davis PM, Skala S, Potin D, Launay M, Dhar TG, Barrish JC, Susulic V, Shuster DJ, McIntyre KW, McKinnon M, Salter-Cid L.

J Immunol. 2010 Apr 1;184(7):3917-26. doi: 10.4049/jimmunol.0901095. Epub 2010 Feb 26.

8.

Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.

Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Hamilton E, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Scullion P, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Bruin J, Hamilton W, Uitdehaag J, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. doi: 10.1016/j.bmcl.2010.01.100. Epub 2010 Jan 25.

PMID:
20149657
9.

Design of LFA-1 antagonists based on a 2,3-dihydro-1H-pyrrolizin-5(7aH)-one scaffold.

Dodd DS, Sheriff S, Chang CJ, Stetsko DK, Phillips LM, Zhang Y, Launay M, Potin D, Vaccaro W, Poss MA, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1908-11. Epub 2007 Jan 24.

PMID:
17291752
10.

Discovery and development of 5-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl-methyl]-3-thiophenecarboxylic acid (BMS-587101)--a small molecule antagonist of leukocyte function associated antigen-1.

Potin D, Launay M, Monatlik F, Malabre P, Fabreguettes M, Fouquet A, Maillet M, Nicolai E, Dorgeret L, Chevallier F, Besse D, Dufort M, Caussade F, Ahmad SZ, Stetsko DK, Skala S, Davis PM, Balimane P, Patel K, Yang Z, Marathe P, Postelneck J, Townsend RM, Goldfarb V, Sheriff S, Einspahr H, Kish K, Malley MF, DiMarco JD, Gougoutas JZ, Kadiyala P, Cheney DL, Tejwani RW, Murphy DK, Mcintyre KW, Yang X, Chao S, Leith L, Xiao Z, Mathur A, Chen BC, Wu DR, Traeger SC, McKinnon M, Barrish JC, Robl JA, Iwanowicz EJ, Suchard SJ, Dhar TG.

J Med Chem. 2006 Nov 30;49(24):6946-9.

PMID:
17125246
11.

De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.

Potin D, Launay M, Nicolai E, Fabreguette M, Malabre P, Caussade F, Besse D, Skala S, Stetsko DK, Todderud G, Beno BR, Cheney DL, Chang CJ, Sheriff S, Hollenbaugh DL, Barrish JC, Iwanowicz EJ, Suchard SJ, Dhar TG.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1161-4.

PMID:
15686933
12.

Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.

Potin D, Parnet V, Teulon JM, Camborde F, Caussade F, Meignen J, Provost D, Cloarec A.

Bioorg Med Chem Lett. 2000 Apr 17;10(8):805-9.

PMID:
10782691

Supplemental Content

Support Center