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Items: 38

1.

Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112).

McComsey DF, Smith-Swintosky VL, Parker MH, Brenneman DE, Malatynska E, White HS, Klein BD, Wilcox KS, Milewski ME, Herb M, Finley MF, Liu Y, Lubin ML, Qin N, Reitz AB, Maryanoff BE.

J Med Chem. 2013 Nov 27;56(22):9019-30. doi: 10.1021/jm400894u. Epub 2013 Nov 11.

2.

Discovery and SAR of 5-aminooctahydrocyclopentapyrrole-3a-carboxamides as potent CCR2 antagonists.

Cai C, McComsey DF, Hou C, O'Neill JC, Opas E, McKenney S, Johnson D, Sui Z.

Bioorg Med Chem Lett. 2014 Feb 15;24(4):1239-42. doi: 10.1016/j.bmcl.2013.05.024. Epub 2013 Jun 28.

PMID:
23916257
3.

Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket.

Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Gibbs AC, Connelly MA.

Bioorg Med Chem Lett. 2012 Aug 15;22(16):5326-9. doi: 10.1016/j.bmcl.2012.06.008. Epub 2012 Jun 17.

PMID:
22795331
4.

Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.

Maryanoff BE, O'Neill JC, McComsey DF, Yabut SC, Luci DK, Jordan AD Jr, Masucci JA, Jones WJ, Abad MC, Gibbs AC, Petrounia I.

ACS Med Chem Lett. 2011 Apr 18;2(7):538-43. doi: 10.1021/ml200070g. eCollection 2011 Jul 14. Erratum in: ACS Med Chem Lett. 2012 Mar 8;3(3):263.

5.

Novel, broad-spectrum anticonvulsants containing a sulfamide group: advancement of N-((benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into human clinical studies.

Parker MH, Smith-Swintosky VL, McComsey DF, Huang Y, Brenneman D, Klein B, Malatynska E, White HS, Milewski ME, Herb M, Finley MF, Liu Y, Lubin ML, Qin N, Iannucci R, Leclercq L, Cuyckens F, Reitz AB, Maryanoff BE.

J Med Chem. 2009 Dec 10;52(23):7528-36. doi: 10.1021/jm801432r.

PMID:
19388676
6.

Carbonic anhydrase-II inhibition. what are the true enzyme-inhibitory properties of the sulfamide cognate of topiramate?

Maryanoff BE, McComsey DF, Lee J, Smith-Swintosky VL, Wang Y, Minor LK, Todd MJ.

J Med Chem. 2008 Apr 24;51(8):2518-21. doi: 10.1021/jm7015649. Epub 2008 Mar 26.

PMID:
18363349
7.

Suzuki-Miyaura approach to JNJ-26076713, an orally active tetrahydroquinoline-containing alphaVbeta3/alphaVbeta5 integrin antagonist. enantioselective synthesis and stereochemical studies.

Kinney WA, Teleha CA, Thompson AS, Newport M, Hansen R, Ballentine S, Ghosh S, Mahan A, Grasa G, Zanotti-Gerosa A, Dingenen J, Schubert C, Zhou Y, Leo GC, McComsey DF, Santulli RJ, Maryanoff BE.

J Org Chem. 2008 Mar 21;73(6):2302-10. doi: 10.1021/jo702551t. Epub 2008 Feb 16.

PMID:
18278942
8.

7-fluoroindazoles as potent and selective inhibitors of factor Xa.

Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR.

J Med Chem. 2008 Jan 24;51(2):282-97. Epub 2007 Dec 27.

PMID:
18159923
9.

Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.

Xiang MA, Rybczynski PJ, Patel M, Chen RH, McComsey DF, Zhang HC, Gunnet JW, Look R, Wang Y, Minor LK, Zhong HM, Villani FJ, Demarest KT, Damiano BP, Maryanoff BE.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6623-8. Epub 2007 Sep 19.

PMID:
17942308
10.
11.

Exploration of potential prodrugs of RWJ-445167, an oxyguanidine-based dual inhibitor of thrombin and factor Xa.

Maryanoff BE, McComsey DF, Costanzo MJ, Yabut SC, Lu T, Player MR, Giardino EC, Damiano BP.

Chem Biol Drug Des. 2006 Jul;68(1):29-36.

PMID:
16923023
12.

Inhibition of carbonic anhydrase-II by sulfamate and sulfamide groups: an investigation involving direct thermodynamic binding measurements.

Klinger AL, McComsey DF, Smith-Swintosky V, Shank RP, Maryanoff BE.

J Med Chem. 2006 Jun 15;49(12):3496-500.

PMID:
16759092
13.

Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.

Maryanoff BE, McComsey DF, Costanzo MJ, Hochman C, Smith-Swintosky V, Shank RP.

J Med Chem. 2005 Mar 24;48(6):1941-7.

PMID:
15771438
14.

Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Zhang HC, Derian CK, McComsey DF, White KB, Ye H, Hecker LR, Li J, Addo MF, Croll D, Eckardt AJ, Smith CE, Li Q, Cheung WM, Conway BR, Emanuel S, Demarest KT, Andrade-Gordon P, Damiano BP, Maryanoff BE.

J Med Chem. 2005 Mar 24;48(6):1725-8.

PMID:
15771419
15.

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Zhang HC, White KB, Ye H, McComsey DF, Derian CK, Addo MF, Andrade-Gordon P, Eckardt AJ, Conway BR, Westover L, Xu JZ, Look R, Demarest KT, Emanuel S, Maryanoff BE.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3049-53.

PMID:
12941331
16.

High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.

Zhang HC, White KB, McComsey DF, Addo MF, Andrade-Gordon P, Derian CK, Oksenberg D, Maryanoff BE.

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2199-203.

PMID:
12798334
17.

Structural studies on McN-5652-X, a high-affinity ligand for the serotonin transporter in mammalian brain.

Maryanoff BE, McComsey DF, Dukor RK, Nafie LA, Freedman TB, Cao X, Day VW.

Bioorg Med Chem. 2003 May 29;11(11):2463-70.

PMID:
12735993
18.

Thrombin receptor (PAR-1) antagonists. Solid-phase synthesis of indole-based peptide mimetics by anchoring to a secondary amide.

Zhang HC, McComsey DF, White KB, Addo MF, Andrade-Gordon P, Derian CK, Oksenberg D, Maryanoff BE.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2105-9.

PMID:
11514149
19.

Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats.

Andrade-Gordon P, Derian CK, Maryanoff BE, Zhang HC, Addo MF, Cheung Wm, Damiano BP, D'Andrea MR, Darrow AL, de Garavilla L, Eckardt AJ, Giardino EC, Haertlein BJ, McComsey DF.

J Pharmacol Exp Ther. 2001 Jul;298(1):34-42.

PMID:
11408522
20.

Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes.

Maryanoff BE, Santulli RJ, McComsey DF, Hoekstra WJ, Hoey K, Smith CE, Addo M, Darrow AL, Andrade-Gordon P.

Arch Biochem Biophys. 2001 Feb 15;386(2):195-204.

PMID:
11368342
21.

Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.

Zhang HC, Derian CK, Andrade-Gordon P, Hoekstra WJ, McComsey DF, White KB, Poulter BL, Addo MF, Cheung WM, Damiano BP, Oksenberg D, Reynolds EE, Pandey A, Scarborough RM, Maryanoff BE.

J Med Chem. 2001 Mar 29;44(7):1021-4. No abstract available.

PMID:
11297447
23.

Thrombin receptor-activating peptides (TRAPs): investigation of bioactive conformations via structure-activity, spectroscopic, and computational studies.

Ceruso MA, McComsey DF, Leo GC, Andrade-Gordon P, Addo MF, Scarborough RM, Oksenberg D, Maryanoff BE.

Bioorg Med Chem. 1999 Nov;7(11):2353-71.

PMID:
10632045
24.

Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.

Hoekstra WJ, Maryanoff BE, Damiano BP, Andrade-Gordon P, Cohen JH, Costanzo MJ, Haertlein BJ, Hecker LR, Hulshizer BL, Kauffman JA, Keane P, McComsey DF, Mitchell JA, Scott L, Shah RD, Yabut SC.

J Med Chem. 1999 Dec 16;42(25):5254-65.

PMID:
10602710
25.

Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.

Andrade-Gordon P, Maryanoff BE, Derian CK, Zhang HC, Addo MF, Darrow AL, Eckardt AJ, Hoekstra WJ, McComsey DF, Oksenberg D, Reynolds EE, Santulli RJ, Scarborough RM, Smith CE, White KB.

Proc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62.

26.

Potential anxiolytic agents. 3. Novel A-ring modified pyrido[1,2-a]benzimidazoles.

Maryanoff BE, Nortey SO, McNally JJ, Sanfilippo PJ, McComsey DF, Dubinsky B, Shank RP, Reitz AB.

Bioorg Med Chem Lett. 1999 Jun 7;9(11):1547-52.

PMID:
10386933
27.

Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).

McComsey DF, Hawkins MJ, Andrade-Gordon P, Addo MF, Oksenberg D, Maryanoff BE.

Bioorg Med Chem Lett. 1999 May 17;9(10):1423-8.

PMID:
10360749
28.

Macrocyclic hexapeptide analogues of the thrombin receptor (PAR-1) activation motif SFLLRN.

McComsey DF, Hecker LR, Andrade-Gordon P, Addo MF, Maryanoff BE.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):255-60. Erratum in: Bioorg Med Chem Lett 1999 May 17;9(10):1475.

PMID:
10021940
29.

Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.

Hoekstra WJ, Hulshizer BL, McComsey DF, Andrade-Gordon P, Kauffman JA, Addo MF, Oksenberg D, Scarborough RM, Maryanoff BE.

Bioorg Med Chem Lett. 1998 Jul 7;8(13):1649-54.

PMID:
9873407
30.

Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.

Maryanoff BE, McComsey DF, Martin GE, Shank RP.

Bioorg Med Chem Lett. 1998 Apr 21;8(8):983-8.

PMID:
9871525
31.

Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors.

Maryanoff BE, Ho W, McComsey DF, Reitz AB, Grous PP, Nortey SO, Shank RP, Dubinsky B, Taylor RJ Jr, Gardocki JF.

J Med Chem. 1995 Jan 6;38(1):16-20. No abstract available.

PMID:
7837226
32.

Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.

Maryanoff BE, Vaught JL, Shank RP, McComsey DF, Costanzo MJ, Nortey SO.

J Med Chem. 1990 Oct;33(10):2793-7.

PMID:
2213832
33.

McN-5652: a highly potent inhibitor of serotonin uptake.

Shank RP, Vaught JL, Pelley KA, Setler PE, McComsey DF, Maryanoff BE.

J Pharmacol Exp Ther. 1988 Dec;247(3):1032-8.

PMID:
2905001
34.

Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships.

Maryanoff BE, McComsey DF, Gardocki JF, Shank RP, Costanzo MJ, Nortey SO, Schneider CR, Setler PE.

J Med Chem. 1987 Aug;30(8):1433-54. Erratum in: J Med Chem 1988 Jan;31(1):276.

PMID:
3039136
35.

Preclinical evaluation of McN-5707 as a potential antidepressant.

Shank RP, Gardocki JF, Schneider CR, Vaught JL, Setler PE, Maryanoff BE, McComsey DF.

J Pharmacol Exp Ther. 1987 Jul;242(1):74-84.

PMID:
3039115
36.

Pyrroloisoquinoline antidepressants. Potent, enantioselective inhibition of tetrabenazine-induced ptosis and neuronal uptake of norepinephrine, dopamine, and serotonin.

Maryanoff BE, McComsey DF, Castanzo MJ, Setler PE, Gardocki JF, Shank RP, Schneider CR.

J Med Chem. 1984 Aug;27(8):943-6. No abstract available.

PMID:
6747993
37.

Cardiac-slowing amidines containing the 3-thioindone group. Potential antianginal agents.

Zelesko MJ, McComsey DF, Hageman WE, Nortey SO, Baker CA, Maryanoff BE.

J Med Chem. 1983 Feb;26(2):230-7.

PMID:
6687480
38.

Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.

Maryanoff BE, McComsey DF, Taylor RJ Jr, Gardocki JF.

J Med Chem. 1981 Jan;24(1):79-88.

PMID:
6259354

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