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Items: 27

1.

Pharmacologic characterization of JNJ-42226314, [1-(4-fluorophenyl)indol-5-yl]-[3-[4-(thiazole-2-carbonyl)piperazin-1-yl]azetidin-1-yl]methanone, a reversible, selective and potent monoacylglycerol lipase inhibitor.

Wyatt RM, Fraser I, Welty N, Lord B, Wennerholm M, Sutton SW, Ameriks MK, Dugovic C, Yun S, White A, Nguyen L, Koudriakova T, Tian G, Suarez J, Szewczuk L, Bonnette W, Ahn K, Ghosh B, Flores CM, Connolly PJ, Zhu B, Macielag MJ, Brandt MR, Chevalier K, Zhang SP, Lovenberg TW, Bonaventure P.

J Pharmacol Exp Ther. 2019 Dec 9. pii: jpet.119.262139. doi: 10.1124/jpet.119.262139. [Epub ahead of print]

2.

Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators.

Savall BM, Wu D, Swanson DM, Seierstad M, Wu N, Vives Martinez J, García Olmos B, Lord B, Coe K, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK.

ACS Med Chem Lett. 2018 Dec 26;10(3):267-272. doi: 10.1021/acsmedchemlett.8b00599. eCollection 2019 Mar 14.

PMID:
30891124
3.

1H-Pyrrolo[3,2-b]pyridine GluN2B-Selective Negative Allosteric Modulators.

Chrovian CC, Soyode-Johnson A, Wall JL, Rech JC, Schoellerman J, Lord B, Coe KJ, Carruthers NI, Nguyen L, Jiang X, Koudriakova T, Balana B, Letavic MA.

ACS Med Chem Lett. 2019 Jan 10;10(3):261-266. doi: 10.1021/acsmedchemlett.8b00542. eCollection 2019 Mar 14.

PMID:
30891123
4.

Lead Optimization of 5-Aryl Benzimidazolone- and Oxindole-Based AMPA Receptor Modulators Selective for TARP γ-8.

Ravula S, Savall BM, Wu N, Lord B, Coe K, Wang K, Seierstad M, Swanson DM, Ziff J, Nguyen M, Leung P, Rynberg R, La D, Pippel DJ, Koudriakova T, Lovenberg TW, Carruthers NI, Maher MP, Ameriks MK.

ACS Med Chem Lett. 2018 Jul 13;9(8):821-826. doi: 10.1021/acsmedchemlett.8b00215. eCollection 2018 Aug 9.

5.

Erratum to "Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes" Bioorg. Med. Chem. Lett. 28 (2018) [841-846].

Winters MP, Sui Z, Wall M, Wang Y, Gunnet J, Leonard J, Hua H, Yan W, Suckow A, Bell A, Clapper W, Jenkinson C, Haug P, Koudriakova T, Huebert N, Murray WV.

Bioorg Med Chem Lett. 2018 May 15;28(9):1676-1678. doi: 10.1016/j.bmcl.2018.03.053. Epub 2018 Mar 28. No abstract available.

PMID:
29605534
6.

Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes.

Winters MP, Sui Z, Wall M, Wang Y, Gunnet J, Leonard J, Hua H, Yan W, Suckow A, Bell A, Clapper W, Jenkinson C, Haug P, Koudriakova T, Huebert N, Murray WV.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):841-846. doi: 10.1016/j.bmcl.2018.02.013. Epub 2018 Feb 8. Erratum in: Bioorg Med Chem Lett. 2018 Mar 28;:.

PMID:
29456108
7.

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA.

J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20.

PMID:
29211470
8.

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.

J Med Chem. 2017 Jun 8;60(11):4559-4572. doi: 10.1021/acs.jmedchem.7b00408. Epub 2017 May 25.

PMID:
28493698
9.

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA.

J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8.

PMID:
27548392
10.

Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists.

Ziff J, Rudolph DA, Stenne B, Koudriakova T, Lord B, Bonaventure P, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA, Shireman BT.

ACS Chem Neurosci. 2016 Apr 20;7(4):498-504. doi: 10.1021/acschemneuro.5b00304. Epub 2016 Jan 19.

PMID:
26754558
11.

Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia.

Bonaventure P, Shelton J, Yun S, Nepomuceno D, Sutton S, Aluisio L, Fraser I, Lord B, Shoblock J, Welty N, Chaplan SR, Aguilar Z, Halter R, Ndifor A, Koudriakova T, Rizzolio M, Letavic M, Carruthers NI, Lovenberg T, Dugovic C.

J Pharmacol Exp Ther. 2015 Sep;354(3):471-82. doi: 10.1124/jpet.115.225466. Epub 2015 Jul 15.

PMID:
26177655
12.

Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.

Letavic MA, Bonaventure P, Carruthers NI, Dugovic C, Koudriakova T, Lord B, Lovenberg TW, Ly KS, Mani NS, Nepomuceno D, Pippel DJ, Rizzolio M, Shelton JE, Shah CR, Shireman BT, Young LK, Yun S.

J Med Chem. 2015 Jul 23;58(14):5620-36. doi: 10.1021/acs.jmedchem.5b00742. Epub 2015 Jul 8.

PMID:
26087021
13.

Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model.

Yamazaki S, Skaptason J, Romero D, Vekich S, Jones HM, Tan W, Wilner KD, Koudriakova T.

Drug Metab Dispos. 2011 Mar;39(3):383-93. doi: 10.1124/dmd.110.035857. Epub 2010 Nov 23.

PMID:
21098644
14.

Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16.

PMID:
20561786
15.

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy.

Zhang C, Lundgren K, Yan Z, Arango ME, Price S, Huber A, Higgins J, Troche G, Skaptason J, Koudriakova T, Nonomiya J, Yang M, O'Connor P, Bender S, Los G, Lewis C, Jessen B.

Mol Cancer Ther. 2008 Apr;7(4):818-28. doi: 10.1158/1535-7163.MCT-07-0440.

16.

Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse models.

Yamazaki S, Skaptason J, Romero D, Lee JH, Zou HY, Christensen JG, Koup JR, Smith BJ, Koudriakova T.

Drug Metab Dispos. 2008 Jul;36(7):1267-74. doi: 10.1124/dmd.107.019711. Epub 2008 Apr 1.

PMID:
18381487
17.

An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms.

Zou HY, Li Q, Lee JH, Arango ME, McDonnell SR, Yamazaki S, Koudriakova TB, Alton G, Cui JJ, Kung PP, Nambu MD, Los G, Bender SL, Mroczkowski B, Christensen JG.

Cancer Res. 2007 May 1;67(9):4408-17.

18.

Ocular disposition, pharmacokinetics, efficacy and safety of nanoparticle-formulated ophthalmic drugs.

Bu HZ, Gukasyan HJ, Goulet L, Lou XJ, Xiang C, Koudriakova T.

Curr Drug Metab. 2007 Feb;8(2):91-107. Review.

PMID:
17305490
19.

Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors.

Jessen BA, Lee L, Koudriakova T, Haines M, Lundgren K, Price S, Nonomiya J, Lewis C, Stevens GJ.

J Appl Toxicol. 2007 Mar-Apr;27(2):133-42.

PMID:
17211896
20.

Quantitation and mapping of aflatoxin B1-induced DNA damage in genomic DNA using aflatoxin B1-8,9-epoxide and microsomal activation systems.

Denissenko MF, Cahill J, Koudriakova TB, Gerber N, Pfeifer GP.

Mutat Res. 1999 Apr 6;425(2):205-11.

PMID:
10216213
21.

The p53 codon 249 mutational hotspot in hepatocellular carcinoma is not related to selective formation or persistence of aflatoxin B1 adducts.

Denissenko MF, Koudriakova TB, Smith L, O'Connor TR, Riggs AD, Pfeifer GP.

Oncogene. 1998 Dec 10;17(23):3007-14.

22.
23.

Isolation and identification of major urinary metabolites of rifabutin in rats and humans.

Utkin I, Koudriakova T, Thompson T, Cottrell C, Iatsimirskaia E, Barry J, Vouros P, Gerber N.

Drug Metab Dispos. 1997 Aug;25(8):963-9.

PMID:
9280404
24.

Metabolism of rifabutin in human enterocyte and liver microsomes: kinetic parameters, identification of enzyme systems, and drug interactions with macrolides and antifungal agents.

Iatsimirskaia E, Tulebaev S, Storozhuk E, Utkin I, Smith D, Gerber N, Koudriakova T.

Clin Pharmacol Ther. 1997 May;61(5):554-62.

PMID:
9164417
25.

In vivo disposition and metabolism by liver and enterocyte microsomes of the antitubercular drug rifabutin in rats.

Koudriakova T, Iatsimirskaia E, Tulebaev S, Spetie D, Utkin I, Mullet D, Thompson T, Vouros P, Gerber N.

J Pharmacol Exp Ther. 1996 Dec;279(3):1300-9.

PMID:
8968354
26.

In vitro and in vivo evaluation of 6-azido-2',3'-dideoxy-2'-fluoro-beta-D-arabinofuranosylpurine and N6-methyl-2',3'-dideoxy-2'-fluoro-beta-D-arabinofuranosyladenine as prodrugs of the anti-HIV nucleosides 2'-F-ara-ddA and 2'-F-ara-ddI.

Koudriakova T, Manouilov KK, Shanmuganathan K, Kotra LP, Boudinot FD, Cretton-Scott E, Sommadossi JP, Schinazi RF, Chu CK.

J Med Chem. 1996 Nov 8;39(23):4676-81.

PMID:
8917656
27.

Enhanced brain delivery of an anti-HIV nucleoside 2'-F-ara-ddI by xanthine oxidase mediated biotransformation.

Shanmuganathan K, Koudriakova T, Nampalli S, Du J, Gallo JM, Schinazi RF, Chu CK.

J Med Chem. 1994 Mar 18;37(6):821-7.

PMID:
8145233

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