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Items: 1 to 50 of 71

1.

Preclinical Characterization of NVR 3-778, a First-in-Class Capsid Assembly Modulator against Hepatitis B Virus.

Lam AM, Espiritu C, Vogel R, Ren S, Lau V, Kelly M, Kuduk SD, Hartman GD, Flores OA, Klumpp K.

Antimicrob Agents Chemother. 2018 Dec 21;63(1). pii: e01734-18. doi: 10.1128/AAC.01734-18. Print 2019 Jan.

2.

MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate.

Beshore DC, N Di Marco C, Chang RK, Greshock TJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Fuerst J, Hartman GD, Bilodeau MT, Ray WJ, Kuduk SD.

ACS Med Chem Lett. 2018 Apr 30;9(7):652-656. doi: 10.1021/acsmedchemlett.8b00095. eCollection 2018 Jul 12.

PMID:
30034595
3.

Preclinical to Human Translational Pharmacology of the Novel M1 Positive Allosteric Modulator MK-7622.

Uslaner JM, Kuduk SD, Wittmann M, Lange HS, Fox SV, Min C, Pajkovic N, Harris D, Cilissen C, Mahon C, Mostoller K, Warrington S, Beshore DC.

J Pharmacol Exp Ther. 2018 Jun;365(3):556-566. doi: 10.1124/jpet.117.245894. Epub 2018 Mar 21.

PMID:
29563325
4.

Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.

Skudlarek JW, DiMarco CN, Babaoglu K, Roecker AJ, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Wuelfing WP, Garson SL, Fox SV, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Kuduk SD, Coleman PJ.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1364-1370. doi: 10.1016/j.bmcl.2017.02.012. Epub 2017 Feb 9.

PMID:
28216403
5.

Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.

Stump CA, Cooke AJ, Bruno J, Cabalu TD, Gotter AL, Harell CM, Kuduk SD, McDonald TP, O'Brien J, Renger JJ, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5809-5814. doi: 10.1016/j.bmcl.2016.10.019. Epub 2016 Oct 14.

PMID:
27818110
6.

Pharmacological evaluation of orexin receptor antagonists in preclinical animal models of pain.

McDonald T, Liang HA, Sanoja R, Gotter AL, Kuduk SD, Coleman PJ, Smith KM, Winrow CJ, Renger JJ.

J Neurogenet. 2016 Mar;30(1):32-41. doi: 10.3109/01677063.2016.1171862.

PMID:
27276194
7.

Inhibition of Orexin Signaling Promotes Sleep Yet Preserves Salient Arousability in Monkeys.

Tannenbaum PL, Tye SJ, Stevens J, Gotter AL, Fox SV, Savitz AT, Coleman PJ, Uslaner JM, Kuduk SD, Hargreaves R, Winrow CJ, Renger JJ.

Sleep. 2016 Mar 1;39(3):603-12. doi: 10.5665/sleep.5536.

8.

The M1 Muscarinic Positive Allosteric Modulator PQCA Improves Performance on Translatable Tests of Memory and Attention in Rhesus Monkeys.

Lange HS, Cannon CE, Drott JT, Kuduk SD, Uslaner JM.

J Pharmacol Exp Ther. 2015 Dec;355(3):442-50. doi: 10.1124/jpet.115.226712. Epub 2015 Oct 7.

PMID:
26446308
9.

Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties.

Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Garson SL, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2488-92. doi: 10.1016/j.bmcl.2015.04.066. Epub 2015 Apr 29.

PMID:
25981685
10.

The selective positive allosteric M1 muscarinic receptor modulator PQCA attenuates learning and memory deficits in the Tg2576 Alzheimer's disease mouse model.

Puri V, Wang X, Vardigan JD, Kuduk SD, Uslaner JM.

Behav Brain Res. 2015;287:96-9. doi: 10.1016/j.bbr.2015.03.029. Epub 2015 Mar 20.

PMID:
25800972
11.

Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.

Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4992-4999. doi: 10.1016/j.bmcl.2014.12.081. Epub 2015 Jan 6.

PMID:
25613676
12.

Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.

Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23.

PMID:
25577040
13.

Improved cognition without adverse effects: novel M1 muscarinic potentiator compares favorably to donepezil and xanomeline in rhesus monkey.

Vardigan JD, Cannon CE, Puri V, Dancho M, Koser A, Wittmann M, Kuduk SD, Renger JJ, Uslaner JM.

Psychopharmacology (Berl). 2015 Jun;232(11):1859-66. doi: 10.1007/s00213-014-3813-x. Epub 2014 Dec 10.

PMID:
25491927
14.

Differential sleep-promoting effects of dual orexin receptor antagonists and GABAA receptor modulators.

Gotter AL, Garson SL, Stevens J, Munden RL, Fox SV, Tannenbaum PL, Yao L, Kuduk SD, McDonald T, Uslaner JM, Tye SJ, Coleman PJ, Winrow CJ, Renger JJ.

BMC Neurosci. 2014 Sep 22;15:109. doi: 10.1186/1471-2202-15-109.

15.

SAR studies on carboxylic acid series M(1) selective positive allosteric modulators (PAMs).

Kuduk SD, Beshore DC.

Curr Top Med Chem. 2014;14(15):1738-54. Review.

PMID:
25176125
16.

Orexin receptor antagonist-induced sleep does not impair the ability to wake in response to emotionally salient acoustic stimuli in dogs.

Tannenbaum PL, Stevens J, Binns J, Savitz AT, Garson SL, Fox SV, Coleman P, Kuduk SD, Gotter AL, Marino M, Tye SJ, Uslaner JM, Winrow CJ, Renger JJ.

Front Behav Neurosci. 2014 May 16;8:182. doi: 10.3389/fnbeh.2014.00182. eCollection 2014.

17.

Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.

Yang ZQ, Shu Y, Ma L, Wittmann M, Ray WJ, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT, Kuduk SD.

ACS Med Chem Lett. 2014 Feb 20;5(5):604-8. doi: 10.1021/ml500055h. eCollection 2014 May 8.

18.

Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.

Kuduk SD, Skudlarek JW, Di Marco CN, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1784-9. doi: 10.1016/j.bmcl.2014.02.026. Epub 2014 Feb 19.

PMID:
24630562
19.

Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.

Kuduk SD, Di Marco CN, Saffold JR, Ray WJ, Ma L, Wittmann M, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT, Beshore DC.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1417-20. doi: 10.1016/j.bmcl.2014.01.012. Epub 2014 Jan 13.

PMID:
24485781
20.

Dual orexin receptor antagonists show distinct effects on locomotor performance, ethanol interaction and sleep architecture relative to gamma-aminobutyric acid-A receptor modulators.

Ramirez AD, Gotter AL, Fox SV, Tannenbaum PL, Yao L, Tye SJ, McDonald T, Brunner J, Garson SL, Reiss DR, Kuduk SD, Coleman PJ, Uslaner JM, Hodgson R, Browne SE, Renger JJ, Winrow CJ.

Front Neurosci. 2013 Dec 24;7:254. doi: 10.3389/fnins.2013.00254. eCollection 2013.

21.

The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold.

Gotter AL, Winrow CJ, Brunner J, Garson SL, Fox SV, Binns J, Harrell CM, Cui D, Yee KL, Stiteler M, Stevens J, Savitz A, Tannenbaum PL, Tye SJ, McDonald T, Yao L, Kuduk SD, Uslaner J, Coleman PJ, Renger JJ.

BMC Neurosci. 2013 Aug 28;14:90. doi: 10.1186/1471-2202-14-90.

22.

Quantitative electroencephalography within sleep/wake states differentiates GABAA modulators eszopiclone and zolpidem from dual orexin receptor antagonists in rats.

Fox SV, Gotter AL, Tye SJ, Garson SL, Savitz AT, Uslaner JM, Brunner JI, Tannenbaum PL, McDonald TP, Hodgson R, Yao L, Bowlby MR, Kuduk SD, Coleman PJ, Hargreaves R, Winrow CJ, Renger JJ.

Neuropsychopharmacology. 2013 Nov;38(12):2401-8. doi: 10.1038/npp.2013.139. Epub 2013 May 31.

23.

Orexin receptor antagonists differ from standard sleep drugs by promoting sleep at doses that do not disrupt cognition.

Uslaner JM, Tye SJ, Eddins DM, Wang X, Fox SV, Savitz AT, Binns J, Cannon CE, Garson SL, Yao L, Hodgson R, Stevens J, Bowlby MR, Tannenbaum PL, Brunner J, Mcdonald TP, Gotter AL, Kuduk SD, Coleman PJ, Winrow CJ, Renger JJ.

Sci Transl Med. 2013 Apr 3;5(179):179ra44. doi: 10.1126/scitranslmed.3005213.

24.

Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.

Kuduk SD, Chang RK, Greshock TJ, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

ACS Med Chem Lett. 2012 Oct 13;3(12):1070-4. doi: 10.1021/ml300280g. eCollection 2012 Dec 13.

25.

Novel M(1) allosteric ligands: a patent review.

Kuduk SD, Beshore DC.

Expert Opin Ther Pat. 2012 Dec;22(12):1385-98. doi: 10.1517/13543776.2012.731395. Epub 2012 Oct 23. Review.

PMID:
23092292
26.

The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque.

Uslaner JM, Eddins D, Puri V, Cannon CE, Sutcliffe J, Chew CS, Pearson M, Vivian JA, Chang RK, Ray WJ, Kuduk SD, Wittmann M.

Psychopharmacology (Berl). 2013 Jan;225(1):21-30. doi: 10.1007/s00213-012-2788-8. Epub 2012 Jul 24.

PMID:
22825578
27.

Drug Design Strategies for GPCR Allosteric Modulators.

Conn PJ, Kuduk SD, Doller D.

Annu Rep Med Chem. 2012;47:441-457. No abstract available.

28.

Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.

Kuduk SD, Chang RK, Di Marco CN, Pitts DR, Greshock TJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT, Ray WJ.

J Med Chem. 2011 Jul 14;54(13):4773-80. doi: 10.1021/jm200400m. Epub 2011 Jun 17.

PMID:
21682298
29.

Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).

Kuduk SD, Chang RK, Di Marco CN, Dipardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4255-8. doi: 10.1016/j.bmcl.2011.05.064. Epub 2011 May 27.

PMID:
21669528
30.

Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.

Kuduk SD, Chang RK, Di Marco CN, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1710-5. doi: 10.1016/j.bmcl.2011.01.094. Epub 2011 Jan 28.

PMID:
21324684
31.

Fused heterocyclic M1 positive allosteric modulators.

Kuduk SD, Di Marco CN, Cofre V, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2011 May 1;21(9):2769-72. doi: 10.1016/j.bmcl.2010.10.028. Epub 2010 Oct 16.

PMID:
21055928
32.

Indazole derivatives as novel bradykinin B1 receptor antagonists.

Bodmer-Narkevitch V, Anthony NJ, Cofre V, Jolly SM, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7011-4. doi: 10.1016/j.bmcl.2010.09.121. Epub 2010 Sep 29.

PMID:
20971001
33.

Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators.

Kuduk SD, Chang RK, Di Marco CN, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

ACS Med Chem Lett. 2010 Jun 4;1(6):263-7. doi: 10.1021/ml100095k. eCollection 2010 Sep 9.

34.

Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.

Kuduk SD, DiPardo RM, Beshore DC, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2538-41. doi: 10.1016/j.bmcl.2010.02.095. Epub 2010 Mar 10.

PMID:
20346667
35.

Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.

Kuduk SD, Di Marco CN, Chang RK, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2533-7. doi: 10.1016/j.bmcl.2010.02.096. Epub 2010 Mar 3.

PMID:
20303264
36.

N-heterocyclic derived M1 positive allosteric modulators.

Kuduk SD, Di Marco CN, Cofre V, Pitts DR, Ray WJ, Ma L, Wittmann M, Veng L, Seager MA, Koeplinger K, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1334-7. doi: 10.1016/j.bmcl.2010.01.013. Epub 2010 Jan 11.

PMID:
20097564
37.

Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567.

Kuduk SD, Di Marco CN, Bodmer-Narkevitch V, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Sain N, Liang A, Spencer RH, Kane SA, Hartman GD, Bilodeau MT.

ACS Chem Neurosci. 2010 Jan 20;1(1):19-24. doi: 10.1021/cn9000186. Epub 2009 Oct 6.

38.

Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.

Kuduk SD, Di Marco CN, Cofre V, Pitts DR, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger K, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):657-61. doi: 10.1016/j.bmcl.2009.11.059. Epub 2009 Dec 2. Erratum in: Bioorg Med Chem Lett. 2010 Mar 1;20(5):1796. Seager, Matthew [corrected to Seager, Matthew A].

PMID:
19962304
39.

Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3).

Kuduk SD, Chang RK, Wai JM, Di Marco CN, Cofre V, DiPardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4059-63. doi: 10.1016/j.bmcl.2009.06.021. Epub 2009 Jun 13.

PMID:
19553111
40.

Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).

Kuduk SD, Di Marco CN, Chang RK, Dipardo RM, Cook SP, Cato MJ, Jovanovska A, Urban MO, Leitl M, Spencer RH, Kane SA, Bilodeau MT, Hartman GD, Bock MG.

Bioorg Med Chem Lett. 2009 May 1;19(9):2514-8. doi: 10.1016/j.bmcl.2009.03.029. Epub 2009 Mar 14.

PMID:
19339181
41.
42.

Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.

Kuduk SD, Chang RK, Dipardo RM, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5107-10. doi: 10.1016/j.bmcl.2008.07.126. Epub 2008 Aug 5.

PMID:
18722115
43.

CYP2C75-involved autoinduction of metabolism in rhesus monkeys of methyl 3-chloro-3'-fluoro-4'-{(1R)-1-[({1-[(trifluoroacetyl)amino]cyclopropyl}carbonyl)amino]ethyl}-1,1'-biphenyl-2-carboxylate (MK-0686), a bradykinin B1 receptor antagonist.

Tang C, Carr BA, Poignant F, Ma B, Polsky-Fisher SL, Kuo Y, Strong-Basalyga K, Norcross A, Richards K, Eisenhandler R, Carlini EJ, Di Marco CN, Kuduk SD, Yu NX, Raab CE, Rushmore T, Frederick CB, Bock MG, Prueksaritanont T.

J Pharmacol Exp Ther. 2008 Jun;325(3):935-46. doi: 10.1124/jpet.107.136044. Epub 2008 Feb 29.

PMID:
18310472
44.

A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.

Feng DM, DiPardo RM, Wai JM, Chang RK, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG, Kuduk SD.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):682-7.

PMID:
18240388
45.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Wood MR, Schirripa KM, Kim JJ, Kuduk SD, Chang RK, Di Marco CN, DiPardo RM, Wan BL, Murphy KL, Ransom RW, Chang RS, Holahan MA, Cook JJ, Lemaire W, Mosser SD, Bednar RA, Tang C, Prueksaritanont T, Wallace AA, Mei Q, Yu J, Bohn DL, Clayton FC, Adarayn ED, Sitko GR, Leonard YM, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):716-20. Epub 2007 Nov 19.

PMID:
18061443
46.

Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.

Kuduk SD, DiPardo RM, Chang RK, Di Marco CN, Murphy KL, Ransom RW, Reiss DR, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3608-12. Epub 2007 Apr 24.

PMID:
17482459
47.

Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.

Kuduk SD, Di Marco CN, Chang RK, Wood MR, Schirripa KM, Kim JJ, Wai JM, DiPardo RM, Murphy KL, Ransom RW, Harrell CM, Reiss DR, Holahan MA, Cook J, Hess JF, Sain N, Urban MO, Tang C, Prueksaritanont T, Pettibone DJ, Bock MG.

J Med Chem. 2007 Jan 25;50(2):272-82.

PMID:
17228869
48.

Diclofenac hydroxylation in monkeys: efficiency, regioselectivity, and response to inhibitors.

Tang C, Fang Y, Booth-Genthe C, Kuo Y, Kuduk SD, Rushmore TH, Carr BA.

Biochem Pharmacol. 2007 Mar 15;73(6):880-90. Epub 2006 Nov 25.

PMID:
17223083
49.

5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.

Kuduk SD, Di Marco CN, Chang RK, Wood MR, Kim JJ, Schirripa KM, Murphy KL, Ransom RW, Tang C, Torrent M, Ha S, Prueksaritanont T, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2006 May 15;16(10):2791-5. Epub 2006 Mar 10.

PMID:
16529929
50.

Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

Kuduk SD, Chang RK, Ng C, Murphy KL, Ransom RW, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3925-9.

PMID:
15993596

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