Publications by authors named "Mark G Bock"

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Profile of NT-0527, a brain penetrant NLRP3 Inflammasome inhibitor suitable as an tool compound for neuroinflammatory disorders.
David Harrison, Andy Billinton, Mark G Bock, Nicholas P Clarke, Zsofia Digby

RSC Med Chem· September 2025

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The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1.
John R Doedens, Christine Diamond, David Harrison, Mark G Bock, Nicholas Clarke

Biochem Pharmacol· September 2024

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Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency.
Pamela Smolak, MyTrang Nguyen, Christine Diamond, Heather Wescott, John R Doedens, Mark G Bock

J Pharmacol Exp Ther· February 2024

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Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders.
David Harrison, Andy Billinton, Mark G Bock, John R Doedens, Christopher A Gabel

J Med Chem· November 2023

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Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.
David Harrison, Mark G Bock, John R Doedens, Christopher A Gabel, M Katharine Holloway

ACS Med Chem Lett· August 2022

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Discovery of Potent, Selective, and State-Dependent Na1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides.
Vidya Ramdas, Rashmi Talwar, Vijay Kanoje, Rajesh M Loriya, Moloy Banerjee, Mark G Bock

J Med Chem· June 2020

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The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders.
Thomas Troxler, Dominik Feuerbach, Xuechun Zhang, Charles R Yang, Bharat Lagu, Mark G Bock

ChemMedChem· July 2019

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From ergolines to indoles: improved inhibitors of the human H3 receptor for the treatment of narcolepsy.
Yves P Auberson, Thomas Troxler, Xuechun Zhang, Charles R Yang, Dominik Feuerbach, Mark G Bock

ChemMedChem· February 2015

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3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.
Thomas Ullrich, Sanjita Sasmal, Venkatesham Boorgu, Srinivasu Pasagadi, Srisailam Cheera, Mark G Bock

J Med Chem· September 2014

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Ergoline-derived inverse agonists of the human h3 receptor for the treatment of narcolepsy.
Yves P Auberson, Thomas Troxler, Xuechun Zhang, Charles R Yang, Markus Fendt, Mark G Bock

ChemMedChem· August 2014

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Indazole derivatives as novel bradykinin B1 receptor antagonists.
Vera Bodmer-Narkevitch, Neville J Anthony, Victoria Cofre, Samson M Jolly, Kathy L Murphy, Mark G Bock

Bioorg Med Chem Lett· December 2010

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Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.
Kelly-Ann S Schlegel, Zhi-Qiang Yang, Thomas S Reger, Youheng Shu, Rowena Cube, Mark G Bock

Bioorg Med Chem Lett· September 2010

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Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.
James C Barrow, Kenneth E Rittle, Thomas S Reger, Zhi-Qiang Yang, Phung Bondiskey, Mark G Bock

ACS Med Chem Lett· May 2010

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Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Scott D Kuduk, Christina N Di Marco, Ronald K Chang, Robert M Dipardo, Sean P Cook, Mark G Bock

Bioorg Med Chem Lett· May 2009

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Bradykinin B1 receptor antagonists as novel analgesics: a retrospective of selected medicinal chemistry developments.
Scott D Kuduk, Mark G Bock

Curr Top Med Chem· December 2008

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Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Zhi-Qiang Yang, James C Barrow, William D Shipe, Kelly-Ann S Schlegel, Youheng Shu, Mark G Bock

J Med Chem· October 2008

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Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.
Scott D Kuduk, Ronald K Chang, Robert M Dipardo, Christina N Di Marco, Kathy L Murphy, Mark G Bock

Bioorg Med Chem Lett· September 2008

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Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
William D Shipe, James C Barrow, Zhi-Qiang Yang, Craig W Lindsley, F Vivien Yang, Mark G Bock

J Med Chem· July 2008

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2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.
Dai-Shi Su, John L Lim, Elizabeth Tinney, Bang-Lin Wan, Kathy L Murphy, Mark G Bock

J Med Chem· July 2008

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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.
Cuyue Tang, Brian A Carr, Frédéric Poignant, Bennett Ma, Stacey L Polsky-Fisher, Mark G Bock

J Pharmacol Exp Ther· June 2008

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Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.
Michael R Wood, Kathy M Schirripa, June J Kim, Scott D Kuduk, Ronald K Chang, Mark G Bock

Bioorg Med Chem Lett· January 2008

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A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.
Dong-Mei Feng, Robert M DiPardo, Jenny M Wai, Ronald K Chang, Christina N Di Marco, Mark G Bock

Bioorg Med Chem Lett· January 2008

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Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.
Scott D Kuduk, Robert M DiPardo, Ronald K Chang, Christina N Di Marco, Kathy L Murphy, Mark G Bock

Bioorg Med Chem Lett· July 2007

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Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.
Dai-Shi Su, John L Lim, M Kristine Markowitz, Bang-Lin Wan, Kathy L Murphy, Mark G Bock

Bioorg Med Chem Lett· June 2007

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Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists.
Scott D Kuduk, Christina N Di Marco, Ronald K Chang, Michael R Wood, Kathy M Schirripa, Mark G Bock

J Med Chem· January 2007

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