Marc D. Chioda
Merck & Co.
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Featured researches published by Marc D. Chioda.
ACS Medicinal Chemistry Letters | 2011
Harry R. Chobanian; Yan Guo; Ping Liu; Marc D. Chioda; Thomas J. Lanza; Linda Chang; Theresa M. Kelly; Yanqing Kan; Oksana C. Palyha; Xiao-Ming Guan; Donald J. Marsh; Joseph M. Metzger; Judith N. Gorski; Kate A. Raustad; Sheng-Ping Wang; Alison M. Strack; Randy R. Miller; Jianmei Pang; Maria Madeira; Kathy Lyons; Jasminka Dragovic; Marc L. Reitman; Ravi P. Nargund; Linus S. Lin
Extensive structure-activity relationship studies of a series derived from atropisomer 1, a previously described chiral benzodiazepine sulfonamide series, led to a potent, brain penetrant and selective compound with excellent preclinical pharmacokinetic across species. We also describe the utilization of a high throughput mouse pharmacodynamic assay which allowed for expedient assessment of pharmacokinetic and brain distribution.
ACS Medicinal Chemistry Letters | 2011
Ping Liu; Thomas J. Lanza; Marc D. Chioda; Carrie K. Jones; Harry R. Chobanian; Yan Guo; Linda Chang; Theresa M. Kelly; Yanqing Kan; Oksana C. Palyha; Xiao-Ming Guan; Donald J. Marsh; Joseph M. Metzger; Katie Ramsay; Sheng-Ping Wang; Alison M. Strack; Randy R. Miller; Jianmei Pang; Kathy Lyons; Jasminka Dragovic; Jian G. Ning; Wes Schafer; Christopher J. Welch; Xiaoyi Gong; Ying-Duo Gao; Viktor Hornak; Richard G. Ball; Nancy N. Tsou; Marc L. Reitman; Matthew J. Wyvratt
We report herein the discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 (BRS-3) agonists and their unusual chirality. Starting from a high-throughput screening lead, we prepared a series of BRS-3 agonists with improved potency and pharmacokinetic properties, of which compound 8a caused mechanism-based, dose-dependent food intake reduction and body weight loss after oral dosing in diet-induced obese mice. This effort also led to the discovery of a novel family of chiral molecules originated from the conformationally constrained seven-membered diazepine ring.
ACS Medicinal Chemistry Letters | 2014
Harry R. Chobanian; Yan Guo; Ping Liu; Marc D. Chioda; Selena Fung; Thomas J. Lanza; Linda Chang; Raman K. Bakshi; James Dellureficio; Qingmei Hong; Mark McLaughlin; Kevin M. Belyk; Shane W. Krska; Amanda K. Makarewicz; Elliot J. Martel; Joseph F. Leone; Lisa Frey; Bindhu V. Karanam; Maria Madeira; Raul F. Alvaro; Joyce Shuman; Gino Salituro; Jenna L. Terebetski; Nina Jochnowitz; Shruti Mistry; Erin McGowan; Richard Hajdu; Mark Rosenbach; Catherine Abbadie; Jessica Alexander
We report herein the identification of MK-4409, a potent and selective fatty acid amide hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal chemistry efforts focused on optimizing of FAAH inhibition in vitro potency, improving the pharmacokinetic (PK) profile, and increasing in vivo efficacy in rodent inflammatory and neuropathic pain assays.
Bioorganic & Medicinal Chemistry | 2012
Harry R. Chobanian; Yan Guo; Ping Liu; Thomas J. Lanza; Marc D. Chioda; Linda Chang; Theresa M. Kelly; Yanqing Kan; Oksana C. Palyha; Xiao-Ming Guan; Donald J. Marsh; Joseph M. Metzger; Katie Raustad; Sheng-Ping Wang; Alison M. Strack; Judith N. Gorski; Randy R. Miller; Jianmei Pang; Kathy Lyons; Jasminka Dragovic; Jian G. Ning; Wes Schafer; Christopher J. Welch; Xiaoyi Gong; Ying-Duo Gao; Viktor Hornak; Marc L. Reitman; Ravi P. Nargund; Linus S. Lin
Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-7725(1) Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.
ACS Medicinal Chemistry Letters | 2013
Ping Liu; Terence G. Hamill; Marc D. Chioda; Harry R. Chobanian; Selena Fung; Yan Guo; Linda Chang; Raman K. Bakshi; Qingmei Hong; James Dellureficio; Linus S. Lin; Catherine Abbadie; Jessica Alexander; Hong Jin; Suzanne M. Mandala; Lin-Lin Shiao; Wenping Li; Sandra Sanabria; David J. Williams; Zhizhen Zeng; Richard Hajdu; Nina Jochnowitz; Mark Rosenbach; Bindhu V. Karanam; Maria Madeira; Gino Salituro; Joyce R. Powell; Ling Xu; Jenna L. Terebetski; Joseph F. Leone
We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [(11)C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.
Archive | 2009
Harry R. Chobanian; Linus S. Lin; Ping Liu; Marc D. Chioda; Robert J. DeVita; Ravi P. Nargund; Yan Guo
Tetrahedron Letters | 2007
Harry R. Chobanian; Ping Liu; Marc D. Chioda; Yan Guo; Linus S. Lin
Archive | 2011
Harry R. Chobanian; Linus S. Lin; Ping Liu; Marc D. Chioda; Robert J. DeVita; Ravi P. Nargund; Yan Guo; Terence G. Hamill; Wenping Li; Darrell A. Henze
Archive | 2007
Robert K. Baker; Linda L. Chang; Marc D. Chioda; Harry R. Chobanian; Ying-Duo Gao; Yan Guo; Linus S. Lin; Ping Liu; Ravi P. Nargund; Kathleen M. Rupprecht; Shouwu Miao
Archive | 2017
Darrell A. Henze; Harry R. Chobanian; Linus S. Lin; Marc D. Chioda; Ping Liu; Ravi P. Nargund; Robert J. DeVita; Terence G. Hamill; Wenping Li; Yan Guo