Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Larry J. Jolivette"'
Autor:
Joseph E. Pero, Dennis A. Holt, Carl Brooks, Matthews Jay M, Melissa H. Costell, Raynold Shenje, John J. McAtee, David J. Behm, Ralph A. Rivero, Larry J. Jolivette, Sanchez Robert, Brent W. Mccleland, Lamont Roscoe Terrell, Jaclyn R. Patterson, Edward J. Brnardic, Theresa J. Roethke, Brian G. Lawhorn, Linda S. Barton
Publikováno v:
Journal of Medicinal Chemistry. 62:9270-9280
GSK3527497, a preclinical candidate for the inhibition of TRPV4, was identified starting from the previously reported pyrrolidine sulfonamide TRPV4 inhibitors 1 and 2. Optimization of projected human dose was accomplished by specifically focusing on
Autor:
Guosen Ye, Arthur Shu, Dennis A. Holt, Patrick Stoy, Carla A. Donatelli, Larry J. Jolivette, Ralph A. Rivero, Mark Youngman, Lamont Roscoe Terrell, Jaclyn R. Patterson, Brian G. Lawhorn, Theresa J. Roethke
Publikováno v:
Journal of medicinal chemistry. 63(23)
Investigation of TRPV4 as a potential target for the treatment of pulmonary edema associated with heart failure generated a novel series of acyclic amine inhibitors displaying exceptional potency and PK properties. The series arose through a scaffold
Autor:
Melissa H Costell, Nicolas eAncellin, Roberta E Bernard, Shufang eZhao, John J Upson, Lisa A Morgan, Kristeen eHauk, Alan R Olzinski, Victoria L T Ballard, Kenny eHerry, Pascal eGrondin, Nerina eDodic, Olivier eMirguet, Anne eBouillot, Francoise eGellibert, Robert W Coatney, John J Lepore, Beat M. Jucker, Larry J Jolivette, Robert N Willette, Christine G Schnackenberg, David J Behm
Publikováno v:
Frontiers in Pharmacology, Vol 3 (2012)
Soluble guanylate cyclase (sGC), the primary mediator of nitric oxide (NO) bioactivity, exists as reduced (NO-sensitive) and oxidized (NO-insensitive) forms. We tested the hypothesis that the cardiovascular protective effects of NO-insensitive sGC ac
Externí odkaz:
https://doaj.org/article/7de0d838ef7f45aba69ae237f3a44947
Autor:
Alan P. Graves, Brian G. Lawhorn, Lara S. Kallander, Gatto Gregory J, Lisa M. Shewchuk, Dennis A. Holt, Katrina Rivera, Larry J. Jolivette, Joanne Philp
Publikováno v:
Journal of Medicinal Chemistry. 61:3076-3088
Structure-guided progression of a purine-derived series of TNNI3K inhibitors directed design efforts that produced a novel series of 4,6-diaminopyrimidine inhibitors, an emerging kinase binding motif. Herein, we report a detailed understanding of the
Autor:
Brian G. Lawhorn, Brian Budzik, Karl F. Erhard, Huijie Li, Carla A. Donatelli, Kalindi Vaidya, Melissa H. Costell, Joseph E. Pero, John J. McAtee, Carl Brooks, Lorraine M. Posobiec, Larry J. Jolivette, Dennis A. Holt, Theresa J. Roethke, Stephen H. Eisennagel, Michael C. Fischer, Matthews Jay M, Arthur Shu, Brent W. Mccleland, Lamont Roscoe Terrell, Sender Matthew Robert, Katrina Rivera, David J. Behm, Israil Pendrak, Ralph A. Rivero, Xiaoping Xu, Edward J. Brnardic, Peng Li
Publikováno v:
Journal of medicinal chemistry. 61(24)
Pulmonary edema is a common ailment of heart failure patients and has remained an unmet medical need due to dose-limiting side effects associated with current treatments. Preclinical studies in rodents have suggested that inhibition of transient rece
Autor:
Yun Ding, Lisa M. Shewchuk, Martin Brandt, Ami L. Shaw, David I. Israel, Stephen A. Douglas, Gregory D. Brown, Dennis A. Holt, Christine G. Schnackenberg, Rusty E. Fries, Jeffrey W. Gross, Larry J. Jolivette, Tracy Mandichak, Jason W. Dodson, Melissa H. Costell, Mark R. Harpel, Steve H. Eisennagel, Jeff J. McAtee, Theresa J. Roethke, Reema K. Thalji, Svetlana L. Belyanskaya, Hu Li, Wensheng Xie, Joseph P. Marino, Quinn Lu, Benjamin Schwartz, David J. Behm, Daniel J. Krosky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3584-3588
1-(1,3,5-Triazin-yl)piperidine-4-carboxamide inhibitors of soluble epoxide hydrolase were identified from high through-put screening using encoded library technology. The triazine heterocycle proved to be a critical functional group, essential for hi
Publikováno v:
Journal of Pharmaceutical Sciences. 100:3862-3874
The purpose of this investigation was to compare selected pharmacokinetic (PK) parameters obtained by cassette and discrete dosing of compounds in rats. The concordance of PK properties obtained by the two dosing strategies was evaluated for 116 comp
Autor:
Larry J. Jolivette, Erding Hu, Andrew Q. Viet, Lois L Wright, Edward Dul, Robert B. Kirkpatrick, Robert A. Stavenger, Haifeng Cui, Weiwei Xu, Gren Z. Wang, David Kendallc Jung, Ross Bentley, David J. Behm, Robert L. Ivy, Dimitri E. Gaitanopoulos, Christopher P. Doe, Tracey Yi, Dennis Lee, Krista B. Goodman, Sarah E. Dowdell, Sanjay S. Khandekar, Gary K Smith, Christopher P. Evans, Guosen Ye, Harvey E. Fries, Simon Semus, Clark A. Sehon
Publikováno v:
Journal of Medicinal Chemistry. 50:6-9
Rho kinase (ROCK1) mediates vascular smooth muscle contraction and is a potential target for the treatment of hypertension and related disorders. Indazole amide 3 was identified as a potent and selective ROCK1 inhibitor but possessed poor oral bioava
Autor:
Robert Lafferty, Tracey Yi, Ross G. Bentley, Dennis Lee, Sanjay S. Khandekar, Christine Webb, Joseph P. Marino, Mark James Bamford, Gary K. Smith, Erding Hu, Robert N. Willette, Zunxuan Chen, Robert B. Kirkpatrick, Eugene T. Grygielko, Robert A. Stavenger, David J. Behm, Larry J. Jolivette, Lois L. Wright, David Kendall Jung, Terry Panchal, Chris P. Doe, Edward Dul
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 320:89-98
Increased Rho kinase (ROCK) activity contributes to smooth muscle contraction and regulates blood pressure homeostasis. We hypothesized that potent and selective ROCK inhibitors with novel structural motifs would help elucidate the functional role of
Publikováno v:
Drug Metabolism and Disposition. 34:1255-1265
The prediction of human pharmacokinetics from preclinical species is an integral component of drug discovery. Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for