Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Isaac E. Marx"'
Autor:
Stefan I. McDonough, Min-Hwa Jasmine Lin, Erin F. DiMauro, Violeta Yu, Angel Guzman-Perez, Kristin Taborn, Christiane Bode, Thomas Kornecook, Thomas Dineen, Xin Huang, Robert T. Fremeau, Margaret Chu-Moyer, James R. Coats, Bingfan Du, Jeff S. McDermott, Hakan Gunaydin, Daniel S. La, Hua Gao, Bryan D. Moyer, Russell Graceffa, Alessandro Boezio, Charles Kreiman, Matthew Weiss, Hanh Nho Nguyen, David J. Matson, Joseph Ligutti, Christopher P Ilch, Isaac E. Marx, Emily A. Peterson, Howard Bregman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:3477-3485
The voltage-gated sodium channel NaV1.7 has received much attention from the scientific community due to compelling human genetic data linking gain- and loss-of-function mutations to pain phenotypes. Despite this genetic validation of NaV1.7 as a tar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b9bf06b4e0a447e6a5e64c58b6fc67fa
https://doi.org/10.1016/j.bmcl.2017.05.070
https://doi.org/10.1016/j.bmcl.2017.05.070
Autor:
Jessica Able, Benjamin C. Milgram, Loren Berry, Melanie Cooke, Liyue Huang, John Butler, Hongbing Huang, Violeta Yu, Kristin Taborn, John D. Roberts, Steven Altmann, Margaret Y. Chu-Moyer, John Yeoman, Jean Wang, Roman Shimanovich, Russell Graceffa, Matthew Weiss, Thomas Kornecook, Christopher P Ilch, Bryan D. Moyer, Christiane Boezio, Isaac E. Marx, Brian A. Sparling, Emily A. Peterson, Gwen Rescourio, Charles Kreiman, Elma Feric Bojic, Karina R. Vaida, Angel Guzman-Perez, Dawn Zhu, Hua Gao, Laurie B. Schenkel, Michael Jarosh, Hanh Nho Nguyen, Joseph Ligutti, Alessandro Boezio, Hakan Gunaydin, Daniel S. La, Thomas Dineen, Robert T. Fremeau, Robert S. Foti, Min-Hwa Jasmine Lin, Erin F. DiMauro, John Stellwagen
Publikováno v:
Journal of Medicinal Chemistry. 60:5990-6017
Because of its strong genetic validation, NaV1.7 has attracted significant interest as a target for the treatment of pain. We have previously reported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors that demo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bb6062704d531ce83c1a6122ecc44600
https://doi.org/10.1021/acs.jmedchem.6b01850
https://doi.org/10.1021/acs.jmedchem.6b01850
Autor:
Robert T. Fremeau, Isaac E. Marx, Emily A. Peterson, Charles Kreiman, Thomas Dineen, Hua Gao, Alessandro Boezio, Hakan Gunaydin, Min-Hwa Jasmine Lin, Steven Altmann, Elma Feric Bojic, Kristin Taborn, Robert S. Foti, Russell Graceffa, Daniel S. La, Liyue Huang, Matthew Weiss, Paul E. Rose, Angel Guzman-Perez, Beth D. Youngblood, Hongbing Huang, Violeta Yu, Dong Liu, Thomas Kornecook, Bryan D. Moyer, Howard Bregman, Hanh Nho Nguyen, Joseph Ligutti, Margaret Y. Chu-Moyer, Michael Jarosh, Erin F. DiMauro
Publikováno v:
Journal of Medicinal Chemistry. 60:5969-5989
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. The optimization of a series of internal NaV1.7 leads that address
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3616b7030b42538cb45a4828f9c4821e
https://doi.org/10.1021/acs.jmedchem.6b01851
https://doi.org/10.1021/acs.jmedchem.6b01851
Autor:
Russell F, Graceffa, Alessandro A, Boezio, Jessica, Able, Steven, Altmann, Loren M, Berry, Christiane, Boezio, John R, Butler, Margaret, Chu-Moyer, Melanie, Cooke, Erin F, DiMauro, Thomas A, Dineen, Elma, Feric Bojic, Robert S, Foti, Robert T, Fremeau, Angel, Guzman-Perez, Hua, Gao, Hakan, Gunaydin, Hongbing, Huang, Liyue, Huang, Christopher, Ilch, Michael, Jarosh, Thomas, Kornecook, Charles R, Kreiman, Daniel S, La, Joseph, Ligutti, Benjamin C, Milgram, Min-Hwa Jasmine, Lin, Isaac E, Marx, Hanh N, Nguyen, Emily A, Peterson, Gwen, Rescourio, John, Roberts, Laurie, Schenkel, Roman, Shimanovich, Brian A, Sparling, John, Stellwagen, Kristin, Taborn, Karina R, Vaida, Jean, Wang, John, Yeoman, Violeta, Yu, Dawn, Zhu, Bryan D, Moyer, Matthew M, Weiss
Publikováno v:
Journal of medicinal chemistry. 60(14)
Because of its strong genetic validation, Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::b8ea84d65ab7dd59414c7bfc36426140
https://pubmed.ncbi.nlm.nih.gov/28324649
https://pubmed.ncbi.nlm.nih.gov/28324649
Autor:
Matthew M, Weiss, Thomas A, Dineen, Isaac E, Marx, Steven, Altmann, Alessandro, Boezio, Howard, Bregman, Margaret, Chu-Moyer, Erin F, DiMauro, Elma, Feric Bojic, Robert S, Foti, Hua, Gao, Russell, Graceffa, Hakan, Gunaydin, Angel, Guzman-Perez, Hongbing, Huang, Liyue, Huang, Michael, Jarosh, Thomas, Kornecook, Charles R, Kreiman, Joseph, Ligutti, Daniel S, La, Min-Hwa Jasmine, Lin, Dong, Liu, Bryan D, Moyer, Hanh N, Nguyen, Emily A, Peterson, Paul E, Rose, Kristin, Taborn, Beth D, Youngblood, Violeta, Yu, Robert T, Fremeau
Publikováno v:
Journal of medicinal chemistry. 60(14)
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7836a4ad57471118cec766361a3f5db3
https://pubmed.ncbi.nlm.nih.gov/28287723
https://pubmed.ncbi.nlm.nih.gov/28287723
Autor:
Robert T. Fremeau, Robert S. Foti, Hanh Nho Nguyen, Jeff S. McDermott, Jean Wang, Christiane Bode, Bingfan Du, Joseph Ligutti, Thomas Dineen, Hua Gao, Thomas Kornecook, Jonathan Roberts, Brian E. Hall, Charles Kreiman, Liyue Huang, Matthew Weiss, Jessica Able, Min-Hwa Jasmine Lin, Paul E. Rose, Isaac E. Marx, Emily A. Peterson, Violeta Yu, Erin F. DiMauro, Bryan D. Moyer, Daniel S. La, Beth D. Youngblood, Dong Liu, Margaret Y. Chu-Moyer, Hakan Gunaydin, Howard Bregman
Human genetic evidence has identified the voltage-gated sodium channel Na
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e82bfc2625ad2b8c686cc56a8b01002
https://europepmc.org/articles/PMC5346988/
https://europepmc.org/articles/PMC5346988/
Autor:
Paul H. Wen, Robert C. Wahl, Ryan White, Oleg Epstein, Stephen J. Wood, Katayoun Derakhchan, Douglas A. Whittington, Chuck E. Kreiman, Isaac E. Marx, Thomas Dineen, Dean Hickman, Kui Chen, Matthew Weiss, Joel Esmay, Vinod F. Patel, Alan C. Cheng, Robert T. Fremeau
Publikováno v:
Journal of Medicinal Chemistry. 57:9811-9831
We have previously shown that the aminooxazoline xanthene scaffold can generate potent and orally efficacious BACE1 inhibitors although certain of these compounds exhibited potential hERG liabilities. In this article, we describe 4-aza substitution o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c9b3095ff7f5efcf8cbc5e633bdfc8f
https://doi.org/10.1021/jm5012676
https://doi.org/10.1021/jm5012676
Autor:
Min-Hwa Jasmine Lin, Paul E. Rose, Violeta Yu, Hakan Gunaydin, Robert T. Fremeau, Charles Kreiman, Daniel S. La, Joseph Ligutti, Matthew Weiss, Beth D. Youngblood, Thomas Dineen, Thomas Kornecook, Dong Liu, Bingfan Du, Brian E. Hall, Erin F. DiMauro, Jean Wang, Isaac E. Marx, Robert S. Foti, Emily A. Peterson, Jessica Able, Liyue Huang, Margaret Chu-Moyer, Jeff S. McDermott, Christiane Bode, Bryan D. Moyer, Howard Bregman, Jonathan Roberts, Hua Gao
Human genetic evidence has identified the voltage-gated sodium channel NaV1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide 3 as a potent and selective inhibitor of NaV1.7. Optimization to reduce b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a45d3cf7f30dc5240f9068aa183a1600
https://europepmc.org/articles/PMC5150675/
https://europepmc.org/articles/PMC5150675/
Autor:
Ryan White, Erin F. DiMauro, Stephen Hitchcock, Robert T. Fremeau, Ming Y. Huang, Isaac E. Marx, Jason Brooks Human, Liyue Huang, Josie H. Lee, Alan C. Cheng, Vinod F. Patel, Xingwen Li, Matthew W. Martin, Renee Emkey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:31-35
A series of α-amidosulfones were found to be potent and selective agonists of CB2. The discovery, synthesis, and structure–activity relationships of this series of agonists are reported. In addition, the pharmacokinetic properties of the most prom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e0daa5a47b3ce311b575c1293b5ea28
https://doi.org/10.1016/j.bmcl.2008.11.026
https://doi.org/10.1016/j.bmcl.2008.11.026
Autor:
Paul H. Wen, Robert C. Wahl, Ryan White, Zihao Hua, Robert T. Fremeau, Thomas Dineen, Stephen J. Wood, Jason Brooks Human, Vinod F. Patel, Marian C. Bryan, Oleg Epstein, Douglas A. Whittington, Katayoun Derakhchan, Charles Kreiman, Matthew Weiss, Alan C. Cheng, Dean Hickman, Xiao Mei Zheng, Isaac E. Marx
Publikováno v:
Journal of medicinal chemistry. 57(23)
The optimization of a series of aminooxazoline xanthene inhibitors of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is described. An early lead compound showed robust Aβ lowering activity in a rat pharmacodynamic model, but advancement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e24e5ad84e0c301aadb1173bf80a9f3
https://pubmed.ncbi.nlm.nih.gov/25389560
https://pubmed.ncbi.nlm.nih.gov/25389560