Zobrazeno 1 - 10
of 62
pro vyhledávání: '"Jeffrey J. Hale"'
Autor:
Jiaqiang Cai, Bimjhana Bishwokarma, Dennis Leung, William J. Morris, Feroze Ujjainwalla, Candice Alleyne, Xiaoxing Du, Vincent J. Colandrea, Jennifer Piesvaux, Jianwu Bai, Liming Yang, Carla Alpert, Joseph M. Metzger, Vincenzo Pucci, Xiaofang Li, Jeffrey J. Hale, Dominique Stickens, Weiguo Quan, Byron G. DuBois, Rongqiang Liu, Mark Zielstorff, Chi-Sung Chiu, Christopher Joseph Sinz, Mangeng Cheng, Kallol Ray, Liping Wang, Ping Liu, Stella H. Vincent, Alejandro Crespo
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1193-1198
[Image: see text] We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia. In order to mitigate the concerns for potential sys
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d76215d13beffa00c0fc7a79f728fdec
https://doi.org/10.1021/acsmedchemlett.8b00274
https://doi.org/10.1021/acsmedchemlett.8b00274
Autor:
Hiroshi Nagabukuro, Sean M. Smith, Richard A. Berger, Melissa Costa, Nam Fung Kar, Bart Harper, Karen H. Dingley, Gino Salituro, Liping Wang, Jerry Di Salvo, Scott D. Edmondson, Bing Li, Xiaofang Li, Cheng Zhu, Christopher Moyes, Stephen D. Goble, Sookhee Ha, Mary Struthers, Jeffrey J. Hale, Amanda L. Hurley, Randy R. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:1094-1098
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β3-adrenergic receptor for the treatment of overactive bladder (OAB) is described. The SAR studies directed towards maintaining well established β3 potency
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a81656be92fb37eb8138200c6f4a9e90
https://doi.org/10.1016/j.bmcl.2016.12.033
https://doi.org/10.1016/j.bmcl.2016.12.033
Autor:
Cheng Zhu, Mary Struthers, Jerry Di Salvo, Bing Li, Jeffrey J. Hale, Ann E. Weber, Xiaofang Li, Randy R. Miller, Scott D. Edmondson, Melissa Costa, Nam Fung Kar, Sookhee Ha, Karen H. Dingley, Amanda L. Hurley, Gino Salituro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:55-59
The paper will describe the synthesis and SAR studies that led to the discovery of benzamide (reverse amide) as potent and selective human β3-adrenergic receptor agonist. Based on conformationally restricted pyrrolidine scaffold we discovered earlie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e27d3b6f5e7b1c5dde05b81dd6b0cf4
https://doi.org/10.1016/j.bmcl.2015.11.030
https://doi.org/10.1016/j.bmcl.2015.11.030
Autor:
Julie A. DeMartino, James A. Milligan, Edward C. Sherer, Thomas F. Walsh, Richard Hajdu, Russell B. Lingham, Xinchun Tong, Michael Wolff, Denise M. Visco, Mikhail Reibarkh, Matthew J. Clements, Jeffrey T. Kuethe, Randy R. Miller, Christina B. Madsen-Duggan, Lisa M. Sonatore, Scott P. Salowe, Dominique Stickens, Jianmei Pang, Jeffrey J. Hale, Dan Zhou, John S. Debenham
Publikováno v:
Journal of medicinal chemistry. 59(24)
The discovery of novel 4-hydroxy-2-(heterocyclic)pyrimidine-5-carboxamide inhibitors of hypoxia-inducible factor (HIF) prolyl hydroxylases (PHD) is described. These are potent, selective, orally bioavailable across several species, and active in stim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45d6d174fbd4111c1eb7c610defd4bfd
https://pubmed.ncbi.nlm.nih.gov/28002958
https://pubmed.ncbi.nlm.nih.gov/28002958
Autor:
Yong Zhang, Jeffrey J. Hale, Andreas Verras, Shirly Pinto, Huaibing He, Zhu Shen, Urmi R. Bhatt, Elaine C. Tung, John S. Debenham, Matthew J. Clements, Dunlu Chen, Dong-Ming Shen, Wayne M. Geissler, Thomas H. Graham, JeanMarie Lisnock, Qing Chen, Suoyu Xu, Xiaohua Li, Margarita Garcia-Calvo, Wensheng Liu, Xinchun Tong, Judyann Wiltsie, Christina B. Madsen-Duggan, Jeffrey T. Kuethe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6228-6233
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33a2d166f3f282c60327beda62c09726
https://doi.org/10.1016/j.bmcl.2013.09.094
https://doi.org/10.1016/j.bmcl.2013.09.094
Autor:
Bart H, Harper, Liping, Wang, Cheng, Zhu, Nam F, Kar, Bing, Li, Christopher R, Moyes, Stephen D, Goble, Melissa, Costa, Karen, Dingley, Jerry, Di Salvo, Sookhee N, Ha, Amanda, Hurley, Xiaofang, Li, Randy R, Miller, Hiroshi, Nagabukuro, Gino M, Salituro, Sean, Smith, Mary, Struthers, Jeffrey J, Hale, Scott D, Edmondson, Richard, Berger
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(4)
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::4f91c75780a40046061dd474805e2a80
https://pubmed.ncbi.nlm.nih.gov/28089699
https://pubmed.ncbi.nlm.nih.gov/28089699
Autor:
Fa-Xiang Ding, Urmi R. Bhatt, Hong C. Shen, Wayne M. Geissler, Judith N. Gorski, Ranabir SinhaRoy, Margarita Garcia-Calvo, Jinlong Jiang, Xinchun Tong, Renee M. Chabin, Beth Ann Murphy, Dong-Ming Shen, Shirly Pinto, Jeffrey J. Hale, Dan Xie, Andreas Verras, Mike E. Lassman, Qing Chen, Suoyu Xu, Judyann Wiltsie, Zhu Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1550-1556
A series of benzodihydroisofurans were discovered as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase (PrCP) inhibitors. The structure–activity relationship (SAR) is focused on improving PrCP activity and metabolic stability,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c0fea705f75363de3cf1cb0edafcd87
https://doi.org/10.1016/j.bmcl.2012.01.002
https://doi.org/10.1016/j.bmcl.2012.01.002
Autor:
Thomas H. Graham, Urmi R. Bhatt, Dong-Ming Shen, Xinchun Tong, Mike E. Lassman, Kelly Bleasby, Dan Xie, Qing Chen, Shirly Pinto, Margarita Garcia-Calvo, Andreas Verras, Renee M. Chabin, Zhicai Wu, Steven L. Colletti, Suoyu Xu, Cangming Yang, James R. Tata, Zhu Shen, Ranabir SinhaRoy, Jeffrey J. Hale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1727-1730
Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good Pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1612ca458599f3caa91f1160e81053f8
https://doi.org/10.1016/j.bmcl.2011.12.098
https://doi.org/10.1016/j.bmcl.2011.12.098
Autor:
Junying Wang, Richard G. Ball, Chun-Pyn Shen, Richard Z. Chen, Julie Lao, Vijay Bhasker G. Reddy, Xinchun Tong, Jeffrey J. Hale, Alison M. Strack, Jing Chen Xiao, Lauren P. Shearman, John S. Debenham, Tung M. Fong, D. Sloan Stribling, Christina B. Madsen-Duggan, Pei Huo, Lin Yan, Nancy N. Tsou, Thomas Bateman
Publikováno v:
Journal of Medicinal Chemistry. 53:4028-4037
This paper describes the discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596, 12c) as a novel cannabinoid-1 receptor (CB1R) inverse agonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8b223fd3b459aa0c611a30e5f8e83030
https://doi.org/10.1021/jm100023j
https://doi.org/10.1021/jm100023j
Autor:
Rose M. Cubbon, Kevin T. Chapman, Sunita Malkani, Edward A. O'Neill, Ruixiu Wang, Lihu Yang, Silvi Luell, James E. Thompson, Songnian Lin, Jeffrey J. Hale, Wen Xiao Zhang, Sander G. Mills, Ester Carballo-Jane, Matthew Lombardo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3238-3242
Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas are described as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). These compounds demonstrate potent in vitro activity against the enzyme with IC(50) values as low as 15
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d386e3279774277617f59ef7ab810cee
https://doi.org/10.1016/j.bmcl.2009.04.088
https://doi.org/10.1016/j.bmcl.2009.04.088