Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Stephen D, Goble"'
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:
James M. Balkovec, Kevin D. Dykstra, Beth Ann Murphy, Edward C. Sherer, Donald M. Sperbeck, Claire Lee, Tim Cernak, James Cuff, Jeffrey T. Kuethe, Ravi P. Nargund, Andreas Verras, Zhi-Cai Shi, Spencer D. Dreher, Shuwen He, Maud Reiter, Petr Vachal, Stephen D. Goble, Dong-Ming Shen, Zhicai Wu, Yang Yu, Robert J. DeVita, Nicholas Perrotto, Steven Williams, Lisa M. Sonatore, Shirly Pinto, Nathan J. Gesmundo, Maria Madeira
Publikováno v:
Journal of medicinal chemistry. 60(9)
Miniaturization and parallel processing play an important role in the evolution of many technologies. We demonstrate the application of miniaturized high-throughput experimentation methods to resolve synthetic chemistry challenges on the frontlines o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::572283ae6d3dcf65fa072d0c3033562b
https://pubmed.ncbi.nlm.nih.gov/28252959
https://pubmed.ncbi.nlm.nih.gov/28252959
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:
Beata Zamlynny, Stuart A. Green, Karen H. Dingley, Liping Wang, Ann E. Weber, Katherine L. Villa, Amanda L. Hurley, Dong-Ming Shen, Gregori J. Morriello, Scott D. Edmondson, Sookhee Ha, Anthony Sanfiz, Dorothy Levorse, Nam Fung Kar, Beatrice Sacre-Salem, Hiroshi Nagabukuro, Nina Jochnowitz, Aileen Fitzmaurice, Gino Salituro, Tara L. Frenkl, Jerry Di Salvo, Richard G. Ball, Loise Gichuru, James D. Ormes, Cheng Zhu, Christopher Moyes, Stephen D. Goble, Randy R. Miller, Mary Struthers, Bart Harper, Shruty Mistry, Andra S. Stevenson, Richard A. Berger
Publikováno v:
Journal of medicinal chemistry. 59(2)
The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical β3-AR agonist MK-0634 (3) exhibited efficacy in humans for the treatment of OAB, but dev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f522169161222843c23eb180bd9c7b46
https://pubmed.ncbi.nlm.nih.gov/26709102
https://pubmed.ncbi.nlm.nih.gov/26709102
Autor:
Richard Jiao, Pasquale P. Vicario, Gabor Butora, Shankaran Kothandaraman, Stephen D. Goble, Mary Struthers, Gregori J. Morriello, Julie A. DeMartino, Sander G. Mills, Malcolm MacCoss, Julia M. Ayala, Margaret A. Cascieri, Karla L. Donnely, Changyou Zhou, Lihu Yang, Alexander Pasternak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1830-1834
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37cf3150520d0f4c125edd804b8e5959
https://doi.org/10.1016/j.bmcl.2008.12.050
https://doi.org/10.1016/j.bmcl.2008.12.050
Autor:
Julie A. DeMartino, Stephen D. Goble, Mary Struthers, Jerry Di Salvo, Pasquale P. Vicario, Alexander Pasternak, Julia M. Ayala, Sander G. Mills, Lihu Yang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:994-998
This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04e9718f074913bae396e0a7019b2df3
https://doi.org/10.1016/j.bmcl.2007.12.029
https://doi.org/10.1016/j.bmcl.2007.12.029
Autor:
Patricia Brown, Anthony Sanfiz, Ann E. Weber, Richard A. Berger, Liping Wang, Katherine L. Villa, Scott D. Edmondson, Christopher Moyes, Amanda L. Hurley, Andra S. Stevenson, Aileen Fitzmaurice, Dong-Ming Shen, Stephen D. Goble, Nina Jochnowitz, Karen H. Dingley, Jerry Di Salvo, Mary Struthers, Loise Gichuru, Randall R. Miller, Hiroshi Nagabukuro, Gino Salituro, Airu S. Chen, Beata Zamlynny, Alka Bansal, Bart Harper, Shruty Mistry
Publikováno v:
Journal of medicinal chemistry. 57(4)
A series of conformationally restricted acetanilides were synthesized and evaluated as β3-adrenergic receptor agonists (β3-AR) for the treatment of overactive bladder (OAB). Optimization studies identified a five-membered ring as the preferred conf
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc1d1a538eaf74c7d6dfb1e647bd93e6
https://pubmed.ncbi.nlm.nih.gov/24437735
https://pubmed.ncbi.nlm.nih.gov/24437735
Autor:
Julia M. Ayala, Lihu Yang, Julie A. DeMartino, Pasquale P. Vicario, Jerry Di Salvo, Stephen D. Goble, Mary Struthers, Alexander Pasternak, Ruth Kilburn, Sander G. Mills, Thomas Wisniewski
This report describes the discovery of a potent, orally bioavailable CC chemokine receptor 2 (CCR2) antagonist which, while optimized for CCR2 potency, also had potent CC chemokine receptor 5 (CCR5) activity.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6cc5f5b1921326dc3ea9ab791d131d11
https://europepmc.org/articles/PMC4007850/
https://europepmc.org/articles/PMC4007850/
Autor:
Alexander Pasternak, Paul Mazur, Michael R. Tota, Stephen D. Goble, Lihu Yang, Donna L. Hreniuk, Andrew D. Howard, Reynalda deJesus, Sander G. Mills, Christine C. Chung, Scott D. Feighner
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(21)
This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fdfcd1b4cde935121608bb1f09ea58b2
https://pubmed.ncbi.nlm.nih.gov/19767208
https://pubmed.ncbi.nlm.nih.gov/19767208
Autor:
George A. Doss, Nancy N. Tsou, Julie A. DeMartino, Julia M. Ayala, Alexander Pasternak, Sander G. Mills, Stephen D. Goble, Mary Struthers, Pasquale P. Vicario, Lihu Yang, Gabor Butora
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(4)
In an effort to shed light on the active binding conformation of our 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists, we prepared several conformationally constrained analogs resulting from backbone cyclization. Evaluation of CCR2 binding a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::70f06adbeaca3d9c57a97da85021cd5f
https://pubmed.ncbi.nlm.nih.gov/18215519
https://pubmed.ncbi.nlm.nih.gov/18215519