Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Bart Harper"'
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:
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:
Donna L. Hreniuk, Ann E. Weber, Gino Salituro, Michael A. Robbins, Liping Wang, Stephen D. Goble, Mary Struthers, Eloisa Watkins, Amanda L. Hurley, Richard A. Berger, Jiafang He, Eric Streckfuss, Emma R. Parmee, Alka Bansal, Bart Harper, Anthony Sanfiz, Jerry DiSalvo, Scott D. Feighner, Scott D. Edmondson, K. Lulu Howell, Linda Brockunier
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1895-1899
A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c34d91e7b6660bccd41d2e2f4d3ffc8
https://doi.org/10.1016/j.bmcl.2010.01.130
https://doi.org/10.1016/j.bmcl.2010.01.130
Autor:
Joseph K. Wu, Reshma A. Patel, Nancy A. Thornberry, Ann E. Weber, Jason M. Cox, Shiyao Xu, Bing Zhu, Barbara Leiting, Kathryn A. Lyons, Scott D. Edmondson, Ranabir Sinha Roy, Bart Harper, Huaibing He, Anthony Mastracchio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4579-4583
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98884c494e47764737b50f0ae2565589
https://doi.org/10.1016/j.bmcl.2007.05.087
https://doi.org/10.1016/j.bmcl.2007.05.087
Autor:
Min Shu, William J. Greenlee, Alan Hruza, Harold B. Wood, Min Park, Shawn P. Walsh, Kenneth P. Ellsworth, Yi-Heng Chen, Lisa M. Sonatore, Bart Harper, Bing Li, Aurash Sharipour, Richard A. Berger, Cameron J. Smith, Esther Kim, Edward C. Sherer, Paul Reichert, Jane Y. Wu, Wayne M. Geissler, Jiayi Xu, Sunita V. Dewnani, James M. Balkovec, Dann L. Parker, Ting Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(11)
Two high-throughput screening hits were investigated for SAR against human factor IXa. Both hits feature a benzamide linked to a [6-5]-heteroaryl via an alkyl amine. In the case where this system is a benzimidazolyl-ethyl amine the binding potency fo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6383cff65e1e05696a8b9c62363937ea
https://pubmed.ncbi.nlm.nih.gov/25937013
https://pubmed.ncbi.nlm.nih.gov/25937013
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:
Alexa Hansen, Richard A. Berger, Michael Wolff, Cheng Zhu, James Hubert, Jie Pan, Alison M. Strack, Ann E. Weber, Bart Harper, Zhesheng Chen, Marc L. Reitman, Tom G. Holt, Su Qian, Susan J. Lee, Scott D. Edmondson, Drew T. Weingarth, Douglas J. MacNeil
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(17)
The discovery and structure–activity relationship of 1,2-diarylimidazole piperazine carboxamides bearing polar side chains as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are described. Optimization of this series resulted in th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c52e1f9c735c83e89a573ce6753cffe
https://pubmed.ncbi.nlm.nih.gov/18684621
https://pubmed.ncbi.nlm.nih.gov/18684621
Autor:
Joseph K. Wu, Anthony Mastracchio, Nancy A. Thornberry, Alexsandr Petrov, George J. Eiermann, Barbara Leiting, Ranabir Sinha Roy, Park Yj, Giovanna Scapin, Robert J. Mathvink, Suoyu Xu, Ann E. Weber, Dorothy Levorse, Jackie Shang, Joseph F. Leone, Reshma A. Patel, Huaibing He, Jiafang He, Scott D. Edmondson, Kathy Lyons, Shil Patel, Bart Harper, Adrian L. Smith, Di Salvo J, Bing Zhu, Maria G. Beconi
Publikováno v:
Journal of medicinal chemistry. 49(12)
A series of beta-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::582eb905eb7d002f3b739890783bcdfd
https://pubmed.ncbi.nlm.nih.gov/16759103
https://pubmed.ncbi.nlm.nih.gov/16759103