Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Neil Flynn"'
Autor:
Jeffrey A. Robl, Michael Thomas, Mary Ann Pelleymounter, Brian Gemzik, Anthony V. Azzara, Brian J. Murphy, Sharon N. Bisaha, Helen E. Godonis, Daniel Longhi, Neil Flynn, William N. Washburn, Kenneth W. Rohrbach, Khehyong Ngu, Saleem Ahmad, Susan Harvey, Christine Huang, Evan B. Janovitz, Andres S. Hernandez, James Devenny, Hongwei Zhang, Lisa Zhang, Susan Glick, Suzanne Rooney, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8848-8858
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Autor:
Neil Flynn, Mary Jane Cullen, Hongwei Zhang, Wei Wang, Susan Glick, Lisa Zhang, Jeffrey A. Robl, Pratik Devasthale, Andres S. Hernandez, Christian Caporuscio, Brian J. Murphy, Suzanne Rooney, Ning Huang, Mary Ann Pelleymounter, Kenneth W. Rohrbach, Kishore Renduchintala, Anthony V. Azzara, Helen E. Godonis, Yi-Xin Li, Radhakrishnan Sridhar, Michael Thomas, Susan Harvey, Paul Stetsko, Mary F. Grubb, Chris Freeden, Fang Moore, Christine Huang, James Devenny, Daniel Longhi, William N. Washburn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2793-2799
Our investigation of the structure–activity and structure–liability relationships for dihydropyrrolopyrazol-6-one MCHR1 antagonists revealed that off-rate characteristics, inferred from potencies in a FLIPR assay following a 2 h incubation, can i
Autor:
Carrie Xu, George C. Morton, Vinayak Hosagrahara, Shung Wu, Denis E. Ryono, Jonathan Lippy, Narayanan Hariharan, Kenneth T. Locke, Xiang-Xang Ye, Wei Wang, Liqun Gu, Yi-Xin Li, Fucheng Qu, Peter T. W. Cheng, Sean S. Chen, Kevin O’Malley, Michael Cap, Robert Zahler, Tao Wang, Lori Kunselman, Charles Z. Ding, Cuixia Chu, Rebecca A. Smirk, Neil Flynn, Pratik Devasthale, Hao Zhang, Nathan Morgan, Atsu Apedo, Thomas Harrity, Lisa Zhang, Dennis Farrelly, Arthur M. Doweyko, Zhi Lai, Tim Herpin, Pathanjali Kadiyala
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1196-1205
The design, synthesis and structure–activity relationships of a novel series of 3,4-disubstituted pyrrolidine acid analogs as PPAR ligands is outlined. In both the 1,3- and 1,4-oxybenzyl pyrrolidine acid series, the preferred stereochemistry was sh
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Autor:
William R. Ewing, Carrie Xu, Heng Liu, Brian J. Murphy, Neil Flynn, Tao Wang, Douglas B. Moore, Lori Kunselman, Bruce A. Ellsworth, Elizabeth A. Jurica, Kimberly A. Foster, Atsu Apedo, Yuan Tian, Yang Hong, Arvind Mathur, Bradley A. Zinker, Biji Jacob, Kristin N. Williams, Min Zhou, Brad D. Maxwell, Gary Cao, Andres S. Hernandez, Qin Sun, Hong Cai, Jean M. Whaley, Elizabeth A. Dierks, Joel C. Barrish, Dora M. Schnur, Ximao Wu, Doree F. Sitkoff, Mary Ellen Cvijic, Richard Rampulla, Chunshan Xie, David S. Nirschl, Reshma Panemangalore, Michael B. Hicks, Jeffrey A. Robl, Jason J. Wilkes
Publikováno v:
Journal of medicinal chemistry. 60(4)
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-
Autor:
Jeffrey A. Robl, Guohua Zhao, Joel C. Barrish, Bei Wang, Brad D. Maxwell, Christian Caporuscio, Hongwei Zhang, James Devenny, Mary F. Grubb, Zhenghua Wang, Suzanne Rooney, James Mignone, Lisa Zhang, Brian J. Murphy, Wei Wang, Daniel Longhi, William N. Washburn, Kenneth W. Rohrbach, Evan B. Janovitz, Mark C. Manfredi, Mary Ann Pelleymounter, Michael Thomas, Hong Yang, Paul Stetsko, Saleem Ahmad, Atsu Apedo, Mary Jane Cullen, Brian Gemzik, Ning Huang, Chris Freeden, Susan Harvey, Anthony V. Azzara, Khehyong Ngu, Christine Huang, Rulin Zhao, Susan Glick, Neil Flynn, Pratik Devasthale, Andres S. Hernandez, Helen E. Godonis
Publikováno v:
Journal of Medicinal Chemistry. 57:7509-7522
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high affinity allowed us
Autor:
Saleem, Ahmad, William N, Washburn, Andres S, Hernandez, Sharon, Bisaha, Khehyong, Ngu, Wei, Wang, Mary Ann, Pelleymounter, Daniel, Longhi, Neil, Flynn, Anthony V, Azzara, Kenneth, Rohrbach, James, Devenny, Suzanne, Rooney, Michael, Thomas, Susan, Glick, Helen, Godonis, Susan, Harvey, Hongwei, Zhang, Brian, Gemzik, Evan B, Janovitz, Christine, Huang, Lisa, Zhang, Jeffrey A, Robl, Brian J, Murphy
Publikováno v:
Journal of medicinal chemistry. 59(19)
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Publikováno v:
Talent Assessment ISBN: 9781315611815
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::12841a2e4ef27b09af5dbf86c0f46f00
https://doi.org/10.4324/9781315611815-13
https://doi.org/10.4324/9781315611815-13
Publikováno v:
Talent Assessment ISBN: 9781315611815
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a54e1b2f18ef1ec5cba8b0824f544686
https://doi.org/10.4324/9781315611815-9
https://doi.org/10.4324/9781315611815-9
Publikováno v:
Talent Assessment ISBN: 9781315611815
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d005724d6f05366e4bc4bb36a9bc8015
https://doi.org/10.4324/9781315611815-14
https://doi.org/10.4324/9781315611815-14