Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Brian Lee Venables"'
Autor:
Carolyn Diane Dzierba, Linda J. Bristow, Ramkumar Rajamani, Jie Chen, Rick L. Pieschl, Sing-Yuen Sit, Brian Lee Venables, Michele Matchett, Ronald J. Knox, Lorin A. Thompson, Nicholas A. Meanwell, Yong-Jin Wu, Jason M. Guernon, James Herrington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:659-663
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led t
Autor:
Nicholas A. Meanwell, Kevin J. Robbins, Carolyn Diane Dzierba, Rick L. Pieschl, Ramkumar Rajamani, James Herrington, Lorin A. Thompson, Andrea McClure, Yong-Jin Wu, Michele Matchett, Ronald J. Knox, Brian Lee Venables, Jason M. Guernon, Linda J. Bristow, Richard E. Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:958-962
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from m
Autor:
Umesh Hanumegowda, Sharon Zhang, Yan Chen, Zheng Liu, Ira B. Dicker, Zhufang Li, Sing-Yuen Sit, Ny Sin, Jacob Swidorski, Brian Terry, Himadri Samanta, Tricia Protack, Brian Lee Venables, Zeyu Lin, Yongnian Sun, Jie Chen, Beata Nowicka-Sans, Alicia Regueiro-Ren, Nicholas A. Meanwell, Matthew D. Healy, Mark Krystal, Mark I. Cockett
Publikováno v:
Antimicrobial Agents and Chemotherapy
BMS-955176 is a second-generation human immunodeficiency virus type 1 (HIV-1) maturation inhibitor (MI). A first-generation MI, bevirimat, showed clinical efficacy in early-phase studies, but ∼50% of subjects had viruses with reduced susceptibility
Autor:
Sing-Yuen Sit, Ny Sin, Umesh Hanumegowda, Dawn D. Parker, Zheng Liu, Alicia Regueiro-Ren, Xiaohua S. Huang, Brian Lee Venables, Brian Terry, Brett R. Beno, Sharon Zhang, Ira B. Dicker, Roy Haskell, Jacob Swidorski, Zhufang Li, Mark I. Cockett, Beata Nowicka-Sans, Zeyu Lin, Nicholas A. Meanwell, Tricia Protack, Sandhya Rahematpura, Juliang Zhu, Susan Jenkins, Himadri Samanta, Mark Krystal, Yan Chen, Kenneth S. Santone, Jie Chen
Publikováno v:
ACS Medicinal Chemistry Letters. 7:568-572
HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad polymorphic spectrum coverage and good oral exposure has been challenging. Herein, we describe
Autor:
Jacob Swidorski, Brian Lee Venables, Beata Nowicka-Sans, Sandhya Rahematpura, Zheng Liu, Ira B. Dicker, Jie Chen, Yan Chen, Brian Terry, Sing-Yuen Sit, Ny Sin, Umesh Hanumegowda, Tricia Protack, Susan Jenkins, Nicholas A. Meanwell, Dawn D. Parker, Alicia Regueiro-Ren, Mark Krystal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1925-1930
We have recently reported on the discovery of a C-3 benzoic acid (1) as a suitable replacement for the dimethyl succinate side chain of bevirimat (2), an HIV-1 maturation inhibitor that reached Phase II clinical trials before being discontinued. Rece
Autor:
Umesh Hanumegowda, Sandhya Rahematpura, Sing-Yuen Sit, Ny Sin, Mark Krystal, Yan Chen, Jacob Swidorski, Brian Terry, Dawn D. Parker, Alicia Regueiro-Ren, Zeyu Lin, Nicholas A. Meanwell, Brian Lee Venables, Beata Nowicka-Sans, Zhufang Li, Zheng Liu, Tricia Protack, Susan Jenkins, Ira D. Dicker, Jie Chen
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(9)
The design and synthesis of a series of C28 amine-based betulinic acid derivatives as HIV-1 maturation inhibitors is described. This series represents a continuation of efforts following on from previous studies of C-3 benzoic acid-substituted betuli
Autor:
Danshi Li, Herbert E. Klei, Sing-Yuen Sit, Piyasena Hewawasam, Ny Sin, Brian Lee Venables, Paul Levesque, Qi Gao, Bilder Donna M, Dennis M. Grasela, Dennis Hernandez, Anthony J. Cocuzza, Amy K. Sheaffer, Richard J. Colonno, Jeffrey Tredup, Kathy Mosure, Stanley D'andrea, Jialong Zhu, Lucy Sun, Fei Yu, Paul Falk, Alan Xiangdong Wang, Steven Levine, Fiona McPhee, Andrew C. Good, Huabin Sun, Jay O. Knipe, Barbara Zheng, Richard Schartman, Nicholas A. Meanwell, Jie Chen, Maria Donoso, James Loy, Guangzhi Zhai, Ramkumar Rajamani, Li-Qiang Sun, Stephen P. Adams, Luciano Mueller, Tatyana Zvyaga, Yong Tu, Hong Shi, Paul Michael Scola, Chaoqun Chen, William Warner, Yan Chen, Yong-Hae Han, Diana Barry, Jacques Friborg, Kevin Kish, Michael Sinz
Publikováno v:
Journal of Medicinal Chemistry. 57:1730-1752
The discovery of asunaprevir (BMS-650032, 24) is described. This tripeptidic acylsulfonamide inhibitor of the NS3/4A enzyme is currently in phase III clinical trials for the treatment of hepatitis C virus infection. The discovery of 24 was enabled by
Autor:
Alan Xiangdong Wang, Barbara Zheng, Min S. Lee, Dennis Hernandez, Andrew C. Good, Stanley D'andrea, Amy K. Sheaffer, Fiona McPhee, Christoph Gesenberg, Sing-Yuen Sit, Ny Sin, Paul Falk, Danshi Li, Piyasena Hewawasam, Yan Chen, Yong-Hae Han, Paul Levesque, Brian Lee Venables, Nicholas A. Meanwell, Michael Sinz, Wenying Li, Qi Gao, Li-Qiang Sun, Jay O. Knipe, Chaoqun Chen, Caly Chien, Diana Barry, Guangzhi Zhai, Anthony J. Cocuzza, Tatyana Zvyaga, Stephen P. Adams, Jialong Zhu, Fei Yu, Dennis M. Grasela, Richard J. Colonno, Yong Tu, Ramkumar Rajamani, Herbert E. Klei, Jianqing Li, Min Ding, Jan Willem Thuring, Jie Chen, Susan Jenkins, Keith D. Combrink, Jeffrey Allen Campbell, Kenneth S. Santone, Paul Michael Scola, Eric Hughes, Bilder Donna M
Publikováno v:
Journal of Medicinal Chemistry. 57:1708-1729
The discovery of BMS-605339 (35), a tripeptidic inhibitor of the NS3/4A enzyme, is described. This compound incorporates a cyclopropylacylsulfonamide moiety that was designed to improve the potency of carboxylic acid prototypes through the introducti
Autor:
Huabin Sun, Hua Fang, Richard Rampulla, Alan Xiangdong Wang, Bilder Donna M, Bang-Chi Chen, Zhao Qian, Chaoqun Chen, Brian Lee Venables, Fiona McPhee, Jie Chen, Maria Donoso, Barbara Zheng, Paul Falk, Ying-Kai Wang, Yan Chen, Nicholas A. Meanwell, Yong-Hae Han, Qi Gao, Richard Schartman, Luciano Mueller, Steven Levine, Herbert E. Klei, Jacques Friborg, Stephen P. Adams, Ramkumar Rajamani, Anthony J. Cocuzza, Theerthagiri Palani, Dennis M. Grasela, Dennis Hernandez, Fei Yu, Sivakumar Ganesan, James Loy, Tatyana Zvyaga, Paul Levesque, Li-Qiang Sun, Amy K. Sheaffer, Eric Mull, Arvind Mathur, Kathy Mosure, Jeffrey Tredup, Stanley D'andrea, Pirama Nayagam Arunachalam, Jialong Zhu, Mark I. Cockett, Hong Shi, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Jay O. Knipe, Alicia Ng, William Warner, Kevin Kish, Lucy Sun, Michael Sinz, Danshi Li
Publikováno v:
Journal of medicinal chemistry. 59(17)
The discovery of a back-up to the hepatitis C virus NS3 protease inhibitor asunaprevir (2) is described. The objective of this work was the identification of a drug with antiviral properties and toxicology parameters similar to 2, but with a preclini
Publikováno v:
Magnetic Resonance in Chemistry. 48:873-876
In this article, we describe the characteristic (15)N chemical shifts of isatin oxime ethers and their isomer nitrone. These oxime ethers and nitrones are the alkylation reaction products of isatin oximes. In our study, the (15)N chemical shifts obse