Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Owen B, Wallace"'
Autor:
Nicholas A, Meanwell, Owen B, Wallace, Haiquan, Fang, Henry, Wang, Milind, Deshpande, Tao, Wang, Zhiwei, Yin, Zhongxing, Zhang, Bradley C, Pearce, Jennifer, James, Kap-Sun, Yeung, Zhilei, Qiu, J J, Kim Wright, Zheng, Yang, Lisa, Zadjura, Donald L, Tweedie, Suresh, Yeola, Fang, Zhao, Sunanda, Ranadive, Brett A, Robinson, Yi-Fei, Gong, Hwei-Gene Heidi, Wang, Timothy P, Spicer, Wade S, Blair, Pei-Yong, Shi, Richard J, Colonno, Pin-Fang, Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1977-1981
The effects of introducing simple halogen, alkyl, and alkoxy substituents to the 4, 5, 6 and 7 positions of 1-(4-benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione, an inhibitor of the interaction between HIV gp120 and host cell CD4 receptors,
Autor:
Samuel W. Oldham, Hongqi Tian, Ilene R. Cohen, Ronald Jay Hinklin, Jeffrey Alan Dodge, Timothy Ivo Richardson, Christian Alexander Clarke, Bai-Ping Ying, Kin Chiu Fong, Daniel G. Rudmann, Minmin Wang, Daniel Timothy Kohlman, Owen B. Wallace, Denis J. McCann, George Sal Lewis, Alan David Palkowitz, David E. Coutant, Andrew G. Geiser, Robert Dean Dally, Conrad Wilson Hummel, Henry Uhlman Bryant, Timothy Alan Shepherd, Judith W. Henck, Scott Alan Jones, Scott Alan Frank
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3544-3549
Structure–activity relationship studies are described, which led to the discovery of novel selective estrogen receptor modulators (SERMs) for the potential treatment of uterine fibroids. The SAR studies focused on limiting brain exposure and were g
Autor:
Garry Pairaudeau, William Pennie, Sam Mandrell, Robert M. Owen, John Arrowsmith, Jibo Wang, Owen B. Wallace, Andrew R. Leach, Alex Weir, Paul D. Leeson, Michael J. Waring, Stephen D. Pickett
Publikováno v:
Nature reviews. Drug discovery. 14(7)
The pharmaceutical industry remains under huge pressure to address the high attrition rates in drug development. Attempts to reduce the number of efficacy- and safety-related failures by analysing possible links to the physicochemical properties of s
Autor:
Thomas P. Burris, Owen B. Wallace, Jeffrey Alan Dodge, Joel R. Calvin, Scott A. May, Kenneth S Lauwers, Andrew G. Geiser, Ronald Jay Hinklin, Pamela K. Shetler, Mary D. Adrian, Masahiko Sato, Henry Uhlman Bryant
Publikováno v:
Journal of Medicinal Chemistry. 49:843-846
A selective estrogen receptor modulator (SERM) for the potential treatment of hot flushes is described. (R)-(+)-7,9-difluoro-5-[4-(2-piperidin-1-ylethoxy)phenyl]-5H-6-oxachrysen-2-ol, LSN2120310, potently binds ERalpha and ERbeta and is an antagonist
Autor:
George Sal Lewis, Andrew G. Geiser, Ilene R. Cohen, Kin Chiu Fong, Minmin Wang, Owen B. Wallace, Robert Dean Dally, Yong Wang, Timothy Alan Shepherd, Denis J. McCann, Jeffrey Alan Dodge, Conrad Wilson Hummel, Scott Alan Jones, Ronald Jay Hinklin, Daniel G. Rudmann, Hongqi Tian, Scott Alan Frank, Henry Uhlman Bryant
Publikováno v:
Journal of Medicinal Chemistry. 48:6772-6775
The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and beta (ERalpha and ERbeta, respectively) and
Autor:
Andrew G. Geiser, Draper Michael William, Mary D. Adrian, Denis J. McCann, Owen B. Wallace, Judith W. Henck, Kevin B. Donnelly, Conrad Wilson Hummel, Jeffrey Alan Dodge, Henry Uhlman Bryant, Ilene R. Cohen, Masahiko Sato, Timothy Alan Shepherd, Daniel G. Rudmann, Samuel W. Oldham
Publikováno v:
Endocrinology. 146:4524-4535
The use of selective estrogen receptor modulators for the treatment of estrogen-dependent diseases in premenopausal women has been hindered by undesirable ovarian stimulation and associated risks of ovarian cysts. We have identified a selective estro
Autor:
Frederick E. Ziegler, Owen B. Wallace
Publikováno v:
The Journal of Organic Chemistry. 60:3626-3636
Autor:
Nicholas A, Meanwell, Owen B, Wallace, Henry, Wang, Milind, Deshpande, Bradley C, Pearce, Ashok, Trehan, Kap-Sun, Yeung, Zhilei, Qiu, J J Kim, Wright, Brett A, Robinson, Yi-Fei, Gong, Hwei-Gene Heidi, Wang, Timothy P, Spicer, Wade S, Blair, Pei-Yong, Shi, Pin-fang, Lin
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(17)
1-(4-Benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1a) has been characterized as an inhibitor of HIV-1 attachment that interferes with the interaction of viral gp120 with the host cell receptor CD4. In previous studies, the effect of indo
Publikováno v:
ChemInform. 36
For selective estrogen receptor modulators (SERMs), the orientation of the basic side chain relative to the SERM core has a significant impact on function. The synthesis and biological evaluation of two series of SERMs are disclosed, where the ligand
Autor:
C V C, Prasad, Owen B, Wallace, Jeffrey W, Noonan, Charles P, Sloan, Wai, Lau, Shikha, Vig, Michael F, Parker, David W, Smith, Steven B, Hansel, Craig T, Polson, Donna M, Barten, Kevin M, Felsenstein, Susan B, Roberts
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(8)
Using a cell-based assay, we have identified optimal residues and key recognition elements necessary for inhibition of gamma-secretase. An (S)-hydroxy group or 3,5-difluorophenylacetyl group at the amino terminus and N-methyltertiary amide moiety at