Zobrazeno 1 - 10
of 36
pro vyhledávání: '"George A. Moniz"'
Autor:
Kevin L. Otipoby, Sarah Sheikh, Douglas Marcotte, George A. Moniz, Michael Humora, Brian T. Hopkins, Judy Bai, Karen Smirnakis, J. Michael Macphee, Tonika Bohnert, Timothy R. Chan, Devangi Mehta, Bin Ma, Million Arefayene, Zheng Fengmei, Lei Zhang, Patricia Schroeder, Annick Prefontaine, Eris Bame, Urjana Poreci, Evelyne Polack, Eric Tien, Claire M. Metrick, Bekim Bajrami
Publikováno v:
Journal of Medicinal Chemistry. 63:12526-12541
Autoreactive B cell-derived antibodies form immune complexes that likely play a pathogenic role in autoimmune diseases. In systemic lupus erythematosus (SLE), these antibodies bind Fc receptors on myeloid cells and induce proinflammatory cytokine pro
Autor:
Chaomin Li, Yiqing Lin, John Guzowski, Lloyd Franklin, Brian T. Hopkins, Michael MacPhee, Daniel Patience, Bin Ma, Zheng Fengmei, Michael Humora, Robbie Chen, Erin M. O’Brien, George A. Moniz, William F. Kiesman, Steven Ferguson, Tamera Mack
Publikováno v:
Organic Process Research & Development. 24:1199-1206
Chemical process development efforts leading to multikilogram production of BIIB068 hemiadipate are discussed. Process optimization resulted in (1) removal of transition metal from the process, (2)...
Autor:
Francis G. Fang, Kazuhiro Yoshizawa, Atsushi Kamada, Taiju Nakamura, Masaaki Matsuda, Katsuya Tagami, Nobuaki Sato, Takeo Sasaki, Yongbo Hu, George A. Moniz, Minetaka Isomura, Yoshihiro Nishikawa, Gordon D. Wilkie, Daiju Hasegawa, Yorihisa Hoshino, Kazato Inanaga, Toshiyuki Uemura
Publikováno v:
Organic Process Research & Development. 23:603-613
Process studies of E2212 (1) toward rapid clinical introduction are described. Through comprehensive route-finding studies and optimization of key condensation and cyclization steps, a racemate-based manufacturing route was established and successful
Autor:
Kenichi Nomoto, Kuan-Chun Huang, Donna Kolber-Simonds, Natalie C. Twine, George A. Moniz, Paul Chang, Jue-lon Shie, Jingzang Tao Miu, Karen Ackermann, Zhihong Chen, Sharon McGonigle, Jiayi Wu
Publikováno v:
Oncotarget
Impact Journals/National Center for Biotechnology Information (U.S.)
Impact Journals/National Center for Biotechnology Information (U.S.)
Inhibition of Poly(ADP-ribose) Polymerase1 (PARP1) impairs DNA damage repair, and early generation PARP1/2 inhibitors (olaparib, niraparib, etc.) have demonstrated clinical proof of concept for cancer treatment. Here, we describe the development of t
Autor:
Steven Mathieu, George A. Moniz
Publikováno v:
Tetrahedron Letters. 55:5855-5858
A bromination process has been developed using a salt-based brominating reagent and a non-chlorinated solvent system. The process affords enhanced selectivity and enables product isolation by simple filtration of the reaction mixture, resulting in a
Cope elimination mediated by human FMO1 leads to formation of reactive Michael Acceptor intermediate
Publikováno v:
Drug Metabolism and Pharmacokinetics. 34:S58
Publikováno v:
Tetrahedron Letters. 52:5613-5616
The diastereoselective alkylation of a series of 5-alkyl-2-aminothiazolones utilizing a C 2 -symmetric chiral tetraamine base is reported.
Publikováno v:
Drug Metabolism and Disposition. 39:61-70
10-((4-Hydroxypiperidin-1-yl)methyl)chromeno[4,3,2-de]phthalazin-3(2H)-one (E7016), an inhibitor of poly(ADP-ribose) polymerase, is being developed for anticancer therapy. One of the major metabolites identified in preclinical animal studies was the
Autor:
Clarence Hale, Martin Henriksson, Randall W. Hungate, Renee Komorowski, Kyung H. Gahm, Jiandong Zhang, Murielle M. Véniant, Janan Jona, Vivian S. W. Li, Andrew Hague, Maurice Emery, Christopher H. Fotsch, Steven R. Jordan, Smriti Joseph, David J. St. Jean, Lars Johansson, Minghan Wang, Rashid Syed, Jeffrey Adams, George A. Moniz, Rod Cupples, Ki Won Kim, Michael D. Bartberger, Jerk Vallgarda, Michelle Chen, Meredith Williams
Publikováno v:
Journal of Medicinal Chemistry. 53:4481-4487
Thiazolones with an exo-norbornylamine at the 2-position and an isopropyl group on the 5-position are potent 11beta-HSD1 inhibitors. However, the C-5 center was prone to epimerization in vitro and in vivo, forming a less potent diastereomer. A methyl
Publikováno v:
Chirality. 22:50-55
The separation of R,R-, S,S-, and meso-Koga bases on derivatized amylose chiral stationary phases (CSP) has been studied using different alcohol and alcohol-hexane mixtures as eluant. Straight-chain and branched alcohols with carbon numbers from one