Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Isao Sakurada"'
Autor:
Daniel P. Walker, Antonia F. Stepan, Mark A. Moen, Gregg D. Cappon, Christopher Houle, Annie C Won, Joshua R. Dunetz, Michael John Bohanon, Lei Zhang, Marc B. Skaddan, Patrick Robert Verhoest, Susan E. Drozda, Xinjun Hou, Kenneth R. Zasadny, Julie Cianfrogna, Deborah L. Smith, Ann S. Wright, John T. Lazzaro, Steven Victor O'neil, Patrick Trapa, Emily Miller, Somraj Ghosh, Gabriela Barreiro, John M. Marcek, Margaret M. Zaleska, Jason Barricklow, Michelle Marie Claffey, Lois K. Chenard, Jessica Mancuso, Christopher L. Shaffer, Jessica Whritenour, Gayatri Balan, Brian P. Boscoe, Vinod D. Parikh, Karen J. Coffman, Laigao Chen, Isao Sakurada, Jamison B. Tuttle, Matthew R. Reese, Karki Kapil Kumar
Publikováno v:
Journal of Medicinal Chemistry. 60:7764-7780
We previously observed a cutaneous type IV immune response in nonhuman primates (NHP) with the mGlu5 negative allosteric modulator (NAM) 7. To determine if this adverse event was chemotype- or mechanism-based, we evaluated a distinct series of mGlu5
Autor:
Harold B. Wood, Kunal Desai, Daming Feng, Jamie McCabe-Dunn, Yi-Heng Chen, Edward C. Sherer, Jane Y. Wu, Marc Poirier, Hong Li, Dongfang Meng, Ting Zhang, Kenneth P. Ellsworth, Liangqin Guo, Teruyuki Nishimura, Jiayi Xu, Tomokazu Hirabayashi, Sunita V. Dewnani, Patrick Andre, Louis-Charles Campeau, Richard Tschirret-Guth, Isao Sakurada, Paul Reichert, Cameron J. Smith, Robert K. Orr, Lisa M. Sonatore, Wayne M. Geissler, Thomas Bateman, Kazuto Araki, Joe Metzger, Alan Hruza, Richard A. Berger, Dann L. Parker, Tianying Jian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5437-5443
Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) s
Autor:
Isao Sakurada
Publikováno v:
Tetrahedron Letters. 58:3188-3190
Facile synthetic routes to bromo- and iodo-1,2,3-triazoles were achieved. Diiodo-1,2,3-triazole was directly obtained from 1,2,3-triazole, and dihalo-1,2,3-triazoles were converted to halo-1,2,3-triazoles in good yields without protection by NH. Unsy
Autor:
Patrick Robert Verhoest, Susan E. Drozda, Kenneth R. Zasadny, Emily Miller, Lei Zhang, Kari R. Fonseca, Gabriela Barreiro, Patrick Trapa, Michelle Marie Claffey, Julie Cianfrogna, Marc B. Skaddan, Deborah L. Smith, Margaret M. Zaleska, Joshua R. Dunetz, Christopher L. Shaffer, Jessica Mancuso, Isao Sakurada, Gayatri Balan, Jamison B. Tuttle, Lois K. Chenard, Bruce N. Rogers, Matthew R. Reese, Antonia F. Stepan, Paul Galatsis, Brian P. Boscoe, Daniel P. Walker, Sarah Grimwood, Ann S. Wright, John T. Lazzaro, Karen J. Coffman, Laigao Chen
Publikováno v:
Journal of Medicinal Chemistry. 57:861-877
A novel series of pyrazolopyrazines is herein disclosed as mGluR5 negative allosteric modulators (NAMs). Starting from a high-throughput screen (HTS) hit (1), a systematic structure-activity relationship (SAR) study was conducted with a specific focu
Autor:
Harold B. Wood, Shunsuke Shimada, Hiroshi Nagasue, Takashi Mizuno, Tomokazu Hirabayashi, Toshiya Endo, Shigeki Matsumoto, Yutaka Kato, Shoji Furusako, Katsuyoshi Hikita, Ting Zhang, Keiko Taguchi, Yoshitaka Maeda, Kazunari Nakao, Alan Hruza, Paul Reichert, Isao Sakurada, Teruyuki Nishimura, Tooru Yokoyama, Yoshitaka Hosaka, Mikihiko Shinozaki, Katsutoshi Takeuchi
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(11)
Using structure based drug design, novel aminobenzisoxazoles as coagulation factor IXa inhibitors were designed and synthesized. Highly selective inhibition of FIXa over FXa was demonstrated. Anticoagulation profile of selected compounds was evaluate
Autor:
Miyako Matsumizu, Hirohisa Shimokawa, Makoto Kawai, Hirotaka Tanaka, Hiroshi Nakamura, Mitsuhiro Kawamura, Ando Kazuo, Isao Sakurada, Kazunari Hattori, Seiji Nukui, Atsuko Ohta, Atsushi Omura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5533-5536
Novel NR2B antagonists with an amide tether were found by an approach to avoid pharmacophoric similarity to dofetilide. Structure–activity relationship investigation led to N-[cis-4-hydroxy-4-(5-hydroxypyridin-2-yl)cyclohexyl]-3-henylpropanamide 14
Autor:
Edward C. Sherer, Robert K. Orr, Wayne M. Geissler, Kazuto Araki, Thomas Bateman, Ting Zhang, Xiaoxia Qian, Kenneth P. Ellsworth, Teruyuki Nishimura, Andrew Nolting, Patrick Andre, Yi-Heng Chen, Paul Reichert, Kunal Desai, Harold B. Wood, Liangqin Guo, Dann L. Parker, Dongfang Meng, Cameron J. Smith, Lisa M. Sonatore, Tianying Jian, Richard Tschirret-Guth, Alan Hruza, Min Shu, Louis-Charles Campeau, Isao Sakurada
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(21)
Using structure based drug design (SBDD), a novel class of potent coagulation Factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds demonstrated oral bioavailability in rat IV
Publikováno v:
Tetrahedron Letters. 41:2415-2418
We have succeeded in developing direct syntheses of trans β-azidohydrins and trans 1,2-diol derivatives from olefins catalyzed by dichlorotin oxide. The regioselectivity of these reactions with tri-substituted olefins is high (10:1 in the synthesis
Autor:
Takehiko Iida, Motomu Kanai, Shingo Yamasaki, Richard Goettlich, Isao Sakurada, Masakatsu Shibasaki
Publikováno v:
ChemInform. 31
Publikováno v:
ChemInform. 31
We have succeeded in developing direct syntheses of trans β-azidohydrins and trans 1,2-diol derivatives from olefins catalyzed by dichlorotin oxide. The regioselectivity of these reactions with tri-substituted olefins is high (10:1 in the synthesis