- Discovery of 1-{4[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyrida zin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl ]-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor
[作者:MIWA KAZUHIRO; HITAKA TAKENORI; IMADA TAKASHI; SASAKI SATOSHI; YOSHIMATSU MIE; KUSAKA MASAMI; TANAKA AKIRA; NAKATA DAISUKE; FURUYA SHUICHI; ENDO SATOSHI; HAMAMURA KAZUMASA; KITAZAKI TOMOYUKI,期刊:Journal of Medicinal Chemistry, 页码:4998-5012 , 文章类型: Article,,卷期:2011年54-14]
- We previously discovered an orally active human gonadotropin-releasing hormone (GnRH) receptor antagonist, thieno[2,3-d] Pyrimidine-2,4-dione derivative 1 (sufugolix). To reduce the cytochrome P450 (CYP) inhibitory activ...
- Imidazolopiperazines: Hit to Lead Optimization of New Antimalarial Agents
[作者:WU TAO; NAGLE ADVAIT; KUHEN KELLI; GAGARING KERSTIN; BORBOA RACHEL; FRANCEK CAROLINE; CHEN ZHONG; PLOUFFE DAVID; GOH ANNE; LAKSHMINARAYANA SURESH B; WU JEANETTE; ANG HUI QING; ZENG PEITING; KANG MIN LOW; TAN WILLIAM; TAN MARIA; YE NICOLE; LIN XUENA; CALDWELL CHRISTOPHER; EK JARED; SKOLNIK SUZANNE; LIU FENGHUA; WANG JIANLING; CHANG JONATHAN; LI CHUN; HOLLENBECK THOMAS; TUNTLAND TOVE; ISBELL JOHN; FISCHLI CHRISTOPH; BRUN RETO; ROTTMANN MATTHIAS; DARTOIS VERONIQUE; KELLER THOMAS; DIAGANA THIERRY; WINZELER ELIZABETH; GLYNNE RICHARD; TULLY DAVID C; CHATTERJEE ARNAB K,期刊:Journal of Medicinal Chemistry, 页码:5116-5130 , 文章类型: Article,,卷期:2011年54-14]
- Starting from a hit series from a GNF compound library collection and based on a cell-based proliferation assay of Plasmodium falciparum, a novel imidazolopiperazine scaffold was optimized. SAR for this series of compoun...
- Selectivity of Kinase Inhibitor Fragments
[作者:BAMBOROUGH PAUL; BROWN MURRAY J; CHRISTOPHER JOHN A; CHUNG CHUNWA; MELLOR GEOFF W,期刊:Journal of Medicinal Chemistry, 页码:5131-5143 , 文章类型: Article,,卷期:2011年54-14]
- A kinase-focused screening set of fragments has been assembled and has proved successful for the discovery of ligand-efficient hits against many targets. Here we present some of our general conclusions from this exercise...
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