Potent, selective MCH-1 receptor antagonists

被引:8
|
作者
Erickson, Shawn D. [1 ]
Banner, Bruce [1 ]
Berthel, Steven [1 ]
Conde-Knape, Karin [2 ]
Falcioni, Fiorenza [2 ]
Hakimi, Irina [2 ]
Hennessy, Bernard [1 ]
Kester, Robert F. [1 ]
Kim, Kyungjin [1 ]
Ma, Chun [1 ]
McComas, Warren [1 ]
Mennona, Francis [1 ]
Mischke, Steven [1 ]
Orzechowski, Lucy [1 ]
Qian, Yimin [1 ]
Salari, Hamid [1 ]
Tengi, John [1 ]
Thakkar, Kshitij [1 ]
Taub, Rebecca [2 ]
Tilley, Jefferson W. [1 ]
Wang, Hong [1 ]
机构
[1] Hoffmann La Roche Inc, Discovery Chem, Nutley, NJ 07110 USA
[2] Hoffmann La Roche Inc, Dept Metab Dis, Nutley, NJ 07110 USA
关键词
D O I
10.1016/j.bmcl.2008.01.010
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity pro. le appropriate for in vivo efficacy studies and safety. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1402 / 1406
页数:5
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