Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: Orally efficacious antiobesity therapeutics

被引:75
作者
McBriar, MD [1 ]
Guzik, H [1 ]
Xu, R [1 ]
Paruchova, J [1 ]
Li, SJ [1 ]
Palani, A [1 ]
Clader, JW [1 ]
Greenlee, WJ [1 ]
Hawes, BE [1 ]
Kowalski, TJ [1 ]
O'Neill, K [1 ]
Spar, B [1 ]
Weig, B [1 ]
机构
[1] Schering Plough Corp, Inst Res, Kenilworth, NJ 07033 USA
关键词
D O I
10.1021/jm049035q
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Melanin concentrating hormone (MCH) is involved in regulation of food intake and energy homeostasis. Antagonists of the MCH receptor are expected to affect food intake and weight gain, making MCH-R1 an attractive target for obesity treatment. Herein, we report the discovery of a novel, orally active series of MCH-R1 antagonists that exhibit in vivo efficacy in rodent obesity models.
引用
收藏
页码:2274 / 2277
页数:4
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