期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 10, 页码 3437-3440出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.104
关键词
Cariprazine; RGH-188; Dopamine D-3 and D-2 ligands; Antipsychotic; Chloro-scan
Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D-3/D-2 compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D-3 and D-2 receptors. Several members of this group showed excellent pharmacokinetic and pharmacodynamic properties as demonstrated by outstanding activities in different antipsychotic tests. The most promising representative, 2m (cariprazine) had good absorption, excellent brain penetration and advantageous safety profile. Based on its successful clinical development we are looking forward to the NDA filing of cariprazine in 2012. (C) 2012 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据