Effect of Cathepsin K Inhibitors on Bone Resorption

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• 作者：Naoki Teno ; Keiichi Masuya ; Takeru Ehara ; Takatoshi Kosaka ; Takahiro Miyake ; Osamu Irie ; Yuko Hitomi ; Naoko Matsuura ; Ichiro Umemura ; Genji Iwasaki ; Hiroaki Fukaya ; Kazuhiro Toriyama ; Noriko Uchiyama
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：September 11, 2008
• 年：2008
• 卷：51
• 期：17
• 页码：5459-5462
• 全文大小：115K
• 年卷期：v.51,no.17(September 11, 2008)
• ISSN：1520-4804

文摘

On the basis of the pyrrolopyrimidine core structure that was previously discovered, cathepsin K inhibitors having a spiro amine at the P3 have been explored to enhance the target, bone marrow, tissue distribution. Several spiro structures were identified with improved distribution toward bone marrow. The representative inhibitor 7 of this series revealed in vivo reduction in C-terminal telopeptide of type I collagen in rats and monkeys.