公开(公告)号：US20070037841A1

公开(公告)日：2007-02-15

申请号：US10547234

申请日：2004-02-26

Applicant: Kazuhiko Nakatani ,  Souta Horie ,  Isao Saito ,  Shinya Hagihara ,  Yuki Goto ,  Akio Kobori

Inventor： Kazuhiko Nakatani ,  Souta Horie ,  Isao Saito ,  Shinya Hagihara ,  Yuki Goto ,  Akio Kobori

IPC: A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: An inhibitor contains naphthyridine dimer, a naphthyridine-azaquinolone hybrid, a trinaphthyridine-azaquinolone hybrid, or a trinaphthyridine-azaquinolone hybrid derivative. In order to inhibit binding of 100 nM of RRE to 100 nM of Rev protein, for example, an inhibitor containing naphthyridine dimer is used at a molarity of 1.2 μM to 12 μM, an inhibitor containing the naphthyridine-azaquinolone hybrid is used at a molarity of 2 μM to 20 μM, or an inhibitor containing the trinaphthyridine-azaquinolone hybrid derivative is used at a molarity of 200 nM to 2 μM. This makes it possible to effectively inhibit binding of RRE to Rev protein.

Abstract translation: 抑制剂含有萘啶二聚体，萘啶 - 氮杂喹诺酮杂环，三萘啶 - 氮杂喹诺酮杂环或三萘并氮杂喹啉酮杂合衍生物。 为了抑制100nM的RRE与100nM的Rev蛋白的结合，例如，使用含有萘啶二聚体的抑制剂，摩尔浓度为1.2μM至12μM，含有萘啶 - 氮杂喹诺酮杂化物的抑制剂的摩尔浓度 或者含有三萘并氮杂喹啉酮杂化衍生物的抑制剂的摩尔浓度为200nM至2μM。 这使得有可能有​​效地抑制RRE与Rev蛋白的结合。