基本信息:
- 专利标题： PYRIDINE DERIVATIVES
- 申请号：US15532772 申请日：2015-12-04
- 公开(公告)号：US20170362209A1 公开(公告)日：2017-12-21
- 发明人： Kenichi KAWAGUCHI , Akihiro ISHIHATA , Akira KANAI , Kazuyuki TSUCHIYA , Yusuke INAGAKI , Junichi KAZAMI , Hiroshi MORIKAWA , Masashi HIRAMOTO , Kentaro ENJO , Hajime TAKAMATSU
- 申请人： Astellas Pharma Inc. , KOTOBUKI PHARMACEUTICAL CO., LTD.
- 申请人地址： JP Chuo-ku JP Hanishina-gun
- 专利权人： Astellas Pharma Inc.,KOTOBUKI PHARMACEUTICAL CO., LTD.
- 当前专利权人： Astellas Pharma Inc.,KOTOBUKI PHARMACEUTICAL CO., LTD.
- 当前专利权人地址： JP Chuo-ku JP Hanishina-gun
- 优先权： JP2014-246463 20141205
- 国际申请： PCT/JP2015/084098 WO 20151204
- 主分类号： C07D405/04
- IPC分类号： C07D405/04 ; C07D221/20 ; C07D221/04 ; C07D217/24 ; C07D217/16 ; C07D401/04 ; C07D213/55
摘要：
The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia.The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.
公开/授权文献:
- US10005762B2 Pyridine derivatives 公开/授权日：2018-06-26
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07D | 杂环化合物 |
| ------C07D405/00 | 杂环化合物，含有1个或多个以氧原子作为仅有的杂环原子的环，且含有1个或多个以氮原子作为仅有的杂环原子的环 |
| --------C07D405/02 | .含有两个杂环 |
| ----------C07D405/04 | ..被环原子—环原子的键直接连接的 |