发明名称 |
Benzazepine derivatives useful as vasopressin antagonists |
摘要 |
The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1);
wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like. |
申请公布号 |
US8785386(B2) |
申请公布日期 |
2014.07.22 |
申请号 |
US201314034943 |
申请日期 |
2013.09.24 |
申请人 |
Otsuka Pharmaceutical Co., Ltd. |
发明人 |
Kondo Kazumi;Menjo Yasuhiro;Tomoyasu Takahiro;Miyamura Shin;Tomohira Yuso;Matsuda Takakuni;Yamada Keigo;Kato Yusuke |
分类号 |
A61K38/00;C07D223/16 |
主分类号 |
A61K38/00 |
代理机构 |
Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P. |
代理人 |
Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P. |
主权项 |
1. A benzazepine compound represented by general formula (1)wherein R1 is a group of (1-1):
(1-1) a —CO—(CH2)n—COR2 group wherein n is an integer of 1 to 4, R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group; or a salt thereof. |
地址 |
Osaka JP |