Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists |
| |
| Authors: | Tsukamoto Issei Koshio Hiroyuki Akamatsu Seijiro Kuramochi Takahiro Saitoh Chikashi Yatsu Takeyuki Yanai-Inamura Hiroko Kitada Chika Yamamoto Eisaku Sakamoto Shuichi Tsukamoto Shin-Ichi |
| |
| Institution: | Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan. issei.tsukamoto@jp.astellas.com |
| |
| Abstract: | The present work describes the discovery of novel series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)acetamide derivatives as arginine vasopressin (AVP) V(2) receptor agonists. By replacing the amide juncture in YM-35278 with a direct ring connection gave compound 10a, which acts as a V(2) receptor agonist. These studies provided the potent, orally active non-peptidic V(2) receptor agonists 10a and 10j. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
