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. 2008 Nov 1;16(21):9524-35.
doi: 10.1016/j.bmc.2008.09.039. Epub 2008 Sep 17.

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

Issei Tsukamoto  1 , Hiroyuki Koshio, Seijiro Akamatsu, Takahiro Kuramochi, Chikashi Saitoh, Takeyuki Yatsu, Hiroko Yanai-Inamura, Chika Kitada, Eisaku Yamamoto, Shuichi Sakamoto, Shin-Ichi Tsukamoto
Affiliations

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

Issei Tsukamoto et al. Bioorg Med Chem. .

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.

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