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Bioorg Med Chem. 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.

Author information

1
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.

PMID:
18835174
DOI:
10.1016/j.bmc.2008.09.039
[Indexed for MEDLINE]

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