- Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V2 receptor agonists
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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) V2 receptor agonists. By replacing the amide juncture in YM-35278 with a direct ring connection gave compound 10a, which acts as a V2 receptor agonist. These studies provided the potent, orally active non-peptidic V2 receptor agonists 10a and 10j.
- Tsukamoto, Issei,Koshio, Hiroyuki,Akamatsu, Seijiro,Kuramochi, Takahiro,Saitoh, Chikashi,Yatsu, Takeyuki,Yanai-Inamura, Hiroko,Kitada, Chika,Yamamoto, Eisaku,Sakamoto, Shuichi,Tsukamoto, Shin-ichi
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experimental part
p. 9524 - 9535
(2009/04/05)
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- 4,4-DIFLUORO-1,2,3,4-TETRAHYDRO-5H-1-BENZAZEPINE DERIVATIVES OR SALTS THEREOF
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4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives, which have excellent arginine vasopressin V2 activity and are useful for a drug for the treatment of central diabetes insipidus and/or nocturia.
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- Novel design of nonpeptide AVP V2 receptor agonists: Structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepine as a template
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The discovery of a series of nonpeptide arginine vasopressin V2 receptor agonists is described. After identifying the aniline derivative 8 as our lead compound from the metabolites of compound 7 that showed antidiuretic activity by po administr
- Kondo,Ogawa,Shinohara,Kurimura,Tanada,Kan,Yamashita,Nakamura,Hirano,Yamamura,Mori,Tominaga,Itai
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p. 4388 - 4397
(2007/10/03)
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