168162-46-7

Upstream product

• 14002-52-9 o-phenylbenzoyl chloride 
• 168164-00-9 (E)-methyl [1-(4-aminobenzoyl)-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzo-azepine-5-ylidene]acetate 
• 947-84-2 2-Biphenylcarboxylic acid 
• 79-37-8 oxalyl dichloride 
• 168163-96-0 4,4-difluoro-1-(4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-one 
• 168163-92-6 4,4-difluoro-1-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-5H-1-benzoazepin-5-one 
• 168163-97-1 1-(4-aminobenzoyl)-4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-one 
• 168163-93-7 4-fluoro-1-(p-toluenesulfonyl)-1,2,3,4-tetrahydro-5H-1-benzoazepin-5-one 
• 168163-95-9 4,4-difluoro-1,2,3,4-tetrahydro-benzo[b]azepin-5-one 
• 24310-36-9 1-tosyl-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one 

Downstream Products

• 168162-52-5 (E)-{4,4-difluoro-1-[4-(2-phenylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-1-benzoazepine-5-ylidene}acetic acid 

Relevant academic research and scientific papers

Highly potent and orally active non-peptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 4'-[(4,4,-difluoro-5-methylidene-2,3,4,5-tetrahydro-1H-1-benzoazepin-1-yl)car bonyl]-2-phenylbenzanilide derivatives

A series of compounds structurally related to 4'-[(4,4-difluoro-5-methylidene-2,3,4,5-tetrahydro-1H-1-benzoazepin-1-yl)carb onyl]-2-phenylbenzanilide were synthesized and evaluated for arginine vasopressin (AVP) antagonistic activity. Compounds with a (Z)-olefin geometry at the 5-position of benzoazepine possessed potent affinity for both the V(1A) and V2 receptors. Further study has shown that one of these derivatives, (Z)-4'-({4,4-difluoro-5-[(4-dimethylaminopiperidino)carbonylmethylene]-2,3,4 ,5-tetrahydro-1H-1-benzoazepin-1-yl}carbonyl)-2-phenylbenzanilide monohydrochloride (29, YM-35471), exhibits exceptionally potent affinity for both of V(1A) and V2 receptors, even when administered orally. The synthesis and pharmacological properties of this compound are detailed in this paper.

Benzazepine derivative, pharmaceutical composition thereof, and intermediate thereof

Benzazepine derivatives represented by the following general formula (I) useful as arginine vasopressin antagonists or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and difluorobenzazepinone derivatives represented by the following general formulae (II) and (III) which are useful as production intermediates of the compound (I). STR1