86499-52-7

Usage

Chemical Properties

Off-white Solid

Uses

Intermediate in the preparation of benzazepinone based mercaptoacetyls inhibitors.

Upstream product

• 92278-69-8 ethyl 3-azido-2,3,4,5-tetrahydro-1H-<1>benzazepin-2-one-1-acetate 
• 97278-68-7 3-azido-2,3,4,5-tetrahydro-2-oxo-1 H-1-benzazepine 
• 86499-23-2 3-chloro-2,3,4,5-tetrahydro-1H-<1>benzazepin-2-one 
• 86499-22-1 3,3-dichloro-2,3,4,5-tetrahydro-1H-<1>benzazepin-2-one 
• 4424-80-0 2,3,4,5-tetrahydro-1H-1-benzo[b]azepin-2-one 
• 94793-89-2 3-(S)-amino-1-ethoxycarbonylmethyl-2,3,4,5-tetrahydro-1H-[1]benzazepine-2-one 

Downstream Products

• 160134-52-1 [S-(R*,R*)]-2,3,4,5-Tetrahydro-3-[[2-[(acetylthio)methyl]-1-oxo-3-phenylpropyl]amino]-2-oxo-1H-benzazepine-1-acetic acid, ethyl ester 
• 103129-58-4 1-ethoxycarbonylmethyl-3S-(1S-ethoxycarbonyl-3-phenylpropylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-one 
• 197903-05-2 {(S)-3-[(R)-2-(Benzyloxyamino-methyl)-3-phenyl-propionylamino]-2-oxo-2,3,4,5-tetrahydro-benzo[b]azepin-1-yl}-acetic acid ethyl ester 
• 86541-77-7 (3S)-1-(carboxymethyl)-<<(1S)-1-(ethoxycarbonyl)-3-phenylpropyl>amino>-2,3,4,5-tetrahydro-1H-<1>benzazepin-2-one hydrochloride 
• 86541-78-8 (3S)-1-(carboxymethyl)-<<(1S)-1-carboxy-3-phenylpropyl>amino>-2,3,4,5-tetrahydro-1H-<1>benzazepin-2-one 
• 86541-74-4 benazepril hydrochloride 

Relevant academic research and scientific papers

N-formyl hydroxylamine containing compounds useful as ACE inhibitors and/or NEP inhibitors

N-formyl hydroxylamines are provided which have the structure wherein R is H, alkyl, alkenyl, aryl-(CH2)p—, heteroaryl-(CH2)p— or cycloheteroalkyl-(CH2)p— R1is H or COR2where R2is alkyl, aryl-(CH2)p—, cycloheteroalkyl-(CH2)p—, heteroaryl-(CH2)p—, alkoxy or cycloalkyl-(CH2)p—, p is 0 to 8, and A is a dipeptide derived from an amino acid or is a conformationally restricted dipeptide mimic. The above compounds are useful in treating hypertension congestive heart failure, renal failure, and hepatic cirrhosis.

Phosphonic acid-substituted benzazepinone-n-acetic acid derivatives process for their preparation and pharmaceutical compositions comprising them

Compounds having NEP-inhibitory activity, corresponding to the formula I in whichR 1 is hydrogen or a group forming a biolabile phosphonic acid ester,R 2 is hydrogen or a group forming a biolabile phosphonic acid ester and R. sup.3 is hydrogen or a group forming a biolabile carboxylic acid esterand physiologically acceptable salts of acids of formula I, and pharmaceutical compositions comprising these compounds.

3-Amino-[1]-benzazepin-2-one-1-alkanoic acids

Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotensin converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.

Synthesis and biological properties of (carboxyalkyl)amino-substituted bicyclic lactam inhibitors of angiotensin converting enzyme

Syntheses of the potent angiotensin converting enzyme inhibitor (3S)-1-(carboxymethyl)-3-[[(1S)-1-carboxy-3-phenylpropyl]amino]-2,3,4,5 -tetrahydro-1H-[1]benzazepin-2-one (CGS 14831) and the related monoester prodrug (17a; CGS 14824A) are described together with preparative details for six- and eight-membered ring analogues. Inhibitory potencies and in vivo biological activity of the compounds are discussed. The data indicate that 17a has a biological profile comparable to that of enalapril.

3-Amino-[1]-benzazepin-2-one-1-alkanoic acids

Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin-2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.