Friday, 13 December 2013


phase 2
Daglutril is a novel dual-action endopeptidase inhibitor which had been in phase II clinical development by Solvay for the treatment of hypertension, congestive heart failure (CHF) and pulmonary hypertension; however, no recent development has been reported for this research.
Daglutril inhibits NEP (neutral endopeptidase) and ECE (endothelin-converting enzyme) and thereby exerts vasodilating, blood pressure-lowering and other potentially beneficial effects on the cardiovascular system.
2-[3(S)-[1-[2(R)-(Ethoxycarbonyl)-4-phenylbutyl]cyclopentan-1-ylcarboxamido]-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]acetic acid
 cas182821-27-8, 182560-84-5 (undefined stereochem.)
Cardiovascular Drugs, Heart Failure Therapy, Hypertension, Treatment of, Endothelin-Converting Enzyme Inhibitors, Neprilysin Inhibitors
Neprilysin (Enkephalinase, Neutral Endopeptidase, NEP) Inhibitors
Endothelin-Converting Enzyme (ECE) Inhibitors
182821-27-8,  1H-1-Benzazepine-1-acetic acid, 3-(((1-(2-(ethoxycarbonyl)-4-phenylbutyl)cyclopentyl)carbonyl)amino)-2,3,4,5-tetrahydro-2-oxo-, (S-(R*,S*))-,  1H-1-Benzazepine-1-acetic acid, 3-(((1-((2R)-2-(ethoxycarbonyl)-4-phenylbutyl)cyclopentyl)carbonyl)amino)-2,3,4,5-tetrahydro-2-oxo-, (3S)-,  2-[(3S)-3-[[1-[(2R)-2-carbethoxy-4-phenyl-butyl]cyclopentanecarbonyl]amino]-2-keto-4,5-dihydro-3H-1-benzazepin-1-yl]acetic acid,
The acylation of the chiral amine (I) with the chiral cyclopentanecarboxylic aid (II) by means of N-methylmorphline (NMM), hydroxybenzotriazole (HOBT) and N-(dimethylaminopropyl)-N’-ethylcarbodiimide (EDT) in dichloromethane gives the amide (III), which is then treated with trifluoroacetic acid to elimnate the tert-butyl ester groups.
Benzazepin-, benzoxazepin- and benzothiazepin-N-acetic acid-derivs., their preparation and their pharmaceutical compsns.
Waldeck, H.; ET AL (Kali-Chemie AG)
CA 2172354; EP 0733642; JP 1996269011; US 5677297

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