Derivatives of 2-azabicyclo[3.1.0]hexane-3- carboxylic acid,...

C - Chemistry – Metallurgy – 07 – D

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530/5.06, 167/10

C07D 209/52 (2006.01) A61K 31/40 (2006.01) C07D 221/04 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1263000

HOE 83/F 119 Abstract of the disclosure: The invention relates to compound of the formula I Image (I) in which n denotes 0 or 1, R denotes hydrogen, alkyl, alkenyl or aralkyl, R1 denotes hydrogen or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, aralkyl or aroylalkyl, both of which can be substituted in the aryl radical as defined previously, a monocyclic or bicyclic S- or O- and/radical N-heterocyclic radical or a side chain of an aminoacid, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen, or Y and Z together denote oxygen, X denotes alkyl, alkenyl, cycloalkyl, aryl, which can be monosubstituted, disubstituted or trisubstituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, acylamino, alkyl- amino, dialkylamino and/or methylenedioxy, or 3-indolyl, and to a process for their preparation, agents containing them and their use, and to 2-azabicyclo [3.1Ø] hexane derivatives as inter- mediates, and a process for their preparation. The compounds of the formula I and their salts have a long-lasting and strong hypotensive effect. They are potent inhibitors of angiotensin converting enzyme (ACE inhibitors) and can be employed to control hypertension of a variety of etiologies.

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