Derivatives of tricyclic aminoacids, processes for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/94 (2006.01) A61K 31/40 (2006.01) C07D 209/58 (2006.01) C07D 221/22 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1246554

- 1 - Abstract of the disclosure: The invention relates to new derivatives of tri- cyclic aminoacids, of the formula Image (I) in which n denotes 0 or 1, A denotes -CH=CH- or -CH2-CH2-, R denotes hydrogen, alkyl or aralkyl, R1 denotes hydrogen, or alkyl, which can optionally be substituted by amino, acylamino or benzoylamino, or alkenyl, cycloalkyl, cyclo- alkenyl, cycloalkylalkyl, aryl or partially hydrogenated aryl, each of which can be substituted by alkyl, alkoxy or halogen, or aralkyl or aroylalkyl, both of which can be substituted as defined above, or a monocyclic or bi- cyclic S-, O- and/or N-heterocyclene radical, or a side chain of a naturally occurring aminoacid, which may be protected, R2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes - 2 - alkyl, alkenyl, cycloalkyl, aryl, which can be mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino and/or methylenedioxy, or 3-indolyl, and physiologically acceptable salts thereof, processes for their preparation, agents containing these compounds and their use, and new bicyclic aminoacids as intermediates and processes for their preparation. Compounds of the formula I have long-lasting, intensive hypotensive action and are inhibitors of the angiotension-converting enzyme (ACE inhibitors).

441040

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