N-substituted-amido-amino acids

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.06, 167/10

C07K 5/06 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1264500

ABSTRACT OF THE DISCLOSURE Compounds of the formula Image wherein R and R9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy- lower alkoxy, acylamino-lower alkoxy, acyloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino, R1, R2, R3, R4, R5, R7, and R8 are independently alkyl, alkenyl or alkynyl containing up to 20 carbon atoms, aryl or aryl-lower alkyl containing up to 12 carbon atoms, heterocyclic or heterocyclic-lower alkyl containing up to 12 carbon atoms, or cycloalkyl or cycloalkyl alkyl containing up to 20 carbon atoms. R6 is heterocyclic or heterocyclic alkyl; R2 and R3 taken together with the carbon and nitrogen to which they are respectively attached and R3 and R5 taken together with the nitrogen and carbon to which they are respectively attached form an N-heterocycle containing from 3 to 5 carbon atoms or 2 to 4 carbon atoms and a sulfur atom, and wherein said alkyl, alkenyl, and alkynyl groups can be substituted with hydroxy, lower alkoxy, thio, lower alkylmercapto, amino, lower alklamino, di(lower alkyl) amino, halogen, and nitro; and salts thereof, especially salts with pharmaceutically acceptable acids and bases. The compounds possess hypertensive and antitensin convert- ing enzyme inhibitory activity.

398031

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