| 摘要 |
This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure <IMAGE> I wherein R and R9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-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 hydrogen, alkyl, alkenyl or alkynyl containing up to 20 carbon atoms, aryl or aryl-lower alkyl having from 7 to 12 carbon atoms, heterocyclic or heterocyclic-lower alkyl having from 6 to 12 carbon atoms, cycloalkyl or cycloalkyl-alkyl containing up to 20 carbon atoms in the cycloalkyl group, provided that each of R1 and R2 and R4 and R5 are different; 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; R6 is cycloalkyl, polycycloalkyl, partially saturated cycloalkyl and polycycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl; and wherein each chiral center is in the (S) configuration; and salts thereof with acids or bases especially pharmaceutically acceptable acid and base salts.
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