| 摘要 |
The invention relates to novel derivatives of phosphinic amino acids having formula (I), the preparation method thereof and pharmaceutical compositions containing same. According to the invention, R1 represents hydrogen, alkylcarbonyloxyalkyl, alkylcarbonylthioalkyl, R 2 represents hydrogen, alkylcarbonyloxyalkyl, arylcarbonylthioalkyl, arylalkyl which is optionally substituted, and R3 represents optionally-substituted phenyl, indolyl, the isomers thereof and the pharmaceutically-acceptable base or acid addition salts of same. Alternatively, R1can also represents a linear or branched (C1-C6) alkyl group, R2 represents a linear or branched (C1-C6) alkyl group when R3 represents a phenyl substituted by a hydroxy group, the enantiomers, diastereoisomers and the pharmaceutically-acceptable base addition salts thereof and the hydrates and solvates of same. The inventive novel derivatives of phosphinic amino acids are characterised by their ability to inhibit both the angiotensin conversion enzyme and the endothelin conversion enzyme.
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