| 摘要 |
<p>Mercaptocycloacyl aminoacid inhibitors of endopeptidase of formula (I) or a pharmaceutically acceptable salt thereof, wherein -A- is a 4-, 5- or 6-membered optionally substituted alkylene chain; a 4-, 5- or 6-membered optionally substituted alkenylene chain; a 4-, 5- or 6-membered optionally substituted hetero-atom-containing chain comprising 2 to 5 carbon atoms and 1 or 2 oxygen or sulfur atoms; or an alkylene or hetero-atom-containing chain substituted with a fused benzene ring; Q is hydrogen or R?5CO-; R1¿ is H, alkyl, arylalkyl or aryl; R2 is H, alkyl, alkoxyalkyl, alkylthioalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, arylalkoxyalkyl or arylalkylthioalkyl; R3 is hydroxy, alkoxy, arylalkoxy, or R?2; or R2 and R3¿ form an alkylene chain, thereby, together with the carbons to which they are attached, completing a 5-, 6- or 7-membered ring; R4 is hydroxy, alkoxy, aryloxy, arylalkoxy, amino, alkylamino or dialkylamino; R5 is alkyl or aryl; m is 0 or 1; and n is 0, 1, 2 or 3, use of the compounds, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, use of the compounds in the treatment of nephrotoxicity pain conditions, and pharmaceutical compositions containing said compounds are disclosed.</p> |
