Phosphonic acid derivatives with metallopeptidase inhibitory activity
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United States of America Patent
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Apr 15, 2003
Grant Date -
N/A
app pub date -
May 4, 1998
filing date -
Nov 23, 1995
priority date (Note) -
Expired
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Abstract
Compounds of formula (I) wherein R is an alkyl, aryl or arylalkyl group wherein the aryl is phenyl naphthyl or heterocycle; R.sub.1 and R.sub.2, the same or different, are hydrogen atoms or alkyl groups; R.sub.3 is an aryl or arylalkyl group wherein the aryl is as above; R.sub.4 is a heterocycle optionally substituted with a heterocycle or phenyl, or it is a phenyl group substituted with a heterocycle (R.sub.4 is not imidazole or indole); X is a bond or --OCONH or --CONH-- group, processes for their preparation and pharmaceutical compositions thereof, are described. The compounds of formula (I) are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular disease. ##STR1##
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