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US 5,153,347 AGranted
Phosphonate, phosphinate derivatives useful as antihypertensive agents
AssigneeE. R. Squibb & Sons, Inc.
InventorJohn E. Lloyd
Life of this patent
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Abstract
Novel angiotensin II receptor antagonists of the formula ##STR1## wherein X, X.sub.1, X.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein, are disclosed. These compounds are useful, for example, in the treatment of hypertension, congestive heart failure and cardiac hypertrophy.
Claims5
A compound of the formula ##STR21## or pharmaceutically acceptable salts thereof;
- wherein X is --CH.sub.2 -- or a single bond;
- X.sub.1 is --O-- or a single bond;
- X.sub.2 is --Ch.sub.2 --, --O-- or a single bond;
- R.sub.1 is alkyl of 2 to 10 carbon atoms, alkenyl or alkynyl of 3 to 10 carbon atoms or the same groups substituted with F;
- R.sub.2 is H, COOR.sub.6, alkyl of 1 to 10 carbon atoms, alkenyl of 3 to 10 carbon atoms, or the same groups substituted with F;
- R.sub.3 and R.sub.4 are each independently hydrogen, alkyl, aryl or arylalkyl;
- R.sub.6 is alkyl or perfluoroalkyl of 1 to 8 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, phenyl or benzyl;
- R.sub.14 is ##STR22## R.sub.15 is H, halogen, --NO.sub.2, --CN, alkyl of 1 to 4 carbons, acyloxy of 1 to 4 carbons, alkoxy of 1 to 4 carbons, --CO.sub.2 H, CO.sub.2 R.sub.17, --NHSO.sub.2 CH.sub.3, --NHSO.sub.2 CF.sub.3, --CONHOR.sub.18, --SO.sub.2 NH.sub.2, aryl, furyl or ##STR23## R.sub.16 is H, halogen, alkyl of 1 to 4 carbons or alkoxy of 1 to 4 carbons;
- R.sub.17 is hydrogen or ##STR24## R.sub.18 is hydrogen, methyl or benzyl;
- R.sub.19 is alkyl of 1 to 6 carbons, NR.sub.2 R.sub.21 ;
- R.sub.20 and R.sub.21 are independently hydrogen, benzyl, alkyl of 1 to 6 carbons or taken together are 3 to 6 methylene groups forming a 4- to 7-membered ring with the nitrogen atom to which they are attached;
- R.sub.23 is --CO.sub.2 H, --CO.sub.2 R.sub.17,
- X.sub.3 is a carbon-carbon single bond, --CO--, --CH.sub.2 --, and
10 more elements
A compound having the name 4'-[[[(2-methoxyethoxy)pentylphosphinyl]oxy]-methyl][1,1'-biphenyl]-2-carb oxylic acid, monosodium salt.
Dependencies are inferred from the claim text.