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AssigneeA. H. Robins Company, Incorporated
InventorsWilliam J. Welstead, Jr., Henry W. Moran
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Novel 2-amino-3-(5- and 6-)benzoylphenylacetic acids, esters and metal salts of the formula: ##STR1## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, lower-alkyl, sodium or potassium, R.sup.2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, halogen, nitro or trifluoromethyl, and Am is primary amino (--NH.sub.2) methylamino or dimethylamino. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give the 2-amino-3-(5- and 6-)benzoylphenylacetic acids wherein amino is primary amino. The free acids are converted to the esters and metal salts. The calcium and magnesium salts are disclosed and are within the scope of the present invention. The compounds have anti-inflammatory activity, are effective in lowering the cholesterol levels in hyperlipemic rats and inhibit blood platelet aggregation.
The method for alleviating inflammation in a living animal body with a minimum of undesirable side effects comprising internally administering to said living animal body an effective amount of a compound selected from the group having the formula:
The method for alleviating inflammation in a living animal body with a minimum of undesirable side effects comprising internally administering to said living animal body an effective amount of 2-amino-3-benzoylphenylacetic acid.
The method for alleviating inflammation in a living animal body with a minimum of undesirable side effects comprising internally administering to said living animal body an effective amount of sodium 2-amino-3-benzoyl-5-methoxyphenylacetate sesquihydrate.
The method for alleviating inflammation in a living animal body with a minimum of undesirable side effects comprising internally administering to said living animal body an effective amount of sodium 2-amino-3-benzoylphenylacetate dihydrate.
The method for alleviating inflammation in a living animal body with a minimum of undesirable side effects comprising internally administering to said living animal body an effective amount of potassium 2-amino-3-benzoylphenylacetate hydrate.
A therapeutic composition suitable for alleviating inflammation comprising (a) an effective amount of between about 0.1 and 150 milligrams of a compound selected from the group having the formula:
A therapeutic composition suitable for alleviating inflammation comprising (a) an effective amount of between about 0.1 and 150 milligrams of sodium 2-amino-3-benzoylphenylacetic acid and (b) a pharmaceutically acceptable carrier thereof.
A therapeutic composition suitable for alleviating inflammation comprising (a) an effective amount of between about 0.1 and 150 milligrams of sodium 2-amino-3-benzoyl-5-methoxyphenylacetate sesquihydrate and (b) a pharmaceutically acceptable carrier thereof.
A therapeutic composition suitable for alleviating inflammation comprising (a) an effective amount of between about 0.1 and 150 milligrams of sodium 2-amino-3-benzoyl-phenylacetate dihydrate and (b) a pharmaceutically acceptable carrier thereof.
A therapeutic composition suitable for alleviating inflammation comprising (a) an effective amount of between about 0.1 and 150 milligrams of potassium 2-amino-3-benzoylphenylacetate hydrate and (b) a pharmaceutically acceptable carrier thereof.
A compound selected from the group having the formula:
A compound selected from the group having the formula:
Calcium 2-amino-3-benzoylphenylacetate dihydrate.
Magnesium 2-amino-3-benzoylphenylacetate trihydrate.
2-Amino-3-benzoylphenylacetic acid.
Sodium 2-amino-3-benzoyl-5-methoxyphenylacetate.
Sodium 2-amino-3-benzoyl-5-methoxyphenylacetate sesquihydrate.
Sodium 2-amino-3-benzoylphenylacetate.
Sodium 2-amino-3-benzoylphenylacetate dihydrate.
Potassium 2-amino-3-benzoylphenylacetate.
Potassium 2-amino-3-benzoylphenylacetate hydrate.
Sodium 2-amino-3-(p-chlorobenzoyl)phenylacetate hydrate.
Ethyl 2-amino-3-(p-chlorobenzoyl)phenylacetate.
Sodium 2-amino-3-benzoyl-.alpha.-methylphenylacetate hydrate 2.5.
2-Amino-3-(p-fluorobenzoyl)phenylacetic acid.
Sodium 2-amino-3-(p-fluorobenzoyl)phenylacetate hydrate.
Calcium 2-amino-3-benzoylphenylacetate.
Magnesium 2-amino-3-benzoylphenylacetate.
2-Amino-3-(p-methoxybenzoyl)phenylacetic acid.
Dependencies are inferred from the claim text.