2-amino-3-(5-and 6-)benzoylphenylacetic acids, esters and...

C - Chemistry – Metallurgy – 07 – D

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260/515.5, 260/4

C07D 317/54 (2006.01) C07D 209/08 (2006.01) C07D 209/32 (2006.01) C07D 209/34 (2006.01)

Patent

CA 1087205

Abstract of the Disclosure Novel 2-amino-3-(5- and 6-)benzoylacetic acids, esters and metal salts of tho formula: Image wherein R is hydrogon or lower alkyl, R1 is hydrogen, lower-alkyl, sodium or potassium, R2 is hydrogen, halogen or lower alkoxy, X is hydrogen, lower alkyl, lower alkoxy, halogen, nitro or trifluoromethyl, Y is hydrogen, lower alkyl, lower alkoxy, halogon, nitro or trifluoromethyl or X and Y together form a lower alkylonedioxy group and Am is primary amino (-NH2),or dimethyl- amino but excluding those compounds in which (a) R1, R2 and Y are hydrogen atoms and Am is a primary amino group and the benzoyl group; is attached in the 3- or 5-position. The compounds are prepared by hydrolysis of 4-(5- and 7-)benzoylindolin-2-ones to give tho 2-amino-3-(5- and 6-) benzoylphenylacetic acids wherein amino is priamry 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.

248319

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