Acetic acid derivatives, process for the preparation thereof...

C - Chemistry – Metallurgy – 07 – D

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260/279.2, 260/2

C07D 409/06 (2006.01) C07D 313/12 (2006.01) C07D 337/12 (2006.01)

Patent

CA 1171414

Abstract of the Disclosure: Novel acetic acid derivatives of the formula: Image (I) wherein X is oxygen or sulfur; R1 is hydrogen or a lower alkyl; R2 is hydroxy, an alkoxy, an alkenyloxy, a cyclo- alkyloxy, an aryloxy, a substituted aryloxy, an aryl-lower alkoxy, a substituted aryl-lower alkoxy, an aryl-lower alkenyloxy, a substituted aryl-lower alkenyloxy, an .omega.-di- substituted amino-lower alkoxy, a lower alkoxycarbonyl- lower alkoxy, a lower alkoxy-lower alkoxy, a hydroxy-lower alkoxy-lower alkoxy, an acyl-lower alkoxy, or a group Image wherein R3 is hydrogen, hydroxyl a lower alkyl, an aryl-lower alkyl, a hydroxy-lower alkyl, or a carboxy- lower alkyl, R4 is hydrogen, a lower alkyl or a hydroxy- lower alkyl, or the R3 and R4 may combine together with the nitrogen atom to which they are joined to form a heterocyclic group; and the group -CH(R1)COR2 is joined to the carbon atom at 2- or 3-position, and pharmaceutically acceptable salts thereof, processes for their preparation, and pharmaceutical compositions containing these compounds. They have excellent anti-inflammatory, analgesic and anti- pyretic activities with weak ulcerogenicity in the gastrointestinal tract and toxicity.

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