Novel anti-oxidative, tricyclic, condensed heterocyclic...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/14 (2006.01) C07D 337/14 (2006.01) C07D 493/04 (2006.01)

Patent

CA 2200598

A novel antioxidant tricyclic fused heterocyclic compound represented by general formula (2) and a salt thereof (wherein X-Y represents CH2-C=O, CH2- CH2 or CH=CH; Z represents O, S or S=O; and R1 to R8 represent each hydrogen, hydroxy, halogeno, lower alkyl, lower alkoxy, lower alkyl ketone or CF3, provided at least two groups among R1, R2, R3 and R4 represent each hydroxy). This compound has an antioxidant activity at least equivalent to that of .alpha.-tocopherol, and so is promising as a remedy for various diseases wherein in vivo lipid peroxides participate, such as cancer, arteriosclerotic diseases and liver diseases. It is also expected to be applicable to the preparation of cosmetics and chemicals.

Nouveau composé antioxydant hétérocyclique à trois cycles fusionnés, représenté par la formule générale (I), et sel de ce composé. Dans cette formule, X-Y représente CH¿2?-C=O, CH¿2?-CH¿2? ou CH=CH; Z représente O, S ou S=O; et R¿1? à R¿8? représentent indépendamment hydrogène, hydroxy, halogéno, alkyle inférieur, alcoxy inférieur, cétone alkyle inférieur ou CF¿3?, sous réserve qu'au moins deux groupes parmi R¿1?, R¿2?, R¿3? et R¿4? représentent chacun hydroxy. Ce composé exerce une activité antioxydante au moins équivalente à celle du .alpha.-tocophérol, et présente donc des perspectives interessantes comme remède à diverses maladies dans lesquelles les peroxydes lipidiques in vivo entrent en jeu, comme le cancer, l'artériosclérose et les maladies du foie. Ce composé devrait également pouvoir être employé pour la préparation de cosmétiques et de produits chimiques.

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