Tocopherol derivatives and uses thereof

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 7/18 (2006.01) A61K 31/355 (2006.01) A61K 31/395 (2006.01) A61K 31/4192 (2006.01) A61K 31/695 (2006.01) C07D 311/72 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2590111

Tocopherol derivatives having the general formula: (see formula below) wherein n is an integer of 6 to 13, R1 is hydrogen, a silyl ether or acetate, R2 is an optionally substituted nitrogen-containing heterocycle or a polycyclic nitrogen-containing heterocycle; and pharmaceutically acceptable salts thereof are provided. A method for synthesizing the compounds is also provided. The tocopherol derivatives are capable of inhibiting the primary enzyme responsible for the metabolism of the tocopherols and tocotrienols compounds of vitamin E, namely tocopherol-.omega.-hydroxylase, and thus increase the amount and prolong the availability of these compounds in plasma and tissue.

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