Cardioprotective tocopherol analogs

C - Chemistry – Metallurgy – 07 – F

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C07F 9/655 (2006.01) A61K 31/665 (2006.01)

Patent

CA 2079289

This invention relates to alkylated phosphonium alkylene 2H-1-benzopyran derivatives of the formula Image the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof wherein Q is P~R1R2R3.cndot.X.THETA., X is a halide or OSfO)2Rg, with R4 being H, C1-6 alkyl, aryl or aralkyl, R1, R2 and R3 each individually are a C1-6 lower alkyl, phenyl, benzyl or phenethyl, R5 is H or. C1-6 alkyl, R6 is H or -C(O)R, R being H or C1-9 alkyl, R7 is H or C1-6 alkyl, R8 is H or C1-6 alkyl, and n is an integer of 1 to 6, provided that R1, R2 and R3 are not simultaneously phenyl, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cardioprotective properties and to their end-use appli- cation as therapeutic agents.

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