Benzopyran-containing compounds and method for their use

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 311/60 (2006.01) A61K 31/35 (2006.01) A61K 31/675 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2212856

Disclosed is a compound or pharmaceutically acceptable further salt thereof, the compound having the molecular structure: (see formula I) wherein A- is an anion of a pharmaceutically acceptable acid, wherein R1 and R2 are independently selected from the group consisting of hydroxyl and a moiety convertible in vivo to hydroxyl, and wherein R3 is -CH2- or -CH2CH2-. Disclosed is an optically active compound or pharmaceutically acceptable salt thereof, the compound having molecular structure I: (see formula II) wherein R1 and R2 are independently selected from the group consisting of hydroxyl and a moiety convertible in vivo to hydroxyl, wherein R3 is -CH2CH2-, and wherein the compound is at a purity level sufficiently free of its 2R stereoisomer that molecular structure I predominates.

L'invention porte sur certains antioestrogènes à base de benzopyranne permettant de traiter des maladies sensibles aux oestrogènes telles que le carcinome mammaire. Des formes promédicamenteuses permettent une fabrication facile et garantissent une bonne durée de conservation ainsi qu'une bonne biodisponibilité tandis que les stéréo-isomères préférés dans le cadre de cette invention se sont avérés plus efficaces que des mélanges racémiques.

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