Pharmaceutical solid state forms

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 1/00 (2006.01) A61K 31/569 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2712005

The invention provides and describes solid state 17.alpha.-ethynyl-5.alpha.- androstane-3.alpha.,17.beta.-diol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17.alpha.-ethynyl-5.alpha.-androstane-3.alpha.,17.beta.-diol include Form III anhydrate and Form I solvate. The invention further relates to solid and suspension formulations containing 17.alpha.--ethynyl -5.alpha.-androstane-3.alpha.,17.beta.-diol in a described solid state form and use of the formulations to treat cancers or precancers such as prostate cancer or breast cancer in subjects or human patients. The invention also relates to methods to make liquid formula-tions from solid state forms of 17.alpha.-ethynyl-5.alpha.- androstane- 3.alpha.,17.beta.-diol and uses of such formulations in treating the described conditions.

La présente invention concerne et décrit un 17a-éthynyl-5a-androstane-3a,17ß-diol à l'état solide, comprenant ses formes amorphes et cristallines ainsi que ses formes polymorphes spécifiques. Les anhydrates et les solvates de 17a-éthynyl-5a-androstane-3a,17ß-diol comprennent l'anhydrate de forme III et le solvate de forme I. L'invention concerne en outre des formulations solides et de suspension contenant un 17a-éthynyl-5a-androstane-3a,17ß-diol sous une forme solide décrite ainsi que l'utilisation des formulations pour traiter des cancers ou précancers tels que le cancer de la prostate et le cancer du sein chez des sujets ou des patients humains. La présente invention concerne également des procédés de fabrication de formulations liquides à partir de formes solides de 17a-éthynyl-5a-androstane-3a,17ß-diol et les utilisations de ces formulations dans le traitement des conditions décrites.

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