Pharmaceutical compositions and methods of use of highly...

C - Chemistry – Metallurgy – 07 – F

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C07F 7/10 (2006.01) A61K 31/695 (2006.01)

Patent

CA 2634724

Novel compositions of silicon-containing sulfhydryl compounds, their preparation and use in methods for treating disease are described. Silicon confers lipophilicity that can enhance the penetration of the silicon derivative sulfhydryl compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The organosilyl group provides compounds having improved pharmacokinetics. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

La présente invention concerne de nouvelles compositions de composés sulfhydryles contenant de la silicone, ainsi que leur préparation et leur utilisation dans des procédés de traitement de maladies. La silicone assure une lipophilicité qui peut augmenter la pénétration des composés sulfhydryles à base d'un dérivé de silicone à travers la paroi intestinale, les membranes cellulaires et la barrière hémato-encéphalique, améliorant ainsi les propriétés thérapeutiques, notamment la biodisponibilité, le métabolisme et/ou la pharmacocinétique. Le groupe organosilyle offre des composés présentant une pharmacocinétique améliorée. La présente invention décrit de nouveaux composés, des analogues, des promédicaments et des sels pharmaceutiquement acceptables de ceux-ci, des compositions pharmaceutiques et des procédés de traitement des maladies et d'autres pathologies ou troubles et analogues. Cette invention concerne également des procédés de préparation de tels composés ainsi que des intermédiaires utiles dans de tels procédés.

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