Immunomodulatory steroids, in particular the hemihydrate of...

C - Chemistry – Metallurgy – 07 – J

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C07J 73/00 (2006.01) A61K 31/565 (2006.01) A61K 31/568 (2006.01) A61K 31/5685 (2006.01) C07J 1/00 (2006.01) C07J 3/00 (2006.01)

Patent

CA 2365081

The invention provides compositions comprising formula 1 steroids, e.g., 16alpha-bromo-3beta-hydroxy-5alpha-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16alpha-bromo-3beta-hydroxy-5alpha- androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

La présente invention concerne des compositions comprenant des stéroïdes de formule (1) par exemple du 16.alpha.-bromo-3.beta.-hydroxy-5.alpha.-androstan-17-one semi-hydrate et un ou plusieurs excipients, cette composition renfermant spécifiquement moins d'environ 3 % d'eau. Ces compositions sont utiles pour préparer des formulations pharmaceutiques améliorées. La présente invention concerne également des procédés de dosage intermittent de composés stéroïdiens tels que des analogues de 16.alpha.-bromo-3.beta.-hydroxy-5.alpha.-androstan-17-one et des compositions utiles dans de tels schémas posologiques de dosage ; des compositions et des procédés permettant d'inhiber la réplication (virale) des pathogènes, d'améliorer les symptômes associés à la dysrégulation du système immun et de moduler les réponses immunitaires chez un individu au moyen de certains stéroïdes et analogues de stéroïdes ; et des procédés de préparation et d'utilisation de ces compositions et de ces formulations immunomodulatrices.

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