C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/06 (2006.01) A61K 31/34 (2006.01) A61K 31/495 (2006.01)
Patent
CA 2291086
This invention relates to a sulfate salt of an HIV protease inhibitor, Compound (A), which is useful in the treatment of AIDS, ARC or HIV infection in adults and children. More specifically, the invention provides a sulfate salt of the HIV protease inhibitor, Compound (A) having substantially improved solibility in dilute HC1 (gastric acid) solution which results in much greater oral absorption and bioavailability in animal models. Processes for making the sulfate salt of the particular HIV protease inhibitor compounds are also disclosed.
L'invention concerne un sel de sulfate d'un inhibiteur de protéase du VIH, représenté ci-après comme composé A, utile dans le traitement du SIDA, du para-SIDA ou de l'infection à VIH chez l'adulte et l'enfant. Plus précisément, l'invention concerne un sel de sulfate d'inhibiteur de protéase du VIH (composé A), à solubilité sensiblement améliorée dans une solution d'acide gastrique (HC1) diluée, ce qui en améliore considérablement l'absorption orale et la biodisponibilité chez les modèles animaux. L'invention concerne également des procédés pour l'élaboration du sel de sulfate du composé inhibiteur de protéase du VIH considéré.
Askin David
Hoerrner R. Scott
Purick Robert M.
Reider Paul
Varsolona Richard J.
Gowling Lafleur Henderson Llp
Merck & Co. Inc.
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