Method for improving the solubility of tricyclic amino...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/88 (2006.01) A61K 9/14 (2006.01) A61K 9/16 (2006.01) A61K 31/343 (2006.01) A61K 31/381 (2006.01) A61K 31/403 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) C07D 209/08 (2006.01) C07D 307/91 (2006.01) C07D 333/76 (2006.01)

Patent

CA 2386373

Compounds useful in the treatment and prevention of diabetes, obesity, hyperlipidemia and so on are provided in the form of oral preparations exhibiting good absorbability in the digestive tract. A method for improving the solubility of tricyclic amino alcohol derivatives of general formula (1) or salts thereof, characterized by using these derivatives or salts in the form of noncrystalline substance, wherein R1 is lower alkyl or benzyl; * represents an asymmetric carbon atom; R2 is hydrogen, halogeno, or hydroxyl; and A is a substituent represented by general formula (2) or (3), (wherein X is NH, O or S).

La présente invention concerne des composés pour le traitement et la prévention du diabète, de l'obésité et de l'hyperlipémie. Ces composés, qui se présentent sous forme de préparations orales, font preuve d'une bonne absorbabilité par le système digestif. L'invention concerne également un procédé permettant d'améliorer la solubilité de dérivés d'alcools aminés tricycliques représentés par la formule générale (1) ou certains de leurs sels, ces procédés faisant intervenir l'utilisation de ces dérivés ou sels sous forme de substance non cristalline. Dans cette formule, R?1¿ est alkyle inférieur ou benzyle. L'astérisque dénote un atome de carbone asymétrique. R?2¿ est hydrogène, halogène ou hydroxyle. A est un substituant représenté par les formules générales (2) ou (3) dans lesquelles X est NH, O ou S.

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