[EN] ENASIDENIB GLYCOSIDES AND METHODS OF TREATING DISEASES ASSOCIATED WITH ISOCITRATE DEHYDROGENASE (IDH) DYSFUNCTION<br/>[FR] GLYCOSIDES D'ENASIDENIB ET PROCÉDÉS DE TRAITEMENT DE MALADIES ASSOCIÉES À UN DYSFONCTIONNEMENT DE L'ISOCITRATE DÉSHYDROGÉNASE (IDH)
申请人:DOUBLERAINBOW BIOSCIENCES INC
公开号:WO2021188456A1
公开(公告)日:2021-09-23
Enasidenib glycosides and methods of making enasidenib glycosides are disclosed. Glycosyl transferases catalyze addition of one or more monosaccharides to enasidenib to yield enasidenib glycosides. Suitable monosaccharides can be in the L- or D- configuration and typically have 5, 6, or 7 carbons. Suitable monosaccharides include allose, apiose, arabinose, fructose, fucitol, fucose, galactose, galacturonate, glucose, glucuronic acid, mannose, N-acetylglucosamine, rhamnose, or xylose. Uridine diphosphate glycosyl transferases can catalyze formation of either an alpha or beta glycosidic bond.
本文介绍了Enasidenib糖苷及其制备方法。糖基转移酶催化将一个或多个单糖添加到Enasidenib中,形成Enasidenib糖苷。适宜的单糖可以是L-或D-构型,并且通常具有5、6或7个碳。适宜的单糖包括阿洛糖、芹糖、阿拉伯糖、果糖、甘露醇、岩藻糖、半乳糖、半乳糖醛酸酯、葡萄糖、葡萄糖醛酸、甘露糖、N-乙酰葡萄糖胺、鼠李糖或木糖。尿苷二磷酸糖基转移酶可以催化α或β糖苷键的形成。