Novel salt of isoquinoline compound and crystal thereof

Details Novel salt of isoquinoline compound and crystal thereof Novel salt of isoquinoline compound and crystal thereof

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/4725 (2006.01) A61P 9/10 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2695973

Provided is a novel salt form of (R)-3-[2-(2- hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1- one. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl- 2H-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products.

L'invention porte sur une nouvelle forme de sel de la (R)-3-[2-(2-hydroxyméthylpyrrolidin-1-yl)éthyl]-5-méthyl-2H-isoquinolin-1-one. Le composé est le monophosphate de (R)-3-[2-(2-hydroxyméthylpyrrolidin-1-yl)éthyl]-5-méthyl-2H-isoquinolin-1-one. Par comparaison avec la forme libre et le monochlorhydrate dihydrate, ce monophosphate est chimiquement plus stable, présente une solubilité supérieure et présente une moindre variation de poids avec l'humidité. C'est un excellent composé destiné à être utilisé comme médicament brut pour des médicaments.

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