Co-crystals of 5-amino-2-oxothiazolo[4,5-d]pyrimidin-3(2H)-yl-5-hydroxymethyl tetrahydrofuran-3-yl acetate and methods for preparing and using the same

US9676793B2 · kind B2 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Urs Schwitter · Reinach, CH
• Fritz Bliss · Hartheim, DE
• Michael Kammerer · Basel, CH
• Florence Tixeront · Basel, CH

Key dates

• Filing date: Dec 21, 2015
• Grant date: Jun 13, 2017
• Expiry date: Dec 21, 2035

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C59/185
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Co-crystals of Formula I compounds and their pharmaceutical compositions are novel therapeutics for the treatment of diseases, such as human immunodeficiency virus (HIV) infection, hepatitis B virus (HBV) infection, hepatitis C virus (HCV) infection and cancer. The co-crystal are more stable to oxidation and aqueous degradation, have a better pharmacokinetic profile and superior biological activity than the corresponding tosylate salt form of Formula I compound.