CO-CRYSTALS OF RIBOCICLIB AND CO-CRYSTALS OF RIBOCICLIB MONO-SUCCINATE, PREPARATION METHOD THEREFOR, COMPOSITIONS THEREOF, AND USES THEREOF

• Main Authors: CHEN JIAN, SHENG XIAOXIA, SHENG XIAOHONG
• Format: Patent
• Language: Chinese; English
• Published: 15.05.2020
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to co-crystals of ribociclib and co-crystals of ribociclib mono-succinate, comprising co-crystals between ribociclib and saccharin, co-crystals between ribociclib and cholic acid, co-crystals between ribociclib and orotic acid, and co-crystals between ribociclib mono-succinate and citric acid. Compared with the prior art, the co-crystals have one or more improved characters. The present invention also relates to a preparation method for the co-crystals between ribociclib and saccharin, the co-crystals between ribociclib and cholic acid, the co-crystals between ribociclib and orotic acid and the co-crystals between ribociclib mono-succinate and citric acid, pharmaceutical compositions thereof, and uses thereof in the preparation of drugs for treating and/or preventing diseases involving in one or more symptoms of protein kinase-related dysfunctions, cancers, transplant rejection and autoimmune diseases. 本发明涉及瑞博西林的共晶和瑞博西林单琥珀酸盐的共晶，包括瑞博西林和糖精的共晶、瑞博西林和胆酸的共晶、瑞博西林和乳清酸的共晶以及瑞博西林单琥珀酸盐和柠檬酸的共