SAXAGLIPTIN CRYSTALLINE FORM AND METHOD FOR PRODUCING THE SAME

• Main Authors: WEI CHENKOU, JACK Z GOUGOUTAS, GREGORY SCOTT JONES, MALLEY MARY F, XIAOTIAN S YIN, SCOTT A SAVAGE, YU JURONG, TRUC CHI VU, JOHN D DIMARCO
• Format: Patent
• Language: English
• Published: 31.07.2014
• Subjects: AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUSPOLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR; CHEMISTRY; CRYSTAL GROWTH; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITHDEFINED STRUCTURE; REFINING BY ZONE-MELTING OF MATERIAL; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITHDEFINED STRUCTURE; SINGLE-CRYSTAL-GROWTH; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL ORUNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL

PROBLEM TO BE SOLVED: To provide a polymorphism crystalline structure of saxagliptin which is a reversible dipeptidyl peptidase-4 (DPP4) inhibitor, a pharmaceutical composition thereof, a method for producing said crystalline structure, and a method for treating disorders such as diabetes using the same.SOLUTION: A pharmaceutical composition containing a structure of substantially pure form of saxagliptin, or its free base monohydrate (H-1 type) and its hydrochloride, HBr salt, HI salt, ammonium sulfate, benzoate, tartrate, fumarate, trifluoroacetate and so on. Also, a method for producing the same, an intermediate used in producing the same, and a method for treating diseases such as diabetes using said structure are provided.