A STABLE POLYMORPH OF THE SALT OF (2R)-4-OXO-4-[3-(TRIFIUOROMETHYL)-5,6- DIHYDRO[L,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-L-(2,4,54RIFLUOROPHENYL)BUTAN-2-AMINE WITH L-TARTARIC ACID

A STABLE POLYMORPH OF THE SALT OF (2R)-4-OXO-4-[3-(TRIFIUOROMETHYL)-5,6- DIHYDRO[L,2,4]TRIAZOLO[4,3-A]PYRAZIN-7(8H)-YL]-L-(2,4,54RIFLUOROPHENYL)BUTAN-2-AMINE WITH L-TARTARIC ACID

A stable polymorph (Form Z1) of the salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [152,4]triazolo[4,3-α]pyrazin-7(8H)-yl]- l-(2s4,5-trifluorophenyl)butan-2-amine (sitagliptin) with L-tartaric acid, of formula 1, which is a very suitable form of the active pharmaceutical ingredient of medici...

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Bibliographische Detailangaben
Hauptverfasser: KREJCIK, LUKAS, JARRAH, KAMAL, RICHTER, JINDRICH, LEHNERT, PETR, DAMMER, ONDREJ
Format: Patent
Sprache:eng ; fre
Schlagworte:
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
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Zusammenfassung:A stable polymorph (Form Z1) of the salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro [152,4]triazolo[4,3-α]pyrazin-7(8H)-yl]- l-(2s4,5-trifluorophenyl)butan-2-amine (sitagliptin) with L-tartaric acid, of formula 1, which is a very suitable form of the active pharmaceutical ingredient of medicinal products intended especially for treatment of diabetes type 2. A method of preparation of the stable polymorph (Form Z1) of the salt of sitagliptin with L-tartaric acid, as well as its use for the preparation of a pharmaceutical composition. L'invention porte sur un polymorphe stable (forme Zl) du sel de (2R)-4-oxo-4-[3-(trifluorométhyl)-5,6- dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]- 1-(2,4,5-trifluorophényl)butan-2-amine (sitagliptine) avec le L-acide tartrique, de formule 1, qui est une forme tout à fait appropriée du principe pharmaceutique actif de produits médicinaux destinés en particulier au traitement du diabète de type 2. L'invention porte également sur un procédé de préparation du polymorphe stable (forme Zl) du sel de sitagliptine avec le L-acide tartrique, ainsi que sur son utilisation pour la préparation d'une composition pharmaceutique.