NOVEL CRYSTALLINE FORMS OF (3S-TRANS)-2-[3,4-DIHYDRO-4-HYDROXY-3-(PHENYLMETHYL)-2H-1-BENZOPYRAN-7-YL]-4-(TRIFLUOROMETHYL)-BENZOIC ACID
The present invention provides novel polymorphic forms of anhydrous crystalline (3S- trans)-2-[3,4-dihydro-4-hydroxy-3-(phenylmethyl)-2H-1-benzopyran-7-yl]-4- (trifluoromethyl)- benzoic acid, hereinafter compound (I), and a novel salt, and a hydrate of said compound, wherein each novel composition h...
Gespeichert in:
Hauptverfasser: | , , |
---|---|
Format: | Patent |
Sprache: | eng ; fre |
Schlagworte: | |
Online-Zugang: | Volltext bestellen |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | The present invention provides novel polymorphic forms of anhydrous crystalline (3S- trans)-2-[3,4-dihydro-4-hydroxy-3-(phenylmethyl)-2H-1-benzopyran-7-yl]-4- (trifluoromethyl)- benzoic acid, hereinafter compound (I), and a novel salt, and a hydrate of said compound, wherein each novel composition has particular characteristics that contribut e to its use in pharmaceutical formulations. The novel monohydrate of compound (1) is described, which can be advantageously isolated from water wet solvents and formulated via we t granulation techniques. The novel ethylene diamine (mono) salt is also described, and demonstrates superior solubility and bioavailability. Additionally, polymorphic forms A a nd B of anhydrous crystalline compound (I) are described, wherein form A has superior thermal stability, and form B has superior solubility. Additionally, there are described pharmaceutical compositions that comprise these substances, and methods for the treatment of disease states therewith, in particular, the treatment of inflammatory diseases. |
---|