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...

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Bibliographische Detailangaben
Hauptverfasser: ALLEN, DOUGLAS JOHN MELDRUM, SAGE, NANCY ANNE, JOSEPH, DAVID BRUNING
Format: Patent
Sprache:eng ; fre
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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.