C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 311/22 (2006.01) A61K 31/353 (2006.01) A61P 11/06 (2006.01) A61P 17/00 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01)
Patent
CA 2349776
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, Image wherein each novel composition has particular characteristics that contribute 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 wet granulation techniques. The novel ethylene diamine (mono) salt is also described, and demonstrates superior solubility and bioavailability. Additionally, polymorphic forms A and 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.
Allen Douglas John Meldrum
Joseph David Bruning
Sage Nancy Anne
Pfizer Products Inc.
Smart & Biggar
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