Polymorphic forms of (S).-tetrahydrofuran-3-yl-3-(3-(3-methoxy-4-(oxazol-5-yl) phenyl) ureido) benzylcarbamate
AssigneeVertex Pharmaceuticals Incorporated
InventorsTodd Blythe, Alex Eberlin, Michael Hurrey, David Jonaitis, Philip Nyce, Stephan Parent, John Snoonian
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Abstract
The present invention relates to polymorphic forms of (S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate (Compound 1): and pharmaceutical compositions thereof. The present invention also relates to processes to prepare compound 1 and pharmaceutical compositions thereof. Compound 1 is an IMPDH inhibitor useful in treating IMPDH-mediated diseases such as immune system related diseases, viral diseases, and cancers.
Claims10
A polymorphic Form A1 of (S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate wherein said polymorph is characterized by peak positions at about 21.8, 11.8, 16.0, 18.5, 20.1 and 23.6 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1 of(S)-tetrahydrofuran-3-yl 3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)benzylcarbamate wherein said polymorph exhibits a melting/decomposition endothermic event at about 215° C. as measured by a Differential Scanning Calorimeter.
A polymorphic Form A1, wherein said polymorphic Form A1 has a peak position at about 21.8 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 has peak position at about 11.8 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 has peak position at about 16.0 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 has peak position at about 18.5 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 has peak position at about 20.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 has peak position at about 23.6 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form A1, wherein said polymorphic Form A1 is characterized by an x-ray powder diffraction pattern as shown in FIG. 1.
Dependencies are inferred from the claim text.