Crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol
The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.
1. A crystal form of 1,3-benzoxazol-5-ol monohydrate, having an X-ray powder diffraction pattern comprising a peak, in terms of 2θ, at about 12.2°.
2. The monohydrate of claim 1 having an X-ray powder diffraction pattern comprising peaks, in terms of 2θ, at about 9.2° and about 12.2°.
3. The monohydrate of claim 1 having an X-ray powder diffraction pattern comprising peaks, in terms of 2θ, at about 9.2°, about 12.2°, and about 15.2°.
4. The monohydrate of claim 1 having an X-ray powder diffraction pattern comprising peaks, in terms of 2θ, at about 9.2°, about 12.2°, about 15.2°, and about 24.3°.
5. The monohydrate of claim 1 having an X-ray powder diffraction pattern comprising peaks, in terms of 2θ, at about 9.2°, about 12.2°, about 15.2°, about 24.3°, about 25.4° and about 28.0°.
6. The monohydrate of claim 1 having an X-ray powder diffraction pattern substantially as shown in FIG. 1 (upper).
7. The monohydrate of claim 1 having a differential scanning calorimetry trace comprising a dehydration endotherm.
8. The monohydrate of claim 1 having a differential scanning calorimetry trace comprising dehydration endotherm having an onset at about 95° C. to about 120° C.
9. The monohydrate of claim 1 having a differential scanning calorimetry trace comprising a dehydration endotherm having an onset of about 95° C. to about 120° C. and a melting endotherm having an onset at about 250° C.
10. The monohydrate of claim 1 having a differential scanning calorimetry trace substantially as shown in FIG. 2 .
11. The monohydrate of claim 1 having a thermogravimetric analysis profile showing about 5% to about 7% weight loss from about 60° C. to about 150° C.
12. The monohydrate of claim 1 having a thermogravimetric analysis profile showing about 5.9% to about 6.4% weight loss from about 60° C. to about 150° C.
13. The monohydrate of claim 1 having a thermogravimetric analysis profile substantially as shown in FIG. 3 .