Crystalline forms of a macrolide, and uses therefor
View Patent ↗New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein.
1. The compound CEM-101 in crystalline form, where the form is Form I having an X-ray powder diffraction pattern including a peak at about °2θ=6.2, 8.5, or 8.8 or a combination thereof, or Form II having an X-ray powder diffraction pattern including a peak at about °2θ=5.6 or 7.9 or a combination thereof.
2. The form of claim 1 which is Form I of CEM-101 having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=6.2, 8.5, 8.8, 10.5, 13.2, and 18.6.
3. The form of claim 1 which is Form I of CEM-101 having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=8.8, 10.5, 13.2, and 18.6.
4. The form of claim 1 which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=6.2 and 8.8.
5. The form of claim 1 which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=8.5 and 8.8.
6. The form of claim 1 which is Form I of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=6.2, 8.5, and 8.8.
7. CEM-101, comprising Form I of CEM-101 according to claim 2 having an X-ray powder diffraction pattern including at least three peaks at approximate positions selected from the group consisting of about °2θ=8.5, 8.8, 10.5, 13.2, and 18.6.
8. CEM-101 according to claim 7 that is substantially free of Form II.
9. CEM-101 according to claim 7 as determined by the X-ray powder diffraction pattern, wherein one or more peaks at °2θ=5.6, 7.9, 9.8, or 11.7 are absent or nearly absent.
10. CEM-101 according to claim 7 as determined by the X-ray powder diffraction pattern, wherein one or more peaks at °2θ=5.6 or 7.9 are absent or nearly absent.
11. The form of claim 1 which is Form II of CEM-101 having an X-ray powder diffraction pattern with at least three peaks at approximate positions selected from the group consisting of about °2θ=5.6, 7.9, 9.3, 9.8, 11.7, 12.9, and 16.7.
12. The form of claim 1 which is Form II of CEM-101 having an X-ray powder diffraction pattern with at least three peaks at approximate positions selected from the group consisting of about °2θ=5.6, 7.9, 9.8, 11.7, 12.9, and 16.7.
13. The form of claim 1 which is Form II of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=5.6 and 7.9.
14. The form of claim 1 which is Form II of CEM-101 having an X-ray powder diffraction pattern including peaks at approximate positions of about °2θ=5.6, 7.9, and 9.8.
15. CEM-101, comprising Form 11 of CEM-101 according to claim 11 having an X-ray powder diffraction pattern with at least three peaks at approximate positions selected from the group consisting of about °2θ=5.6, 7.9, 9.8, 11.7, 12.9 and 16.7.
16. CEM-101 according to claim 15 that is substantially free of Form I.
17. CEM-101 according to claim 15 as determined by the X-ray powder diffraction pattern, wherein one or more peaks at about °2θ=8.5 or 8.8 are absent or nearly absent.
18. The form of claim 1 having an X-ray powder diffraction pattern substantially the same as that of FIG. 1 .
19. The form of claim 1 having an X-ray powder diffraction pattern substantially the same as that of FIG. 2 .
20. A pharmaceutical composition comprising CEM-101 in crystalline form according to claim 1 and further comprising at least one pharmaceutically acceptable carrier, diluent, or excipient, or a combination thereof.
21. A method of treatment of a bacterial infection, a protozoal infection, or a disorder caused at least in party by a bacterial infection or protozoal infection in a host animal, the method comprising the step of administering to the host animal a therapeutically effective amount of CEM-101 in crystalline form according to claim 1 , or a pharmaceutical composition thereof further comprising at least one pharmaceutically acceptable carrier, diluent, or excipient, or a combination thereof.
22. The method of claim 21 wherein the host animal is a mammal, a fish, a bird or a reptile.
23. The method of claim 21 wherein the host animal is a human.