Crystalline forms of an antiviral prodrug

HK40137761APending Publication Date: 2026-09-18EXAVIR THERAPEUTICS
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Patent Information

Application Number
HK62026125328
Authority / Receiving Office
HK · HK
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-03-17
Filing Date
2026-06-25
Publication Date
2026-09-18
Estimated Expiration
2044-03-12

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Abstract

Disclosed herein, in part, are crystalline forms of a prodrug of an antiviral agent and methods of using the same in the treatment of viral infections.
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Description

Abstract This article partially reveals the crystalline forms of antiviral drug prodrugs and their application in the treatment of viral infections.

Claims

CLAIMS1. A crystalline form of a compound represented by:characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 17.8.

2. The crystalline form of claim 1, characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 20 at about 7.4, 17.8, and 22.2.

3. The crystalline form of claim 1 or 2, characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 20 at about 7.4, 17.5, 17.8, 18.7, and 22.2.

4. The crystalline form of any one of claims 1-3, characterized by a powder X-ray diffraction pattern having characteristic peaks in degrees 20 at about 6.8, 7.4, 16.7, 16.9, 17.5, 17.8, 18.2, 18.7, 21.9, and 22.2.

5. The crystalline form of any one of claims 1-4, characterized by a powder X-ray diffraction pattern substantially as depicted in Figure 1.

6. The crystalline form of any one of claims 1-5, wherein the powder X-ray diffraction pattern was obtained using Cu Ka radiation.

7. The crystalline form of any one of claims 1-6, characterized by a differential scanning calorimetry (DSC) profile having a characteristic endotherm with an onset of about 118 °C and a peak of about 120 °C.

8. A crystalline form of a compound represented by:characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 5.6.

9. The crystalline form of claim 8, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 5.6, 16.0, and 21.8.

10. The crystalline form of claim 8 or 9, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 5.6, 16.0, 21.8, 23.1, and 23.4.

11. The crystalline form of any one of claims 8-10, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 5.6, 7.4, 16.0, 16.9, 17.8, 18.3, 19.0, 21.8, 23. 1, and 23.4.

12. The crystalline form of any one of claims 8-11, characterized by a powder X-ray diffraction pattern substantially as depicted in Figure 2.

13. The crystalline form of any one of claims 8-12, wherein the powder X-ray diffraction pattern was obtained using Cu Ka radiation.

14. The crystalline form of any one of claims 8-13, characterized by a differential scanning calorimetry (DSC) profile having a characteristic endotherm with an onset of about 117 °C and a peak of about 120 °C.

15. A crystalline form of a compound represented by:characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 21.6.

16. The crystalline form of claim 15, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 7.0, 21.6, and 22.9.

17. The crystalline form of claim 15 or 16, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 7.0, 16.4, 21.6, 22.9, and 23.6.

18. The crystalline form of any one of claims 15-17, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 6.8, 7.0, 16.4, 16.6, 20.0, 21.6, 22.0, 22.7, 22.9, and 23.6.

19. The crystalline form of any one of claims 15-18, characterized by a powder X-ray diffraction pattern substantially as depicted in Figure 3.

20. The crystalline form of any one of claims 15-19, wherein the powder X-ray diffraction pattern was obtained using Cu Ka radiation.

21. The crystalline form of any one of claims 15-20, characterized by a differential scanning calorimetry (DSC) profile having a characteristic endotherm with an onset at about 119 °C and a peak at about 122 °C.

22. A mixture of crystalline forms of a compound represented by:characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 21.6.

23. The mixture of claim 22, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 7.0, 17.8, and 21.6.

24. The mixture of claim 22 or 23, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 7.0, 7.4, 17.8, 21.6, and 23.6.

25. The mixture of any one of claims 22-24, characterized by a powder X-ray diffraction pattern having a characteristic peak in degrees 20 at about 7.0, 7.4, 14.0, 16.3, 16.8, 17.8, 21.6, 23.6, 24.3, and 26.1.

26. The mixture of any one of claims 22-25, characterized by an XRPD pattern substantially as depicted in Figure 4.

27. The mixture of any one of claims 22-26, characterized by a differential scanning calorimetry (DSC) profile having a characteristic endotherm with an onset of about 119 °C and a peak of about 122 °C.

28. The mixture of any one of claims 33-27, wherein the powder X-ray diffraction pattern was obtained using Cu Ka radiation.

29. A method of treating, inhibiting, and / or preventing a viral infection in a patient in need thereof, comprising administering to the patient an effective amount the crystalline form of any one of claims 1-21.

30. A method of treating, inhibiting, and / or preventing a viral infection in a patient in need thereof, comprising administering to the patient an effective amount the mixture of any one of claims 22-28.

31. The method of claim 29 or 30, wherein the viral infection is a retroviral infection.

32. The method of any one of claims 29-31, wherein the viral infection is an HIV infection.