Crystal form of five-membered n heterocyclic compound, and application thereof
Disclosed are a crystalline form of a five-membered N heterocyclic compound, particularly, a crystalline form of a compound as represented by formula I, and an application of the crystalline form in preparation of a medication for preventing or treating a disease benefiting from inhibition of capsid protein assembly.
1. A crystal of a compound of formula I,
wherein the crystal has characteristic diffraction peaks in an X-ray powder diffraction pattern at the following 20 angles: 8.25±0.20°, 10.10±0.20°, 14.46±0.20°, 15.48±0.20° and 18.97±0.20°.
2. The crystal of the compound of formula I according to claim 1 , wherein the XRPD pattern of the crystal is as shown in FIG. 1 .
3. The crystal of the compound of formula I according to claim 1 , wherein the crystal has a DSC curve having an endothermic peak at 227.34±5° C.
4. A crystalline form composition, wherein the crystal of the compound of formula I according to claim 1 accounts for 50% or more of the weight of the crystalline form composition.
5. A pharmaceutical composition, comprising a therapeutically effective amount of the crystal of the compound of formula I according to claim 1 .
6. The crystal of the compound of formula I according to claim 1 , wherein the crystal has characteristic diffraction peaks in an X-ray powder diffraction pattern at the following 20 angles: 8.25±0.20°, 9.46±0.20°, 10.10±0.20°, 14.46±0.20°, 15.48±0.20°, 18.97±0.20°, 20.33±0.20° and 22.02±0.20°.
7. The crystal of the compound of formula I according to claim 1 , wherein the crystal has characteristic diffraction peaks in an X-ray powder diffraction pattern at the following 20 angles: 8.25±0.20°, 9.46±0.20°, 10.10±0.20°, 14.46±0.20°, 15.48±0.20°, 18.97±0.20°, 20.33±0.20°, 20.80±0.20°, 21.67±0.20°, 22.02±0.20°, 24.37±0.20°, 26.37±0.20° and 30.77±0.20°.
8. The crystal of the compound of formula I according to claim 1 , wherein the crystal has characteristic diffraction peaks in an X-ray powder diffraction pattern at the following 20 angles: 8.25±0.20°, 9.46±0.20°, 10.10±0.20°, 14.46±0.20°, 15.48±0.20°, 18.97±0.20°, 20.33±0.20°, 20.80±0.20°, 21.67±0.20°, 22.02±0.20°, 22.88±0.20°, 23.93±0.20°, 24.37±0.20°, 24.97±0.20°, 26.37±0.20°, 28.68±0.20° and 30.77±0.20°.
9. The crystalline form composition according to claim 4 , wherein the crystal of the compound of formula I according to claim 1 accounts for 80% or more of the weight of the crystalline form composition.
10. The crystalline form composition according to claim 4 , wherein the crystal of the compound of formula I according to claim 1 accounts for 90% or more of the weight of the crystalline form composition.
11. The crystalline form composition according to claim 4 , wherein the crystal of the compound of formula I according to claim 1 accounts for 95% or more of the weight of the crystalline form composition.
12. A pharmaceutical composition, comprising a therapeutically effective amount of the crystalline form composition according to claim 5 .
13. A method for treating a disease benefiting from the inhibition of capsid protein assembly, comprising administering to a mammal in need of such treatment a therapeutically effective amount of the crystal of the compound of formula I according to claim 1 , wherein the disease benefiting from the inhibition of capsid protein assembly is a disease caused by hepatitis B virus infection.
14. A method for treating a disease benefiting from the inhibition of capsid protein assembly, comprising administering to a mammal in need of such treatment a therapeutically effective amount of the crystalline form composition according to claim 4 , wherein the disease benefiting from the inhibition of capsid protein assembly is a disease caused by hepatitis B virus infection.
15. A method for treating a disease benefiting from the inhibition of capsid protein assembly, comprising administering to a mammal in need of such treatment a therapeutically effective amount of the pharmaceutical composition according to claim 5 , wherein the disease benefiting from the inhibition of capsid protein assembly is a disease caused by hepatitis B virus infection.
16. A method for treating hepatitis B virus infection, comprising administering to a mammal in need of such treatment a therapeutically effective amount of the crystal of the compound of formula I according to claim 1 .