Crystal form of tenofovir alafenamide salt, preparation method and use thereof
AssigneeShanghai Begreat Pharmatech
InventorXiaoming MENG
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Abstract
Disclosed are a new polymorph II, crystal form A and B of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate, and preparation methods and pharmaceutical use thereof. The crystal form II is a hemi-fumarate; the crystal form A is a mono-fumarate; and the crystal form B is a sesqui-fumarate. Compared with the existing crystal form, the new crystal forms have obvious advantages in solubility, stability and preparation process.
Claims22
A crystalline form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate designated as crystalline form A, having an X-ray powder diffraction pattern comprising diffraction peaks at at least one 2θ value of:
- 23.8±0.2, 10.5±0.2, 28.5±0.2, 21.2±0.2, or 19.5±0.2.
A crystalline form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate designated as crystalline form B, having an X-ray powder diffraction pattern comprising diffraction peaks at at least one 2θ value of:
- 10.5±0.2, 21.0±0.2, 10.9±0.2, 27.2±0.2, or 22.5±0.2.
A crystalline form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate designated as crystalline form II, having an X-ray powder diffraction pattern comprising diffraction peaks at at least one 2θ value of:
- 26.6±0.2, 21.3±0.2, 27.1±0.2, 19.6±0.2, or 18.7±0.2.
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Dependencies are inferred from the claim text.