Crystal form of tenofovir prodrug, preparation method thereof, and method of use thereof
US9840525B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 21, 2015 |
| Grant date | Dec 12, 2017 |
| Priority date | — |
| Expiry date | Jul 21, 2035 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/13
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A crystal form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxyl]propyl]adenine fumarate of formula (I) is provided. Also provided is a preparation method and method of using the crystal form. Specifically, a crystal form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxyl]propyl]adenine fumarate of formula (I) having an X-ray powder diffraction (XRPD) spectrum including diffraction peaks at 2θ±0.20° of 5.08, 12.44, 13.18, 22.37, 23.37 and 28.56 is provided. The crystal form provided herein has high bioavailability, significant efficacy, good stability, high yield and high purity, and contributes to the selection and design of a drug administration route and the determination of process parameters of a pharmaceutical preparation, thereby improving drug production quality.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.