NEW POLYCRYSTALLINE FORM OF TENOFOVIR PRODRUG AND METHOD FOR PRODUCTION THEREOF AND USE THEREOF Russian patent published in 2019 - IPC C07F9/6561 A61K31/675 A61P31/18 A61P31/20 

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel crystalline form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate, method obtaining a pharmaceutical composition based thereon and use thereof for treating or preventing AIDS or hepatitis. Disclosed is a novel crystalline form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate of formula (I)

characterized by an X-ray powder diffraction pattern with the following diffraction peaks at 2θ ±0.20°: 5.08, 12.44, 13.18, 22.37, 23.37 and 28.56. Disclosed is a method of producing said crystalline form, involving dissolving any form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine fumarate in anhydrous methanol/n-heptane, anhydrous ethanol or isopropanol/methyl-tert-butyl ether while heating, cooling obtained solution for crystal deposition and filtering out the crystal.

EFFECT: disclosed is a crystalline form which is characterized by high bioavailability and stability, improving quality of medicinal products production, effective method of its preparation, as well as a composition based on it, effective for treating or preventing AIDS or hepatitis B.

11 cl, 3 ex, 2 tbl, 2 dwg