CRYSTALLINE FORMS OF 9-AMINOMETHYL-SUBSTITUTED TETRACYCLINE COMPOUND AND THEIR PRODUCTION METHOD Russian patent published in 2022 - IPC C07D209/54 A61K31/65 A61P31/00 A61P31/04 A61P35/00 A61P3/10 

Abstract RU 2764723 C2

FIELD: medicine.

SUBSTANCE: invention relates to a method for producing a crystalline form I of a compound of (4S,4aS,5aR,12aS)-9-(3-azabicyclo[3.1.0]hexan-3-ylmethyl)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a, 5,5a, 6,11,12a-octahydrotetracene-2-carboxamide, represented by the formula (1), where the specified crystalline form is characterized by the presence of powder X-ray diffractograms having following characteristic peaks expressed with 2θ degrees, when measuring using Cu-Ka radiation: 10,6°±0,2°, 13,3°±0,2°, 15,9°±0,2°, 24,0°±0,2°; intended for the production of a drug for the treatment and/or prevention of an infectious disease caused by bacteria sensitive to tetracycline and/or bacteria resistant to tetracycline. The method is characterized in that the compound represented by the formula (1) is placed in anhydrous acetonitrile or in tetrahydrofuran, the resulting mixture is heated at mixing with the following isolation of the crystalline form I by filtration.

EFFECT: obtaining a stable crystalline form of a compound of the formula (1).

formula (1)

1 cl, 2 tbl, 14 dwg, 4 ex

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RU 2 764 723 C2

Authors

Huang, Zhenhua

Hong, Mei

Jiang, Chen

Dates

2022-01-19Published

2017-06-22Filed