NEW POLYMORPHS OF CALCIUM SALT AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATING AGENTS Russian patent published in 2023 - IPC C07C233/60 A61K31/16 A61P37/00 

Abstract RU 2797511 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to methods for preparing a white crystalline polymorph A of the Ca hydrate salt of a compound according to formula I

Formula I

with the molar ratio of the specified compound in accordance with formula I to calcium 2±0.3 characterized by an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2 theta at the values shown below± 0.2:

2 theta=5.91°, 9.64°, 16.78°, 17.81°, 19.81°, 25.41° which includes the following steps:

•washing of the calcium salt of Vidofludimus Calcium or a solvate and/or hydrate thereof, preferably a crystalline polymorph Ca salt of vidofludimus or a solvate and/or hydrate thereof, with an aprotic organic solvent, preferably selected from the group consisting of DMF, DMSO, NMP, THF, Acetone, Dioxane, 2-Methyl-THF or (Methanol/CH2Cl2 (1:3)), preferably acetone, and

• suspending the obtained isolated Calcium-vidofludimus or its solvate and/or hydrate in an alcoholic solvent selected from the group consisting of methanol, ethanol or isopropanol, and adding water to the suspension at 15–80°C.

EFFECT: new method for obtaining a compound according to formula I in the form of a white crystalline polymorph A Ca salt, which can be used for the treatment and prevention of diseases where inhibition of dihydroorotate dehydrogenase (DHODH) is useful.

13 cl, 6 dwg, 3 tbl, 8 ex

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RU 2 797 511 C2

Authors

Vitt, Daniel

Muehler, Andreas

Groeppel, Manfred

Kohlhof, Hella

Dates

2023-06-06Published

2019-03-15Filed