CRYSTAL ANHYDROUS DELTA MODIFICATION OF N-(2-CHLORINE-6-METHYLPHENYLDIAZOMETHANE)-2-[6-[4-(2-HYDROXYETHYL)-1-PIPERAZINYL]-2-METHYL-4-PIRIMIDINYL]AMINO]-5-THIAZOLCARBOXAMIDE, METHOD OF ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION BASED ON IT Russian patent published in 2015 - IPC C07D417/12 A61K31/506 A61P35/00 A61P37/00 

Abstract RU 2567537 C1

FIELD: biotechnologies.

SUBSTANCE: invention relates to crystal anhydrous δ-modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide, characterized by the following set of interplanar distances (d, E) and the intensities corresponding to them (Irel., %): 9.637-69.1%; 7.928-29.2%; 6.415-100%; 5.819-39.4%; 5.529-3.0%; 4.941-27.2%; 4.887-5.6%; 4.549-72.6%; 4.092-3.8%; 4.037-3.2%; 3.847-35.0%; 3.782-5.8%; 3.751-5.2%; 3.642-3.9%; 3.607-2.7%; 3.442-16.6%; 3.383-3.0%; 3.183-27.4%; 3.122-21.7%; 3.099-5.6%; 2.958-6.9%; 2.905-3.4%; 2.763-7.5%; 2.757-7.8%; 2.694-9.2%; 2.551-12.6%; 2.516-2.6%; 2.463-3.9%; 2.292-3.9%; 2.270-5.0%; 2.137-4.0%; 2.112-3.5%; 2.024-3.7%; 1.906-3.4%; 1.867-3.0%; 1.780-6.0%. Crystal anhydrous delta modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide is obtained by dissolving of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide in organic solvent. Crystallites are extracted from the solution using the solvent switch method of replacement or by cooling with subsequent filtering, washing, the crystallites are frozen and subjected to sublimation drying during 22-27 hours at the final temperature on the product 25°C minimum. Crystal anhydrous δ-modification of N-(2-chlorine-6-methylphenyldiazomethane)-2-[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pirimidinyl]amino]-5-thiazolcarboxamide, which is characterized by inhibitory activity with reference to the tyrosine kinase, for preparation of pharmaceutical composition for treatment of immunological and oncological diseases.

EFFECT: increase of biological activity.

5 cl, 6 dwg, 3 tbl, 2 ex

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RU 2 567 537 C1

Authors

Malin Aleksandr Aleksandrovich

Mikhajlov Oleg Rostislavovich

Uvarov Nikolaj Aleksandrovich

Dates

2015-11-10Published

2014-04-23Filed