RU2014116196A - Crystal Anhydrous Delta Modification of N- (2-Chloro-6-Methylphenyl) -2 - [[6- [4- (2-Hydroxyethyl) -1-Piperazinyl] -2-Methyl-4-Pyrimidinyl] Amino] THIAZOLCARBOXAMIDE, METHOD FOR ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION ON ITS BASIS - Google Patents
Crystal Anhydrous Delta Modification of N- (2-Chloro-6-Methylphenyl) -2 - [[6- [4- (2-Hydroxyethyl) -1-Piperazinyl] -2-Methyl-4-Pyrimidinyl] Amino] THIAZOLCARBOXAMIDE, METHOD FOR ITS PRODUCTION AND PHARMACEUTICAL COMPOSITION ON ITS BASIS Download PDFInfo
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- RU2014116196A RU2014116196A RU2014116196/04A RU2014116196A RU2014116196A RU 2014116196 A RU2014116196 A RU 2014116196A RU 2014116196/04 A RU2014116196/04 A RU 2014116196/04A RU 2014116196 A RU2014116196 A RU 2014116196A RU 2014116196 A RU2014116196 A RU 2014116196A
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- piperazinyl
- pyrimidinyl
- methylphenyl
- hydroxyethyl
- chloro
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Abstract
1. Кристаллическая безводная δ-модификация N-(2-хлор-6-метилфенил)-2-[[6-[4-(2-гидроксиэтил)-1-пиперазинил]-2-метил-4-пиримидинил]амино]-5-тиазолкарбоксамида, характеризующаяся следующим набором межплоскостных расстояний (d, Å) и соответствующих им интенсивностей (I, %): 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%.2. Способ получения кристаллической безводной δ-модификации N-(2-хлор-6-метилфенил)-2-[[6-[4-(2-гидроксиэтил)-1-пиперазинил]-2-метил-4-пиримидинил]амино]-5-тиазолкарбоксамида по п. 1, характеризующейся тем, что растворяют N-(2-хлор-6-метилфенил)-2-[[6-[4-(2-гидроксиэтил)-1-пиперазинил]-2-метил-4-пиримидинил]амино]-5-тиазолкарбоксамид в органическом растворителе, выделяют кристаллиты из раствора методом замены растворителя или охлаждением с последующим фильтрованием, промыванием, замораживают кристаллиты и подвергают сублимационной сушке в течение 22-27 часов при конечной температуре на продукте не менее 25°C.3. Способ по п. 2, характеризующийся тем, что для промывания используют дистиллированную воду.4. Способ по п. 2 или 3, характеризующийся тем, что конечная температура при сублимационной сушке на продукте составляет 25°C-60°C.5. Применение кристаллической безводной δ-модификации N-(2-хлор-6-метилфенил)-2-[[6-[4-(2-гидроксиэтил)-1-пиперазинил]-2-метил-4-пиримидинил]амино]-5-тиазолкарбоксамида по п. 1, обладающей ингибирующей активностью в отношении тирозинкиназ, для приготовления фармацевтической композиции для лечен�1. Crystalline anhydrous δ-modification of N- (2-chloro-6-methylphenyl) -2 - [[6- [4- (2-hydroxyethyl) -1-piperazinyl] -2-methyl-4-pyrimidinyl] amino] - 5-thiazolecarboxamide, characterized by the following set of interplanar distances (d, Å) and their corresponding intensities (I,%): 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%; 2.777 - 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% .2. The method of obtaining crystalline anhydrous δ-modification of N- (2-chloro-6-methylphenyl) -2 - [[6- [4- (2-hydroxyethyl) -1-piperazinyl] -2-methyl-4-pyrimidinyl] amino] - 5-thiazolecarboxamide according to claim 1, characterized in that N- (2-chloro-6-methylphenyl) -2 - [[6- [4- (2-hydroxyethyl) -1-piperazinyl] -2-methyl-4 is dissolved -pyrimidinyl] amino] -5-thiazolecarboxamide in an organic solvent, crystallites are isolated from the solution by solvent replacement or cooling, followed by filtration, washing, crystallites are frozen and freeze-dried for 22-27 hours a final product temperature of at least 25 ° C.3. The method according to claim 2, characterized in that distilled water is used for washing. The method according to claim 2 or 3, characterized in that the final temperature during freeze-drying on the product is 25 ° C-60 ° C. 5. The use of crystalline anhydrous δ-modification of N- (2-chloro-6-methylphenyl) -2 - [[6- [4- (2-hydroxyethyl) -1-piperazinyl] -2-methyl-4-pyrimidinyl] amino] -5 -thiazolecarboxamide according to claim 1, having tyrosine kinase inhibitory activity, for the preparation of a pharmaceutical composition for the treatment of
Claims (5)
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RU2014116196/04A RU2567537C1 (en) | 2014-04-23 | 2014-04-23 | 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 |
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RU2014116196/04A RU2567537C1 (en) | 2014-04-23 | 2014-04-23 | 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 |
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