КРИСТАЛЛИЧЕСКАЯ БЕЗВОДНАЯ ДЕЛЬТА-МОДИФИКАЦИЯ N-(2-ХЛОР-6-МЕТИЛФЕНИЛ)-2-[[6-[4-(2-ГИДРОКСИЭТИЛ)-1-ПИПЕРАЗИНИЛ]-2-МЕТИЛ-4-ПИРИМИДИНИЛ]АМИНО]-5-ТИАЗОЛКАРБОКСАМИДА, СПОСОБ ЕЕ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕЕ ОСНОВЕ
Малин Александр Александрович (RU),Михайлов Олег Ростиславович (RU),Уваров Николай Александрович (RU)
申请号：
RU2014116196/04
公开号：
RU2014116196A
申请日:
2014.04.23
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
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 spacings (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% 2,757 - 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. A process for preparing 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 the dissolved N- (2-chloro-6-methylphenyl) -2 -. [[6- [4- (2-hydroxyethyl) -1-piperazinyl] -2-methyl-4 pyrimidinyl] amino] -5-thiazolecarboxamide in an organic solvent solution of crystallites separated by replacing the solvent or cooling followed by filtration, washing, crystallites frozen and freeze-dried for 22-27 hours, etc. a final product temperature of at least 25 ° C.3. A method according to claim. 2, characterized in that it is used for washing distilled vodu.4. A method according to claim. 2 or 3, characterized in that the final temperature of the freeze-dried product is at 25 ° C-60 ° C.5. 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 -tiazolkarboksamida according to claim. 1, having inhibitory activity against tyrosine kinases, for preparing a pharmaceutical composition for the treatment1. Кристаллическая безводная δ-модификация N-(2-хлор-6-метилфенил)-2-[[
