STOKBRUKS Sigrid Karl Marija (BE),СТОКБРУКС Сигрид Карл Мария (BE),LEJS Karina (BE),ЛЕЙС Карина (BE),SUINNI Kelli Ehnn (BE),СУИННИ Келли Энн (BE),VUJTS Stejn (BE),ВУЙТС Стейн (BE),KhORVAT Andrash (BE),STOKBRUKS SIGRID KARL MARIJA,СТОКБРУКС Сигрид Карл Мария,LEJS KARINA,ЛЕЙС Карина,SUINNI KELLI EHNN,СУИННИ Келли Энн,VUJTS STEJN,ВУЙТС Стейн,KHORVAT ANDRASH,ХОРВАТ Андраш
申请号:
RU2009132660/04
公开号:
RU0002533830C2
申请日:
2008.02.01
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a crystalline form of a solid-state compound of formulahaving an X-ray powder diffraction characterised by peaks as follows: (i) 8.5°±0.2°, 10.7°±0.2°, 13.7°±0.2°, 14.8°±0.2° and 17.1°±0.2° at a diffraction angle, two theta (form I); (ii) 4.6°±0.2°, 6.5°±0.2°, 10.2°±0.2°, 12.9°±0.2° and 14.4°±0.2° at a diffraction angle, two theta (form II); (iii) 6.5°±0.2°, 9.8°±0.2° and 17.8°±0.2° at a diffraction angle, two theta (form III); (iv) 5.6°±0.2°, 9.6°±0.2°, 11.8°±0.2°, 15.9°±0.2° and 17.1°±0.2° at a diffraction angle, two theta (form IV); (v) 9.6°±0.2° and 19.0°±0.2° at a diffraction angle, two theta (form V); (vi) 4.4°±0.2°, 6.5°±0.2°, 9.9°±0.2°, 10.5°±0.2° and 12.9°±0.2° at a diffraction angle, two theta (form VI). The invention also refers to a mixture of two or more crystalline forms I, II, III, IV, V and VI of the compound of formula (I) for treating HCV and to a mixture of two or more crystalline forms I, II, III, IV, V and VI of the compound of formula (I) and an amorphic form of the compound of formula (I) for treating HCV. The crystalline form (I) is prepared by: a) boiling the mixture of polymorphs I and II in 1-butanol or 2-propanol in a back flow condenser to produce a transparent solution; and b) spontaneous cooling of the solution to a room temperature while stirring, and then filtering and recovering crystalline form I. The method for preparing crystalline form II involves: a) preparing a suspension of the amorphic form of the compound of formula (I) in isopropanol; b) mixing the suspension at a room temperature; and c) fusing the suspension with fusing crystals of form II or form I while stirring, then filtering and drying at 60°C. There are also presented versions of the method for preparing the crystalline form (I) and (II) and forms (III), (IV) (V) and (VI). Besides, the invention refers to a pharmaceutical composition for treating HCV containing the crystalline form of the compound of for