ZHEN Pinda (US),ЖЭНЬ Пинда (US),MARTIN Majkl (US),МАРТИН Майкл (US),IZBESTER Pol (US),ИЗБЕСТЕР Пол (US),LEJN Bendzhamin S. (US),ЛЭЙН Бенджамин С. (US),KROPP Dzhejson (US),КРОПП Джейсон (US),ZHEN Pinda,ЖЭНЬ Пинда,MARTIN Majkl,МАРТИН Майкл,IZBESTER Pol,ИЗБЕСТЕР Пол,LEJN Bendzhamin S.,ЛЭЙН Бенджамин С.,KROPP Dzhejson,КРОПП Джейсон
申请号:
RU2013137424
公开号:
RU0002626883C2
申请日:
2012.01.10
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to new polymorphic forms of the compounds of formula (I), having inhibitory action against phosphoinositide 3-kinase (PI3K). The compounds may be used to treat cancer, such as leukemia, lymphoma, inflammatory disease and autoimmune disease. The polymorphic forms of the compound of formula (I)is the polymorphic form C of the hydrate of the compound of formula (I), which has characteristic peaks in the x-ray powder diffraction pattern (XRPD) 2θ=10.4°(±0.2°), 13.3°(±0.2°) and 24.3°(±0.2°); Polymorph A, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 12.2°(±0.2°), and 18.3°(±0.2°); Polymorph B, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=7.9°(±0.2°), 13.4°(±0.2°), and 23.4°(±0.2°); polymorphic form D, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=11.4°(±0.2°), 17.4°(±0.2°), and 22.9°(±0.2°); polymorphic form E, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=6.7°(±0.2°), 9.3°(±0.2°) and 24.4°(±0.2°); Polymorphic form F, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.6°(±0.2°), 17.3°(±0.2°), and 24.6°(±0.2°); Polymorphic form G which is the solvate of the tert-butyl methyl ether of the compound of formula (I) and has characteristic peaks in the powder XRPD pattern 2θ=6.7°(±0.2°), 9.5°(±0.2°) and 19.0°(±0.2°); Polymorphic form H, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=8.9°(±0.2°), 9.2°(±0.2°) and 14.1°(±0.2°); Polymorphic Form I, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.7°(±0.2°), 19.3°(±0.2°), and 24.5°(±0.2°), and the polymorphic form J, which has characteristic peaks in the X-ray powder diffraction pattern (XRPD) 2θ=9.1°(±0.2°), 17.3°(±0.2°) and 18.3°(±0.2°). The invention also relates to a process of preparing form C. For example, mentioned process comprisi