RESH Ester (DE),РЕШ Эстер (DE),KHELIG Peter (DE),ХЕЛИГ Петер (DE),LINDLI Devid Dzh. (US),ЛИНДЛИ Дэвид Дж. (US),SANZGIRI Jeshvant D. (US),САНЗГИРИ Йешвант Д. (US),TUN Pin (US),ТУН Пин (US),RESH Ester,РЕШ Эстер,KHELIG Peter,ХЕЛИГ Петер,LINDLI Devid Dzh.,ЛИНДЛИ Дэвид Дж.,SANZGIRI Jeshvant D.,САНЗГИРИ Йешвант Д.,TUN Pin,ТУН Пин
申请号：
RU2016104763
公开号：
RU0002633353C1
申请日:
2011.10.05
申请国别(地区):
RU
年份:
2017
代理人:
摘要：
FIELD: pharmacology.SUBSTANCE: dispersion includes a compound of Formula I , where the value of R0, R1, R2, R3, R4, A, B, R5, X, Y and R6 groups is determined in the claims, or a pharmaceutically acceptable salt thereof. The compound of Formula I or its pharmaceutically acceptable salt are dispersed in a solid matrix which contains (a) at least one pharmaceutically acceptable water-soluble polymer carrier, and (b) at least one pharmaceutically acceptable surfactant. At least 5% of the compound of Formula I or its pharmaceutically acceptable salt is presented in the crystalline form, as studied by X-ray diffractometry. The compound or its pharmaceutically acceptable salt is presented in an amount equal to an amount of the parent compound from approximately 5% to approximately 40% by weight； at least one pharmaceutically acceptable water-soluble polymer carrier is presented in an amount from approximately 40% to approximately 85% by weight, and at least one pharmaceutically acceptable surfactant is presented in an amount from approximately 5% to approximately 20% by weight. A compound of Formula I in which R0 is chlorine, R1 and R2 are H, R3 and R4 are methyl, A is N, B is CH, R5 is nitro, X is -NH-, Y is - (CH2)n-, where n=1 , and R6 is selected from the group consisting of tetrahydropyranyl and 4-hydroxy-4-methylcyclohexyl, is excluded from the scope of the compound of Formula I. Methods for preparation of a solid dispersion suitable for oral delivery, a pharmaceutical dosage form and a solid dispersion for use as a medicament are also proposed.EFFECT: solid dispersion is applicable for oral administration to the patient in need of treatment of a disease characterised by overexpression of one or more Bcl-2 family antiapoptotic proteins.51 cl, 1 dwg, 17 tbl, 19 exИзобретение относится к твердой дисперсии, пригодной для индукции апоптоза. Дисперсия включает соединение Формулы Iгде значение групп R0, R1, R2, R3, R4, A, В, R5, X, Y и R6 определено в формуле изобретения
