ГОКХАЛЕ Раджив (US),МАРШ Кеннан К. (US),ШИ И. (US)
申请号：
RU2012101627/15
公开号：
RU2012101627A
申请日:
2010.06.14
申请国别(地区):
RU
年份:
2013
代理人:
摘要：
1. A liquid pharmaceutical composition comprising an aqueous medium containing a particulate solid compound suspended in it, having a particle size D of not more than about 3 microns； where the compound is represented by formula I: wherein X is chloro or fluoro； and (1) X is azepan-1-yl, morpholin-4-yl, l, 4-oxazepan-4-yl, pyrrolidin-1-yl, -N (CH), -N (CH) (CH (CH) ), 7-azabicyclo [2.2.1] heptan-7-yl or 2-oxa-5-azabicyclo [2.2.1] hept-5-yl； and R is where X is —CH—, —C (CH) - or —CHCH—； X and Xoba are —H or both are methyl； and X is fluoro, chloro, bromo or iodo； or (2) X is azepan-1-yl, morpholin-4-yl, pyrrolidin-1-yl, -N (CH) (CH (CH)) or 7-azabicyclo [ 2.2.1] heptan-7-yl； and R is where X, X, and X are as described above； or (3) X is morpholin-4-yl or —N (CH)； and R is where X is as defined above； or a pharmaceutically acceptable salt, prodrug, prodrug salt or metabolite thereof； and wherein the aqueous medium further comprises at least one pharmaceutically acceptable surfactant and at least one pharmaceutically acceptable alkalizing agent in amounts that, taken together, are effective in inhibiting particle size increase. The composition of claim 1, wherein the compound has a particle size D of not more than approximately 800 nm and / or a particle size of D of not more than approximately 350 nm. A composition according to claim 1 or 2, wherein the drug compound is present in an amount of about 20 to 200 mg / ml. The composition of claim 1, wherein the at least one surfactant is selected from the group consisting of chloro1. Жидкая фармацевтическая композиция, включающая водную среду, содержащую суспендированное в ней твердое соединение в форме частиц, имеющее размер частиц Dне более чем приблизительно 3 мкм； где соединение представлено формулой I:гдеXпредставляет собой хлор или фтор； и(1) Xпредставляет собой азепан-1-ил, морфолин-4-ил, l,4-оксазепан-4-ил, пирролидин-1-ил, -N(CH), -N(CH)(CH(CH)), 7-азабицикло[2.2.1]гептан-7-ил или 2-окса-5-азабицикло[2.2.1]гепт-
