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EXTRUSION-PRODUCED SOLID DISPERSIONS CONTAINING AN APPTOSIS INDICATING PRODUCT
专利权人:
ЭБОТТ ГМБХ УНД КО.КГ (DE);ЭББВИ ИНК. (US)
发明人:
РЕШ Эстер (DE),ХЕЛИГ Петер (DE),ЛИНДЛИ Дэвид Дж. (US),САНЗГИРИ Йешвант Д. (US),ТУН Пин (US)
申请号:
RU2013124823/04
公开号:
RU2013124823A
申请日:
2011.10.05
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A solid dispersion comprising, in a substantially non-crystalline form, a compound of Formula I where: R is halogen; R and R are H or independently methyl or methoxy; R and R are independently methyl or methoxy if R and R are H, or H if R and R are independently methyl or methoxy; A and A are each independently CH or N; R is C 1-6 alkyl or haloalkyl, C 1-6 alkylsulfonyl or haloalkylsulfonyl, halogen, nitro or cyano; X is —O— or —NH—; Y is - (CH), where n = 0 , 1, 2 or 3; and R is an unsubstituted or substituted 3-7 membered carbocyclic or heterocyclic ring, as defined herein, or is NRR; wherein, if R is NRR, R and R are each independently H or R- (CH) -, and not more than one of R and R denotes H, where each R independently represents a 3-7 membered carbocyclic or heterocyclic ring, optionally substituted with no more than two Z groups, as defined below, and each m independently represents 0 or 1; and, if R denotes a substituted carbocyclic or heterocyclic ring, the substituents on it represent no more than two Z and / or no more than one Z group, and the Z groups are independently selected from (a) C 1-6 alkyl, C 2-6 alkenyl, C 1 2 alkoxy, C 1-6 alkylthio, C 1-6 alkyl, C 1-6 alkylsulfonyl, C 1-6 alkylsulfonylamino, C 1-6 alkylcarbonyl, C 1-6 alkylcarbonylamino and C 1-6 alkylcarboxy, each of which may optionally be substituted with one or more substituents independently selected from halogen, hydroxy, C 1 alkoxy, amino, C 1-6 alkyl, di (C 1-6 alkyl) amines o and cyano, (b) halogen, (e) hydroxy, (f) amino, and (g) oxo groups, and wherein Zoboznachaet (i) another 3-6 membered carbocysteine1. Твердая дисперсия, включающая, в по существу некристаллической форме, соединение Формулы Iгде:Rобозначает галоген;Rи Rобозначают Н или независимо обозначают метил или метокси;Rи Rнезависимо обозначают метил или метокси, если Rи Rобозначают Н, или обозначают Н, если Rи Rнезависимо обозначают метил или метокси;Aи Aобозначают, каждый независимо, CH или N;Rобозначает Cалкил или га
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