ROSCH, Esther,HOELIG, Peter,LINDLEY, David J.,SANZGIRI, Yeshwant D.,TONG, Ping
申请号：
PE0012302017
公开号：
PE12422017A1
申请日:
2011.10.05
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to Solid Dispersions containing a Melt Extruded apoptosis Inducing Agent of formula (i), where R0 is Halo R1 and R2 is H, Methyl or methoxy R3 and R4 are Methyl or methoxy if R1 and R2 are H or H IF R1 and R2 are Methyl or methoxy A1 and A2 are CH o n R5 is c1-c4 alkyl or halo Alkyl X is - or or - NH - and is - (CH2) n n is 0, 1,2 or 3 R6 is a Ring or heterocycle carbociclico between 3 and 7 members optionally replaced, among others. It is a selected Compound 4 - (4 - [2 - (4-chlorophenyl) - 4.4 - dimetilciclohex - 1 - 1 - il] methyl} piperazin-1-yl) - 2 - (1h indole - 5 - iloxi) - N - [3 - [4 - (Nitro 1 - tetrahydro - 2H - piran - 4 - ilpiperidin - 4-yl) amino] phenyl] sulfonyl) benzamide among others.This Compound is an inhibitor of the bcl-2 Family of Proteins are dispersed in a Solid Matrix comprising (a) a pharmaceutically acceptable water-soluble polymeric vehicle and (b) a pharmaceutically acceptable surfactant.It also relates to a Preparation Process which includes subjecting to high temperature Compound of formula I, (a) and (b)To provide a extruible semisolid mixture Extruding the mixture to cool The resulting semisolid Extruded and to provide a Solid Matrix which includes the vehicle and the Surfactant and Polymer in which the compound is dispersed in a non Crystalline form essentially.These Dispersions are useful in the treatment of neoplastic diseases such as cancer, mesothelioma, among othersSe refiere a dispersiones solidas extruidas por fusion que contienen un agente inductor de apoptosis de formula (I), donde R0 es halo R1 y R2 son H, metilo o metoxi R3 y R4 son metilo o metoxi si R1 y R2 son H, o son H si R1 y R2 son metilo o metoxi A1 y A2 son CH o N R5 es C1-C4 alquilo o haloalquilo, entre otros X es -O- o -NH- Y es -(CH2)n- n es 0, 1, 2 o 3 R6 es un anillo carbociclico o heterociclico de entre 3 y 7 miembros opcionalmente sustituido, entre otros. Es un compuesto seleccionado 4-(4-{[2-(4-clorofenil)-4,4-dimetilciclohex-1-en-1-il]metil}pipe
