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COMBINACIONES FARMACEUTICAS
专利权人:
NOVARTIS AG
发明人:
CHEN, YAN,HUANG, XIZHONG,MURPHY, LEON,NYFELER, BEAT
申请号:
PE0007762013
公开号:
PE02032014A1
申请日:
2011.10.03
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Referring to a Pharmaceutical Combination comprising: a) a compound derived from imidazoquinolina inhibitor of phosphatidyl inositol 3 Kinase (PI3K) catalytic \/ mammalian target of rapamycin (mTOR) of formula (i), wherein R1 is optionally substituted phenyl or naphthyl with Halogen, haloalqui So, among others R2 is o or s C1 - C7 R3 is alkyl R4 is piridilo, pirimidinilo, quinolinilo,Among others, R5 is H or Halogen n is 0 OR 1 R6 R7 is H or Amine oxide and (b) a compound such as allosteric inhibitor of mTOR Rapamycin (sirolimus, everolimus (RAD) RAD001), CCI 779 and deferolimus (AP \/ mk 9570 23573).Preferred compounds of formula (i): 2 - methyl - 2 - [4 - (3 - methyl - 2 - oxo - 8 - quinolin-1 - 3 - il - 2,3 Dihydro imidazo [4,5-c] quinolin-1 - 1 - il) phenyl] - propionitrilo, (6 - 8 - methoxy pyridin-3-yl) - 3 - methyl - 1 - [4 - (piperazin-1-yl - 3 - trifluoro methyl phenyl) - 1,3 Dihydro imidazo [4,5-c] quinolin-2 - ona, among others. This combination is useful in the treatment of a proliferative disease of the kinase mTOR dependentREFERIDA A UNA COMBINACION FARMACEUTICA QUE COMPRENDE: a) UN COMPUESTO DERIVADO DE IMIDAZOQUINOLINA INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 CATALITICA (PI3K)/OBJETIVO DE MAMIFERO DE RAPAMICINA (mTOR) DE FORMULA (I), DONDE R1 ES NAFTILO O FENILO OPCIONALMENTE SUSTITUIDOS CON HALOGENO, HALOALQUILO, ENTRE OTROS R2 ES O O S R3 ES ALQUILO C1-C7 R4 ES PIRIDILO, PIRIMIDINILO, QUINOLINILO, ENTRE OTROS R5 ES H O HALOGENO n ES 0 O 1 R6 ES OXIDO R7 ES H O AMINO Y b) UN COMPUESTO ALOSTERICO INHIBIDOR DE mTOR TAL COMO RAPAMICINA RAD (SIROLIMUS), EVEROLIMUS (RAD001), CCI-779 Y DEFEROLIMUS (AP-23573/MK-8669). SON COMPUESTOS PREFERIDOS DE FORMULA (I): 2-METIL-2-[4-(3-METIL-2-OXO-8-QUINOLIN-3-IL-2,3-DIHIDRO-IMIDAZO-[4,5-c]-QUINOLIN-1-IL)-FENIL]-PROPIONITRILO, 8-(6-METOXI-PIRIDIN-3-IL)-3-METIL-1-(4-PIPERAZIN-1-IL-3-TRIFLUORO-METIL-FENIL)-1,3-DIHIDRO-IMIDAZO-[4,5-c]-QUINOLIN-2-ONA, ENTRE OTROS. DICHA COMBINACION ES UTIL EN EL TRATAMIENTO DE UNA EN
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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