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Inhibitors of the PI3K benzoxepina compounds and Methods of use
专利权人:
F. HOFFMANN - LA ROCHE AG
发明人:
FOLKES, ADRIAN,GOLDSMITH, RICHARD,HEFFRON, TIM,STABEN, STEVEN,NDUBAKU, CHUDI,BLAQUIERE, NICOLE,DO, STEVEN,DUDLEY, DANETTE,HEALD, ROBERT,KOLESNIKOV, ALEKSANDR,OLIVERO, ALAN G,PRICE, STEPHEN,WEI, BINQIN
申请号:
ECSP12011752
公开号:
ECSP12011752A
申请日:
2012.09.28
申请国别(地区):
EC
年份:
2012
代理人:
摘要:
The benzoxepine compounds of the formula I, including their stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts, in which: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C (R7) 2, (x) X1 is C (R7) 2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, they are useful for inhibiting lipid kinases, including p110 alpha and other isoforms of PI3K,And treating diseases like cancer through fat quinine. Describe the use of the first formulation compound used to diagnose, prevent or treat these "in vitro" disorders,In situ" and "current" or related pathologies in mammalian cells.Los compuestos de benzoxepina de la fórmula I, incluidos sus estereoisómeros, isómeros geométricos, tautómeros, solvatos, metabolitos y sales farmacéuticamente aceptables, en los que: Z1 es CR1 o N; Z2 es CR2 o N; Z3 es CR3 o N; Z4 es CR4 o N; y en los que (i) X1 es N y X2 es S, (ii) X1 es S y X2 es N, (iii) X1 es CR7 y X2 es S, (iv) X1 es S y X2 es CR7; (v) X1 es NR8 y X2 es N, (vi) X1 es N y X2 es NR8, (vii) X1 es CR7 y X2 es O, (viii) X1 es O y X2 es CR7, (ix) X1 es CR7 y X2 es C(R7)2, (x) X1 es C(R7)2 y X2 es CR7; (xi) X1 es N y X2 es O, o (xii) X1 es O y X2 es N, son útiles para inhibir las lípido-quinasas, incluidas la p110 alfa y otras isoformas de la PI3K, y para tratar trastornos tales como el cáncer mediado por las lípido-quinasas. Se describen métodos de uso de los compuestos de la fórmula I para el diagnóstico, la prevención o el tratamiento de dichos trastornos "in vitro", "in situ" e "in vivo" en células de mamíferos, o de estados patológicos asociados.
来源网站:
中国工程科技知识中心
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