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专利权人:
F. HOFFMANN-LA ROCHE AG.*
发明人:
GOLDSMITH, RICHARD, A.,OLIVERO, ALAN, G.,PRICE, STEPHEN,DO, STEVEN,HEFFRON, TIM,STABEN, STEVEN,HEALD, ROBERT,NDUBAKU, CHUDI,BLAQUIERE, NICOLE,DUDLEY, DANETTE,FOLKES, ADRIAN, J.,KOLESNIKOV, ALEKSANDR,W
申请号:
MX2012003641
公开号:
MX2012003641A
申请日:
2010.09.27
申请国别(地区):
MX
年份:
2012
代理人:
摘要:
Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: 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, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of P13K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.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 lípidoquinasas, 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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http://www.ckcest.cn/home/

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