BLAQUIERE, Nicole N,DO, Steven S,DUDLEY, Danette D,FOLKES, Adrian J. AJ,GOLDSMITH, Richard A. RA,HEALD, Robert R,HEFFRON, Tim T,KOLESNIKOV, Aleksandr A,NDUBAKU, Chudi C,OLIVERO, Alan G. AG,PRICE, Step,.布拉奎爾,.多,.達德利,.福克斯,.戈德史密斯,.希爾德,.赫夫龍,.科萊斯尼科夫,NDUB
申请号:
HK16104456.1
公开号:
HK1216529A
申请日:
2013.03.04
申请国别(地区):
HK
年份:
2016
代理人:
摘要:
Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z 1 is CR 1 or N; Z 2 is CR 2 or N; Z 3 is CR 3 or N; Z 4 is CR 4 or N; and where (i) X 1 is N and X 2 is S, (ii) X 1 is S and X 2 is N, (iii) X 1 is CR 7 and X 2 is S, (iv) X 1 is S and X 2 is CR 7 ; (v) X 1 is NR 8 and X 2 is N, (vi) X 1 is N and X 2 is NR 8 , (vii) X 1 is CR 7 and X 2 is O, (viii) X 1 is O and X 2 is CR 7 , (ix) X 1 is CR 7 and X 2 is C(R 7 ) 2 , (x) X 1 is C(R 7 ) 2 and X 2 is CR 7 ; (xi) X 1 is N and X 2 is O, or (xii) X 1 is O and X 2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, 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.