摘要 |
<p>-368- BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE Abstract 5 Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, 11 2 solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z is CR or N; Z 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 and 7 X 2 is S, (iv) X 1 is S and X 2 is CR ; 7 (v) X 1 is NR and 8 X 2 is N, (vi) X is 1 N and X 2 is NR , 8 (vii) X 1 is CR 7 and X 2 is O, (viii) X is 1 O and X 2 is CR , 7 (ix) X 1 is CR 7 and X 2 10 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 pi 10 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. 15 (No suitable figure)</p> |
申请人 |
F. HOFFMANN-LA ROCHE AG |
发明人 |
BLAQUIERE, NICOLE;DO, STEVEN;DUDLEY, DANETTE;FOLKES, ADRIAN J.;GOLDSMITH, RICHARD A.;HEALD, ROBERT;HEFFRON, TIM;KOLESNIKOV, ALEKSANDR;NDUBAKU, CHUDI;OLIVERO, ALAN G.;PRICE, STEPHEN;STABEN, STEVEN;WEI, BINQING |