BLAQUIERE, NICOLE,DO, STEVEN,DUDLEY, DANETTE,FOLKES, ADRIAN J.,HEALD, ROBERT,HEFFRON, TIMOTHY,JONES, MARK,KOLESNIKOV, ALEKSANDR,NBUDAKU, CHUDI,OLIVERO, ALAN G.,PRICE, STEPHEN,STABEN, STEVEN,WANG, LAN
申请号：
PE2012000390
公开号：
PE20121025A1
申请日:
2010.09.27
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
The invention relates to a benzoxazepina derivative of formula (I),Where Z1 is CR1 or N； Z2 is CR2 or N； Z3 is CR3 or N； Z4 is Cr4 or N； B is a pyrazole or pyridan ring combined with benzoxazepina ring, such as (a),(b)(c)Among others, R1, R2, R3 and R4 are h, F, CN, NO2； a is C (= O) nr5r6, nr5r6, etc.； R5 is h or C1-C12 tar, which can be replaced by F, Cl, CN, COH, etc.； R6 is C1-C12, arilo c6-c20, carboc3-c12, etc. 1,1,1,1,1,1,1,1,1,1,1,1,1,1,1,4]]] - dibenzo-2,2,4-triazole-5-il-8-bromo-4,5-dihydrobenzo-2h-oxepino - [4,5-d] pyrazole,There are others A pharmaceutical composer was also mentioned These compounds inhibit the activity of quiescent enzyme PI3 and are useful tools for the treatment of cancer.REFERIDA A UN DERIVADO DE BENZOXAZEPINA DE FORMULA (I), DONDE Z1 ES CR1 O N； Z2 ES CR2 O N； Z3 ES CR3 O N； Z4 ES CR4 O N； B ES UN ANILLO PIRAZOLILO O IMIDAZOLILO FUSIONADO CON EL ANILLO DE LA BENZOXAZEPINA TAL COMO (a), (b), (c), ENTRE OTROS； R1, R2, R3 Y R4 SON H, F, CN, NO2, ENTRE OTROS； A ES C(=O)NR5R6, NR5R6, ENTRE OTROS； R5 ES H O ALQUILO C1-C12 OPCIONALMENTE SUSTITUIDO CON F, Cl, CN, COOH, ENTRE OTROS； R6 ES ALQUILO C1-C12, ARILO C6-C20, CARBOCICLILO C3-C12, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-(2,4-DIFLUORFENIL)-N-METIL-4,5-DIHIDROBENZO[b]PIRAZOLO-[1,5-d][1,4]OXAZEPINA-2-CARBOXAMIDA, 2-(1-(2-CLOROFENIL)-1H-1,2,4-TRIAZOL-5-IL)-5,6-DIHIDRO-BENZO[f]IMIDAZO[1,2-d][1,4]-OXAZEPINA-10-CARBOXAMIDA, 2-(1-(2,4-DIFLUORFENIL)-1H-1,2,4-TRIAZOL-5-IL)-8-BROMO-4,5-DIHIDROBENZO-2H-OXEPINO-[4,5-d]PIRAZOL, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA QUINASA PI3 Y SON UTILES EN EL TRATAMIENTO DEL CANCER
