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：
PE0003902012
公开号：
PE10252012A1
申请日:
2010.09.27
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a benzoxazepina Derivative of formula (i), where n is Z1 or Z2 is CR1, CR2 and Cr3 or n is n Z3 Z4 CR4 is o n, B is a ring pirazolilo or imidazolilo merged with the Ring of the benzoxazepina as (a), (b), (c) among others, R1, R2, R3 and R4 are h, F, CN, NO2, among others it is (= C Or nr5r6), nr5r6, among others R5 C1 C12 is H or alkyl optionally substituted with F, CL, CN, COOH,Among others, R6 is C1 - C6 C12 alkyl, aryl - C20, carbociclilo C3 - C12, among others.Preferred compounds are: N - (2 - difluorfenil) - n-methyl - 4.5 - dihidrobenzo pyrazolo - [b] [1.5] [1,4] oxazepina - D - 2 - carboxamide, 2 - (1 - (2-chlorophenyl) - 1h-1,2,4-triazole - 5 - yl) - 5.6 - dihydro - benzo [f] imidazo [1,2-d] [1,4] - oxazepina - 10 - carboxamide, 2 - (1 - (2 - difluorfenil) - 1h-1,2,4-triazole - 5 - il) - 8 - Bromine - 4.5 - dihidroben - zo - 2H - oxepino [4,5-d] pyrazole, among others. It also relates to a Pharmaceutical composition.These compounds inhibit the activity of PI3 Kinase and are useful in the treatment of cancerREFERIDA 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
