BLAQUIERE, NICOLE,DO, STEVEN,DUDLEY, DANETTE,FOLKES, ADRIAN J.,GOLDSMITH, RICHARD A.,HEALD, ROBERT,HEFFRON, TIM,KOLESNIKOV, ALEKSANDR,NDUBAKU, CHUDI,OLIVERO, ALAN G.,STABEN, STEVEN,WEI, BINQING,PRICE,
申请号：
PE0003972012
公开号：
PE15592012A1
申请日:
2010.09.27
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Referring to a benzoxepina derivative Compound of formula (i), where n is Z1 or Z2 is CR1, CR2 and Cr3 or Z3 is n n n or Z4 is CR4 x1 and x2 are n, o, S, C (R7) 2 or CR7 r1 is H, halogen, NS, CF3, NO2 or c1-c4 alkyl R2, R3, R4 and R7 are h, halogen, CN, NO2, among others C6 C20 is aryl, heteroaryl C1 - C20, among others.Preferred compounds are: ((R) - 2 - Hydroxymethyl pyrrolidin-1-yl) - [8 - (1h-pyrazol-4-yl) - 4,5-dihydro - 6 - 3 - oxa - tia - 1 - aza benzo [e] 2 - Blue - il] methanone -, isopropyl - Methyl amide acid 8 - (1h-pyrazol-4-yl) - 4,5-dihydro - 6 - 3 - oxa - tia - 1 - aza benzo [e] Azulene - 2 - 4 - carboxylic acid, 2 - {[2 - (2 - isopropyl - 2H - [1,2,4] triazol 3 - il) - 4,5-dihydro - 6 - 3 - oxa - tia - 1 - aza benzo [e] Blue - il - 8 - pyrazol-1-yl]} - ethanol8 - [1 - (2 - (4 - il - ethyl) - 1h-pyrazol-4-yl] - 2 - [2 - (2,2,2 - trifluor - ethyl) - 2H - [1,2,4] - 3 - triazol yl] - 4,5-dihydro - 6 - - 3 - oxa - Tia 1 - aza benzo [e] Azulene, among Others. It also relates to a Pharmaceutical composition. These compounds have Inhibitory activity of phosphatidylinositol 3 Kinase (PI3) and are useful in the treatment of cancerREFERIDA A UN COMPUESTO DERIVADO DE BENZOXEPINA DE FORMULA (I), DONDE Z1 ES CR1 O N Z2 ES CR2 O N Z3 ES CR3 O N Z4 ES CR4 O N X1 Y X2 SON N, O, S, C(R7)2 O CR7 R1 ES H, HALOGENO, CN, CF3, NO2 O ALQUILO C1-C4 R2, R3, R4 Y R7 SON H, HALOGENO, CN, NO2, ENTRE OTROS A ES ARILO C6-C20, HETEROARILO C1-C20, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ((R)-2-HIDROXIMETIL-PIRROLIDIN-1-IL)-[8-(1H-PIRAZOL-4-IL)-4,5-DIHIDRO-6-OXA-3-TIA-1-AZA-BENZO[e]AZULEN-2-IL]-METANONA, ISOPROPIL-METIL-AMIDA DEL ACIDO 8-(1H-PIRAZOL-4-IL)-4,5-DIHIDRO-6-OXA-3-TIA-1-AZA-BENZO[e]AZULENO-2-CARBOXILICO, 2-{4-[2-(2-ISOPROPIL-2H-[1,2,4]TRIAZOL-3-IL)-4,5-DIHIDRO-6-OXA-3-TIA-1-AZA-BENZO-[e]AZULEN-8-IL]-PIRAZOL-1-IL}-ETANOL, 8-[1-(2-MORFOLIN-4-IL-ETIL)-1H-PIRAZOL-4-IL]-2-[2-(2,2,2-TRIFLUOR-ETIL)-2H-[1,2,4]-TRIAZOL-3-IL]-4,5-DIHIDRO-6-OXA-3-TIA-1-AZA-BENZO[e]AZULENO, ENTRE OTR
