VENDEVILLE, Sandrine Marie Helene,LAST, Stefaan Julien,DEMIN, Samuel Dominique,GROSSE, Sandrine Celine,HACHE, Geerwin Yvonne Paul,HU, Lili,PIETERS, Serge Maria Aloysius,ROMBOUTS, Geert,VANDYCK, Koen,V
申请号:
PE2017002525
公开号:
PE4102018A1
申请日:
2016.07.01
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
Refers to compounds of formula (I sulfamoilarilamida cycled -) where the aryl ring is monociclico of 5 or 6 members optionally containing one or two heteroatoms; RingB Member 6 is aryl optionally containing one atom of N; X is - cr2r3, where R2 is H, alkyl C1 - C10, alquinilo c2-c4, among others; R3 is H, alkyl of C1 - C6Among others, and is alcanodiilo C1 - C7 alquenodiilo C2 or C7; Z is a Link, or NH; ra, RB, RC and Rd are each h, halogen, CHF2, CN, among others; r1 is H, or C1 - C10 alkyl.Preferred compounds are: N - (3-chloro-4-fluorophenyl) - 3.7 - 1,1 - dimethyl - [3 - (3-pyridylmethyl) - 2.4 - 5-methyl-4-oxo-1,4-dihydropyrrolo [3,4-b] [1,4,5] oxatiazepino - 6 - carboxamide, N - (2 - chlorine - 4 - 3 - pyridyl)7 - dimethyl - 3 - [(3 - 5 - metilisoxazol - yl) methyl] - [- 1,1 - 2.4 - 5-methyl-4-oxo-1,4-dihydropyrrolo [3,4-b] [1,4,5] oxatiazepino - 6 - carboxamide, among others.I refers to a process of Preparation and to a Pharmaceutical composition.These compounds are inhibitors of the replication of the hepatitis B virus (HBV) is useful for the treatment of hepatitis BSE REFIERE A COMPUESTOS DERIVADOS DE SULFAMOILARILAMIDA CICLADOS DE FORMULA (I-A) DONDE EL ANILLO A ES ARILO MONOCICLICO DE 5 O 6 MIEMBROS QUE CONTIENE OPCIONALMENTE UNO O DOS HETEROATOMOS; EL ANILLO B ES ARILO DE 6 MIEMBROS QUE CONTIENE OPCIONALMENTE UN ATOMO DE N; X ES -CR2R3-, EN DONDE R2 ES H, ALQUILO C1-C10, ALQUINILO C2-C4, ENTRE OTROS; R3 ES H, ALQUILO C1-C6, ENTRE OTROS; Y ES ALCANODIILO C1-C7 O ALQUENODIILO C2-C7; Z ES UN ENLACE, NH U O; Ra, Rb, Rc Y Rd SON CADA UNO H, HALOGENO, CHF2, CN, ENTRE OTROS; R1 ES H O ALQUILO C1-C10. SON COMPUESTOS PREFERIDOS: N-(3-CLORO-4-FLUOROFENIL)-3,7-DIMETIL-1,1-DIOXO-3-(3-PIRIDILMETIL)-2,4-DIHIDROPIRROLO[3,4-b][1,4,5]OXATIAZEPINO-6-CARBOXAMIDA, N-(2-CLORO-4-PIRIDIL)-3,7-DIMETIL-3-[(5-METILISOXAZOL-3-IL)METIL]-1,1-DIOXO-2,4-DIHIDROPIRROLO[3,4-b][1,4,5]OXATIAZEPINO-6-CARBOXAMIDA, ENTRE OTROS. TASMBIEN SE REFIERE A UN PROCESO DE PREPARACION Y A UNA COMPOSIC