STEADMAN, Victoria Alexandra,POULLENNEC, Karine G.,LAZARIDES, Linos,ACIRO, Caroline,DEAN, David Kenneth,KEATS, Andrew John,SIEGEL, Dustin Scott,SCHRIER, Adam James,MACKMAN, Richard,JANSA, Petr,HIGHTON
申请号：
ES13729240
公开号：
ES2672480T3
申请日:
2013.06.07
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
A compound of Formula I: ** Formula ** or a pharmaceutically acceptable salt, an isotope, a stereoisomer, a mixture of stereoisomers, a tautomer or an ester thereof, wherein: A is an (C1-C2) alkylene group； A1 is (C1-C5) alkylene, (C2-C5) alkenylene, C2-C5 alkynylene, arylene, heteroarylene, cycloalkylene, heterocycloalkylene, aryl-C1-C2 alkylene, (C1-C2) heteroarylalkylene, C1-cycloalkylalkylene -C2) or heterocycloalkylalkylene (C1-C2), wherein a sp3 carbon atom of A1 is optionally replaced by -O-, -S (O) n-, -NH- or -N ((C1-C4) alkyl) -, and wherein a sp3 or sp2 carbon atom of A1 is optionally substituted with one or more groups selected from the group consisting of halo, (C1-C8) alkyl, (C2-C8) alkenyl, (C2-C8) alkynyl ), aryl, heterocycloalkyl, cycloalkyl, arylalkyl (C1-C4), cycloalkylalkyl (C1-C4), heterocycloalkylalkyl (C1-C4), arylheterocycloalkylalkyl (C1-C4), -OR9, -SR9, -S (O) R9, - S (O) 2R9 and -N (R9) 2； A2 is -CH (R8) -arylene or -CH (R8) -heteroarylene； L1 is -OC (O) -, -O-CH2-, -NR11-C (O) -, -NR10-CH2-, -NH-C (R10) 2- or -NH-S (O) 2-, wherein each R10 is independently H, (C1-C4) alkyl, halo (C1-C4) alkyl, (C1-C4) alkenyl or cycloalkyl； and R11 is (C1-C4) alkyl, halo (C1-C4) alkyl, (C1-C4) alkenyl or cycloalkyl； X1 is -O-, -NH- or -N (CH3) -； R1 and R2, when taken together with the carbon to which they are attached, form -C (>； = O) -； R3 is H or (C1-C4) alkyl which is optionally substituted with halo, cyano, hydroxyl or (C1-C4) alkoxy； R4a and R4b are independently H, (C1-C8) alkyl, aryl, arylalkyl (C1-C4), heterocycloalkyl, heterocycloalkylalkyl (C1-C4), cycloalkyl or cycloalkylalkyl (C1-C4), wherein each R4a and R4b is optionally substituted with one or more substituents selected from the group consisting of cyano, - COOH, halo, hydroxyl, amino, (C1-C8) alkoxy, mono (C1-C8) alkylamino, (C1-C8) dialkylamino, aryl and heteroaryl； R5a and R5b are independently H, (C1-C8) alkyl, (C2-C8) alkenyl, (C2-C8) alkynyl, (C1-C8) alkoxy, aryl, heterocycloalkyl
