LI, JUN,SAFINA, BRIAN,SUTHERLIN, DANIEL P.,SWEENEY, ZACHARY
申请号：
ES11736322
公开号：
ES2536780T3
申请日:
2011.07.13
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound selected from Formula I: ** Formula ** and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein 5 R1 is selected from ** Formula ** where the wavy line indicates the binding site； R2 is selected from H, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, - (C1-C12 alkylene) - (C3-C12 carbocyclyl), - (C1-C12 alkylene) - (heterocyclyl with 3 to 20 ring atoms), - (C1-C12 alkylene) -C (>； = O) - (heterocyclyl with 3 to 20 ring atoms), - (C1-C12 alkylene) - (C6-C20 aryl), and - (C1-C12 alkylene) - (heteroaryl with 5 to 20 ring atoms), in which alkyl, alkenyl, alkynyl, alkylene, carbocyclyl, heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from F , Cl, Br, I, -CH3, -CH2CH3, -C (CH3) 3, -CH2OH, -CH2CH2OH, -C (CH3) 2OH, -CH2OCH3, -CN, -CF3, -CO2H, -COCH3, -COC (CH3) 3, -CO2CH3, -CONH2, -CONHCH3, -CON (CH3) 2, -C (CH3) 2CONH2, -NO2, -NH2, -NHCH3, -N (CH3) 2, -NHCOCH3, -NHS ( O) 2CH3, -N (CH3) C (CH3) 2CONH2, -N (CH3) CH2CH2S (O) 2CH3,>； = O, -OH, -OCH3, -S (O) 2N (CH3) 2, -SCH3, -S (O) 2CH3, cyclopropyl, cyclobutyl, oxetanyl, morpholino, and 1,1-dioxo-thiopiran-4-yl； R3 is a bicyclic heteroaryl group: ** Formula ** where the wavy line indicates the binding site, and where R8 is hydrogen, C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C12 carbocyclyl, heterocyclyl with 3 to 20 ring atoms, C6-C20 aryl, heteroaryl with 5 to 20 ring atoms, - (C1-C12 alkylene) - (heterocyclyl with 3 to 20 ring atoms), -NH- (alkylene C1-C12) - (heterocyclyl with 3 to 20 ring atoms), -N (C1-C12 alkyl) - (C1-C12 alkylene) - (heterocyclyl with 3 to 20 ring atoms), -NH- (heterocyclyl with 3 to 20 ring atoms), -O- (heterocyclyl with 3 to 20 ring atoms), -NH- (C3-C12 carbocyclyl), -O- (C3-C12 carbocyclyl), F, Cl, Br , I, -CN, -CO2H, -CONH2, -CONH (C1-C12 alkyl), -CON (C1-C12 alkyl) 2, -CO2 (C1-C12 alkyl), -NO2, -NH2, -NH (alkyl C1-C12), -N (C1-C12 alkyl) 2, -NHCO (C1-C12 alkyl), -NHS (O) 2 (C1-C12 alkyl), -N (C
