DOTSON, JENNAFER,HEALD, ROBERT ANDREW,HEFFRON, TIMOTHY,JONES, GRAHAM ELGIN,KRINTEL, SUSSIE LERCHE,MCLEAN, NEVILLE JAMES,NDUBAKU, CHUDI,OLIVERO, ALAN G.,SALPHATI, LAURENT,WANG, LAN,WEI, BINQING
申请号：
ES11808454
公开号：
ES2530545T3
申请日:
2011.12.15
申请国别(地区):
ES
年份:
2015
代理人:
摘要：
A compound chosen from the formula I: ** Formula ** and stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts thereof, in which: the broken lines indicate an optional double bond, but at least one broken line is a double bond； X1 is N, CR1 or -C (R1) 2O-； X2 is N； X3 is C or CR3； A is a carbocyclic or heterocyclic ring of 5, 6 or 7 links, fused with X2 and X3, optionally substituted by one or more R5 groups； R1 and R3 are independently selected from H, 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) 2CO-NH2, -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； R4 is selected from C6-C20 aryl, heterocyclyl having 3-20 ring atoms and heteroaryl having 5-20 atoms, each of which is optionally substituted by one or more R6 groups independently selected from F, Cl, Br, I, -CH3, -CH2CH3, -CH (CH3) 2, -CH2CH (CH3) 2, -CH2CH3, -CH2CN, -CN, -CF3, -CH2OH, -CO2H, -CONH2, -CONH (CH3) , -CO-N (CH3) 2, -NO2, -NH2, -NHCH3, -NHCOCH3, -OH, -OCH3, -OCH2CH3, -OCH (CH3) 2, -SH, -NHC (>； = O) NHCH3, -NHC (>； = O) NHCH2CH3, -NHS (O) 2CH3, -N (CH3) C (>； = O) OC (CH3) 3, -S (O) 2CH3, benzyl, benzyloxy, morpholinyl, morpholinomethyl and 4- methylpiperazin-1-yl； and R5 is independently selected from C1-C12 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, - (C1-C12 alkylene) - (C3-C12 carbocyclyl), - (C1-C12 alkylene) - (heterocyclyl having 3 -20 ring atoms), - (C1-C12 alkylene) -C (>； = O) - (hetero-cyclyl having 3-20 ring atoms), - (C1-C12 alkylene) - (C6 aryl- C20), and - (C1-C12 alkylene) - (heteroaryl having 5-20 atoms)； or two R5 geminal groups form a carbocyclic or heterocyclic ring of 3, 4, 5 or 6 links, said alkyl, alkenyl, alkynyl, alkylene, carb
