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New piperazine analogues as broad spectrum influenza antivirals
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
CIANCI, CHRISTOPHER,GERRITZ, SAMUEL,LI, GUO,PEARCE, BRADLEY,PENDRI, ANNAPURNA,SHI, SHUHAO,ZHAI, WEIXU,ZHU, SHIRONG
申请号:
ES11758034
公开号:
ES2533068T3
申请日:
2011.09.06
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of formula I, which includes pharmaceutically acceptable salts thereof: ** Formula ** in which Het is a heterocycle of 5 or 6 elements with -N, -O or -S adjacent to the substituent -Ar or adjacent to the point of binding for the substituent -Ar; Ar is aryl or heteroaryl; R is -CH3, -CH2F or -CH>; = CH2; W is -NO2, -Cl, -Br, -CHO, -CH>; = CH2 or -CN; X is -Cl, -CH3 or -CN; Y is -CH or -N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl, the term "cycloalkyl" refers to a monocyclic or fused carbon all ring group in which one or more rings do not have a fully conjugated electron-pi system; wherein the monocyclic or fused carbon all ring group may be unsubstituted or substituted with one or more substituent group (s) individually selected from alkyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, heteroaryloxy, heteroalicycloxy , thiohydroxy, thioalkoxy, thioaryloxy, thioheteroaryloxy, thioheteroalicycloxy, cyano, halo, nitro, carbonyl, thiocarbonyl, O-carbamyl, N-carbamyl, O-thiocarbamyl, N-thiocarbamyl, C-amido, C-thioamido, N -carboxy, O-carboxy, sulfinyl, sulfonyl, sulfonamido, trihalo-methanesulfonamido, trihalomethanesulfonyl, silyl, guanyl, guanidino, ureido, phosphonyl, amino and -NRxRy, the term "substituted aryl" means that the aryl is substituted with one or more Substituent groups selected from alkyl, cycloalkyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, heteroaryloxy, heteroalicycloxy, thiohydroxy, thioaryloxy, thioheteroaryloxy, thioheteroalicycloxy, cyano, halogen, nitro, car Bonyl, O-carbamyl, N-carbamyl, C-amido, N-amido, C-carboxy, O-carboxy, sulfinyl, sulfonyl, sulfonamido, trihalomethyl, ureido, amino and -NRxRy, the term "substituted heteroaryl" means that the heteroaryl is substituted with one or more substituent groups selected from alkyl, cycloalkyl, aryl, he
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