发明名称 Inhibitors of HIF and angiogenesis
摘要 Inhibitors of the Hypoxia Inducible Factor (HIF) and angiogenesis and their methods of use including the treatment of cancer, hypoxia related pathologies, disorders leading to ischemia, for example stroke and ischemic heart disease, and non-cancerous angiogenic diseases are provided.
申请公布号 US9062072(B2) 申请公布日期 2015.06.23
申请号 US201113642836 申请日期 2011.04.20
申请人 Emory University;Georgia State University Research Foundation 发明人 Van Meir Erwin G.;Wang Binghe
分类号 A61K31/44;A61K31/47;A61K31/35;A61K31/34;C07D491/052;C07D215/12;C07D307/81;C07D311/04;C07D405/12;C07D311/58 主分类号 A61K31/44
代理机构 Emory Patent Group 代理人 Emory Patent Group
主权项 1. A compound of Formula I or salt, ester, or prodrug thereof wherein, is a single bond; A is —CR5R6—, —CR7═CR8—, or —CR7R9—CR8R10—; E is O; G is —SO2—; X is CR12; Y is CR13; Z is N; R1 is alkyl, carbocyclyl, aryl, or heterocyclyl, wherein R1 is optionally substituted with one or more, the same or different, R15; R2 is alkyl, carbocyclyl, aryl, or heterocyclyl, wherein R2 is optionally substituted with one or more, the same or different, R16; R3 is alkyl optionally substituted with one or more, the same or different, R17; R4 is R4 is alkyl optionally substituted with one or more, the same or different, R18; R5, R6, R7, R8, R9, R10, R11, R12, and R13 are each individually and independently selected from hydrogen, alkyl, halogen, nitro, cyano, hydroxy, amino, mercapto, formyl, carboxy, carbamoyl, alkoxy, alkylthio, alkylamino, (alkyl)2amino, alkylsulfinyl, alkylsulfonyl, arylsulfonyl, carbocyclyl, aryl, or heterocyclyl, optionally substituted with one or more, the same or different, R19; R15, R16, R17, R18, and R19 are halogen, nitro, cyano, hydroxy, trifluoromethoxy, trifluoromethyl, amino, formyl, carboxy, carbamoyl, mercapto, sulfamoyl, methyl, ethyl, methoxy, ethoxy, acetyl, acetoxy, methylamino, ethylamino, dimethylamino, diethylamino, N-methyl-N-ethylamino, acetylamino, N-methylcarbamoyl, N-ethylcarbamoyl, N,N-dimethylcarbamoyl, N,N-diethylcarbamoyl, N-methyl-N-ethylcarbamoyl, methylthio, ethylthio, methylsulfinyl, ethylsulfinyl, mesyl, ethylsulfonyl, methoxycarbonyl, ethoxycarbonyl, N-methylsulfamoyl, N-ethylsulfamoyl, N,N-dimethylsulfamoyl, N,N-diethylsulfamoyl, N-methyl-N-ethylsulfamoyl, carbocyclyl, aryl, or heterocyclyl.
地址 Atlanta GA US