发明名称 Methods and compositions for treating Ewings sarcoma family of tumors
摘要 Compounds, compositions and methods relating to EWS-FLI1 protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors.
申请公布号 US9290449(B2) 申请公布日期 2016.03.22
申请号 US201314388671 申请日期 2013.04.11
申请人 Georgetown University 发明人 Toretsky Jeffrey A.;Brown Milton Lang;Tosso Perrer N.;Uren Aykut;Kong Yali
分类号 C07D209/38;C07D209/34 主分类号 C07D209/38
代理机构 Knobbe, Martens, Olson & Bear LLP 代理人 Knobbe, Martens, Olson & Bear LLP
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of hydrogen, C1-6 alkyl, one amino acid, two amino acids linked together, three amino acids linked together, R3 is selected from the group consisting hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, —C(═O)NH2, —NO2, —NH2, —OH, —N (R15)2, and —SR15; R4, R5, R9, and R14 are each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, —C(═O)NH2, —NO2, —NH2, —OH, —NH(R15), —N (R15)2, and —SR15; R10 is selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, —C(═O)NH2, —NO2, —NH2, —OH, —NH(R15), —N(R15)2, and —SR15; R11, R12, and R13 are each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, —C(═O)NH2, —NO2, —NH2, —OH,—NH(R15), —N(R15)2, and —SR15; R6 is C1-6 dialkyl amine; R7 is selected from the group consisting of hydrogen and C1-6 alkyl; R8 and R15 are each independently C1-6 alkyl; each R16 is independently hydrogen, —OH, or C1-6 alkoxy; n is an integer from 0 to 4; p is 1 or 3; and the dashed line represents an optional double bond where said double bond has a configuration selected from the group consisting of cis and trans, with the proviso that at least one of R4, R5, R9, and R14 is selected from the group consisting of —NH(R15), —N(R15)2, and —SR15, or R3 is selected from the group consisting of —N(R15)2, and —SR15.
地址 Washington DC US