利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

7 条记录 (耗时 0.017 秒)

    Substituted pyrrolo[2,1-a]phthalazines and benzo[g]pyrrolo[2,1-a]phthalazines for the treatment of cancer
    1.
    发明授权
    Substituted pyrrolo[2,1-a]phthalazines and benzo[g]pyrrolo[2,1-a]phthalazines for the treatment of cancer 有权

    公开(公告)号：US11066412B2

    公开(公告)日：2021-07-20

    申请号：US16764873

    申请日：2018-11-16

    申请人： Academia Sinica

    发明人： Te-Chang Lee ,  Tsann-Long Su ,  Tai-Lin Chen

    IPC分类号： C07D487/14 ,  C07D487/22 ,  C07D487/04 ,  A61P35/02 ,  A61K45/06

    摘要： Disclosed herein are novel bifunctional compounds and their uses for the treatment and/or prophylaxis of cancers. The bifunctional compound disclosed herein has the structure of formula (I), wherein, optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl, C(O)H, OH, O(alkyl), O(CO)alkyl, O(aryl), aryl, and —O(CH2)xN(Rb)2; R1 is an alkyl optionally substituted with one or more substituents independently selected from the group consisting of halo, —OR, —O(CO)CH3, —OSO2R, and —OCONHR; R is hydrogen, alkyl, cycloalkyl, or aryl; R2 is hydrogen, alkyl, cycloalkyl, aryl or heteroaryl, in which the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of C1-6 alkyl, O(alkyl), halo, cyano, nitro, —N(Rc)2, OCH2O—, O(CH2)2O—, pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and 4—(piperido)piperidinyl; R3 is -NRARB, or -NHPhRC, or -NRARB are taken together to form pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-y)piperidin-l-yl, or 4-(piperidin-4-yl)piperidin-l-yl, wherein the piperazin-l-yl or 4-(piperidin-4-yl) piperidin-l-yl is optionally substituted with one or more substituents independently selected from the group consisting of alky, and —(CH2)nCONH(CH2)mNRARB; RA and RB are independently H or C1-C6 alkyl; RC is hydrogen, halo, alkyl, alkenyl, alknyl, O(alkyl), —NHCORa, —NHC(O)ORa, heterocyclyl or aryl, in which the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl C(O)H, OC(O)alkyl, O(aryl), and aryl, in which the aryl is optionally substituted with one or more substituents independently selected from the group consisting of halo, CN, C1-6 alkyl, N(Rc)2, NO2, O(alkyl), —OCH2O—, —O(CH2)2O—,pyrrolidinyl, pepiridinyl, piperazinyl, morpholino, and 4-(piperido)piperidinyl; Ra is C1-6 alkyl or aryl; Rb is C1-10 alkyl, pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-yl)piperidin-l-yl, or 4-(piperidin-4-yl)piperidin-l-yl; Rc, is hydrogen or C1-10 alkyl; and. x, n and m are independently an integral between 1 to 5.