RAPADOCINS, INHIBITORS OF EQUILIBRATIVE NUCLEOSIDE TRANSPORTER 1 AND USES THEREOF
    5.
    发明申请
    RAPADOCINS, INHIBITORS OF EQUILIBRATIVE NUCLEOSIDE TRANSPORTER 1 AND USES THEREOF 审中-公开
    平衡核苷转运蛋白1的抑制剂及其用途

    公开(公告)号:WO2017136717A1

    公开(公告)日:2017-08-10

    申请号:PCT/US2017/016494

    申请日:2017-02-03

    CPC classification number: C07D519/00 C07D498/18

    Abstract: A compound of Formula (I), and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.

    Abstract translation: 提供式(I)的化合物及其类似物。 包括式I的组合物可用于抑制人平衡核苷转运蛋白1,增加腺苷信号传导并产生包括增加抗病毒活性,增加抗寄生虫活性,增加酒精耐受性,减少对局部缺血以及许多其他病症的保护作用的疼痛的效果。 p>

    ITRACONAZOLE ANALOGS AND USE THEREOF
    8.
    发明申请

    公开(公告)号:WO2020072830A1

    公开(公告)日:2020-04-09

    申请号:PCT/US2019/054583

    申请日:2019-10-03

    Abstract: Itraconazole, a widely used antifungal drug, has been found to possess potent anti-angiogenic and anti-hedgehog activities, exhibiting promising antitumor activity in several human clinical studies. The wider use of itraconazole in the treatment of cancer, however, has been limited by its potent inhibition of the drug metabolic enzyme CYP3A4 which causes drug-drug interactions. In an effort to eliminate the CYP3A4 inhibition of itraconazole while retaining its anti-angiogenic activity, we synthesized a series of itraconazole derivatives. The newly synthesized analogs of itraconazole were evaluated for their cytotoxicity against human umbilical vein endothelial cells (HUVEC) and their inhibitory activity against CYP3A4 enzyme.

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