Composition and Method for Treating Hematologic Cancers

    公开(公告)号:US20210145792A1

    公开(公告)日:2021-05-20

    申请号:US16688319

    申请日:2019-11-19

    发明人: Eric A. Wachter

    摘要: A method of treating a mammalian subject having hematologic, non-tumorous cancer cells is disclosed. The method comprises the steps of: (A) administering to such a mammalian subject a therapeutically effective amount of a halogenated xanthene, a pharmaceutically acceptable salt or a C1-C4 alkyl ester thereof as a first cancer cytotoxic agent dissolved or dispersed in a pharmaceutically acceptable aqueous medium. The mammalian subject is maintained for a period of time sufficient to induce death of hematologic, non-tumorous cancer cells. A contemplated administration is typically repeated. A contemplated treatment method can also be carried out in conjunction with administration to said mammalian subject of a second therapeutically effective amount of a second, differently-acting cancer cytotoxic agent dissolved or dispersed in a pharmaceutically acceptable medium. The second cancer cytotoxic agent can be a small molecule or an intact antibody or paratope-containing portion thereof.

    In Vitro and Xenograft Anti-Tumor Activity of a Halogenated-Xanthene Against Refractory Pediatric Solid Tumors

    公开(公告)号:US20190350893A1

    公开(公告)日:2019-11-21

    申请号:US16412872

    申请日:2019-05-15

    IPC分类号: A61K31/343 C07K16/28

    摘要: A method of treating a pediatric cancerous solid tumor in a mammalian subject is disclosed that comprises intralesionally administering an amount of a halogenated xanthene or a pharmaceutically acceptable salt thereof, preferably Rose Bengal disodium, that elicits ablation of tumor cells of the administered tumor. Another contemplated method comprises the steps of intralesionally administering an amount of a halogenated xanthene or a pharmaceutically acceptable salt thereof, preferably Rose Bengal disodium, that elicits ablation of tumor cells of the administered tumor and systemically administering a tumor-inhibiting effective amount of a systemic anti-cancer medication that provides synergistic cytotoxicity with the halogenated xanthene. The two administrations can occur concurrently, or one prior to the other.

    Process for the synthesis of 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one(Rose Bengal) and related xanthenes
    30.
    发明授权
    Process for the synthesis of 4,5,6,7-tetrachloro-3′,6′-dihydroxy-2′,4′,5′,7′-tetraiodo-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one(Rose Bengal) and related xanthenes 有权
    合成4,5,6,7-四氯-3',6'-二羟基-2',4',5',7'-四碘-3H-螺[异苯并呋喃-1,9'-呫吨] -3-one(玫瑰红)和相关呫吨

    公开(公告)号:US09422260B2

    公开(公告)日:2016-08-23

    申请号:US13916408

    申请日:2013-06-12

    CPC分类号: C07D311/82 C07D493/10

    摘要: A new process for the manufacture of iodinated xanthenes in high purity includes a cyclization step followed by an iodination step. No extraction, chromatographic or solvent concentration steps are required, and the intermediate as well as final compounds are isolated via filtration or similar means. The process requires a single organic solvent, and the steps are completed at temperatures below 100° C. The exclusion of chloride ions, of chloride free-radicals, hypochlorite ions, or hypochlorous acid as reagents or from reagents that may generate these species in situ in the presence of oxidants, prevents undesirable impurity formation. Several new compounds have been conceived and isolated using these methods. These new compounds are also formed into new medicaments.

    摘要翻译: 用于制造高纯度碘化呫吨的新方法包括环化步骤,然后进行碘化步骤。 不需要萃取,色谱或溶剂浓缩步骤,通过过滤或类似方法分离中间体和最终化合物。 该方法需要单一的有机溶剂,并且步骤在低于100℃的温度下完成。排除氯化物离子,氯化物自由基,次氯酸根离子或次氯酸作为试剂或从原位产生这些物质的试剂 在存在氧化剂的情况下,可防止不希望有的杂质形成。 已经使用这些方法构思和分离了几种新化合物。 这些新化合物也形成新的药物。