FORMULATIONS FOR PARENTERAL ADMINISTRATION OF (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES
    1.
    发明申请
    FORMULATIONS FOR PARENTERAL ADMINISTRATION OF (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES 审中-公开
    (E)-2,6-二烷氧基苯乙烯基-4-取代苯磺酸盐的肠胃外给药制剂

    公开(公告)号:WO2008088803A2

    公开(公告)日:2008-07-24

    申请号:PCT/US2008/000523

    申请日:2008-01-16

    CPC classification number: A61K31/496 A61K9/0019 A61K47/02 A61K47/10

    Abstract: Formulations are provided for parenteral administration of (amino substituted (e)-2,6-dialkoxystyryl 4-substituted benzylsulfones and the sodium and potassium salts thereof for the prevention and/or treatment of conditions mediated by abnormal cell proliferation. Composition for parenteral administration are provided which comprise an effective amount of a compound of formula (I) or a compound of formula (IIa) and at least about 50% by weight of at least one water soluble polymerselected from the group consisting essentially of polyethylene glycol (PEG), poly-oxyethylene, poly-oxyethylene-poly-oxypropylene copolymers, polyglycerol, polyvinylalcohol, polyvinylpyrrolidone (PVP), polyvinylpyridine N-oxide, copolymer of vinylpyridine N-oxide and vinylpyridine.

    Abstract translation: (氨基取代的(e)-2,6-二烷氧基苯乙烯基-4-取代的苄基砜及其钠盐和钾盐用于预防和/或治疗异常介导的病症的肠胃外给药制剂 提供了包含有效量的式(I)化合物或式(IIa)化合物和至少约50重量%的至少一种水溶性聚合物的肠胃外给药组合物,所述水溶性聚合物选自 聚乙二醇(PEG),聚氧乙烯,聚氧乙烯 - 聚氧丙烯共聚物,聚甘油,聚乙烯醇,聚乙烯吡咯烷酮(PVP),聚乙烯基吡啶N-氧化物,乙烯基吡啶N-氧化物和乙烯基吡啶的共聚物。

    FORMULATION OF RADIOPROTECTIVE α, β UNSATURATED ARYL SULFONES
    2.
    发明申请
    FORMULATION OF RADIOPROTECTIVE α, β UNSATURATED ARYL SULFONES 审中-公开
    制备放射性保护剂a,ß不饱和芳基磺酸盐

    公开(公告)号:WO2007016201A2

    公开(公告)日:2007-02-08

    申请号:PCT/US2006/029109

    申请日:2006-07-28

    CPC classification number: A61K31/192 A61K31/10 A61K31/724 A61K2300/00

    Abstract: A pharmaceutical composition is provided for administration prior to or after exposure to ionizing radiation for reducing toxic effects of the radiation in a subject. An effective amount of the pharmaceutical composition provided comprising an effective amount of at least one radioprotective α, β unsaturated aryl sulfone, and at least one component selected from the group consisting of a) at least one water soluble polymer in an amount between about 0.5% and about 90% w/v, b) at least one chemically modified cyclodextrin in an amount between about 20% and about 60% w/v, and c) DMA in an amount between about 10% and about 50% w/v.

    Abstract translation: 提供药物组合物用于在暴露于电离辐射之前或之后施用以减少受试者的辐射的毒性作用。 提供的有效量的药物组合物包含有效量的至少一种放射性保护性α,β-不饱和芳基砜和至少一种选自以下的组分:a)至少一种水溶性聚合物,其量为约0.5% 和约90%w / v,b)至少一种量为约20%至约60%w / v的化学改性的环糊精,和c)约10%至约50%w / v之间的量的DMA。

    ACTIVATED CYTOTOXIC COMPOUNDS FOR ATTACHMENT TO TARGETING MOLECULES FOR THE TREATMENT OF MAMMALIAN DISEASE CONDITIONS
    4.
    发明申请
    ACTIVATED CYTOTOXIC COMPOUNDS FOR ATTACHMENT TO TARGETING MOLECULES FOR THE TREATMENT OF MAMMALIAN DISEASE CONDITIONS 审中-公开
    激活的细胞毒素化合物用于治疗哺乳动物疾病的分子靶向治疗

    公开(公告)号:WO2008033475A2

    公开(公告)日:2008-03-20

    申请号:PCT/US2007/019943

    申请日:2007-09-14

    Abstract: Activated cytotoxic compounds are described for attachment to targeting molecules for the treatment of a mammalian disease condition which comprise, an activator, a spacer linker, a linker (e.g., self-immolative), and a cytotoxic drug selected from the group consisting of AMINO-SUBSTITUTED (E)-2,6-DIALKOXYSTYRYL 4-SUBSTITUTED BENZYLSULFONES, AMINO-AND- HYDROXY SUBSTITUTED STYRYLSULFONANILIDES, and SUBSTITUTED PHENOXY- AND PHENYLTHIO-STYRYLSULFONE DERIVATIVES. Activated cytotoxic compound attached to a targeting molecule are described wherein the targeting molecule is selected from the group consisting essentially of an antibody, a receptor, a ligand, a cytokine, a hormone, and a signal transduction molecule. The invention is further directed to a method of treatment of disease conditions.

    Abstract translation: 描述了激活的细胞毒性化合物与靶向分子的连接,用于治疗哺乳动物疾病状况,所述哺乳动物疾病状况包括激活剂,间隔物接头,接头(例如自我免疫)和细胞毒性药物 选自氨基取代的(E)-2,6-二烷氧基苯乙烯基-4-取代的苄基磺酸,氨基 - 和 - 羟基取代的苯基磺酰基苯胺和取代的苯氧基 - 和苯基硫代 - 苯乙烯基砜衍生物。 描述了与靶向分子连接的活化细胞毒性化合物,其中靶向分子选自基本上由抗体,受体,配体,细胞因子,激素和信号转导分子组成的组。 本发明还涉及一种治疗疾病状况的方法。

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