Compositions and Methods for Cancer Treatment
    1.
    发明申请
    Compositions and Methods for Cancer Treatment 审中-公开
    癌症治疗的组合和方法

    公开(公告)号:US20100144671A1

    公开(公告)日:2010-06-10

    申请号:US11885606

    申请日:2006-03-03

    CPC分类号: A61K31/59

    摘要: Bromoacetoxycalcidiol (B3CD), which is structurally related to calcidiol, exhibits cytotoxic and apoptotic activity toward cancer cells, including highly aggressive neuroblastoma cells. A series of small molecules designed around the structure of B3CD is expected to have growth inhibitory and apoptogenic activities toward a wide range of malignancies. B3CD shows no apparent toxicity in vivo, indicating potential value as a chemotherapeutic agent which will be particularly useful in treating highly aggressive tumors.

    摘要翻译: 与calcidiol结构相关的溴乙酰氧基胆钙二醇(B3CD)对癌细胞(包括高度侵袭性的神经母细胞瘤细胞)表现出细胞毒性和凋亡活性。 围绕B3CD结构设计的一系列小分子预计具有朝向广泛恶性肿瘤的生长抑制和凋亡活性。 B3CD在体内没有明显的毒性,表明作为化学治疗剂的潜在价值,其将特别可用于治疗高度侵袭性的肿瘤。

    Vinyl sulfide compounds and a process for their preparation
    3.
    发明授权
    Vinyl sulfide compounds and a process for their preparation 失效
    乙烯硫醚化合物及其制备方法

    公开(公告)号:US5883287A

    公开(公告)日:1999-03-16

    申请号:US981448

    申请日:1997-12-22

    CPC分类号: C07C323/16 C07C2103/74

    摘要: Vinyl sulfides bearing protected arlyoxy substituents and a process for their preparation are provided. In the process a vinyl sulfide is formed by coupling a ketone compound and a thioester compound with a low valent titanium reagent to form both carbon-carbon bonds in the same step. The vinyl sulfide compounds are useful as intermediates which are convertible into triggerable sulfur-substituted dioxetanes by addition of oxygen to the double bond. The sulfur-substituted dioxetanes additionally are useful for producing chemiluminescence or for further conversion into triggerable alkoxy, alkenyloxy, alkynloxy, aryloxy, aralkyloxy, or acyloxy-substituted dioxetanes. Triggerable dioxetanes are useful for producing chemiluminescence and in detecting activating agents in assays such as immunoassays and nucleic acid hybridization assays.

    摘要翻译: PCT No.PCT / US96 / 09249 Sec。 371 1997年12月22日第 102(e)1997年12月22日PCT PCT 1996年6月19日PCT公布。 出版物WO97 / 00849 日期1997年1月9日提供了具有保护的芳氧基取代基的乙烯基硫化物及其制备方法。 在该方法中,通过在相同步骤中将酮化合物和硫酯化合物与低价钛试剂偶联以形成碳碳键来形成乙烯基硫醚。 乙烯基硫化物化合物可用作通过向双键中加入氧而转化为可触发的硫取代的二氧杂环丁烷的中间体。 硫取代的二氧杂环丁烷另外可用于产生化学发光或进一步转化成可触发的烷氧基,烯氧基,炔氧基,芳氧基,芳烷氧基或酰氧基取代的二氧杂环丁烷。 可触发的二氧杂环丁烷可用于生产化学发光和在诸如免疫测定和核酸杂交测定的测定中检测活化剂。

    Process for the preparation of mercaptoalcohols
    10.
    发明授权
    Process for the preparation of mercaptoalcohols 失效
    巯基醇的制备方法

    公开(公告)号:US4985586A

    公开(公告)日:1991-01-15

    申请号:US462987

    申请日:1990-01-10

    CPC分类号: C07C319/02

    摘要: This invention relates to improvement to a process for the preparation of mercaptoalcohols containing, more particularly, up to 24 carbon atoms and, preferably, more than 3 carbon atoms, by reaction of the corresponding vicinal epoxides with hydrogen sulphide.The process comprises incorporating into the reaction mixture a catalyst comprising a guanidine and/or of organic derivatives of a guanidine, and/or of guanidine salts, in particular of guanidine salts. The catalyst can be either in liquid and/or solid form, depending on the nature of the catalyst and its solubility in the reaction mixture, or fixed and/or impregnated into various solid materials. The materials can be organic in nature such as neutral and/or basic polymer resins, polymers or copolymers, or can be inorganic in nature such as alumninas, silicas, aluminosilicates, zeolites, active charcoals, oxides and/or metal salts.This process enables mercaptoalcohols to be obtained in a high overall yield while permitting relatively short reaction times.

    摘要翻译: 本发明涉及通过相应的邻位环氧化物与硫化氢的反应来改进含有更特别地至多24个碳原子,优选多于3个碳原子的巯基醇的制备方法。 该方法包括向反应混合物中加入包含胍和/或胍的有机衍生物和/或胍盐,特别是胍盐的催化剂。 催化剂可以是液体和/或固体形式,这取决于催化剂的性质及其在反应混合物中的溶解性,或固定和/或浸渍到各种固体材料中。 这些材料本质上可以是有机的,例如中性和/或碱性聚合物树脂,聚合物或共聚物,或者在本质上可以是无机的,例如校准子,二氧化硅,铝硅酸盐,沸石,活性炭,氧化物和/或金属盐。 该方法能够以高的总产率获得巯基醇,同时允许相对较短的反应时间。