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    Method For The Synthesis Of Alkane-1-Hydroxy-1,1-Diphosphonic Acid
    4.
    发明申请
    Method For The Synthesis Of Alkane-1-Hydroxy-1,1-Diphosphonic Acid 审中-公开
    烷基-1-羟基-1,1-二膦酸的合成方法

    公开(公告)号：US20160251385A1

    公开(公告)日：2016-09-01

    申请号：US15030797

    申请日：2014-10-24

    申请人： STRAITMARK HOLDING AG

    发明人： Samuel Cogels ,  Patrick Pierre Notté

    IPC分类号： C07F9/38

    CPC分类号： C07F9/386 ,  Y02P20/582

    摘要： The present invention is related to a new method for the synthesis of alkane-1-hydroxy-,1-diphosphonic acid or its salts which includes the steps of —reacting tetraphosphorus hexaoxide and a carboxylic acid under controlled reaction conditions; —hydrolyzing the formed alkane-1-hydroxy-1,1-diphosphonic acid condensates to form alkane-1-hydroxy-1,1-diphosphonic acid; —precipitating the alkane-1-hydroxy-1,1-diphosphonic acid through the use of a suitable solvent; —filtering the alkane-1-hydroxy-1,1-diphosphonic acid and recovering the mother liquor and the suitable solvent.1 The process according to the method of the present invention is highly controllable and is further characterized by a high selectivity.

    摘要翻译： 本发明涉及一种合成烷烃-1-羟基-1-膦酸或其盐的新方法，其包括在受控反应条件下反应四氧化六磷和羧酸的步骤; 水解所形成的烷烃-1-羟基-1,1-二膦酸缩合物以形成烷烃-1-羟基-1,1-二膦酸; 通过使用合适的溶剂沉淀烷烃-1-羟基-1,1-二膦酸; 过滤烷烃-1-羟基-1,1-二膦酸并回收母液和合适的溶剂.1根据本发明方法的方法是高度可控的，并且进一步以高选择性表征。

    ANTICANCER AGENT
    6.
    发明申请
    ANTICANCER AGENT 审中-公开
    ANTICANCER代理

    公开(公告)号：US20140199240A1

    公开(公告)日：2014-07-17

    申请号：US14130344

    申请日：2012-07-02

    申请人： Jan Rijn Zeevaart ,  Xavier Yangkou Mbianda ,  Zoltan Szucs

    发明人： Jan Rijn Zeevaart ,  Xavier Yangkou Mbianda ,  Zoltan Szucs

    IPC分类号： A61K51/04

    CPC分类号： A61K51/0497 ,  C07B59/004 ,  C07F9/386 ,  C07F9/3873

    摘要： The invention relates to a method for preparing a bisphosphonate covalently bonded to a nanostructure. This invention also relates to a bisphosphonate having incorporated therein a radioisotope selected from 32p or 33P, preferably 33p, wherein the bisphosphonate is covalently bonded to a nanostructure directly or by way of a linker, and to the use thereof in a method of treating calcific tumours in a patient.

    摘要翻译： 本发明涉及一种制备与纳米结构共价键合的二膦酸盐的方法。 本发明还涉及其中掺入了32p或33P，优选33p的放射性同位素的双膦酸盐，其中双膦酸盐直接或通过连接体与纳米结构共价键合，以及其在治疗钙化肿瘤的方法中的用途 在病人身上

    Bisphosphonate Compounds and Methods with Enhanced Potency for Multiple Targets including FPPS, GGPPS, AND DPPS
    8.
    发明申请
    Bisphosphonate Compounds and Methods with Enhanced Potency for Multiple Targets including FPPS, GGPPS, AND DPPS 有权
    双膦酸盐化合物和具有增强效力的多膦酸酯化合物和方法，包括FPPS，GGPPS和DPPS

    公开(公告)号：US20080255070A1

    公开(公告)日：2008-10-16

    申请号：US12101484

    申请日：2008-04-11

    申请人： Eric OLDFIELD ,  Yonghui ZHANG

    发明人： Eric OLDFIELD ,  Yonghui ZHANG

    IPC分类号： A61K31/675 ,  C07F9/38 ,  A61K31/663 ,  A61P35/00 ,  C12Q1/34 ,  C12N9/99 ,  C12N5/06 ,  C07F9/58

    CPC分类号： C07F9/3865 ,  C07F9/386 ,  C07F9/3873 ,  C07F9/5414 ,  C07F9/58 ,  C07F9/6506 ,  C07F9/65517 ,  C07F9/655345 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/72 ,  G01N33/5011

    摘要： The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.

    摘要翻译： 本公开尤其提供了新的双膦酸盐化合物以及制备和使用这些化合物的方法。 在某些实施方案中，本发明的化合物包括能够选择性抑制法呢基二磷酸合成酶（FPPS），香叶基香叶基二磷酸合成酶（GGPPS）和癸酰焦磷酸合酶（DPPS）中的一种或多种的双膦酸盐。 在优选的实施方案中，本发明的化合物能够选择性地抑制FPPS，GGPPS和DPPS中的两种或更多种。 在实施方案中，本发明的化合物和方法表现出优异的活性水平，例如在抗癌情境，免疫刺激背景和其他情况下，其在若干情况下超过前一代二膦酸药物的活性水平达数量级。 在实施方案中，本发明提供了与研究和治疗应用相关的化合物和方法，例如用于肿瘤或癌细胞生长抑制，Gammadelta T细胞的活化，与甲羟戊酸代谢途径相关的某些酶的抑制，骨吸收疾病，癌症， 免疫疾病，免疫治疗和传染病。