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162 条记录 (耗时 0.025 秒)

    Method for the synthesis of ethane-1-hydroxy-1,1-diphosphonic acid
    61.
    发明授权
    Method for the synthesis of ethane-1-hydroxy-1,1-diphosphonic acid 有权

    公开(公告)号：US09777027B2

    公开(公告)日：2017-10-03

    申请号：US15030823

    申请日：2014-10-24

    申请人： Straitmark Holding AG

    发明人： Patrick Pierre Notté ,  Samuel Cogels

    IPC分类号： C07F9/38

    CPC分类号： C07F9/386 ,  Y02P20/582

    摘要： The present invention is related to a method for the synthesis of ethane-1-hydroxy-1,1-diphosphonic acid or its salt which includes the steps of reacting tetraphosphorus hexaoxide and acetic acid under controlled reaction conditions; hydrolyzing the formed ethane-1-hydroxy-1,1-diphosphonic acid condensates to form ethane-1-hydroxy-1,1-diphosphonic acid; further processing the ethane-1-hydroxy-1,1-diphosphonic acid solution. The process according to the method of the present invention is highly controllable and further is characterized by a high selectivity.

    Bisphosphonate compounds and methods with enhanced potency for multiple targets including FPPS, GGPPS, and DPPS
    64.
    发明授权
    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药效的方法，包括FPPS，GGPPS和DPPS

    公开(公告)号：US08012949B2

    公开(公告)日：2011-09-06

    申请号：US12101484

    申请日：2008-04-11

    申请人： Eric Oldfield ,  Yonghui Zhang ,  Fenglin Yin

    发明人： Eric Oldfield ,  Yonghui Zhang ,  Fenglin Yin

    IPC分类号： A61K31/675 ,  C07F9/06

    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。

    Process for making geminal bisphosphonates
    68.
    发明授权
    Process for making geminal bisphosphonates 有权
    制备双膦酸二氢钠的方法

    公开(公告)号：US06562974B2

    公开(公告)日：2003-05-13

    申请号：US09771899

    申请日：2001-01-29

    申请人： Frederick Dana Cazer ,  William Douglas Cramer ,  Dennis Michael Billings ,  Gregory Eugene Parry

    发明人： Frederick Dana Cazer ,  William Douglas Cramer ,  Dennis Michael Billings ,  Gregory Eugene Parry

    IPC分类号： C07F958

    CPC分类号： C07F9/3873 ,  C07F9/386 ,  C07F9/58

    摘要： The present invention relates to a novel process for making geminal bisphosphonates. The process provides for bisphosphorylation using phosphorus trihalide, phosphorous acid as a reactant/solvent, and a base as an acid acceptor/solvent. The present invention is directed to a process for making geminal bisphosphonates of the general formula: wherein Q is oxygen, —NR4—, sulfur, selenium, or a single bond; m+n is an integer from 0 to about 5, Z is a ring selected from the group consisting of pyridine, pyridazine, pyrimidine, and pyrazine; R1 is hydrogen, substituted or unsubstituted amino, amido, hydroxy, alkoxy, halogen, carboxylate, substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 6 carbon atoms, substituted or unsubstituted aryl, or substituted or unsubstituted benzyl; each R2 is independently, hydrogen, or substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 4 carbon atoms; R3 is one or more substituents selected from the group consisting of hydrogen, substituted or unsubstituted alkyl (saturated or unsaturated) having from 1 to about 6 carbon atoms, substituted and unsubstituted aryl, substituted and unsubstituted benzyl, hydroxy, halogen, carbonyl, alkoxy, nitro, amido, amino, substituted amino, carboxylate, and combinations thereof; R4 is hydrogen, substituted alkyl (saturated or unsaturated) having from 1 to about 4 carbon atoms, or acyl.

    摘要翻译： 本发明涉及一种制备偕双膦酸盐的新方法。 该方法提供使用三卤化磷，亚磷酸作为反应物/溶剂和碱作为酸受体/溶剂的双磷酸化。 本发明涉及制备以下通式的偕二膦酸盐的方法：其中Q为氧，-NR4-，硫，硒或单键; m + n是0至约5的整数，Z是选自吡啶，哒嗪，嘧啶和吡嗪的环; R 1是氢，取代或未取代的氨基，酰氨基，羟基，烷氧基，卤素，羧酸酯，取代或未取代的具有1至约6个碳原子的烷基（饱和或不饱和的），取代或未取代的芳基或取代或未取代的苄基; 每个R 2独立地为氢，或具有1至约4个碳原子的取代或未取代的烷基（饱和或不饱和的）; R3是一个或多个选自氢，取代或未取代的具有1至约6个碳原子的烷基（饱和或不饱和的），取代和未取代的芳基，取代和未取代的苄基，羟基，卤素，羰基，烷氧基， 硝基，酰胺基，氨基，取代的氨基，羧酸酯及其组合; R4是氢，具有1至约4个碳原子的取代烷基（饱和或不饱和的）或酰基。

    Estrogen mimetics lacking reproductive tract effects
    70.
    发明申请
    Estrogen mimetics lacking reproductive tract effects 有权
    雌激素模拟物缺乏生殖道效应

    公开(公告)号：US20020045664A1

    公开(公告)日：2002-04-18

    申请号：US09981617

    申请日：2001-10-15

    申请人： The University of Georgia Research Foundation, Inc

    发明人： Peter C. Ruenitz

    IPC分类号： A61K031/192

    CPC分类号： C07D257/04 ,  A61K31/192 ,  C07C43/23 ,  C07C59/68 ,  C07F9/386

    摘要： A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) 1 wherein R1 is nullO(CH2)mR3 or null(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or nullOH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is nullO(CH2)mR3 or null(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2is H or nullOH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para nullOH when m is 1 and R3 is nullCOOH.

    摘要翻译： 使用式（I）的三芳烷（其中R 1为-O（CH 2）m R 3或 - （CH 2）n R 3）治疗对雌激素治疗有反应的外生殖道组织中的症状，疾病和状况的方法。 其中R3是阴离子取代基; m是1至4的整数; 且n为0至4的整数; 并且其中R2是H或-OH。 R1和R2中的每一个可以是其相应的苯基乙基链的间位或对位。 具有式（I）的化合物，其中R 1为-O（CH 2）m R 3或 - （CH 2）n R 3; R3是阴离子取代基; m为1,2,3或4; n为0,1,2,3或4; R2是H或-OH; 并且其中R 1和R 2各自独立地为其各自的苯乙基的间位或对位，条件是当m为1时，R 2不为对位-OH，且R 3为-COOH。