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407 条记录 (耗时 0.032 秒)

    Pharmaceutical compounds
    41.
    发明申请
    Pharmaceutical compounds 失效
    药物化合物

    公开(公告)号：US20060030605A1

    公开(公告)日：2006-02-09

    申请号：US11234084

    申请日：2005-09-26

    申请人： Piero Soldato

    发明人： Piero Soldato

    IPC分类号： A61K31/426 ,  A61K31/405 ,  A61K31/4172

    CPC分类号： C07H15/252 ,  C07C219/06 ,  C07C219/22 ,  C07C219/24 ,  C07C271/28 ,  C07C2601/14 ,  C07F9/3873 ,  C07K5/0222

    摘要： Compounds or their salts having general formulas (I) and (II) wherein: s=is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A is the radical of a drug and is such as to meet the pharmacological tests reported in the description, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological test reported in the description.

    摘要翻译： 具有通式（I）和（II）的化合物或其盐，其中：s =等于1或2的整数，优选s = 2; b0 = 0或1; A是药物的基团，并且是为了满足说明书中报道的药理学试验，C和C 1是两个二价基团。 基团B和B 1的前体是为了满足说明书中报道的药理学试验。

    Novel hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof
    47.
    发明申请
    Novel hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof 失效
    阿仑膦酸钠的新型水合物形式，其制备方法及其药物组合物

    公开(公告)号：US20030065214A1

    公开(公告)日：2003-04-03

    申请号：US09898756

    申请日：2001-07-03

    发明人： Nina Finkelstein ,  Ramy Lidor-Hadas ,  Judith Aronhime

    IPC分类号： C07F009/28

    CPC分类号： C07F9/3873

    摘要： New hydrate forms of alendronate sodium, having water content of between about one and about twelve percent, and processes for their manufacture, are disclosed. New crystalline forms of alendronate sodium B, D, E, F, G and H, and processes for manufacturing them, are also disclosed. These new forms of alendronate sodium are suitable for incorporation into pharmaceutical compositions for combating bone resorption in bone diseases.

    摘要翻译： 公开了水含量为约1至约12％的阿仑膦酸钠的新水合物形式及其制备方法。 还公开了阿仑膦酸钠B，D，E，F，G和H的新结晶形式及其制备方法。 这些新形式的阿仑膦酸钠适于掺入用于对抗骨疾病中的骨吸收的药物组合物中。

    Radiolabelled bisphosphonates and method
    48.
    发明授权
    Radiolabelled bisphosphonates and method 失效
    放射性标记的双膦酸盐和方法

    公开(公告)号：US06534488B1

    公开(公告)日：2003-03-18

    申请号：US10031760

    申请日：2002-05-08

    申请人： Alexander Mark Gibson ,  Marivi Mendizabal ,  Richard Pither ,  Shirley Elizabeth Pullan ,  Vaughan Griffiths ,  Philip Duncanson

    发明人： Alexander Mark Gibson ,  Marivi Mendizabal ,  Richard Pither ,  Shirley Elizabeth Pullan ,  Vaughan Griffiths ,  Philip Duncanson

    IPC分类号： C07F938

    CPC分类号： C07B59/004 ,  C07F9/386 ,  C07F9/3873 ,  C07F9/409

    摘要： The present invention relates to 32P or 33P-labelled bisphosphonates as radiotherapeutic radiopharmaceuticals. The 32P- or 33P-labelled bisphosphonates, which are chemically identical to the unlabelled agent, are expected to target the lesion site in an identical manner, but also deliver a significant radiocytotoxic effect to the surrounding cells. This should result, given the favorable energetics of the &bgr; particle emission from the 33P nuclide, in a loss of proliferative capacity of cells associated with the tumor lesion. The relative stability and in vivo localisation of bisphosphonates makes them good candidates as 32P/33P delivery vehicles.

    摘要翻译： 本发明涉及作为放射治疗放射性药物的32P或33P标记的双膦酸盐。 与未标记试剂化学相同的32P或33P标记的双膦酸盐预期以相同的方式靶向病变部位，但也对周围细胞产生显着的放射性细胞毒性作用。 考虑到来自33P核素的β粒子发射的有利能量，与肿瘤病变相关的细胞的增殖能力丧失将导致这一点。 双膦酸盐的相对稳定性和体内定位使其成为32P / 33P递送载体的良好候选物。

    Novel process for preparing alendronic acid
    50.
    发明申请
    Novel process for preparing alendronic acid 审中-公开
    制备阿仑膦酸的新方法

    公开(公告)号：US20020052527A1

    公开(公告)日：2002-05-02

    申请号：US09812469

    申请日：2001-03-20

    发明人： Ramy Lidor-Hadas ,  Revital Lifshitz

    IPC分类号： C07F009/38

    CPC分类号： C07F9/3873

    摘要： A novel process for the preparation of alendronic acid is disclosed. The method comprises the steps of reacting a compound of formula I with H3PO3 1 wherein R is an imido group and R1 is selected from the group consisting of chloro, bromo, iodo, fluoro, hydroxy, amino, nullOR2 or nullOC(O)R2, wherein R2 is C1-C12 alkyl, C1-C12 cycloalkyl or C1-C12 aryl; and then reacting the product of the first step with a deprotecting agent. Alendronic acid is then recovered. The method is safe, efficient and suitable for use on a large scale.

    摘要翻译： 公开了一种制备阿仑膦酸的新方法。 该方法包括使式I化合物与H 3 PO 3反应的步骤，其中R是亚氨基，R 1选自氯，溴，碘，氟，羟基，氨基，-OR 2或-OC（O）R 2 其中R2为C1-C12烷基，C1-C12环烷基或C1-C12芳基; 然后使第一步的产物与脱保护剂反应。 然后回收阿仑膦酸。 该方法安全，高效，适合大规模使用。