RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF
    1.
    发明申请
    RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF 审中-公开
    放射性核苷类似物及其制备方法及其用途

    公开(公告)号:US20120178919A1

    公开(公告)日:2012-07-12

    申请号:US13194247

    申请日:2011-07-29

    摘要: A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.

    摘要翻译: 提供放射性标记的核苷类似物,其包括放射性碘123I / 131I和选自胞苷,胸苷,尿苷及其衍生物的核苷类似物。 还提供了制备放射性标记的核苷类似物的方法及其用途。 通过制备方法制备的核苷类似物,具有短的合成时间和高放射化学产率,具有长的体内生理半衰期和高血清稳定性,作为放射性药物组合物,可用于肿瘤增生诊断的发展 或治疗预后评估,进一步有助于观察药物的长时间体内代谢。

    METHOD FOR PREPARING PRECURSOR USED FOR LABELING HEPATOCYTE RECEPTOR AND CONTAINING TRISACCHARIDE AND DTPA LIGAND
    2.
    发明申请
    METHOD FOR PREPARING PRECURSOR USED FOR LABELING HEPATOCYTE RECEPTOR AND CONTAINING TRISACCHARIDE AND DTPA LIGAND 有权
    制备用于标记肝细胞受体和含有TRISACCHARIDE和DTPA配体的前体的方法

    公开(公告)号:US20140046045A1

    公开(公告)日:2014-02-13

    申请号:US13571731

    申请日:2012-08-10

    IPC分类号: C07H15/04 C07H1/06

    CPC分类号: C07H1/06 C07H15/04 C07K1/13

    摘要: A method for preparing a precursor used to label hepatocyte receptors is revealed. The precursor contains a bifunctional structure including trisaccharide and DTPA ligand. During synthesis processes of the precursor, silica gel columns and Reverse phase-18 (RP-18) columns are used for purification. Thus both the purification times and cost of each purification are reduced. Moreover, use diethyl ether to facilitate precipitation of products and remove a part of coupling reagent. Removing the coupling reagent helps purification of products. Furthermore, Nα,Nα-bis(carboxymethyl)-L-lysine hydrate and benzyl chloroformate are coupled to form a trisaccharide skeleton so as to ensure the yield rate of trisaccharide structure.

    摘要翻译: 揭示了制备用于标记肝细胞受体的前体的方法。 该前体含有包括三糖和DTPA配体的双功能结构。 在前体的合成过程中,使用硅胶柱和反相18(RP-18)柱进行纯化。 因此,每次纯化的纯化时间和成本均降低。 此外,使用乙醚促进产物沉淀并除去一部分偶联剂。 去除偶联剂有助于净化产品。 此外,Nalpha,Nalpha-双(羧甲基)-L-赖氨酸水合物和氯甲酸苄酯偶联形成三糖骨架,以确保三糖结构的产率。

    LIVER- RECEPTOR IMAGING INJECTION, DISPENSING METHOD AND PHARMACEUTICAL COMPOSITION THEREOF
    3.
    发明申请
    LIVER- RECEPTOR IMAGING INJECTION, DISPENSING METHOD AND PHARMACEUTICAL COMPOSITION THEREOF 有权
    肝脏摄取成像注射,分配方法及其药物组合物

    公开(公告)号:US20120107236A1

    公开(公告)日:2012-05-03

    申请号:US13243225

    申请日:2011-09-23

    IPC分类号: A61K103/20 C07F5/00 A61P43/00

    摘要: The present invention is related to a pharmaceutical composition for a liver-receptor imaging injection, the pharmaceutical composition including a bi-functional compound which has a ASGPR specificity, wherein the bi-functional compound includes a backbone of alpha-amino acid (or the derivatives thereof) and a poly-galactosamine chain (or a poly-lactose chain) connected to the alpha-amino acid. Thereby, the pharmaceutical composition can quantify potential of liver storage ability and evaluate severity of the course of liver disease. A liver-receptor imaging injection using the same and the one-step dispensing method thereof are also provided to improve defects of iodine-labeled and overcome disadvantages of the reduced labeling-yield and the instability after autoclave sterilization.

    摘要翻译: 本发明涉及一种肝 - 受体成像注射用药物组合物,该药物组合物包含具有ASGPR特异性的双功能化合物,其中双官能化合物包括α-氨基酸(或其衍生物 )和与α-氨基酸连接的聚半乳糖胺链(或聚乳糖链)。 因此,药物组合物可以量化肝脏储存能力的潜力并评估肝脏疾病过程的严重程度。 还提供使用其的肝受体成像注射器及其一步式分配方法,以改善碘标记的缺陷,克服降压标记产率和高压灭菌后的不稳定性的缺点。

    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS
    5.
    发明申请
    NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS 有权
    新型肝脏靶向药物及其合成

    公开(公告)号:US20110077386A1

    公开(公告)日:2011-03-31

    申请号:US12891004

    申请日:2010-09-27

    IPC分类号: C07H15/02 C07C229/02

    CPC分类号: C07H15/04

    摘要: This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.

    摘要翻译: 本发明提供新型肝靶向剂及其合成方法。 公开了以赖氨酸为基础的三乙酸结构作为骨架的肝靶向剂,其以糖基取代多价,与半乳糖胺链或乳糖链结合。 特别地,仅涉及一个氨基酸L-赖氨酸以提供三价值。 N,N-苄氧羰基-Nα-二羧甲基-L-赖氨酸中的所有羧基可以在一个步骤中与αGalNAc或ahLac的三种糖苷缀合。 本发明还提供了六乳糖苷。 特别地,TFA-AHA-Asp用于缀合2摩尔NTA(ahLac)3。 本发明还提供了一种在NTA和DTPA之间添加间隔物的方法。 延长的肝细胞特异性糖配体比未延长的肝细胞特异性糖配体具有更高的111In-放射性标记产率。

    GRAVITATIONAL POTENTIAL ENERGY CONVERTING DEVICE

    公开(公告)号:US20240018947A1

    公开(公告)日:2024-01-18

    申请号:US17865439

    申请日:2022-07-15

    IPC分类号: F03G3/00

    CPC分类号: F03G3/00

    摘要: A gravitational energy conversion device is configured to rotate or translate on a support surface. The gravitational energy conversion device has a weight and multiple energy converters; the energy converters are mounted around an exterior of the weight and disposed apart from each other. When the weight rotates or translates to make the energy converters contact the support surface, the weight presses down the energy converters due to gravity. When the weight rotates or translates to make the energy converters separate from the support surface, energy in the energy converters is released and transformed into kinetic energy of the weight. Therefore, the device is effective in energy-saving and cushioning.