BIFUNCTIONAL CHELATING AGENTS
    1.
    发明申请
    BIFUNCTIONAL CHELATING AGENTS 审中-公开
    双功能螯合剂

    公开(公告)号:US20140088314A1

    公开(公告)日:2014-03-27

    申请号:US13626918

    申请日:2012-09-26

    Abstract: A chelating agent, a metal-chelate, and a contrast agent are provided, wherein the chelating agent comprises a compound of structure (I) wherein R1, R2, R3, R8, R7, R′7 R′1, R′2, R′3 and R8′ are selected from a hydrogen, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; R4 and R′4 are selected from a hydrogen, a hydroxyl group, a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; n is an integer between 0 and 4; R5 and R′5 are selected from a hydrogen, a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals; R9 and R′9 are selected form a hydrogen or a protecting group selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals, m is an integer between 0 and 10; and at least one of R7 and R′7 is acidic group or a protected acidic group.

    Abstract translation: 提供螯合剂,金属螯合物和造影剂,其中螯合剂包括结构式(I)的化合物,其中R1,R2,R3,R8,R7,R'7R'1,R'2, R'3和R 8'选自氢,被保护的C 1 -C 3羟烷基,C 1 -C 3烷基; R 4和R 4选自氢,羟基,保护的羟基,被保护的C 1 -C 3羟烷基,C 1 -C 3烷基; n是0和4之间的整数; R 5和R 5选自氢,选自C 1 -C 30脂族基,C 3 -C 30脂环族基,C 2 -C 30芳族基的保护基; R 9和R 9选自由C 1 -C 30脂族基团,C 3 -C 30脂环族基团,C 2 -C 30芳族基团组成的组中的氢或保护基团,m为0至10的整数; 并且R 7和R 7中的至少一个是酸性基团或被保护的酸性基团。

    Contrast enhancement agents and method of use thereof
    3.
    发明授权
    Contrast enhancement agents and method of use thereof 有权
    对比增强剂及其使用方法

    公开(公告)号:US09155804B2

    公开(公告)日:2015-10-13

    申请号:US13626942

    申请日:2012-09-26

    CPC classification number: A61K49/126

    Abstract: A contrast agent composition and a method of diagnostic imaging are provided. The composition comprises a pharmaceutically acceptable carrier and a metal-complex comprising a ligand having structure (XXX): wherein R1, R2, R3, R7, R8, R′1, R′2, R′3, R7′ and R8′ are selected form hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group; R4, R′4 are selected from a hydrogen, a hydroxyl, a protected hydroxyl group, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; n is an integer between 0 and 4; R5, R′5 are selected from a hydrogen, a protecting group comprising C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals, m is an integer between 1 and 10; at least one of R7 and R′7 is acidic groups or protected acidic groups; Y comprises a protein or peptide moiety, a particle, a micelle, a liposome, an organic molecule, oligomer, polymer or a hydrophilic moiety.

    Abstract translation: 提供造影剂组合物和诊断成像方法。 该组合物包含药学上可接受的载体和包含具有结构(XXX)的配体的金属络合物:其中R1,R2,R3,R7,R8,R'1,R'2,R'3,R7'和R8'是 选自氢,受保护的C1-C3羟烷基或C1-C3烷基; R 4,R'4选自氢,羟基,被保护的羟基,保护的C 1 -C 3羟烷基,C 1 -C 3烷基; n是0和4之间的整数; R5,R'5选自氢,包含C1-C30脂族基团,C3-C30脂环族基团,C2-C30芳族基团的保护基,m是1-10之间的整数; R 7和R 7中的至少一个是酸性基团或被保护的酸性基团; Y包括蛋白质或肽部分,颗粒,胶束,脂质体,有机分子,低聚物,聚合物或亲水部分。

    FUNCTIONALIZED PEPTIDE TRANSPORTERS FOR CELLULAR UPTAKE
    4.
    发明申请
    FUNCTIONALIZED PEPTIDE TRANSPORTERS FOR CELLULAR UPTAKE 审中-公开
    用于细胞摄取的功能性肽运输机

    公开(公告)号:US20170035914A1

    公开(公告)日:2017-02-09

    申请号:US14818372

    申请日:2015-08-05

    CPC classification number: A61K49/0056 A61K49/0043

    Abstract: Disclosed are novel cell-penetrating transporters for enhancing cellular uptake of peptide fusion proteins into live cells. The cell-penetrating transporters comprise a functionalized peptide construct comprising a cell importation peptide covalently bound to a cargo, the cell importation peptide in an unreactive monomeric form, and a pharmaceutical carrier. In certain embodiments, the cargo further comprises a nuclear localization sequence (NLS) allowing the cargo to be transported across the nuclear membrane.

    Abstract translation: 公开了用于增强肽融合蛋白到活细胞中的细胞摄取的新型细胞穿透转运蛋白。 细胞穿透转运蛋白包含功能化的肽构建体,其包含与货物共价结合的细胞进入肽,细胞进口肽以非反应性单体形式和药物载体。 在某些实施方案中,货物还包括允许货物跨过核膜运输的核定位序列(NLS)。

    PROBING OF BIOLOGICAL SAMPLES
    5.
    发明申请
    PROBING OF BIOLOGICAL SAMPLES 有权
    探索生物样本

    公开(公告)号:US20150099650A1

    公开(公告)日:2015-04-09

    申请号:US14047233

    申请日:2013-10-07

    Abstract: Disclosed are high throughput methods of probing multiple targets in a biological sample where the recurrent time-consuming antibody incubation steps and individual signal modification and activation steps are replaced by simultaneous hybridization of biomarkers and sequential detection by combining signal removal and activation into a single step. Also disclosed are images obtained by such methods.

    Abstract translation: 公开了探测生物样品中多个靶标的高通量方法,其中复发耗时的抗体孵育步骤和单独的信号修饰和激活步骤被生物标志物的同时杂交和通过将信号去除和活化组合到单个步骤中的顺序检测来代替。 还公开了通过这种方法获得的图像。

    CONTRAST ENHANCEMENT AGENTS AND METHOD OF USE THEREOF
    6.
    发明申请
    CONTRAST ENHANCEMENT AGENTS AND METHOD OF USE THEREOF 有权
    对比增强剂及其使用方法

    公开(公告)号:US20140086846A1

    公开(公告)日:2014-03-27

    申请号:US13626942

    申请日:2012-09-26

    CPC classification number: A61K49/126

    Abstract: A contrast agent composition and a method of diagnostic imaging are provided. The composition comprises a pharmaceutically acceptable carrier and a metal-complex comprising a ligand having structure (XXX): wherein R1, R2, R3, R7, R8, R′1, R′2, R′3, R7′ and R8′ are selected form hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group; R4, R′4 are selected from a hydrogen, a hydroxyl, a protected hydroxyl group, a protected C1-C3 hydroxyalkyl group, a C1-C3 alkyl group; n is an integer between 0 and 4; R5, R′5 are selected from a hydrogen, a protecting group comprising C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, C2-C30 aromatic radicals, m is an integer between 1 and 10; at least one of R7 and R′7 is acidic groups or protected acidic groups; Y comprises a protein or peptide moiety, a particle, a micelle, a liposome, an organic molecule, oligomer, polymer or a hydrophilic moiety.

    Abstract translation: 提供造影剂组合物和诊断成像方法。 该组合物包含药学上可接受的载体和包含具有结构(XXX)的配体的金属络合物:其中R1,R2,R3,R7,R8,R'1,R'2,R'3,R7'和R8'是 选自氢,受保护的C1-C3羟烷基或C1-C3烷基; R 4,R'4选自氢,羟基,被保护的羟基,保护的C 1 -C 3羟烷基,C 1 -C 3烷基; n是0和4之间的整数; R5,R'5选自氢,包含C1-C30脂族基团,C3-C30脂环族基团,C2-C30芳族基团的保护基,m是1-10之间的整数; R 7和R 7中的至少一个是酸性基团或被保护的酸性基团; Y包括蛋白质或肽部分,颗粒,胶束,脂质体,有机分子,低聚物,聚合物或亲水部分。

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