COX-2-TARGETING, PLATINUM-CONTAINING CONJUGATES AND THEIR USE IN THE TREATMENT OF TUMORS AND CANCERS
    1.
    发明申请
    COX-2-TARGETING, PLATINUM-CONTAINING CONJUGATES AND THEIR USE IN THE TREATMENT OF TUMORS AND CANCERS 审中-公开
    COX-2-靶向含铂的结合物及其在肿瘤和癌症治疗中的应用

    公开(公告)号:WO2016111834A1

    公开(公告)日:2016-07-14

    申请号:PCT/US2015/066886

    申请日:2015-12-18

    CPC classification number: C07F15/0013 A61K47/55

    Abstract: The present disclosure provides platinum-containing conjugates that selectively target and kill tumor/cancer cells. The conjugates contain a moiety that selectively targets COX-2, which is overexpressed by a broad range of tumor/cancer cells. The present disclosure provides conjugates that selectively target and kill tumor/cancer cells. The expression of cyclooxygenase II (COX-2) is upregulated in many benign and malignant tumor/cancer cells. In some embodiments, the conjugates comprise a COX-2-targeting moiety and a platinumcontaining antitumor agent. The term "antitumor agents" includes antitumor agents and anticancer agents. In some embodiments, the COX-2-targeting moiety comprises a non-steroidal anti-inflammatory drug (NSAID). In certain embodiments, the COX-2-targeting moiety comprises a COX-2-selective inhibitor.

    Abstract translation: 本公开提供了选择性靶向和杀死肿瘤/癌细胞的含铂共轭物。 缀合物包含选择性靶向COX-2的部分,其被广泛的肿瘤/癌细胞过表达。 本公开提供了选择性靶向和杀死肿瘤/癌细胞的缀合物。 环氧合酶II(COX-2)的表达在许多良性和恶性肿瘤/癌细胞中上调。 在一些实施方案中,缀合物包含COX-2-靶向部分和含铂的抗肿瘤剂。 术语“抗肿瘤剂”包括抗肿瘤剂和抗癌剂。 在一些实施方案中,COX-2靶向部分包含非甾体抗炎药(NSAID)。 在某些实施方案中,COX-2-靶向部分包含COX-2-选择性抑制剂。

    PREPARATION OF PLATINUM GROUP METAL AND RHENIUM CARBOXYLATES
    5.
    发明申请
    PREPARATION OF PLATINUM GROUP METAL AND RHENIUM CARBOXYLATES 审中-公开
    铂族金属和羟基甲酸钠的制备

    公开(公告)号:WO1992010460A1

    公开(公告)日:1992-06-25

    申请号:PCT/US1991008802

    申请日:1991-11-22

    CPC classification number: C07F15/0013 C07C51/412 C07F13/005

    Abstract: The present invention relates to a process for preparing platinum group metal and rhenium salts of organic carboxylic acids and products obtained using the disclosed process. The process comprises reacting an alkali or alkaline earth metal salt of an organic carboxylic acid with a platinum group metal or rhenium salt in an organic liquid which at least partially dissolves the alkali and/or alkaline earth metal salt, the platinum group metal or rhenium salt and the desired platinum group metal or rhenium carboxylate product, but is not a solvent for the salt formed between the alkali or alkaline earth metal and the anion of the platinum group metal or rhenium salt.

    MIXED LIGAND COMPLEXES AND USES THEREOF AS BINDING AGENTS AND PROBRES TO DNA
    9.
    发明申请
    MIXED LIGAND COMPLEXES AND USES THEREOF AS BINDING AGENTS AND PROBRES TO DNA 审中-公开
    混合配体复合物及其作为结合剂和DNA的用途

    公开(公告)号:WO1990005732A1

    公开(公告)日:1990-05-31

    申请号:PCT/US1989004989

    申请日:1989-11-07

    Abstract: This invention concerns a coordination complex or salt thereof which is spectroscopically or photoactively determinable when bound to DNA having formula (I), wherein M is a suitable transition metal and each of R1, R2 and R3 is ehtylenediamine, bipyridine, phenanthroline, diazafluorene-9-one or a substituted derivative thereof, or phenanthrenequinonediimine or a substituted derivative thereof, dypyridophenazine or a substituted derivative thereof; wherein R1, R2 and R3 are bound to M by coordination bonds; provided that at least one of R1, R2 or R3 is dypyridophenazine or a substituted derivative thereof. The invention also concerns a labelled DNA probe which comprises the complex covalently bound to the DNA probe. Further the invention concerns a method of detecting the presence in a sample of a target DNA of interest which comprises contacting the sample containing the target DNA with a complementary labelled DNA probe under hydridizing conditions and measuring the resulting luminescence emitted from the labelled DNA probe, a change in the luminescense as compared with the luminescense in the absence of the sample indicating the presence of the target DNA.

    Abstract translation: 本发明涉及当与具有式(I)的DNA结合时光谱或光活性测定的配位络合物或其盐,其中M为合适的过渡金属,R 1,R 2和R 3各自为乙二胺,联吡啶,菲咯啉,二氮杂芴-9 或其取代衍生物,或菲醌亚胺或其取代衍生物,二吡啶并吩嗪或其取代的衍生物; 其中R1,R2和R3通过配位键与M结合; 条件是R 1,R 2或R 3中的至少一个是二吡啶并吩嗪或其取代的衍生物。 本发明还涉及标记的DNA探针,其包含共价结合DNA探针的复合物。 此外,本发明涉及一种检测目标DNA样品中存在的方法,该方法包括在杂交条件下使包含靶DNA的样品与补体标记的DNA探针接触,并测量从标记的DNA探针发射的所得发光, 在不存在样品表明靶DNA存在的情况下,与发光体相比,发光体的变化。

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