Zwitterionic zinc(II) carboxylate compounds and their use

    公开(公告)号:US10023594B2

    公开(公告)日:2018-07-17

    申请号:US15251300

    申请日:2016-08-30

    Abstract: A method of preparing a crystalline zwitterionic zinc(II)-carboxylate compound includes the steps of preparing a mixture of zinc(II) ions and a first pyridyl ligand having three carboxylic acid moieties; subjecting the mixture to conditions under which a precipitate is formed; separating the precipitate; adding a solvent and optionally a second pyridyl ligand to the separated precipitate; subjecting the obtained mixture to conditions under which crystals of the zwitterionic zinc(II)-carboxylate compound are formed; and separating the crystals of the zwitterionic zinc(II)-carboxylate compound. Preferably but not exclusively, the crystalline zwitterionic zinc(II)-carboxylate compound essentially consists of at least one 1D coordination polymer. The compounds are suitable for providing a sensing platform for detecting the presence or amount of target nucleic acid, particularly HIV-1 ds-DNA, with specificity, and, thus, a method of detecting a target nucleic acid sequence in a sample and a kit including the compounds and an oligonucleotide probe are also provided.

    Lunar Brightness Temperature Modeling Based on the Microwave Radiometer Data

    公开(公告)号:US20180150574A1

    公开(公告)日:2018-05-31

    申请号:US15364239

    申请日:2016-11-29

    Inventor: Zhanchuan CAI

    CPC classification number: G06F17/5009

    Abstract: A computer system executes hierarchical MK splines approximation for lunar brightness temperature (TB) data approximation. The computer system constructs a TB model map by generating a final approximation function for constructing an interpolated surface that approximates the TB data set obtained by lunar probe. The method includes executing MK splines approximation to the TB data set with a hierarchy of control lattice from coarsest lattice to densest lattice to iteratively obtain approximation functions. The TB model map is constructed by generating a final approximation function to construct the interpolated surface.

    CRYSTALLINE CONTRAST AGENT FOR MAGNETIC RESONANCE IMAGING, KIT AND COMPOSITION COMPRISING IT AND THEIR USE

    公开(公告)号:US20180078660A1

    公开(公告)日:2018-03-22

    申请号:US15271368

    申请日:2016-09-21

    Abstract: A method of preparing a crystalline contrast agent for magnetic resonance imaging from a zwitterionic carboxylic pyridyl ligand includes mixing metal ion and the pyridyl ligand and obtaining crystals therefrom. The crystalline contrast agent includes a manganese-organic or gadolinium-organic 3D framework. The crystalline contrast agent is employed in a kit and a pharmaceutically acceptable composition. The method allows for preparing crystalline contrast agents with superior properties with easily available starting materials and with an economic and efficient process. The method allows for preparing crystalline contrast agents with exceptional water-stability and water-solubility, which exhibit high longitudinal relaxivities and with excellent stabilities under physiological conditions and low cytotoxicity. Further provided is a method for in vivo imaging of a subject, in particular a human, comprising administering the crystalline contrast agent to the subject.

    ZWITTERIONIC ZINC(II) CARBOXYLATE COMPOUNDS AND THEIR USE

    公开(公告)号:US20180057512A1

    公开(公告)日:2018-03-01

    申请号:US15251300

    申请日:2016-08-30

    CPC classification number: C07F3/06 C12Q1/703

    Abstract: A method of preparing a crystalline zwitterionic zinc(II)-carboxylate compound includes the steps of preparing a mixture of zinc(II) ions and a first pyridyl ligand having three carboxylic acid moieties; subjecting the mixture to conditions under which a precipitate is formed; separating the precipitate; adding a solvent and optionally a second pyridyl ligand to the separated precipitate; subjecting the obtained mixture to conditions under which crystals of the zwitterionic zinc(II)-carboxylate compound are formed; and separating the crystals of the zwitterionic zinc(II)-carboxylate compound. Preferably but not exclusively, the crystalline zwitterionic zinc(II)-carboxylate compound essentially consists of at least one 1D coordination polymer. The compounds are suitable for providing a sensing platform for detecting the presence or amount of target nucleic acid, particularly HIV-1 ds-DNA, with specificity, and, thus, a method of detecting a target nucleic acid sequence in a sample and a kit including the compounds and an oligonucleotide probe are also provided.

    ALK KINASE INHIBITOR AND ITS USE
    69.
    发明申请

    公开(公告)号:US20180050037A1

    公开(公告)日:2018-02-22

    申请号:US15239288

    申请日:2016-08-17

    CPC classification number: A61K31/519

    Abstract: A compound for treating a disease, in particular cancer like non-small cell lung cancer, exceptionally inhibits activity of oncogenic ALK kinase. Compositions, particularly pharmaceutical compositions, are provided comprising this compound. Methods for targeting cancer cells harboring an abnormality in the ALK gene are also The compound for treating a disease has certain structural elements, namely a tricyclic, more specifically heterocyclic, backbone as the core part of the compound at least one highly electronegative atom in form of a tertiary amine attached to the backbone via an at most 6-membered linking group with a terminal highly electronegative atom in form of a nitrogen as secondary amine, and a further hydrophobic moiety fused to the backbone. The structural components allow for an advantageous interaction with the ALK kinase domain. The compound therefor represents a highly promising treatment option for patients in particular those bearing ALK-dependent non-small cell lung cancer.

    Cobalt-polypyridyl complex for treatment of cancer, a pharmaceutical composition and a kit comprising it

    公开(公告)号:US09895338B1

    公开(公告)日:2018-02-20

    申请号:US15242883

    申请日:2016-08-22

    CPC classification number: A61K31/555 A61K31/28 A61K45/06 A61K2300/00

    Abstract: A method for treating a subject suffering from a cancer, in particular a multidrug-resistant cancer includes administrating a cobalt-polypyridyl complex to the subject. A method for suppressing the growth of cancer cells, in particular inducing autophagy of the cancer cells, inducing cell cycle arrest of the cancer cells and/or inhibiting cell invasion of the cancer cells and for specifically targeting cancer cells with multidrug-resistance includes contacting said cancer cells with the cobalt-polypyridyl complex. A pharmaceutical composition and a kit are provided and include the cobalt-polypyridyl complex. Unexpectedly, the cobalt-polypyridyl complex is especially suitable to treat cancer, in particular multidrug-resistant cancer with an exceptionally increased cytotoxic activity towards multidrug-resistant cancer cells.

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