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    QUINAZOLINE DERIVATIVES AND QUINAZOLINE COMPLEX PROTEIN KINASE INHIBITOR FOR INHIBITING MULTIPLICAITON OF TUMOR CELLS AND PREPARATION METHOD THEREOF
    43.
    发明申请
    QUINAZOLINE DERIVATIVES AND QUINAZOLINE COMPLEX PROTEIN KINASE INHIBITOR FOR INHIBITING MULTIPLICAITON OF TUMOR CELLS AND PREPARATION METHOD THEREOF 有权
    喹诺酮衍生物和喹唑啉复合蛋白激酶抑制剂抑制肿瘤细胞多形性及其制备方法

    公开(公告)号：US20130225811A1

    公开(公告)日：2013-08-29

    申请号：US13882100

    申请日：2011-10-27

    申请人： Fuyi Wang ,  Qun Luo ,  Liyun Ji ,  Wei Zheng ,  Shuang Lv ,  Xianchan Li

    发明人： Fuyi Wang ,  Qun Luo ,  Liyun Ji ,  Wei Zheng ,  Shuang Lv ,  Xianchan Li

    IPC分类号： C07F15/00

    CPC分类号： C07F15/0053 ,  C07D239/94 ,  C07D403/12 ,  C07F15/0046 ,  C07F17/02

    摘要： Quinazoline derivatives represented by general formula (1) and quinazoline complexes as protein kinase inhibitors, and their preparation methods are provided. Wherein, in general formula (1), at least one of R and R′ is a group containing an atom capable of coordinating with noble metals, m and n are either the same or different and are integers from 0 to 5. Said quinazoline complex as protein kinase inhibitor is formed by coordination compound containing noble metal and said quinazoline derivative ligand capable of coordinating with noble metal in the coordination compound. Used as tyrosine protein kinase inhibitors, Quinazoline derivatives and quinazoline complexes as protein kinase inhibitors provided by the present invention have exhibited good inhibitory effect on proliferation of various tumor cells including human breast cancer cells line (drug-resistant) MCF-7/A, human breast cancer cell line (sensitive) MCF-7/S, prostate cancer cell PC-3, keratinocytes Colo-16, human non-small cell lung cancer cell line A549, etc.

    摘要翻译： 提供了由通式（1）表示的喹唑啉衍生物和喹唑啉配合物作为蛋白激酶抑制剂及其制备方法。 其中，在通式（1）中，R和R'中的至少一个是含有与贵金属配位的原子的基团，m和n相同或不同，为0〜5的整数。所述喹唑啉络合物 因为蛋白激酶抑制剂是由含有贵金属的配位化合物和能与配位化合物中的贵金属配位的喹唑啉衍生物配体形成的。 作为酪氨酸蛋白激酶抑制剂，本发明提供的蛋白激酶抑制剂喹唑啉衍生物和喹唑啉配合物对包括人乳腺癌细胞系（耐药性）MCF-7 / A，人类在内的各种肿瘤细胞的增殖具有良好的抑制作用 乳腺癌细胞株（敏感）MCF-7 / S，前列腺癌细胞PC-3，角质形成细胞Colo-16，人非小细胞肺癌细胞株A549等

    METHODS FOR PREPARING RUTHENIUM CARBENE COMPLEX PRECURSORS AND RUTHENIUM VINYLCARBENE COMPLEXES
    47.
    发明申请
    METHODS FOR PREPARING RUTHENIUM CARBENE COMPLEX PRECURSORS AND RUTHENIUM VINYLCARBENE COMPLEXES 有权
    制备碳酸亚乙酯复合前体和乙烯基烯烃复合物的方法

    公开(公告)号：US20130096313A1

    公开(公告)日：2013-04-18

    申请号：US13272788

    申请日：2011-10-13

    申请人： Linda A. Kunz ,  Steven A. Cohen ,  Melvin L. Luetkens, JR.

    发明人： Linda A. Kunz ,  Steven A. Cohen ,  Melvin L. Luetkens, JR.

    IPC分类号： C07F15/00

    CPC分类号： C07F15/0046 ,  B01J31/2295 ,  C07F15/0053

    摘要： A method for preparing a ruthenium carbene complex precursor includes reacting a ruthenium refinery salt with a hydrogen halide to form a ruthenium intermediate, and reacting the ruthenium intermediate with an L-type ligand to form the ruthenium carbene complex precursor. A method for preparing a ruthenium vinylcarbene complex includes converting a ruthenium carbene complex precursor into a ruthenium hydrido halide complex, and reacting the ruthenium hydrido halide complex with a propargyl halide to form the ruthenium vinylcarbene complex. A method for preparing a ruthenium carbene complex includes converting a ruthenium carbene complex precursor into a ruthenium carbene complex having a structure (PR1R2R3)2Cl2Ru═CH—R4, wherein R1, R2, R3, and R4 are alike or different, and wherein covalent bonds may optionally exist between two or more of R1, R2, and R3.

    摘要翻译： 制备钌卡宾络合物前体的方法包括使钌精炼盐与卤化氢反应形成钌中间体，并使钌中间体与L型配体反应以形成钌卡宾复合物前体。 制备钌乙烯基卡巴复合物的方法包括将钌卡宾络合物前体转化为卤化钌卤化物络合物，并使卤化钌卤化物络合物与炔丙基卤反应形成钌乙烯基卡巴复合物。 制备钌卡宾络合物的方法包括将钌卡宾络合物前体转化成具有结构（PR1R2R3）2Cl2Ru = CH-R4的钌卡宾络合物，其中R1，R2，R3和R4是相同或不同的，其中共价键 可以任选地存在于R 1，R 2和R 3中的两个或多个之间。

    Compounds With Modifying Activity Enhanced Under Hypoxic Conditions
    50.
    发明申请
    Compounds With Modifying Activity Enhanced Under Hypoxic Conditions 有权
    低氧条件下改性活性增强的化合物

    公开(公告)号：US20120295880A1

    公开(公告)日：2012-11-22

    申请号：US13564169

    申请日：2012-08-01

    申请人： Frederick M. MacDonnell ,  Thamara K. Janaratne ,  Sanjay Awashti

    发明人： Frederick M. MacDonnell ,  Thamara K. Janaratne ,  Sanjay Awashti

    IPC分类号： C07F15/00 ,  C12N9/99 ,  C12N5/09 ,  A61K31/555 ,  C12N5/071

    CPC分类号： C12N5/0693 ,  A61K31/435 ,  A61K49/0017 ,  C07F15/0046 ,  C07F15/0053 ,  C12N2500/10

    摘要： Compositions and methods for modifying one or more biologic targets are provided. Suitable targets include cells, DNA, proteins, enzymes, and/or a subject in need thereof. The compositions may exist as a monomer or multimer and are active in a biologic environment with enhanced activity in hypoxic environments and, thus, exhibit improved specificity for hypoxic biologic targets (e.g., tumorigenic cells and those undergoing uncontrolled cell growth). A composition typically comprises a complex with an overall charge of 2+ or greater having at least one ruthenium atom attached to a redox active ligand. The redox active ligand helps maintain separation of more than one ruthenium atom. Suitable compositions may further include a terminal ligand comprising a heterocyclic aromatic compound. When provided to a biologic target, the composition modifies the biologic target and no additional compounds need be provided. Suitable compositions are typically catalytic and regenerative in the presence of a reducing agent.

    摘要翻译： 提供了修改一个或多个生物靶标的组合物和方法。 合适的靶标包括细胞，DNA，蛋白质，酶和/或有需要的受试者。 组合物可以作为单体或多聚体存在，并且在缺氧环境中具有增强活性的生物环境中具有活性，因此对缺氧生物靶标（例如致瘤细胞和经受不受控制的细胞生长的那些）表现出改善的特异性。 组合物通常包含具有2+或更大的总电荷的复合物，其具有连接到氧化还原活性配体的至少一个钌原子。 氧化还原活性配体有助于保持多于一个钌原子的分离。 合适的组合物还可以包括包含杂环芳族化合物的末端配体。 当提供给生物靶标时，组合物修饰生物靶标，不需要提供其他化合物。 合适的组合物通常在还原剂存在下是催化和再生的。