SILYL MONOMERS CAPABLE OF MULTIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME
    31.
    发明申请
    SILYL MONOMERS CAPABLE OF MULTIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME 审中-公开
    可在水溶液中多元化的SILYL单体及其使用方法

    公开(公告)号:WO2013058825A1

    公开(公告)日:2013-04-25

    申请号:PCT/US2012/032813

    申请日:2012-04-09

    CPC classification number: A61K31/695 A61K47/481 A61K47/55 C07F7/10

    Abstract: Described herein are silyl monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. Such multimer forming associations of monomers may be promoted by the proximal binding of the monomers to their target biomolecule(s). In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.

    Abstract translation: 本文描述的是当在水性介质中与一种,两种,三种或更多种其它单体接触时能够形成生物学上有用的多聚体的甲硅烷基单体。 单体的这种多聚体形成关联可以通过单体与其目标生物分子的近端结合来促进。 在一个方面,这样的单体可以能够在水性介质中(例如在体内)结合另一单体以形成多聚体(例如二聚体)。 考虑的单体可以包括配体部分,连接体元件和连接配体部分和连接体元件的连接器元件。 在水性介质中,这样预期的单体可以经由每个连接体元件连接在一起,因此可以基本上同时调节一种或多种生物分子,例如调节蛋白质上或不同蛋白质上的两个或多个结合结构域。

    BROMODOMAIN LIGANDS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME
    32.
    发明申请
    BROMODOMAIN LIGANDS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME 审中-公开
    在水溶液中二次分配的BROMODOMAIN配体及其使用方法

    公开(公告)号:WO2013033270A2

    公开(公告)日:2013-03-07

    申请号:PCT/US2012/052943

    申请日:2012-08-29

    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.

    Abstract translation: 本文描述的是当在水性介质中与一种,两种,三种或更多种其它单体接触时,能够形成生物有用的多聚体的单体。 在一个方面,这样的单体可能能够在水性介质(例如体内)中结合另一单体以形成多聚体(例如二聚体)。 考虑的单体可以包括配体部分,连接体元件和连接配体部分和连接体元件的连接器元件。 在水性介质中,这样预期的单体可以经由每个连接体元件连接在一起,因此可以基本上同时调节一种或多种生物分子,例如调节蛋白质上或不同蛋白质上的两个或多个结合结构域。

    CRYSTAL STRUCTURE OF SMYD3 PROTEIN
    34.
    发明申请
    CRYSTAL STRUCTURE OF SMYD3 PROTEIN 审中-公开
    SMYD3蛋白的晶体结构

    公开(公告)号:WO2008137834A3

    公开(公告)日:2009-02-26

    申请号:PCT/US2008062636

    申请日:2008-05-05

    CPC classification number: C12N9/1007 C07K2299/00 G01N2500/04

    Abstract: The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.

    Abstract translation: 本发明涉及SMYD3甲基转移酶(SMYD3),SMYD3结合口袋或SMYD3样结合口袋。 本发明涉及一种计算机,包括用这种结合口袋的结构坐标编码的数据存储介质。 本发明还涉及使用结构坐标来解决同源蛋白质或蛋白质复合物的结构的方法。 本发明涉及使用结构坐标来筛选和设计结合SMYD3甲基转移酶蛋白质的化合物,SMYD3甲基转移酶蛋白质的复合物,其同源物或SMYD3样蛋白质或蛋白质复合物的方法。

    COMBINATION OF IGFR INHIBITOR AND ANTI-CANCER AGENT
    35.
    发明申请
    COMBINATION OF IGFR INHIBITOR AND ANTI-CANCER AGENT 审中-公开
    IGFR抑制剂和抗癌剂的组合

    公开(公告)号:WO2008076143A1

    公开(公告)日:2008-06-26

    申请号:PCT/US2007/009178

    申请日:2007-04-13

    Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an anticancer agent and an IGFlR inhibitor compound of Formula (I) combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an anticancer agent and IGFlR inhibitor compound of Formula (I) combination with a pharmaceutically acceptable carrier. The IGFl R inhibitor is represented by Formula (I): wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein.

    Abstract translation: 本发明提供了一种用于治疗患者的肿瘤或肿瘤转移的方法,其包括向患者同时或依次施用治疗有效量的抗癌剂和式(I)组合的IGF1R抑制剂化合物,其具有或不包含另外的试剂或 治疗,如其他抗癌药物或放射治疗。 本发明还包括由抗癌剂和式(I)的IGF1R抑制剂化合物与药学上可接受的载体组合的药物组合物。 IGF1R抑制剂由式(I)表示:其中X 1,X 2,X 3,X 4, X 1,X 5,X 6,X 7,R 1和Q 1, / SUP>。

    EXTRACTION OF ENERGY FROM FLOWING FLUIDS
    39.
    发明申请
    EXTRACTION OF ENERGY FROM FLOWING FLUIDS 审中-公开
    从流体流中提取能量

    公开(公告)号:WO1998012433A1

    公开(公告)日:1998-03-26

    申请号:PCT/US1997016955

    申请日:1997-09-19

    Applicant: ARNOLD, Lee

    Abstract: Method and apparatus for converting the kinetic energy of a moving fluid stream into useful work by using a cascade of thin aero of hydro foils (2) positioned therein. The foils may be provided with at least two degrees of freedom and adjacent foils move out of phase. The foils are subjected to fluid induced oscillations known as flutter. Barriers (3, 43) may be positioned downstream, above, or at the sides of the apparatus for increasing efficiency. A system of fly wheels (17, 18) to increase inertia of the foils may be used with the hydrofoils. A cascade of aero of hydro foils may be mechanically oscillated.

    Abstract translation: 通过使用位于其中的液压箔(2)的薄层级联将运动流体流的动能转换成有用功的方法和装置。 箔可以设置有至少两个自由度,并且相邻的箔不同相移动。 箔片受到称为颤振的流体诱发振荡。 障碍物(3,43)可以位于设备的下游,上方或两侧,以提高效率。 用于增加箔的惯性的飞轮(17,18)的系统可以与水翼一起使用。 液压翼片的级联可以机械振荡。

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