Phenolic hydrazone macrophage migration inhibitory factor inhibitors
    51.
    发明授权
    Phenolic hydrazone macrophage migration inhibitory factor inhibitors 失效
    酚腙巨噬细胞迁移抑制因子抑制剂

    公开(公告)号:US08742173B2

    公开(公告)日:2014-06-03

    申请号:US13418877

    申请日:2012-03-13

    Applicant: Yousef Al-Abed

    Inventor: Yousef Al-Abed

    CPC classification number: C07C251/86 C07C281/02 C07C311/49

    Abstract: Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

    Abstract translation: 提供式(I)的各种化合物:还提供包含上述化合物的药物组合物。 此外,提供了哺乳动物抑制巨噬细胞迁移抑制因子(MIF)活性的方法,以及治疗或预防哺乳动物炎症的方法。 还提供了治疗具有败血症,败血病和/或内毒素性休克的哺乳动物的方法。 还提供了治疗具有自身免疫疾病的哺乳动物的方法以及治疗具有肿瘤的哺乳动物的方法。

    METHODS FOR PRODUCING BIS(SULFONYL)IMIDE AMMONIUM SALT, BIS(SULFONYL)IMIDE AND BIS(SULFONYL)IMIDE LITHIUM SALT
    56.
    发明申请
    METHODS FOR PRODUCING BIS(SULFONYL)IMIDE AMMONIUM SALT, BIS(SULFONYL)IMIDE AND BIS(SULFONYL)IMIDE LITHIUM SALT 审中-公开
    方法生产双(二氯化物)二氯化铵盐,二(三氟乙酸)二氯化物和二(磺酰)二氯化锂盐

    公开(公告)号:US20120165571A1

    公开(公告)日:2012-06-28

    申请号:US13409302

    申请日:2012-03-01

    CPC classification number: C07C303/38 C07C303/40 C07C311/48 C07C311/49

    Abstract: To provide methods for producing a bis(sulfonyl)imide ammonium salt, a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt simply and in good yield. A method for producing a bis(sulfonyl)imide ammonium salt, which comprises reacting a compound of the formula R—CHF—SO2X (wherein R is a C1-4 fluorinated alkyl group which may contain an etheric oxygen atom, or a fluorine atom, and X is a fluorine atom or a chlorine atom) with ammonia in the absence of a catalyst. Further, methods for producing a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt by using the bis(sulfonyl)imide ammonium salt.

    Abstract translation: 为了提供双(磺酰基)酰亚胺铵盐,双(磺酰基)酰亚胺和双(磺酰基)酰亚胺锂盐的简单且良好的收率的方法。 一种制备双(磺酰基)酰亚胺铵盐的方法,其包括使式R-CHF-SO2X(其中R是可以含有醚性氧原子的C1-4氟化烷基或氟原子) 并且X是氟原子或氯原子)与氨在不存在催化剂的情况下进行。 此外,通过使用双(磺酰基)酰亚胺铵盐制备双(磺酰基)酰亚胺和双(磺酰基)亚胺锂盐的方法。

    SMALL MOLECULE PRINTING
    57.
    发明申请
    SMALL MOLECULE PRINTING 审中-公开
    小分子印刷

    公开(公告)号:US20120021933A1

    公开(公告)日:2012-01-26

    申请号:US13094609

    申请日:2011-04-26

    Abstract: The present invention provides compositions and methods to facilitate the identification of compounds that are capable of interacting with a biological macromolecule of interest. In one aspect, a composition is provided that comprises an array of one or more types of chemical compounds attached to a solid support, wherein the density of the array of compounds is at least 1000 spots per cm2. In particularly preferred embodiments, these compounds are attached to the solid support through a covalent interaction. In general, these inventive arrays are generated by: (1) providing a solid support, wherein said solid support is functionalized with a selected chemical moiety capable of interacting with a desired chemical compound to form an attachment; (2) providing one or more solutions of one or more types of compounds to be attached to the solid support; and (3) delivering said one or more types of compounds to the solid support, whereby an array is formed and the array of compounds has a density of at least 1000 spots per cm2. In another aspect, the present invention provides methods for utilizing these arrays to identify small molecule partners for biological macromolecules of interest comprising: (1) providing an array of compounds, wherein the array has a density of at least 1000 spots per cm2; (2) contacting the array with one of more types of biological macromolecules of interest; and (3) determining the interaction of specific small molecule-biological macromolecule partners.

    Abstract translation: 本发明提供了有助于鉴定能够与感兴趣的生物大分子相互作用的化合物的组合物和方法。 在一个方面,提供了包含连接到固体支持物上的一种或多种类型化学化合物的阵列的组合物,其中化合物阵列的密度为每cm 2至少1000个点。 在特别优选的实施方案中,这些化合物通过共价相互作用连接到固体支持物上。 通常,这些本发明的阵列通过以下方式产生:(1)提供固体支持物,其中所述固体支持物用能够与所需化学化合物相互作用以形成附着物的选定化学部分官能化; (2)提供待连接到固体支持物上的一种或多种类型化合物的一种或多种溶液; 和(3)将所述一种或多种类型的化合物递送到固体支持物,由此形成阵列,并且化合物阵列的密度至少为1000个点/ cm2。 在另一方面,本发明提供了利用这些阵列鉴定感兴趣的生物大分子的小分子伴侣的方法,包括:(1)提供化合物阵列,其中阵列的密度至少为1000个点/ cm2; (2)使阵列与感兴趣的多种生物大分子之一接触; 和(3)确定特定小分子 - 生物大分子伴侣的相互作用。

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