Inhibition of GASC1
    31.
    发明授权
    Inhibition of GASC1 有权
    抑制GASC1

    公开(公告)号:US08420335B2

    公开(公告)日:2013-04-16

    申请号:US12282485

    申请日:2007-03-14

    IPC分类号: G01N33/53 G01N31/00

    摘要: The present invention provides a method of testing the ability of a test compound to bind to and optionally modulate the activity of a protein of the JMJD2 subfamily of Jumonji proteins. The method comprises incubating a test compound with a protein of the JMJD2 subfamily of Jumonji proteins, a co-factor of said protein and, optionally, a substrate for demethylation. The method of the invention can be used for screening large numbers of compounds to identify a group of compounds that are candidate compounds for clinical use for treatment of certain cancers especially prostate cancers. Other compounds that do not have activity in the screening assays can be eliminated from further consideration as candidate compounds. The method of the invention therefore has utility in the pharmaceutical industry.

    摘要翻译: 本发明提供了测试化合物与Jumonji蛋白的JMJD2亚家族蛋白质结合并任选调节其活性的能力的方法。 该方法包括将测试化合物与Jumonji蛋白的JMJD2亚族蛋白质的蛋白质,所述蛋白质的辅因子和任选的脱甲基化底物一起孵育。 本发明的方法可用于筛选大量化合物以鉴定作为临床用于治疗某些癌症,特别是前列腺癌的候选化合物的一组化合物。 在筛选测定中不具有活性的其它化合物可以从作为候选化合物的进一步考虑中消除。 因此,本发明的方法在制药工业中具有效用。

    Compounds useful in the diagnosis and treatment of pregnancy-associated malaria
    33.
    发明授权
    Compounds useful in the diagnosis and treatment of pregnancy-associated malaria 有权
    可用于妊娠相关疟疾诊断和治疗的化合物

    公开(公告)号:US07745580B2

    公开(公告)日:2010-06-29

    申请号:US10543312

    申请日:2003-12-30

    IPC分类号: A61K39/00 C07K1/00 C07K2/00

    摘要: The present invention relates to nucleic acid molecules related to the var2csa gene family as well as amino acid sequences encoded by such nucleic acid molecules with respect to their role in mediating adhesion of infected red blood cells to chondroitin sulphate A (CSA) in the placenta which is characteristic for the pathogenesis of pregnancy associated malaria (PAM). Accordingly, The invention provides the use compounds that are related to VAR2CSA polypeptides var2csa nucleic acid molecules as medicaments, as well as it provides pharmaceutical compositions, in particular immunological compositions and vaccines, hereunder nucleotide-based vaccines comprising these compounds. In addition, the invention provides the use of the compounds mentioned for the manufacture of compositions, such as immunogenic compositions. Other aspects of the invention relates to methods of treatment and prevention of pregnancy associated malaria wherein these methods are based on the nucleic acid molecules and polypeptides the invention. As these compounds can also be used as biotechnological tools the invention provides in vitro diagnostic methods and kits comprising reagents and IgGs/antibodies designated to the use in such methods. The invention also relates to methods of identifying agents capable of modulating the VAR2CSA dependent adhesion to CSA and agent capable of interacting with VAR2CSA. Finally, a method for identifying polypeptides, which will induce a specific IgG/antibody response upon administration to a subject is provided by the invention.

    摘要翻译: 本发明涉及与var2csa基因家族有关的核酸分子,以及由这些核酸分子编码的氨基酸序列,涉及它们在介导感染的红细胞与胎盘中的硫酸软骨素A(CSA)的粘附中的作用, 是怀孕相关疟疾(PAM)发病机制的特征。 因此,本发明提供了与VAR2CSA多肽var2csa核酸分子作为药物相关的用途化合物,以及其提供药物组合物,特别是免疫组合物和疫苗,以下包含这些化合物的基于核苷酸的疫苗。 此外,本发明提供了所述化合物用于制备组合物如免疫原性组合物的用途。 本发明的其它方面涉及治疗和预防妊娠相关疟疾的方法,其中这些方法基于本发明的核酸分子和多肽。 由于这些化合物也可用作生物技术工具,本发明提供了体外诊断方法和试剂盒,其中包括用于此类方法的试剂和IgG /抗体。 本发明还涉及鉴定能够调节VAR2CSA对CSA的依赖性粘附和能够与VAR2CSA相互作用的试剂的鉴定试剂的方法。 最后,本发明提供了鉴定多肽的方法,所述多肽在给予受试者时将诱导特异性IgG /抗体应答。

    Sol-gel based matrix
    36.
    发明授权

    公开(公告)号:US10233328B2

    公开(公告)日:2019-03-19

    申请号:US15028600

    申请日:2014-10-24

    摘要: The present invention relates to a method for the production of a sol-gel based matrix. The method comprises the steps of: a) providing a first alkoxysilane of the general formula: R1—Si(OR2)3 and a second alkoxysilane of the general formula (I): b) preparing a first sol-gel component by polymerization of the first alkoxysilane in the presence of an acid catalyst, c) preparing a second sol-gel component by polymerization of the second alkoxysilane in the presence of an Lewis acid catalyst, d) Mixing the first sol-gel component and the second sol-gel component for the preparation of a sol-gel based matrix. The above method results in a sol-gel based matrix with high stability and high porosity. The sol-gel based material may be used for the production of a composite or sensor suitable for monitoring analytes. Methods for preparing these composites or sensors are provided as well.

    PYRROLIDINE-2-CARBOXYLIC ACID DERIVATIVES AS IGLUR ANTAGONISTS
    40.
    发明申请
    PYRROLIDINE-2-CARBOXYLIC ACID DERIVATIVES AS IGLUR ANTAGONISTS 审中-公开
    吡咯烷-2-羧酸衍生物作为IGLUR ANTAGONISTS

    公开(公告)号:US20140235576A1

    公开(公告)日:2014-08-21

    申请号:US14181169

    申请日:2014-02-14

    发明人: Lennart BUCH

    IPC分类号: C07D207/16 C07F7/18

    CPC分类号: C07D207/16 C07F7/1804

    摘要: The present invention relates to compounds of Formula (I), combinations and use thereof for disease therapy, or pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoismers and polymorphs thereof, which are iGluR receptor inhibitors, and hence are useful in the treatment of psychiatric diseases or neurological disorders or a disease or disorder associated with abnormal activities of iGluR receptors.

    摘要翻译: 本发明涉及式(I)化合物,其用于疾病治疗的组合和用途,或其药学上可接受的盐或溶剂合物,包括iGluR受体抑制剂的所有互变异构体,立体异构体和多晶型物,因此可用于治疗 精神疾病或神经障碍或与iGluR受体的异常活动相关的疾病或病症。