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2351 条记录 (耗时 0.054 秒)

    FLUORINATED AMIDE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS
    13.
    发明申请
    FLUORINATED AMIDE DERIVATIVES AND THEIR USES AS THERAPEUTIC AGENTS 审中-公开
    氟化酰胺衍生物及其作为治疗剂的用途

    公开(公告)号：WO2017070795A1

    公开(公告)日：2017-05-04

    申请号：PCT/CA2016/051260

    申请日：2016-10-31

    申请人： TRILLIUM THERAPEUTICS INC.

    发明人： SLASSI, Abdelmalik

    IPC分类号： C07C235/20 ,  A61K31/165 ,  A61P25/00 ,  C07C237/06

    CPC分类号： C07C237/06 ,  C07B2200/07 ,  C07C235/20

    摘要： The present application relates to novel fluorinated amide derivatives of Formula (I), to processes for preparing them, pharmaceutical compositions containing them, and their use thereof in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain and other related CNS disorders.

    摘要翻译： 本申请涉及式（I）的新型氟化酰胺衍生物，制备它们的方法，含有它们的药物组合物及其在治疗或预防急性和/或慢性神经疾病中的用途 如精神病，癫痫，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷，以及慢性和急性疼痛以及其他相关的CNS疾病。

    COMPOSITION AND METHODS OF USE OF NOVEL PHENYLALANINE SMALL ORGANIC COMPOUNDS TO DIRECTLY MODULATE PCSK9 PROTEIN ACTIVITY
    15.
    发明申请
    COMPOSITION AND METHODS OF USE OF NOVEL PHENYLALANINE SMALL ORGANIC COMPOUNDS TO DIRECTLY MODULATE PCSK9 PROTEIN ACTIVITY 审中-公开
    新型苯丙氨酸小有机化合物直接调节PCSK9蛋白活性的组合物和方法

    公开(公告)号：WO2017034994A1

    公开(公告)日：2017-03-02

    申请号：PCT/US2016/047810

    申请日：2016-08-19

    申请人： PORTOLA PHARMACEUTICALS, INC.

    发明人： BARTA, Thomas, E. ,  BOURNE, Jonathan, William ,  MONROE, Kyle, D. ,  MUEHLEMANN, Michael, M. ,  PANDEY, Anjali ,  BOWERS, Simeon

    IPC分类号： A61K38/17

    CPC分类号： A61K45/06 ,  C07B2200/07 ,  C07C237/20 ,  C07D213/64

    摘要： This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL- cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.

    摘要翻译： 本发明涉及PCSK9生物学领域以及使用小有机化合物作为调节PCSK9生物活性的配体的组成和方法。 特别地，本发明提供了通过改变蛋白质PCSK9的构象来调节低密度脂蛋白的循环水平的小有机化合物的组合物。 将这些小的有机化合物配体与PCSK9结合改变蛋白质的构象，改变PCSK9与内源性低密度脂蛋白受体之间的相互作用，并且可导致循环低密度脂蛋白胆固醇水平的降低或增加。 高LDL-胆固醇水平与心脏病风险增加有关。 低脂低胆固醇水平可能在其他病症如肝功能障碍中有问题; 因此，也可以提高可以提高LDL水平的小有机化合物配体。