1,3-DIPHENYLPROPANE DERIVATIVES, PREPARATIONS AND USES THEREOF
    7.
    发明公开
    1,3-DIPHENYLPROPANE DERIVATIVES, PREPARATIONS AND USES THEREOF 审中-公开
    1,3-二苯基丙烷衍生物,其制备方法和用途

    公开(公告)号:EP2811992A1

    公开(公告)日:2014-12-17

    申请号:EP12808850.7

    申请日:2012-12-28

    申请人: Genfit

    摘要: The present invention relates to novel 1,3-diphenylpropane derivatives, pharmaceutical compositions comprising the same and therapeutic uses thereof, in particular in the fields of human and animal health. The compounds according to the present invention have intrinsic PPAR agonist properties. They are therefore of particular interest in the treatment of metabolic and/or inflammatory diseases and particularly peripheral and central diseases associated with the metabolic syndrome, such as diverse forms of steatohepatitis, type 2 diabetes, diverse neurodegenerative disorders,such as Alzheimer'sdisease, Parkinson's disease and multiple sclerosis.

    摘要翻译: 本发明涉及新的1,3-二苯基丙烷衍生物,包含其的药物组合物和其治疗用途,特别是在人类和动物健康领域。 根据本发明的化合物具有固有的PPAR激动剂性质。 因此,他们特别关注代谢和/或炎性疾病的治疗,特别是与代谢综合征相关的外周和中枢性疾病,如各种形式的脂肪性肝炎,2型糖尿病,多种神经退行性疾病如阿尔茨海默氏病,帕金森病 疾病和多发性硬化症。

    IMPROVED PREPARATION OF CHALCONE DERIVATIVES
    9.
    发明公开
    IMPROVED PREPARATION OF CHALCONE DERIVATIVES 有权
    VERBESSERTE HERSTELLUNG VON CHALCONDERIVATEN

    公开(公告)号:EP2571843A1

    公开(公告)日:2013-03-27

    申请号:EP11720091.5

    申请日:2011-05-16

    申请人: Genfit

    摘要: The invention relates to methods for producing chalcone (1,3-diphenylprop-2-en-1-one) derivatives that have multiple substitutions on a phenyl ring. Intermediate chalcone derivatives are modified by Phase Transfer Catalysis (PTC) for introducing a substituted alkyl group that is provided by a sulfonic acid derivative on a phenyl ring already containing substituent groups on one or two carbon atoms adjacent to the carbon atom where a substituent group is being introduced. The methods of the invention allow producing efficiently, by either S-alkylation or O-alkylation, chalcones derivatives that are characterized for their biological activities that are intermediate compounds for producing molecules having such activities, or that can be used for generating libraries of compounds to be screened by means of in vitro and/or in vivo assays and establishing structure-activity relationships.

    摘要翻译: 本发明涉及在苯环上具有多个取代基的查尔酮(1,3-二苯基丙-2-烯-1-酮)衍生物的方法。 中间查耳酮衍生物通过相转移催化剂(PTC)修饰,用于将由磺酸衍生物提供的取代烷基引入到已经含有一个或两个邻近碳原子上的取代基的取代基的苯环上,其中取代基为 被介绍。 本发明的方法允许通过S-烷基化或O-烷基化有效生产由生物活性表征的查尔酮衍生物,其是用于产生具有这种活性的分子的中间体化合物,或可用于产生化合物文库 通过体外和/或体内测定法筛选并建立结构 - 活性关系。