DISACCHARIDE INTERMEDIATE AND SYNTHESIS METHOD THEREOF
    1.
    发明申请
    DISACCHARIDE INTERMEDIATE AND SYNTHESIS METHOD THEREOF 审中-公开
    不同的中间体及其合成方法

    公开(公告)号:US20160264609A1

    公开(公告)日:2016-09-15

    申请号:US15036390

    申请日:2014-04-28

    IPC分类号: C07H11/00 C07H17/04

    摘要: The present invention relates to a disaccharide intermediate and a synthesis method thereof, relates to the chemical pharmaceutical field, and more specifically relates to a method for preparing a disaccharide segment of a key intermediate for chemically synthesizing heparin and heparinoid compounds. Disclosed are a new disaccharide intermediate and three methods for synthesizing the disaccharide intermediate, that is, compounds of a formula (4) and glucopyranose protected by different anomeric carbon are made to react in the presence of an active agent, to obtain the disaccharide intermediate. According to the technical solutions of the present invention, synthetic raw materials are easy to obtain, have a mild reaction condition, and are suitable for industrialized production.

    摘要翻译: 本发明涉及二糖中间体及其合成方法,涉及化学药物领域,更具体地涉及制备化学合成肝素和类肝素化合物的关键中间体的二糖段的方法。 公开了一种新的二糖中间体和三种合成二糖中间体的方法,即式(4)的化合物和由不同端基异构体碳保护的吡喃葡萄糖在活性剂存在下反应,得到二糖中间体。 根据本发明的技术方案,合成原料易于获得,反应条件温和,适用于工业化生产。

    4-((substituted phenyl) difluoromethyl) phenoxy carboxylic acid derivative, and preparation method and uses thereof
    3.
    发明授权
    4-((substituted phenyl) difluoromethyl) phenoxy carboxylic acid derivative, and preparation method and uses thereof 有权
    4 - ((取代苯基)二氟甲基)苯氧基羧酸衍生物及其制备方法和用途

    公开(公告)号:US09487470B2

    公开(公告)日:2016-11-08

    申请号:US14396455

    申请日:2013-04-25

    摘要: The present invention discloses a 4-((substituted phenyl)difluoromethyl)phenoxycarboxylic acid derivative and preparation process and use thereof. More specifically, the present invention relates to a compound of the following formula I, which is defined in the specification. The compounds according to the present invention can be used as PPAR agonists, and demonstrates a strong effect on reducing the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in blood plasma, and thus the compound according to the present invention can be used in the preparation of a medicament for treating or preventing hyperlipoidemia or cardio-cerebrovascular diseases caused by hyperlipoidemia, such as diabetes, atherosclerosis, stroke, coronary heart disease, etc. The present invention also relates to a novel intermediate compound for the preparation of the compound of formula I and preparation method thereof.

    摘要翻译: 本发明公开了4 - ((取代苯基)二氟甲基)苯氧基羧酸衍生物及其制备方法和用途。 更具体地,本发明涉及在说明书中定义的下式I的化合物。 根据本发明的化合物可用作PPAR激动剂,并且对降低血浆中总胆固醇(TC),甘油三酯(TG)和低密度脂蛋白胆固醇(LDL-C)的水平具有很强的作用, 因此根据本发明的化合物可用于制备用于治疗或预防高脂血症引起的高脂血症或心脑血管疾病如糖尿病,动脉粥样硬化,中风,冠心病等的药物。本发明还涉及 涉及用于制备式I化合物的新型中间体化合物及其制备方法。

    METHOD FOR PREPARING 3-O-BENZYL-1,2-O-ISOPROPYLIDENE-A-L-FURAN IDOSE
    4.
    发明申请
    METHOD FOR PREPARING 3-O-BENZYL-1,2-O-ISOPROPYLIDENE-A-L-FURAN IDOSE 审中-公开
    制备3- O-BENZYL-1,2-O-ISOPROPYLIDENE-A-L-FURAN IDOSE的方法

    公开(公告)号:US20150065700A1

    公开(公告)日:2015-03-05

    申请号:US14380605

    申请日:2013-02-22

    IPC分类号: C07H1/00 C07H19/01

    CPC分类号: C07H1/00 C07H15/18 C07H19/01

    摘要: Provided is a method for preparing 3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose, which comprises: (1) protecting hydroxyl of 3-O-benzyl-1,2-O-isopropylidene-α-D-glucofuranose (III) by benzoyl and methylsulfonyl to obtain 6-O-benzoyl-3-O-benzyl-1,2-O-isopropylidene-5-O-methylsulfonyl-α-D-glucofuranose (V); (2) subjecting compound (V) to a cyclization reaction under an alkaline condition to obtain 5,6-epoxy-3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose (VI); and (3) subjecting compound (VI) to a ring-opening reaction to obtain 3-O-benzyl-1,2-O-isopropylidene-α-L-idofuranose.

    摘要翻译: 提供了一种制备3-O-苄基-1,2- -O-异亚丙基-α-L-异呋喃糖的方法,其包括:(1)保护3-O-苄基-1,2-邻 - 异亚丙基-α D-吡喃葡萄糖(III),得到6-O-苯甲酰基-3-O-苄基-1,2-O-异亚丙基-5-O-甲基磺酰基-α-D-吡喃葡萄糖(V); (2)在碱性条件下使化合物(V)进行环化反应,得到5,6-环氧-3-O-苄基-1,2-邻异丙叉基-α-L-异呋喃糖(VI); 和(3)使化合物(VI)进行开环反应,得到3-O-苄基-1,2-O-异亚丙基-α-L-异呋喃糖。

    4-((SUBSTITUTED PHENYL) DIFLUOROMETHYL) PHENOXY CARBOXYLIC ACID DERIVATIVE, AND PREPARATION METHOD AND USES THEREOF
    7.
    发明申请
    4-((SUBSTITUTED PHENYL) DIFLUOROMETHYL) PHENOXY CARBOXYLIC ACID DERIVATIVE, AND PREPARATION METHOD AND USES THEREOF 有权
    4 - ((取代苯基)二氟甲基)苯氧基羧酸衍生物及其制备方法及其用途

    公开(公告)号:US20150119458A1

    公开(公告)日:2015-04-30

    申请号:US14396455

    申请日:2013-04-25

    摘要: The present invention discloses a 4-((substituted phenyl)difluoromethyl)phenoxycarboxylic acid derivative and preparation process and use thereof. More specifically, the present invention relates to a compound of the following formula I, which is defined in the specification. The compounds according to the present invention can be used as PPAR agonists, and demonstrates a strong effect on reducing the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in blood plasma, and thus the compound according to the present invention can be used in the preparation of a medicament for treating or preventing hyperlipoidemia or cardio-cerebrovascular diseases caused by hyperlipoidemia, such as diabetes, atherosclerosis, stroke, coronary heart disease, etc. The present invention also relates to a novel intermediate compound for the preparation of the compound of formula I and preparation method thereof.

    摘要翻译: 本发明公开了4 - ((取代苯基)二氟甲基)苯氧基羧酸衍生物及其制备方法和用途。 更具体地,本发明涉及在说明书中定义的下式I的化合物。 根据本发明的化合物可用作PPAR激动剂,并且对降低血浆中总胆固醇(TC),甘油三酯(TG)和低密度脂蛋白胆固醇(LDL-C)的水平具有很强的作用, 因此根据本发明的化合物可用于制备用于治疗或预防高脂血症引起的高脂血症或心脑血管疾病如糖尿病,动脉粥样硬化,中风,冠心病等的药物。本发明还涉及 涉及用于制备式I化合物的新型中间体化合物及其制备方法。