Verfahren zur Herstellung von Guanidinderivaten

    公开(公告)号:EP1028106A1

    公开(公告)日:2000-08-16

    申请号:EP00102786.1

    申请日:2000-02-10

    IPC分类号: C07C277/02 C07C279/14

    CPC分类号: C07C277/08 C07C279/14

    摘要: Beschrieben wird ein Verfahren zur Herstellung von Guanidinderivaten, insbesondere Kreatin, bei dem ein Cyanamidderivat und ein primäres oder sekundäres Amin in Gegenwart von Kristallen des Guanidinderivates kontinuierlich vereinigt werden.

    摘要翻译: 胍衍生物(I)的制备包括在(I)的晶种存在下连续地使氰酰胺衍生物(II)与胺(III)反应。 制备式(I)的胍衍生物包括使式(II)的氰酰胺衍生物与式(III)的胺反应。 (II)和(III)在(I)的晶种的存在下连续反应。 R1 = 1-8C烷基或二价5-10C脂环族基团; R2 = H或1-8C烷基; 或NR 1 R 2 =被Z取代的5-6元环; Z = COOR3,SO2OR3或PO(OR3)(OR4); R3 = H或当量的碱金属(ne earth); R4 = H,当量为碱(ne earth)金属或1-6C烷基R5,R6 = H或1-8C烷基; R5',R6'= H,当量为碱金属(ne earth)或1-8C烷基。

    N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
    27.
    发明公开
    N1-CYCLIC AMINE-N5-SUBSTITUTED PHENYL BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
    N1-环胺N5-取代双胍类,生产和药物组合物,以便方法

    公开(公告)号:EP2742019A2

    公开(公告)日:2014-06-18

    申请号:EP12821403.8

    申请日:2012-08-08

    摘要: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.

    摘要翻译: 提供了式1的N1-环胺-N5-substituiertem苯基双胍衍生物或其药学上可接受的盐,其制造方法,以及包括该双胍衍生物或作为活性成分的药学上可接受的盐的药物组合物。 双胍衍生物具有其与能量代谢的控制,即使当小剂量施用相关联的的抑制癌细胞增殖,并因此表现出抗癌活性,包括抑制癌症转移和癌症复发的,因为它们可有效地激活AMPK的效果,所有 与传统药物相比。 因此,双胍衍生物是在由AMPK活化降血糖和脂质浓度高效,因此,它们可以有效地用于治疗糖尿病,肥胖,高脂血症,高胆固醇血症,脂肪肝,冠状动脉病,骨质疏松症,多囊卵巢综合征和代谢 综合征。