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    Modified bile acid conjugates, and their use as pharmaceuticals
    11.
    发明授权
    Modified bile acid conjugates, and their use as pharmaceuticals 失效
    改性胆汁酸共轭物及其作为药物的用途

    公开(公告)号：US5462933A

    公开(公告)日：1995-10-31

    申请号：US208192

    申请日：1994-03-10

    Applicant: Werner Kramer ,  Gunther Wess

    Inventor： Werner Kramer ,  Gunther Wess

    IPC: A61K38/00 ,  A61K31/575 ,  A61K31/58 ,  A61P1/16 ,  A61P3/06 ,  A61P43/00 ,  C07D213/26 ,  C07D213/56 ,  C07D213/81 ,  C07J9/00 ,  C07J17/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07K5/06 ,  C07K5/062

    CPC classification number: C07D213/81 ,  C07D213/26 ,  C07D213/56 ,  C07J17/00 ,  C07J31/006 ,  C07J41/0011 ,  C07J41/0027 ,  C07J41/0055 ,  C07J41/0061 ,  C07J41/0088 ,  C07J43/003 ,  C07J51/00 ,  C07J9/005 ,  C07K5/06026 ,  A61K38/00

    Abstract: Bile acid derivatives, processes for their preparation and use as pharmaceuticals Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the enterohepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.X is a large number of intermediate members or, alternatively, a bond.

    Abstract translation: 胆汁酸衍生物，其制备方法和用作药物式I WXG的胆汁酸衍生物，其中G是胆汁酸根，W是药物的活性化合物部分，X是胆汁酸基团和 活性化合物部分，非常适合于将活性化合物引入肠肝循环。 化合物I被吸收并进入血流。 以这种方式，可以利用胆汁酸的天然重吸收来改善吸收不可吸收或吸收不良的药物。 W可以是例如肽，抗生素，抗病毒物质，抗癌剂，肝保护剂，抗高脂血症，利尿剂，降血压药，肾素抑制剂，用于治疗肝硬化的物质或 用于治疗糖尿病的物质。 G是游离天然或化学改性的酸，酯和酰胺，在醇基上衍生的盐形式和形式的胆汁酸基。 X是大量的中间成员，或者是一个键。

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