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    2,6-Dichlorophenyl-substituted amino-imidazole derivatives and use as hypertensive agents
    3.
    发明授权
    2,6-Dichlorophenyl-substituted amino-imidazole derivatives and use as hypertensive agents 失效
    2,6-二氯苯基取代的氨基咪唑衍生物，用作高血压药

    公开(公告)号：US4275072A

    公开(公告)日：1981-06-23

    申请号：US93247

    申请日：1979-11-13

    申请人： Arto Karjalainen ,  Kauko Kurkela

    发明人： Arto Karjalainen ,  Kauko Kurkela

    IPC分类号： C07D233/88 ,  A61K31/415 ,  C07D233/54

    CPC分类号： C07D233/88

    摘要： The 2,6-dichlorophenyl-substituted amino-imidazole derivatives 1-(2',6'-dichlorophenyl)-2-amino-4-methyl-imidazole, 2-(2',6'-dichloroanilino)-4-methyl-imidazole, their non-toxic, pharmaceutically acceptable, acid addition salts and mixtures thereof, exhibit excellent anti-hypertensive activity which makes the derivatives particularly suitable for treatment of high blood pressure in mammals.The derivatives may be prepared in either of two processes. The first process involves the sequential reaction of a known starting material with ammonia and a halogenated acetone which may be followed by separation of the formed isomers. The second process involves the decarboxylation of the novel intermediates 4-[1-(2',6'-dichlorophenyl)-2-amino)]-imidazoleacetic acid or 4-[2-(2',6'-dichloroanilino)]-imidazoleacetic acid or mixtures thereof. Such intermediates, their lower alkyl esters, their non-toxic, pharmaceutically acceptable acid addition salts or mixtures thereof may also be employed as a diuretic agent.The derivatives are employed in an effective amount and are typically combined with a pharmaceutical carrier. Administration of the derivatives may be accomplished either orally or parenterally.

    摘要翻译： 2,6-二氯苯基取代的氨基咪唑衍生物1-（2'，6'-二氯苯基）-2-氨基-4-甲基咪唑，2-（2'，6'-二氯苯胺基）-4-甲基 - 咪唑，它们的无毒，药学上可接受的酸加成盐及其混合物表现出优异的抗高血压活性，这使得该衍生物特别适用于治疗哺乳动物的高血压。 衍生物可以以两种方法中的任一种制备。 第一种方法是将已知原料与氨和卤代丙酮进行顺序反应，然后分离所形成的异构体。 第二种方法涉及新型中间体4- [1-（2'，6'-二氯苯基）-2-氨基）] - 咪唑乙酸或4- [2-（2'，6'-二氯苯胺基）] - 咪唑乙酸或其混合物。 这样的中间体，它们的低级烷基酯，其无毒的，药学上可接受的酸加成盐或其混合物也可以用作利尿剂。 衍生物以有效量使用，通常与药物载体组合。 衍生物的施用可以口服或胃肠外实施。

    Transmucosal formulations of levosimendan
    4.
    发明授权
    Transmucosal formulations of levosimendan 失效
    左西孟旦的粘膜粘膜制剂

    公开(公告)号：US06399610B1

    公开(公告)日：2002-06-04

    申请号：US09581610

    申请日：2000-08-31

    申请人： Kauko Kurkela ,  Martti Marvola ,  Ilkka Larma ,  Raimo Virtanen ,  Marianne Karlsson

    发明人： Kauko Kurkela ,  Martti Marvola ,  Ilkka Larma ,  Raimo Virtanen ,  Marianne Karlsson

    IPC分类号： A61K3150

    CPC分类号： A61K9/7023 ,  A61K9/0034 ,  A61K9/0043 ,  A61K9/006 ,  A61K31/50

    摘要： A method of administering transmucosally, particularly to oral or nasal mucosa, levosimendan or a pharmaceutically acceptable salt thereof to a patient. The method comprises contacting an intact mucous membrane with a source of levosimendan, and maintaining said source with said mucous membrane for a sufficient time period to deliver levosimendan to the patient. Transmucosal preparations of levosimendan are also described. Levosimendan is useful in the treatment of heart failure.

    摘要翻译： 特别是向口腔或鼻粘膜施用左西孟旦或其药学上可接受的盐给患者的方法。 该方法包括使完整的粘膜与左西孟旦源接触，并将所述源与所述粘膜保持足够的时间以将左西孟旦输送给患者。 还描述了左西孟旦的粘膜下粘膜制剂。 左西孟旦可用于治疗心力衰竭。