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首页> 外国专利> Heteroaryl derivatives aminoguanidine And ALKOKSIGUANIDINOV (Options), methods of making, methods and pharmaceutical compositions to inhibit proteolysis in a mammal, METHOD treating pancreatitis, thrombosis, ischemia, stroke, restenosis, emphysema or inflammatory conditions in mammals, a method of inhibiting THROMBIN-INDUCED platelet aggregation and languish FIBRINOGEN IN PLASMA, METHOD OF INHIBITING THROMBIN IN BLOOD, METHOD OF INHIBITING AGGREGATION

Heteroaryl derivatives aminoguanidine And ALKOKSIGUANIDINOV (Options), methods of making, methods and pharmaceutical compositions to inhibit proteolysis in a mammal, METHOD treating pancreatitis, thrombosis, ischemia, stroke, restenosis, emphysema or inflammatory conditions in mammals, a method of inhibiting THROMBIN-INDUCED platelet aggregation and languish FIBRINOGEN IN PLASMA, METHOD OF INHIBITING THROMBIN IN BLOOD, METHOD OF INHIBITING AGGREGATION

机译：杂芳基衍生物氨基胍和ALKOKSIGUANIDINOV（选项），抑制哺乳动物蛋白水解的制备方法，方法和药物组合物，治疗胰腺炎，血栓形成，局部缺血，中风，再狭窄，肺气肿或炎症的方法，抑制THROMBIN诱导的方法血浆中血小板聚集和纤维蛋白原微弱，血液中凝血酶的抑制方法，血凝抑制方法

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摘要

Aminoguanidine and alkoxyguanidine derivatives are described, including compounds of formula VII, where X is O or NR, and the group Het, R, R, R, R, R, R, R, Z and n are defined in the specification, as well as their hydrates, solvates or pharmaceutically acceptable salts. Also presented are methods for producing such compounds. The compounds of the present invention are effective protease inhibitors, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Some compounds exhibit antithrombotic activity due to direct selective inhibition of thrombin. The invention also includes a composition for inhibiting platelet loss, for inhibiting platelet aggregation, for inhibiting the formation of fibrin, inhibiting the formation of blood clots and the formation of an embolus in mammals, the composition comprising the compound of the invention in a pharmaceutically acceptable carrier. Another field of application for the compounds of the invention is their use as anticoagulants, either included in materials or physically related to materials used to make devices used for collecting blood and storing blood, such as catheters, dialysis machines, syringes and test tubes. for blood collection, circulatory system and stents. In addition, a label can be inserted into the compounds to obtain an image of a thrombus in vivo. The international application was published along with an international search report.
机译：描述了氨基胍和烷氧基胍衍生物，包括式VII的化合物，其中X是O或NR，并且在说明书中还定义了基团Het，R，R，R，R，R，R，R，R，Z和n作为它们的水合物，溶剂化物或药学上可接受的盐。还提供了制备此类化合物的方法。本发明的化合物是有效的蛋白酶抑制剂，尤其是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，凝血酶，纤溶酶和Xa因子。由于对凝血酶的直接选择性抑制，某些化合物具有抗血栓形成的活性。本发明还包括在哺乳动物中用于抑制血小板损失，用于抑制血小板凝集，用于抑制血纤蛋白的形成，用于抑制血凝块的形成和栓塞的形成的组合物，该组合物包含药学上可接受的本发明的化合物。载体。本发明化合物的另一个应用领域是它们作为抗凝剂的用途，其包括在材料中或与用于制造用于收集血液和储存血液的装置（例如导管，透析机，注射器和试管）的材料物理相关。用于血液收集，循环系统和支架。另外，可以将标记插入化合物中以获得体内血栓的图像。国际申请与国际检索报告一同发布。

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