首页> 外国专利> AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS);

AMETHINE, METHYLAMIDINE AND GUANIDA HEAT HYDROARIAL PRODUCTS (OPTIONS) MATERIALS (OPTIONS), PHARMACEUTICAL COMPOSITION (OPTIONS), METHOD FOR INHIBING PROTEASE (OPTIONS) AND SPODA SPEEDS (OPTIONS), SPEED INHIBITION (OPTIONS) AND SPODA PRODUCTS (OPTIONS);

机译:甲胺,甲基丙二烯和瓜纳达热水产品(选择),药物成分(选择),抑制蛋白酶的方法(选择)和SPODA速度(选择),快速抑制(选择)和SPODA产品;

摘要

The present invention is directed to compounds of formula (I), wherein X is O, S, or NR, where R — R, Y, and Z are as defined herein, as well as their hydrates, solvates, or pharmaceutically acceptable salts. Methods for preparing compounds of formula (I) are also described. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain compounds exhibit direct selective inhibition of urokinase or are intermediate products used to produce compounds with such activity. The international application was published together with an international search report.
机译:本发明涉及式(I)的化合物,以及它们的水合物,溶剂化物或药学上可接受的盐,其中X是O,S或NR,其中R,R,Y和Z如本文所定义。还描述了制备式(I)化合物的方法。本发明的新型化合物是蛋白酶的有效抑制剂,尤其是胰蛋白酶样丝氨酸蛋白酶,例如糜蛋白酶,胰蛋白酶,纤溶酶和尿激酶。某些化合物表现出对尿激酶的直接选择性抑制,或者是用于产生具有这种活性的化合物的中间产物。国际申请与国际检索报告一起发布。

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