The present invention relates to a pharmaceutical formulation containing a compound of formula (I), a pharmacologically acceptable salt thereof and a prodrug thereof and its optically active form, a process for its preparation and a compound having a substrate metalloprotease-inhibiting action:;[Formula I];[Wherein,;X, Y and Z are independently of each other oxygen, sulfur or NH; R 1 is a group WV (W is a simple bond or one or several optionally substituted straight or branched C 1 -C 8 alkyl or C 2 -C 8 alkenyl groups, V may contain one or several heteroatoms) Optionally substituted monocyclic or bicyclic, or W-V is a C 1 -C 20 alkyl group optionally substituted with heteroatoms and optionally substituted by one or several carbon atoms; R 2 and R 3 represent hydrogen or one of them represents lower alkyl or lower acyl; R 4 and R 5 independently of one another, AD (where A is-, alkyl, alkenyl, acyl, alkylsulfonyl, sulfonyl, alkylaminocarbonyl, aminocarbonyl, alkoxycarbonyl, oxy-carbon Carbonyl, alkylaminothiocarbonyl, one or several optionally substituted aminothio-carbonyl, D represents hydrogen, monocyclic or bicyclic, wherein monocyclic or bicyclic is optionally inserted one or several times between heteroatoms , Monocyclic or bicyclic is substituted one or several times); R 4 and R 5 together with the adjacent N atoms form a ring].
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机译:[0001]本发明涉及药物制剂,其包含式(I)的化合物,其药学上可接受的盐和其前药以及其光学活性形式,其制备方法和具有底物金属蛋白酶抑制作用的化合物:式I]; [其中,X,Y和Z彼此独立地是氧,硫或NH; R 1 Sub>是基团WV(W是一个简单键或一个或多个可选取代的直链或支链C 1 Sub> -C 8 Sub>烷基或C 2 Sub> -C 8 Sub>烯基,V可以包含一个或多个杂原子)可选取代的单环或双环,或WV为C 1 Sub> -C任选被杂原子取代并且任选被一个或几个碳原子取代的 20 Sub>烷基; R 2 Sub>和R 3 Sub>代表氢或其中一个代表低级烷基或低级酰基; R 4 Sub>和R 5 Sub>彼此独立地是AD(其中A是-,烷基,烯基,酰基,烷基磺酰基,磺酰基,烷基氨基羰基,氨基羰基,烷氧羰基,氧碳羰基,烷基氨基硫代羰基,一个或几个任选取代的氨基硫代羰基,D表示氢,单环或双环,其中单环或双环任选地插入杂原子之间一次或数次,单环或双环被取代一次或数次; R 4 Sub>和R 5 Sub>与相邻的N个原子一起形成环]。
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