Compounds having the structural formula ##STR1## wherein L is N, O or SO.sub.n wherein n is 0, 1 or 2; L-R.sup.1 is a leaving group, H-L-R.sup.1 is the conjugate acid thereof and, when L is N, H-L-R.sup.1 has a pK.sub.a value less than or equal to 6, when L is O, H-L-R.sup.1 has a pK.sub.a value less than or equal to to 8, and when L is SO.sub.n, H-L-R.sup.1 has a pK.sub.a value less than or equal to 5; R.sup.2 is primary or secondary alkyl of two to four carbon atoms, primary alkylamino of one to three carbon atoms, primary alkylmethylamino of two to four carbon atoms, diethylamino or primary alkoxy of one to three carbon atoms; and R.sup.3 is from one to three of a variety of substituents at any or all of the 5-, 6- and 7-positions; or a pharmaceutically acceptable acid addition salt thereof if the compound has a basic functional group or a pharmaceutically acceptable base addition salt thereof if the compound has an acidic functional group, which inhibit the enzymatic activity of proteolytic enzymes, and processes for preparation thereof, method of use thereof in treatment of degenerative diseases and pharmaceutical compositions thereof are disclosed.
本发明涉及结构式##STR1##的化合物,其中L为N,O或SO.sub.n,其中n为0、1或2;L-R.sup.1为离去基团,H-L-R.sup.1为其共轭酸,当L为N时,H-L-R.sup.1的pK.sub.a值小于或等于6,当L为O时,H-L-R.sup.1的pK.sub.a值小于或等于8,当L为SO.sub.n时,H-L-R.sup.1的pK.sub.a值小于或等于5;R.sup.2为二到四个碳原子的一级或二级烷基,一到三个碳原子的一级烷基
氨基,二到四个碳原子的一级烷基甲基
氨基,
二乙基氨基或一到三个碳原子的一级烷氧基;R.sup.3为在5-、6-和7-位置的各种取代基中的一到三个;或其药学上可接受的酸加成盐,如果化合物具有碱性官能团,或其药学上可接受的碱加成盐,如果化合物具有酸性官能团,其抑制
蛋白酶酶活性,公开了其制备方法,治疗退行性疾病的使用方法和其制药组合物。