申请人:Torii & Co., Ltd.
公开号:US04214093A1
公开(公告)日:1980-07-22
Amino- or guanidino-1,2,3,4-tetrahydro-1-naphthoic esters represented by the formula, ##STR1## wherein R.sub.1 is --NH.sub.2 or ##STR2## R.sub.3 is --H, --R.sub.4, --O--R.sub.4, --NHCOCH.sub.3, a halogen, --CN, ##STR3## --COOH, --COOR.sub.4, ##STR4## or --(CH.sub.2).sub.n --COOCH.sub.2 --CO--R.sub.5 ; R.sub.5 is --O--R.sub.4, --NH.sub.2 or ##STR5## n is 0, 1 or 2, and R.sub.4 is a lower alkyl, or pharmaceutically acceptable acid addition salts thereof. Owing to their inhibitory activity on proteolytic enzymes the said esters and acid addition salts thereof are useful in the therapy of diseases caused by such enzymes.
氨基或胍基-1,2,3,4-四氢-1-萘酸酯的化学式为,其中R.sub.1为--NH.sub.2或##STR2## R.sub.3为--H,--R.sub.4,--O--R.sub.4,--NHCOCH.sub.3,卤素,--CN,##STR3## --COOH,--COOR.sub.4,##STR4##或--(CH.sub.2).sub.n--COOCH.sub.2--CO--R.sub.5;R.sub.5为--O--R.sub.4,--NH.sub.2或##STR5## n为0、1或2,而R.sub.4为较低的烷基,或其药学可接受的酸加成盐。由于它们对蛋白酶酶的抑制活性,所述酯和酸加成盐在治疗由这种酶引起的疾病方面是有用的。