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    • 59. 发明授权
    • Derivatives of p-guanidinobenzoic acid
    • 对胍基苯甲酸的衍生物
    • US5247084A
    • 1993-09-21
    • US765749
    • 1991-09-26
    • Katsuhiro ImakiYoshinobu AraiHiroyuki Ohno
    • Katsuhiro ImakiYoshinobu AraiHiroyuki Ohno
    • C07C279/18C07C309/65C07C309/66C07C311/08C07C311/29C07C311/46C07C329/10C07D213/65C07D213/75C07D277/04C07D277/22C07D295/26
    • C07C279/18C07C309/65C07C309/66C07C311/08C07C311/29C07C311/46C07C329/10C07D213/65C07D213/75C07D277/04C07D277/22C07D295/26
    • Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH=CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.] and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings.
    • 由以下通式表示的化合物:其中当Y为氧时,R 2为H,烷基,烷氧基,烷氧基甲基,-COOR 3,-CH 2 COOR 3,-CH = CH-COOR 3,卤素,-CF 3,-COR 4 ,-OCOR4,-CH2OCOR4,-SO2R4,-OSO2R4,-CONR5R6,-OCONR5R6,-SO2NR5R6,-CONH-SO2NR5R6,-NHSO2R7,-NO2,-OH,-CH2OH,胍基,苄氧基,胍基苯硫基甲基,吗啉代磺酰基苯氧基甲基,吡啶氧基甲基或 (1,1-二氧代噻唑-3-基)羰基,或者Y为硫时,R2为H,烷基,烷氧基,卤素,-COOR3,-CH2COOR3,-NO2或-SO2NR5R6,n表示1〜 5,当n表示2以上时,R2各自可以相同或不同。]及其酸加成盐对弹性蛋白酶具有抑制作用,因此可用于治疗和/或预防疾病 通过弹性蛋白酶在哺乳动物,特别是人类中的弹性蛋白酶的作用,由弹性蛋白等蛋白质的异常增强引起的。