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    • 6. 发明授权
    • N-acylamino acid derivatives and their use
    • N-酰基氨基酸衍生物及其用途
    • US5481036A
    • 1996-01-02
    • US179195
    • 1994-01-10
    • Hajime MorishimaYutaka KoikeMasato NakanoShugo AtsuumiSeiichi TanakaKenji Matsuyama
    • Hajime MorishimaYutaka KoikeMasato NakanoShugo AtsuumiSeiichi TanakaKenji Matsuyama
    • A61K31/195A61K31/535C07C59/66C07C317/00C07C317/44C07C323/43C07D207/08C07D211/14C07D215/12C07D233/54C07D239/38C07D257/04C07D265/30C07D285/12C07D285/125C07D295/084C07D295/12C07D295/125C07D295/13C07D295/24C07D307/38C07D319/18C07D401/12C07F7/18C07C321/00
    • C07D207/08C07C323/00C07C323/43C07C59/66C07D211/14C07D215/12C07D233/64C07D239/38C07D257/04C07D285/125C07D295/084C07D295/125C07D295/13C07D295/24C07D307/38C07D319/18C07D401/12C07F7/1856
    • An N-acylamino acid derivative of the formula: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.6 is hydrogen lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from to 4 hetero atoms; each of R.sup.3 and R.sup.5 is hydrogen or lower alkyl; A is --CH(OH)--(CH.sub.2).sub.q R.sup.7 wherein R.sup.7 is hydrogen, lower alkyl, cycloalkyl, cyloalkylalkyl, aryl, aralkyl, a monocyclic or bicyclic heterocyclic group containing from to 4 hereto atoms or --E--R.sup.10 wherein E is --S(O).sub.i -- wherein i is 0, 1 or 2, oxygen, --NR.sup.11 -- wherein R.sup.11 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, or ##STR2## wherein each of R.sup.12 and R.sup.13 is hydrogen, lower alkyl cycloalkyl, cycloalkylalkyl, aryl or aralkyl, and R.sup.10 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms provided that when R.sup.10 is hydrogen, i is 0, and a is an integer of from 0 to 5; or --CH.sub.2 --CHR.sup.8 --CO--R.sup.9 wherein R.sup.8 is hydrogen, lower alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a monocyclic or bicyclic heterocyclic group containing from 1 to 4 hetero atoms, and R.sup.9 is hydroxyl, --OX wherein X is alkyl, aryl, lower alkoxycarbonyloxyalkyl or 1-phthalidyl, or --N(Y.sup.1) (Y.sup.2) wherein each of Y.sup.1 and Y.sup.2 is hydrogen, lower alkyl, aryl, aralkyl or cycloalkyl, or Y and.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may contain a further hereto atom; m is 0, 1 or 2; and n is an integer of from 1 to 5, provided that when R.sup.1 is hydrogen, m is 0; or a salt thereof, which is useful as hypotensive drugs.
    • 下式的N-酰基氨基酸衍生物:其中R 1,R 2,R 4和R 6各自为氢低级烷基,环烷基,环烷基烷基,芳基,芳烷基或含有4个杂原子的单环或双环杂环基 原子 R 3和R 5各自为氢或低级烷基; A是-CH(OH) - (CH 2)q R 7,其中R 7是氢,低级烷基,环烷基,环烷基烷基,芳基,芳烷基,含有至4原子的单环或双环杂环基或-E-R 10,其中E是-S (O)i-其中i是0,1或2,氧,-NR 11 - ,其中R 11是氢,低级烷基,环烷基,环烷基烷基,芳基或芳烷基,或者其中R 12和R 13各自是氢, 环烷基,环烷基烷基,芳基或芳烷基,R 10为含有1至4个杂原子的氢,低级烷基,环烷基,环烷基烷基,芳基,芳烷基或单环或双环杂环基,条件是当R 10为氢时,i为0, 是从0到5的整数; 或-CH 2 -CHR 8 -CO-R 9,其中R 8是氢,低级烷基,环烷基,环烷基烷基,芳基,芳烷基或含有1至4个杂原子的单环或双环杂环基,并且R 9是羟基, ,芳基,低级烷氧基羰氧基烷基或1-苯酞基,或-N(Y1)(Y2),其中Y1和Y2各自为氢,低级烷基,芳基,芳烷基或环烷基,或Y和1和Y2与相邻的氮原子一起形成 可含有其它原子的5-或6-元杂环基; m为0,1或2; 且n为1至5的整数,条件是当R 1为氢时,m为0; 或其盐,其可用作降压药物。