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    Azido, imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids having hypotensive activity
    3.
    发明公开
    Azido, imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids having hypotensive activity 失效
    on ido-。on Pro Pro n n n n n。。。。。。。。。。。。。。。。。。。。。。。。。

    公开(公告)号：EP0042639A2

    公开(公告)日：1981-12-30

    申请号：EP81200619.5

    申请日：1981-06-04

    申请人： E.R. Squibb & Sons, Inc.

    发明人： Krapcho, John ,  Wade, Peter C. ,  Petrillo, Edward W., Jr. ,  Weisenborn, Frank L.

    IPC分类号： C07D207/16 ,  C07D207/404 ,  C07D207/452 ,  C07D211/60 ,  C07D211/88 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

    CPC分类号： C07D231/12 ,  C07D207/16 ,  C07D211/38 ,  C07D211/60 ,  C07D233/56 ,  C07D249/08 ,  Y02P20/55

    摘要： Azido, imido, amido and amino derivatives of mercap- toacyl prolines and pipecolic acids having the formula
    wherein -NR 1 -R 2 is azido or R 1 and R 2 are the same or different and are hydrogen, alkyl, cycloalkyl, 1-adamantyl, aryl, arylalkyl, alkylcarbonyl, arylcarbonyl, arylalkylcarbonyl, alkylsulfonyl, arylsulfonyl, or arylvinylcarbonyl, or together with the nitrogen atom to which they are attached R, and R 2 are 1-pyrrolidinyl, 1-piperidinyl, 1-homopiperidinyl, 4-morpholinyl, 4-alkyl-1-piperazinyl, 4-aryl-1-piperazinyl, 1-imidazolyl, 1-pyrrolidinyl-2,5-dione, 3-alkyl-1-pyrrolidinyl-2,5-dione, 3-aryl-1-pyrrolidinyl-2,5-dione, 1-piperidinyl-2,6-dione,3-alkyl-1- piperidinyl-2,6-dione, 3-aryl-1-piperidinyl,2-6-dione, 2H-isoindol-2-yl-1,3-dione, hexahydro-2H-isoindol-2-yl-1,3-dione, 2,5-dihydro-2,5-dioxo-lH-pyrrol-1-yl, 1,1,3- trioxo-1,2-benzisothiazol-2(3H)-yl, or 1,3-dihydro-1,3-dioxo-2H-benz[de]isoquinolin-2-yl;
    R 3 is hydrogen, alkyl, aryl, arylalkyl, or a hydrolyzable acyl protecting group;

    R 4 is hydrogen, alkyl, alkylthio, or trifluoromethyl;
    R s is hydrogen, alkyl, or arylalkyl;
    n is 0, 1 or 2; and
    p is 1 or 2;

    or a salt thereof, or symmetrical dimer thereof are useful for the treatment of hypertension.

    摘要翻译： 巯基酰基脯氨酸的酰氨基，酰氨基和氨基衍生物和具有式CHEM的哌啶酸，其中-NR 1 -R 2是叠氮基或R 1和R 2相同或不同，为氢，烷基，环烷基，1-金刚烷基，芳基， 芳基烷基，烷基羰基，芳基羰基，芳基烷基羰基，烷基磺酰基，芳基磺酰基或芳基乙烯基羰基，或与它们所连接的氮原子一起R1和R2是1-吡咯烷基，1-哌啶基，1-高哌啶基，4-吗啉基， 1-哌嗪基，4-芳基-1-哌嗪基，1-咪唑基，1-吡咯烷基-2,5-二酮，3-烷基-1-吡咯烷基-2,5-二酮，3-芳基-1-吡咯烷基-2， 5-甲基-5-二酮，1-哌啶基-2,6-二酮，3-烷基-1-哌啶基-2,6-二酮，3-芳基-1-哌啶基，2-6-二酮，2H-异吲哚-2-基 - 1,3-二酮，六氢-2H-异吲哚-2-基-1,3-二酮，2,5-二氢-2,5-二氧代-1H-吡咯-1-基，1,1,3-三氧代 - 1,2-苯并异噻唑-2（3H） - 基或1,3-二氢-1,3-二氧代-2H-苯并[de]异喹啉-2-基; R3是氢，烷基，芳基，芳基烷基或可水解的酰基保护基; R4是氢，烷基，烷硫基或三氟甲基; R5是氢，烷基或芳基烷基; n为0,1或2; p为1或2; 或其盐或其对称二聚体可用于治疗高血压。