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    Amino acyl amino propargyl diol compounds for treatment of hypertension
    23.
    发明授权
    Amino acyl amino propargyl diol compounds for treatment of hypertension 失效
    用于治疗高血压的氨基酰基氨基炔丙基二醇化合物

    公开(公告)号：US5330996A

    公开(公告)日：1994-07-19

    申请号：US784276

    申请日：1991-10-29

    申请人： Gunnar J. Hanson ,  J. Timothy Keane

    发明人： Gunnar J. Hanson ,  J. Timothy Keane

    IPC分类号： C07D277/30 ,  A61K31/425

    CPC分类号： C07D277/30

    摘要： Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is selected from hydrido, alkyl, pyrazolealkyl, pyridylalkyl, thiazolylalkyl, imidazolealkyl, thienylalkyl, furanylalkyl, oxazolylalkyl, isoxazolylalkyl, pyrimidinylalkyl, pyridazinylalkyl and pyrazinylalkyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.7 is cyclohexylmethyl; wherein R.sub.8 is propargyl or a propargyl-containing moiety; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常用氨基酰基氨基炔丙基二醇衍生物表征的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2; 其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，β，β，β-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R5选自氢化，烷基，吡唑烷基，吡啶基烷基，噻唑基烷基，咪唑烷基，噻吩基烷基，呋喃基烷基，恶唑基烷基，异恶唑基烷基，嘧啶基烷基，哒嗪基烷基和吡嗪基烷基。 其中R 4和R 6各自独立地选自氢和甲基; 其中R 7为环己基甲基; 其中R8是炔丙基或含炔丙基的部分; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学上可接受的盐。

    Ethynyl alanine amino diol compounds for treatment of hypertension
    24.
    发明授权
    Ethynyl alanine amino diol compounds for treatment of hypertension 失效
    用于治疗高血压的乙酰胺亚氨基二醇化合物

    公开(公告)号：US5227401A

    公开(公告)日：1993-07-13

    申请号：US783955

    申请日：1991-10-29

    申请人： Gunnar J. Hanson ,  John S. Baran

    发明人： Gunnar J. Hanson ,  John S. Baran

    IPC分类号： A61K31/165 ,  A61K31/18 ,  A61K31/27 ,  A61P9/00 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P27/02 ,  C07C237/22 ,  C07C271/20 ,  C07C311/13 ,  C07C311/18 ,  C07C311/31

    CPC分类号： A61K31/18 ,  A61K31/165 ,  C07C237/22 ,  C07C271/20 ,  C07C311/13 ,  C07C2101/02 ,  C07C2101/14

    摘要： Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常以乙炔基丙氨酸氨基二醇衍生物为特征的化合物可用作治疗高血压的肾素抑制剂。 特别感兴趣的化合物是式I的化合物（I）其中A选自CO和SO 2，其中X选自氧原子和亚甲基; 其中R 1和R 9各自独立地选自氢，甲基，乙基，正丙基，异丙基，苄基，β，β，β-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R1和R9 可以与氧结合形成N-氧化物; 其中R2选自氢，甲基，乙基和异丙基; 其中R 3选自苄基，环己基甲基，苯乙基，咪唑甲基，吡啶基甲基和2-吡啶基乙基; 其中R5是炔丙基或含炔丙基的部分; 其中R 7为环己基甲基; 其中R 4和R 6各自独立地选自氢和甲基; 其中R8选自乙基，正丙基，异丁基，环丙基，环丁基，环戊基，环己基，环丙基甲基，环己基甲基，环己基乙基，烯丙基，乙烯基和氟乙烯基; 其中R 11和R 12各自独立地选自氢，烷基和苯基; 其中m为零; 并且其中n是选自0至3的数字; 或其药学可接受的盐。