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    Use of propargyl glycine amino propargyl diol compounds for treatment of renal failure
    6.
    发明授权
    Use of propargyl glycine amino propargyl diol compounds for treatment of renal failure 失效
    使用炔丙基甘氨酸氨基炔丙醇二醇化合物治疗肾衰竭

    公开(公告)号：US06777572B2

    公开(公告)日：2004-08-17

    申请号：US09996345

    申请日：2001-11-28

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

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

    IPC分类号： C07C30300

    CPC分类号： C07C237/22 ,  C07C271/20 ,  C07C2601/14 ,  C07D277/30

    摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of renal failure. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R5 and R8 is independently propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein each of R11 and R12 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： 通常被称为炔丙基甘氨酸氨基炔丙醇二醇衍生物的化合物可用于治疗肾功能衰竭。 特别感兴趣的化合物是式I的化合物，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，b，b，b-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R 5和R 8各自独立地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。

    Use of propargyl glycine amino propargyl diol compounds for treatment of congestive heart failure
    7.
    发明授权
    Use of propargyl glycine amino propargyl diol compounds for treatment of congestive heart failure 失效
    使用炔丙基甘氨酸氨基炔丙基二醇化合物治疗充血性心力衰竭

    公开(公告)号：US06667414B2

    公开(公告)日：2003-12-23

    申请号：US09996344

    申请日：2001-11-28

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

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

    IPC分类号： C07C30300

    CPC分类号： C07C237/22 ,  C07C271/20 ,  C07C2601/14 ,  C07D277/30

    摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R5 and R8 is independently propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein each of R11 and R12 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： 通常作为炔丙基甘氨酸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，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，b，b，b-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R 5和R 8各自独立地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。

    Use of ethynyl alanine amino diol compounds for treatment of renin-mediated disorders
    9.
    发明授权
    Use of ethynyl alanine amino diol compounds for treatment of renin-mediated disorders 失效
    乙炔丙氨酸二氨基二醇化合物用于治疗肾素介导的疾病

    公开(公告)号：US06174923B1

    公开(公告)日：2001-01-16

    申请号：US09239493

    申请日：1999-01-28

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

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

    IPC分类号： A61K31165

    CPC分类号： A61K31/18 ,  A61K31/165 ,  C07C237/22 ,  C07C271/20 ,  C07C311/13 ,  C07C2601/02 ,  C07C2601/14

    摘要： Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to treat disorders mediated by plasma renin activity. Compounds of particular interest are renin inhibitors of Formula I wherein A is selected from CO and SO2 wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, &bgr;,&bgr;,&bgr;-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5 is propargyl or a propargyl-containing moiety; wherein R7 is cyclohexylmethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R11 and R12 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： 通常被称为乙炔基丙氨酸氨基二醇衍生物的化合物可用于治疗由血浆肾素活性介导的病症。 特别感兴趣的化合物是式I的肾素抑制剂，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; 或其药学上可接受的盐。