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137 条记录 (耗时 0.048 秒)

    Pyrazole derivatives as p38 kinase inhibitors
    71.
    发明授权
    Pyrazole derivatives as p38 kinase inhibitors 失效
    吡唑衍生物作为p38激酶抑制剂

    公开(公告)号：US06503930B1

    公开(公告)日：2003-01-07

    申请号：US09540464

    申请日：2000-03-31

    申请人： Gunnar J. Hanson ,  Shuyuan Liao

    发明人： Gunnar J. Hanson ,  Shuyuan Liao

    IPC分类号： A61K314439

    CPC分类号： C07D401/04

    摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I wherein Q, R1, R2, R3 and R4 are as described in the specification.

    摘要翻译： 描述了一类吡唑衍生物用于治疗p38激酶介导的病症。 特别感兴趣的化合物由式I定义，其中Q，R 1，R 2，R 3和R 4如说明书中所述。

    Amino acyl amino propargyl diol compounds for treatment of a renin-mediated disease
    72.
    发明授权
    Amino acyl amino propargyl diol compounds for treatment of a renin-mediated disease 失效
    用于治疗肾素介导的疾病的氨基酰基氨基炔丙基二醇化合物

    公开(公告)号：US06281235B1

    公开(公告)日：2001-08-28

    申请号：US09317704

    申请日：1999-05-24

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

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

    IPC分类号： A61K31426

    CPC分类号： A61K31/00

    摘要： Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful as renin inhibitors for the treatment of a renin-mediated disease 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, &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 selected from hydrido, alkyl, pyrazolealkyl, pyridylalkyl, thiazolylalkyl, imidazolealkyl, thienylalkyl, furanylalkyl, oxazolylalkyl, isoxazolylalkyl, pyrimidinylalkyl, pyridazinylalkyl and pyrazinylalkyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R7 is cyclohexylmethyl; wherein R8 is propargyl or a propargyl-containing moiety; 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： 通常以氨基酰基氨基炔丙基二醇衍生物表征的化合物可用作肾素抑制剂用于治疗肾素介导的疾病。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，β，β-三氟乙基，叔丁氧基羰基和甲氧基甲基羰基，其中R 1和R 9连接的氮原子 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。

    Amino acyl amino propargyl diol compounds for treatment of hypertension
    74.
    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：US5849773A

    公开(公告)日：1998-12-15

    申请号：US663508

    申请日：1996-06-14

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

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

    IPC分类号： A61K31/00 ,  A61K31/425

    CPC分类号： A61K31/00

    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, isoxazolyalkyl, pyrimidinykalkyl, 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 hydride, 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R 5选自氢，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R11和R12各自独立地选自氢化物，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。

    Alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol compounds for treatment of hypertension
    75.
    发明授权
    Alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol compounds for treatment of hypertension 失效

    公开(公告)号：US5488067A

    公开(公告)日：1996-01-30

    申请号：US376504

    申请日：1995-01-23

    申请人： Gunnar J. Hanson

    发明人： Gunnar J. Hanson

    IPC分类号： C07C317/44 ,  A61K31/16 ,  A61K31/165

    CPC分类号： C07C317/44 ,  C07C2101/14 ,  Y10S514/913

    摘要： Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein q is two or three; wherein r is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl containing moiety; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.12 and R.sup.13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.