利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

137 条记录 (耗时 0.097 秒)

    Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension
    93.
    发明授权
    Piperidinyl-terminated alkylamino ethynl alanine amino diol compounds for treatment of hypertension 失效
    哌啶基封端的烷基氨基乙炔丙氨酸二氨基二醇化合物治疗高血压

    公开(公告)号：US5780494A

    公开(公告)日：1998-07-14

    申请号：US841536

    申请日：1997-04-23

    申请人： Gunnar J. Hanson

    发明人： Gunnar J. Hanson

    IPC分类号： C07D205/04 ,  C07D209/44 ,  C07D209/52 ,  C07D211/14 ,  C07D211/26 ,  C07D211/38 ,  C07D211/70 ,  C07D211/78 ,  C07D217/04 ,  C07D221/22 ,  C07D223/14 ,  C07D295/13 ,  C07D451/02 ,  C07D453/06 ,  A61K31/405 ,  A61K31/40 ,  C07D207/06 ,  C07D209/08

    CPC分类号： C07D221/22 ,  C07D205/04 ,  C07D209/44 ,  C07D209/52 ,  C07D211/14 ,  C07D211/26 ,  C07D211/38 ,  C07D211/70 ,  C07D211/78 ,  C07D217/04 ,  C07D223/14 ,  C07D295/13 ,  C07D451/02 ,  C07D453/06

    摘要： Compounds characterized generally as piperidinyl-terminated alkylamino 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 B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常被称为哌啶基封端的烷基氨基乙炔基丙氨酸氨基二醇衍生物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B选自哌啶基，异吲哚基和氮杂双环壬基; 其中R1选自氢，甲基，乙基，异丙基和正丙基; 其中R2是苯基甲基; 其中R3和R5各自是氢的; 其中R 4选自其中V选自氢和甲基; 其中R6是环己基甲基; 其中R 7选自异丁基，环丙基和环丙基甲基; 其中q是选自0至3的数字（包括端值）; 并且其中n是选自0至3的数字，包括端值; 或其药学上可接受的盐。

    Propargyl glycine amino use of propargyl diol compounds for treatment of ophthalmic disorders
    94.
    发明授权
    Propargyl glycine amino use of propargyl diol compounds for treatment of ophthalmic disorders 失效
    炔丙基甘氨酸氨基使用炔丙基二醇化合物治疗眼科疾病

    公开(公告)号：US5484812A

    公开(公告)日：1996-01-16

    申请号：US199237

    申请日：1994-02-28

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

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

    IPC分类号： C07C237/22 ,  C07C271/20 ,  C07D277/30 ,  A61K31/27

    CPC分类号： C07C237/22 ,  C07C271/20 ,  C07D277/30 ,  C07C2101/14

    摘要： Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. 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, b, b, b-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： PCT No.PCT / US92 / 08840 Sec。 371日期1994年2月28日 102（e）1994年2月28日PCT于1992年10月22日提交PCT。化合物通常表征为甘草酸氨基炔丙基二醇衍生物可用作治疗眼部疾病的肾素抑制剂。 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。

    Use of ethynyl alanine amino diol compounds for treatment of ophthalmic disorders
    95.
    发明授权
    Use of ethynyl alanine amino diol compounds for treatment of ophthalmic disorders 失效
    使用乙炔基丙氨酸氨基二醇化合物治疗眼科疾病

    公开(公告)号：US5484811A

    公开(公告)日：1996-01-16

    申请号：US199211

    申请日：1994-02-23

    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 ophthalmic disorders. 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 B 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 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, cyclohexyimethyl, 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： PCT No.PCT / US92 / 08842 Sec。 371日期1994年2月28日 102（e）日期1994年2月28日PCT提交1992年10月22日PCT公布。 出版物WO93 / 09087 日期：1993年5月13日。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眼科疾病的肾素抑制剂。 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 B B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，环己基二甲基，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。

    Alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkyl-alanine amino-diol compounds for treatment of hypertension
    97.
    发明授权
    Alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkyl-alanine amino-diol compounds for treatment of hypertension 失效
    用于治疗高血压的烷基氨基烷基封端的硫化物/含磺酰基的环烷基 - 丙氨酸氨基二醇化合物

    公开(公告)号：US5416119A

    公开(公告)日：1995-05-16

    申请号：US141771

    申请日：1993-10-25

    申请人： Barbara B. Chen ,  Gunnar J. Hanson ,  John S. Baran

    发明人： Barbara B. Chen ,  Gunnar J. Hanson ,  John S. Baran

    IPC分类号： A61K31/16 ,  A61K31/165 ,  C07C317/44 ,  C07C323/60 ,  C07C323/25

    CPC分类号： C07C323/60 ,  A61K31/16 ,  A61K31/165 ,  C07C317/44 ,  C07C2101/04 ,  C07C2101/14 ,  Y10S514/912 ,  Y10S514/913

    摘要： Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x 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 selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; 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.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 通常作为烷基氨基烷基封端的硫化物/含磺酰基的环烷基烷基丙氨酸氨基二醇衍生物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II的化合物：其中m为2或3; 其中x为0或2; 其中R2选自氢，甲基，乙基和苯基; 其中R 3选自氢，环己基甲基，苄基，氟苄基，氯苄基，氟萘基甲基和氯萘基甲基; 其中R 5选自含有3至约12个碳原子的环烷基烷基; 其中R 7为环己基甲基; 其中R8选自正丙基，异丁基，环丙基，环丙基甲基，烯丙基和乙烯基; 并且其中R 9和R 10各自独立地选自甲基，乙基和异丙基; 或其药学上可接受的盐。