利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

68 条记录 (耗时 0.036 秒)

    N-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for treatment of circulatory disorders
    11.
    发明授权
    N-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for treatment of circulatory disorders 失效
    N-取代（（ALPHA）-IMIDAZOLYL-TOLUYL）用于治疗循环障碍的吡咯化合物

    公开(公告)号：US5187271A

    公开(公告)日：1993-02-16

    申请号：US662584

    申请日：1991-02-28

    申请人： Philippe R. Bovy ,  Joe T. Collins ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  Joe T. Collins ,  Robert E. Manning

    IPC分类号： C07D403/10 ,  C07D403/14

    CPC分类号： C07D403/10 ,  C07D403/14

    摘要： A class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein each of R.sup.0 and R.sup.1 is independently selected from hydrido, alkyl, hydroxyalkyl, formyl, halo, haloalkyl, cycloalkylcarbonyl, alkoxy, aroyl, aryloxy, aralkoxy, alkylcarbonyl, alkoxycarbonyl, cyano, nitro, carboxyl, alkylcarbonyloxy, alkylcarbonyloxyalkyl, alkoxycarbonylalkyl, aralkoxycarbonylalkyl, alkylsulfonyl, aralkylsulfonyl, arylsulfonyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代（α-咪唑基 - 甲苯酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R 0和R 1各自独立地选自氢，烷基，羟基烷基，甲酰基，卤素，卤代烷基，环烷基羰基，烷氧基，芳酰基，芳氧基，芳烷氧基，烷基羰基，烷氧基羰基，氰基，硝基，羧基，烷基羰基氧基，烷基羰基氧基烷基，烷氧基羰基烷基，芳烷氧基羰基烷基， 烷基磺酰基，芳烷基磺酰基，芳基磺酰基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基 ，和羟烷基; 其中R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents
    12.
    发明授权
    Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents 失效
    含有线性游离巯基的寡肽衍生物作为抗高血压药

    公开(公告)号：US5106834A

    公开(公告)日：1992-04-21

    申请号：US290667

    申请日：1988-12-27

    申请人： Philippe R. Bovy ,  Robert E. Manning ,  Joan M. O'Neal

    发明人： Philippe R. Bovy ,  Robert E. Manning ,  Joan M. O'Neal

    IPC分类号： A61K38/00 ,  C07K14/58

    CPC分类号： C07K14/582 ,  A61K38/00

    摘要： Synthesis and use of novel oligopeptides are described, many of which peptides contain one or several unnatural amino acids. These short linear peptide derivatives are characterized by the presence of a free sulfhydryl function. These compounds have a high affinity for the Atrial Natriuretic Peptide (ANP) receptor coupled to particulate guanylate cyclase. Such peptides are full agonists at the ANP receptor as demonstrated by the ability of the peptides to stimulate the production of cGMP and to relax smooth muscles in vitro. In accord with these observations, the compounds of the invention lower blood pressure in mammals. Preferred peptides are the following:Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; and Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH.sub.2.

    摘要翻译： 描述了新型寡肽的合成和应用，其中许多肽含有一个或多个非天然氨基酸。 这些短的线性肽衍生物的特征在于存在游离的巯基官能团。 这些化合物对与鸟苷酸环化酶颗粒偶联的心房利钠肽（ANP）受体具有高亲和力。 这些肽是ANP受体的完全激动剂，如通过肽在体外刺激cGMP的产生和放松平滑肌的能力所证明的。 根据这些观察结果，本发明化合物降低了哺乳动物的血压。 优选的肽如下：Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; 和Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH 2。

    1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
    14.
    发明授权
    1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders 失效
    1-苯基咪唑-2-酮联苯甲基化合物，用于治疗循环系统疾病

    公开(公告)号：US06858636B2

    公开(公告)日：2005-02-22

    申请号：US10649210

    申请日：2003-08-27

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： A61K31/415 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P27/02 ,  A61P27/06 ,  C07D233/70 ,  C07D403/10 ,  A61K31/4166 ,  A61K31/4178

    CPC分类号： C07D403/10 ,  C07D233/70

    摘要： A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein each of R1, R2 and R3 is independently selected from hydrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; with the proviso that at least one of R1, R2 and R3 must be a substituent other than hydrido, and with the further proviso that when each of R1 and R3 is hydrido, then R2 cannot be chloro; wherein R4 is hydrido; wherein R5 is alkyl; and wherein R6 is tetrazolyl; or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述了一类用于治疗循环障碍的1-苯基咪唑-2-酮联苯甲基化合物。 R 1，R 2和R 3各自独立地选自氢，烷基，烷氧基，氰基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基。 ; 烷基羰基和卤代烷基羰基; 条件是R 1，R 2和R 3中的至少一个必须是除氢环以外的取代基，另外条件是当R 1和R 3各自为氢时 那么R 2不能是氯; 其中R 4是氢的; 其中R 5是烷基; 并且其中R 6是四唑基; 或其立体异构体或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    15.
    发明授权
    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders 失效
    用于治疗循环系统疾病的N-芳基杂芳基烷基咪唑-2-酮化合物

    公开(公告)号：US5861420A

    公开(公告)日：1999-01-19

    申请号：US784223

    申请日：1997-01-16

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  A01N43/40 ,  C07D401/00 ,  C07D413/00 ,  C07D417/04

    CPC分类号： C07D401/06 ,  C07D401/10 ,  C07D401/14

    摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is hydrido; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 is hydrido and R.sup.5 must be selected from COOH, SH, P0.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR3## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof.

    摘要翻译： 描述了一类N-芳基杂芳基烷基咪唑-2-酮化合物用于治疗循环系统疾病如高血压和充血性心力衰竭。 特别感兴趣的化合物是下式的血管紧张素II拮抗剂：其中A选自 和，其中m是1; 其中R 1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，2-乙基丁基，正戊基，新戊基，苯基，甲基苯基，二氟苯基， 苯乙基，环己基甲基，环己基乙基，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R 0是氢的; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基 ，和羟烷基; 其中R 3，R 4，R 6，R 7，R 8，R 9，R 10和R 11各自为氢，R 5必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，

    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
    16.
    发明授权
    N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
    用于治疗循环障碍的N-取代的N-（α-三唑基 - 甲苯酰基）吡咯化合物

    公开(公告)号：US5484937A

    公开(公告)日：1996-01-16

    申请号：US117269

    申请日：1993-09-07

    申请人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    发明人： Philippe R. Bovy ,  David B. Reitz ,  Robert E. Manning

    IPC分类号： C07D521/00 ,  C07D403/10 ,  A61K31/41

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from alkyl; and wherein R.sup.2 is selected from alkyl; and wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述用于治疗循环系统疾病的一类N-取代的N-（α-三唑基甲苯磺酰基）吡咯化合物。 特别感兴趣的化合物是式IMAMA的血管紧张素II拮抗剂，其中m是1; 其中R1选自烷基; 并且其中R 2选自烷基; R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自氢，卤素，硝基，三氟甲基，羟基，烷氧基，氰基，羧基和甲氧基羰基; 条件是R 5和R 8中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3，OH，其中R42和R43各自独立地选自氯，氰基，硝基，三氟甲基， 甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。 这些化合物特别可用于治疗或控制高血压和充血性心力衰竭。

    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders
    20.
    发明授权
    N-arylheteroarylalkyl imidazol-2-one compounds for treatment of circulatory disorders 失效
    用于治疗循环障碍的N-亚油酸二甲基咪唑-2-酮化合物

    公开(公告)号：US5164403A

    公开(公告)日：1992-11-17

    申请号：US681011

    申请日：1991-04-05

    申请人： David B. Reitz ,  Robert E. Manning

    发明人： David B. Reitz ,  Robert E. Manning

    IPC分类号： A61K31/4439 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14

    CPC分类号： C07D401/06 ,  A61K31/4439 ,  C07D401/10 ,  C07D401/14

    摘要： A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R.sup.0 is selected from hydrido, methyl, fluoro, chloro, monofluoromethyl, difluoromethyl, trifluoromethyl, formyl, carboxyl and dimethoxymethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and R.sup.11 is hydrido and R.sup.5 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR3## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类N-芳基杂芳基烷基咪唑-2-酮化合物用于治疗循环系统疾病如高血压和充血性心力衰竭。 特别感兴趣的化合物是下式的血管紧张素II拮抗剂：其中A选自 其中m为1; 其中R1选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，4-甲基丁基，正戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，环己基乙基 ，环己酰基，1-氧代-2-环己基乙基，苯甲酰基，1-氧代-2-苯乙基，1-氧代丙基，1-氧代丁基，1-氧代戊基和2-羟基丁基; 其中R 0选自氢，甲基，氟，氯，单氟甲基，二氟甲基，三氟甲基，甲酰基，羧基和二甲氧基甲基; 其中R2选自甲基，乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，叔丁基，正戊基，异戊基，新戊基，苯基，苄基，苯乙基，环己基，环己基甲基，丙硫基，丁硫基 ，和羟烷基; 其中R 3，R 4，R 6，R 7，R 8，R 9，R 10和R 11各自为氢，R 5必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，NNNHR 42和+ RE 其中R 42和R 43各自独立地选自氯，氰基，硝基，三氟甲基，甲氧基羰基和三氟甲基磺酰基; 或其互变异构体或其药学上可接受的盐。