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    Renal-selective biphenylalkyl 1H-substituted-1, 2, 4- triazole angiotensin I I antagonists for treatment of hypertension
    2.
    发明申请
    Renal-selective biphenylalkyl 1H-substituted-1, 2, 4- triazole angiotensin I I antagonists for treatment of hypertension 失效
    用于治疗高血压的肾选择性联苯基烷基1H-取代-1,4-三唑血管紧张素I 1拮抗剂

    公开(公告)号：US20040220245A1

    公开(公告)日：2004-11-04

    申请号：US10852711

    申请日：2004-05-24

    申请人： G.D. Searle & Co.,

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

    IPC分类号： A61K031/4196

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/10 ,  C07D403/10 ,  H01M2/1055 ,  H04B1/3883 ,  H04B2001/3894

    摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-nullnull4null-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnullnull1,1null-biphenylnull-2-ylnullnullcarbonylhydrazide, (shown below) is an example: 1

    摘要翻译： 描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。 这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。 两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。 然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。 特别感兴趣的结合物是联苯甲基1H-取代-1,2,4-三唑化合物的谷氨酰基衍生物，其中N-乙酰谷氨酸5 - [[4' - [（3,5-二丁基-1H-1,2,4-三唑） 4-三唑-1-基）甲基] [1,1'-联苯] -2-基]]羰酰肼，（如下所示）是一个实例：

    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
    5.
    发明申请
    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension 审中-公开
    用于治疗高血压的肾选择性联苯基烷基1H-取代-1,2,4-三唑血管紧张素II拮抗剂

    公开(公告)号：US20040121989A1

    公开(公告)日：2004-06-24

    申请号：US10326942

    申请日：2002-12-19

    申请人： G.D. Searle & Co.

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

    IPC分类号： A61K031/675 ,  A61K031/4196 ,  C07D263/36

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D249/10 ,  C07D403/10 ,  H01M2/1055 ,  H04B1/3883 ,  H04B2001/3894

    摘要： Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-nullnull4null-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnullnull1,1null-biphenylnull-2-ylnullnullcarbonylhydrazide, (shown below) is an example: 1

    摘要翻译： 描述了肾选择性化合物，其在一个实施方案中是优先在肾中转化为能够阻断血管紧张素II（AII）受体的化合物的前药。 这些前药是由两种组分形成的缀合物，即由AII拮抗剂化合物提供的第一组分和当两种组分在缀合物内化学连接时能够从第一组分切割的第二组分。 两种组分通过在肾脏中有选择性地切割的键化学连接，例如通过酶。 然后释放的AII拮抗剂化合物可用于阻断肾脏内的AII受体。 特别感兴趣的结合物是联苯甲基1H-取代-1,2,4-三唑化合物的谷氨酰基衍生物，其中N-乙酰谷氨酸5 - [[4' - [（3,5-二丁基-1H-1,2,4-三唑） 4-三唑-1-基）甲基] [1,1'-联苯] -2-基]]羰酰肼，（如下所示）是一个实例：

    Spironolactone and angiotensin II antagonist combination therapy for treatment of congestive heart failure
    6.
    发明申请
    Spironolactone and angiotensin II antagonist combination therapy for treatment of congestive heart failure 审中-公开
    螺内酯和血管紧张素II拮抗剂联合治疗充血性心力衰竭

    公开(公告)号：US20040102423A1

    公开(公告)日：2004-05-27

    申请号：US10271362

    申请日：2002-10-15

    申请人： G.D. Searle & Co.

    发明人： Todd E. MacLaughlan ,  Joseph R. Schuh

    IPC分类号： A61K031/58

    CPC分类号： A61K31/585 ,  A61K31/415 ,  A61K31/41 ,  A61K2300/00

    摘要： A combination therapy comprising a therapeutically-effective amount of an epoxy-free spirolactone-type aldosterone receptor antagonist and a therapeutically-effective amount of an angiotensin II receptor antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred angiotensin II receptor antagonists are those compounds having high potency and bioavailability and which are characterized in having an imidazole or triazole moiety attached to a biphenylmethyl or pyridinyl/phenylmethyl moiety. A preferred epoxy-free spirolactone-type aldosterone receptor antagonist is spironolactone. A preferred combination therapy includes the angiotensin II receptor antagonist 5-null2-null5-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnull-2-pyridinylnullphenyl-1H-tetrazole and the aldosterone receptor antagonist spironolactone.

    摘要翻译： 描述了包含治疗有效量的无环氧的螺内酯型醛固酮受体拮抗剂和治疗有效量的血管紧张素II受体拮抗剂的联合疗法用于治疗循环障碍，包括心血管疾病如高血压，充血性心力衰竭 ，肝硬化和腹水。 优选的血管紧张素II受体拮抗剂是具有高效力和生物利用度的那些化合物，其特征在于具有连接到联苯甲基或吡啶基/苯甲基部分上的咪唑或三唑部分。 优选的不含环氧的螺旋体醛固酮受体拮抗剂是螺内酯。 优选的联合疗法包括血管紧张素II受体拮抗剂5- [2- [5 - [（3,5-二丁基-1H-1,2,4-三唑-1-基）甲基] -2-吡啶基]苯基-1H- 四唑和醛固酮受体拮抗剂安体舒通。

    Triple therapy of angiotensin converting enzyme inhibitor epoxy-steroidal aldosterone antagonist and diuretic or digoxin for treatment of cardiovascular disease
    8.
    发明申请
    Triple therapy of angiotensin converting enzyme inhibitor epoxy-steroidal aldosterone antagonist and diuretic or digoxin for treatment of cardiovascular disease 审中-公开
    血管紧张素转换酶抑制剂环氧甾体醛固酮拮抗剂和利尿剂或地高辛三联治疗心血管疾病

    公开(公告)号：US20040077611A1

    公开(公告)日：2004-04-22

    申请号：US10440691

    申请日：2003-05-19

    申请人： G.D. Searle & Co.

    发明人： John C. Alexander ,  Barbara Roniker ,  Subhash Desai

    IPC分类号： A61K031/58 ,  A61K031/401

    CPC分类号： C12Q1/48 ,  A61K31/585 ,  A61K38/556 ,  A61K45/06 ,  A61K2300/00

    摘要： Combinations of an ACE inhibitor and an epoxy-steroidal aldosterone receptor antagonist are described for use in treatment of circulatory disorders. Of particular interest are therapies using epoxy-steroidal-type aldosterone receptor antagonist compounds, such as eplerenone, in combination with an angiotensin converting enzyme inhibitor. This co-therapy would be particularly useful to treat congestive heart failure while avoiding or reducing aldosterone-antagonist-induced side effects such as hyperkalemia.

    摘要翻译： 描述了ACE抑制剂和环氧甾体醛固酮受体拮抗剂的组合用于治疗循环障碍。 特别令人感兴趣的是使用环氧甾体类醛固酮受体拮抗剂化合物如依普利酮与血管紧张素转换酶抑制剂组合的疗法。 治疗充血性心力衰竭同时避免或减少醛固酮拮抗剂诱导的副作用如高钾血症，这种联合治疗将特别有用。

    Method to treat cardiofibrosis with a combination of an angiotensin II antagonist and spironolactone
    9.
    发明申请
    Method to treat cardiofibrosis with a combination of an angiotensin II antagonist and spironolactone 审中-公开
    用血管紧张素II拮抗剂和螺内酯组合治疗心纤维化的方法

    公开(公告)号：US20040067915A1

    公开(公告)日：2004-04-08

    申请号：US10429410

    申请日：2003-05-05

    申请人： G.D. Searle & Co.

    发明人： Ellen G. McMahon ,  Gillian M. Olins ,  Joseph R. Schuh

    IPC分类号： A61K031/56 ,  A61K031/519 ,  A61K031/4196 ,  A61K031/4439 ,  A61K031/4184

    CPC分类号： A61K45/06

    摘要： A therapeutic method is described for treating cardiofibrosis or cardiac hypertrophy using a combination therapy comprising a therapeutically-effective amount of an epoxy-free spirolactone-type aldosterone receptor antagonist and a therapeutically-effective amount of an angiotensin II receptor antagonist. Preferred angiotensin II receptor antagonists are those compounds having high potency and bioavailability and which are characterized in having an imidazole or triazole moiety attached to a biphenylmethyl or pyridinyl/phenylmethyl moiety. A preferred epoxy-free spirolactone-type aldosterone receptor antagonist is spironolactone. A preferred combination therapy includes the angiotensin II receptor antagonist 5-null2-null5-null(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methylnull-2-pyridinylnullphenyl-1H-tetrazole and the aldosterone receptor antagonist spironolactone.

    摘要翻译： 描述了一种治疗心脏纤维化或心脏肥大的治疗方法，其使用包含治疗有效量的无环氧的螺旋体型醛固酮受体拮抗剂和治疗有效量的血管紧张素II受体拮抗剂的组合疗法。 优选的血管紧张素II受体拮抗剂是具有高效力和生物利用度的那些化合物，其特征在于具有连接到联苯甲基或吡啶基/苯甲基部分上的咪唑或三唑部分。 优选的不含环氧的螺旋体醛固酮受体拮抗剂是螺内酯。 优选的联合治疗包括血管紧张素II受体拮抗剂5- [2- [5 - [（3,5-二丁基-1H-1,2,4-三唑-1-基）甲基] -2-吡啶基]苯基-1H- 四唑和醛固酮受体拮抗剂安体舒通。