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    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
    3.
    发明授权
    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II 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-1,2,4-三唑血管紧张素II拮抗剂

    公开(公告)号：US07132437B2

    公开(公告)日：2006-11-07

    申请号：US10852711

    申请日：2004-05-24

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

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

    IPC分类号： A61K31/41 ,  C07D249/08

    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-[[4′-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1′-biphenyl]-2-yl]]carbonylhydrazide, (shown below) is an example:

    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：

    1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
    4.
    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：US06630497B2

    公开(公告)日：2003-10-07

    申请号：US09825029

    申请日：2001-04-03

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

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

    IPC分类号： A61K314178

    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。

    Treatment of circulatory disorders using n-substituted (.alpha.-imidazolyl-toluyl) pyrrole angiotensin II antagonists
    8.
    发明授权
    Treatment of circulatory disorders using n-substituted (.alpha.-imidazolyl-toluyl) pyrrole angiotensin II antagonists 失效
    使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯血管紧张素II拮抗剂治疗循环障碍

    公开(公告)号：US5451597A

    公开(公告)日：1995-09-19

    申请号：US66057

    申请日：1993-05-27

    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： A61K31/4178 ,  C07D233/90 ,  C07D403/10 ,  C07D403/14 ,  A61K31/415 ,  A61K31/41 ,  C07D403/04

    CPC分类号： C07D403/10 ,  A61K31/4178 ,  C07D403/14

    摘要： A class of N-substituted (.alpha.-imidazolyltoluyl)pyrrole compounds is 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.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; 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, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sub.3, R.sub.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from CO.sub.2 H and tetrazolyl; 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系统疾病的N-取代的（α-咪唑基甲苯磺酰基）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R 0选自CH 2 OH，CO 2 H，CHO，CO 2 CH 3，CO 2 C 2 H 5，CH 2 OCH 3，CH 2 OCHOCH 3和CH 2 -CO 2 C 2 H 5; 其中R 1选自Cl，CF 3，CHO，正丁基，氰基，CO 2 CH 3和CO 2 CH 2 CH 3; 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，环己基乙基， ，丁硫基和羟烷基; 其中R3，R4，R6，R7，R9和R10各自为氢; 其中R 5和R 8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，甲氧基羰基，条件是R 5和R 8中的至少一个是选自CO 2 H和四唑基的酸性基团。 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-substituted (.alpha.-imidazolyl-toluyl) pyrrole compounds for treatment of circulatory disorders
    10.
    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。