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    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension
    4.
    发明授权
    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension 失效
    环庚咪唑酮化合物作为血管紧张素II拮抗剂用于控制高血压

    公开(公告)号：US5281615A

    公开(公告)日：1994-01-25

    申请号：US840471

    申请日：1992-02-24

    申请人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    发明人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  C07F9/6558 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D403/10

    摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

    摘要翻译： 一类环庚咪唑酮化合物被描述为用于控制高血压的血管紧张素II拮抗剂。 特别感兴趣的化合物是式（*化学结构*）的化合物，其中R 1和R 2各自独立地选自氢，烷基，卤素，烷酰基，羧基，烷氧基羰基，苯基，卤代烷基，烷氧基烷基，甲酰基，氰基，烷氧基，苯氧基 ，苯硫基，烷硫基; 其中R3是烷基，烯基，炔基，羟基烷基和烷氧基烷基; 其中R 5至R 13中的每一个独立地选自氢，烷基，卤代烷基，卤素，硝基，氰基，羟基，烷氧基，烷硫基，芳基，芳氧基，仲氨基和酸性基团如羧酸，条件是至少一个 R9至R13取代基是酸性基团; 或其药学上可接受的酯，酰胺或其盐。

    Treatment of circulatory disorders using n-substituted (.alpha.-imidazolyl-toluyl) pyrrole angiotensin II antagonists
    5.
    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
    6.
    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。

    Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists
    7.
    发明授权
    Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (.alpha.-imidazolyl-toluyl) pyrrole aniotensin II antagonists 失效
    使用N-取代的（α-咪唑基 - 甲苯酰基）吡咯类抗生素II拮抗剂治疗循环障碍的药物组合物

    公开(公告)号：US6008368A

    公开(公告)日：1999-12-28

    申请号：US976757

    申请日：1997-11-24

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

    CPC分类号： C07D403/10

    摘要： Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds 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.sup.3, R.sup.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 C02H and tetrazolyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compositions are particularly useful in treatment or control of hypertension and congestive heart failure.

    摘要翻译： 描述了包含选自一类N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物的化合物的药物组合物用于治疗循环障碍。 特别感兴趣的组合物包括下式的血管紧张素II拮抗剂化合物其中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。 这些组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 (&agr;-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
    9.
    发明授权
    N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders 失效
    用于治疗循环系统疾病的N-取代的（α-咪唑基 - 甲苯酰基）吡咯化合物

    公开(公告)号：US06451833B1

    公开(公告)日：2002-09-17

    申请号：US09704389

    申请日：2000-11-01

    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： A61K314178

    CPC分类号： C07D403/10 ,  C07D403/14

    摘要： A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula wherein m is one; wherein each of R0 and R1 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 R2 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 R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R5 and R8 must be selected from COOH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, wherein each of R42 and R43 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： 一类描述用于治疗循环系统疾病的N-取代（α-咪唑基 - 甲苯酰基）吡咯化合物。 化合物特别有意义的是血管紧张素II拮抗剂， 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。