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68 条记录 (耗时 0.046 秒)

    N-substituted imidazol-2-one compounds for treatment of circulatory disorders
    31.
    发明授权
    N-substituted imidazol-2-one compounds for treatment of circulatory disorders 失效
    用于治疗循环系统疾病的N-取代咪唑-2-酮化合物

    公开(公告)号：US5238952A

    公开(公告)日：1993-08-24

    申请号：US828546

    申请日：1992-01-28

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

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

    IPC分类号： C07D233/70 ,  C07D403/10 ,  C07D409/14

    CPC分类号： C07D403/10 ,  C07D233/70 ,  C07D409/14

    摘要： A class of N-substituted imidazol-2-one 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.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.10 and R.sup.11 is hydrido; with the proviso that at least one of R.sup.5 and R.sup.9 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-aceptable 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N-取代咪唑-2-酮化合物。 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R3，R4，R6，R7，R8，R10和R11各自为氢; 条件是R 5和R 9中的至少一个必须选自COOH，SH，PO3H2，SO3H，CONHNH2，CONHNHSO2CF3 + L，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。

    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
    32.
    发明授权
    Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension 失效
    肾上腺素选择性联苯胺1 H-取代的1,2,4-三唑血管生成素II治疗高血压的拮抗剂

    公开(公告)号：US5217985A

    公开(公告)日：1993-06-08

    申请号：US574314

    申请日：1990-08-28

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

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

    IPC分类号： C07D249/08 ,  C07D249/10 ,  C07D403/10 ,  C07D521/00 ,  H04B1/38

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

    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: ##STR1##

    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）是一个例子：

    High-temperature, high-shear capillary viscometer
    33.
    发明授权
    High-temperature, high-shear capillary viscometer 失效
    高温，高剪切毛细管粘度计

    公开(公告)号：US4723442A

    公开(公告)日：1988-02-09

    申请号：US932858

    申请日：1986-11-20

    申请人： Robert E. Manning ,  Wallis A. Lloyd

    发明人： Robert E. Manning ,  Wallis A. Lloyd

    IPC分类号： G01N11/06

    CPC分类号： G01N11/06

    摘要： A high-temperature, high-shear viscometer includes a closed end tube having a chamber. A first inlet to the tube is for introducing pressurized gas therein. A second inlet to the tube is for introducing the liquid into the chamber and removing excess liquid from the chamber. A capillary tube is in communication with the chamber. An outlet for the liquid is in communication with the capillary tube. A timer is provided for measuring the efflux time of the liquid in the capillary tube. The timer is started by a device in communication with the first inlet. The timer is stopped by a device which senses the movement of the pressurized gas. The movement sensor includes a thermistor.

    摘要翻译： 高温，高剪切粘度计包括具有室的封闭端管。 管的第一入口用于在其中引入加压气体。 管的第二入口是用于将液体引入室中并从室中去除多余的液体。 毛细管与腔室连通。 用于液体的出口与毛细管连通。 提供了用于测量毛细管中的液体的流出时间的定时器。 定时器由与第一入口通信的设备启动。 定时器由感测加压气体的运动的装置停止。 移动传感器包括热敏电阻。

    N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
    37.
    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。

    Conformationally restricted angiotensin II antagonists
    40.
    发明授权
    Conformationally restricted angiotensin II antagonists 失效
    构象上限制的血管紧张素II拮抗剂

    公开(公告)号：US5426105A

    公开(公告)日：1995-06-20

    申请号：US127147

    申请日：1993-09-24

    申请人： Robert E. Manning ,  Horng-Chih Huang

    发明人： Robert E. Manning ,  Horng-Chih Huang

    IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  A61K31/435

    CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04

    摘要： Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders. Compounds of particular interest are of Formula I ##STR1## wherein W is N or CH.sub.2 ; wherein X is N or CR.sup.2 ; wherein Y is (CH.sub.2).sub.n and n is 1 to 3; wherein Z is C.dbd.R.sup.3 or CR.sup.4 R.sup.5, or wherein Y and Z together forms --CR.sup.6 .dbd.CR.sup.7 --, --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 or --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 --CH.sup.2 --; wherein the remainder of the variables are as defined in the specification; or a pharmaceutically suitable salt or tautomer thereof.

    摘要翻译： 描述了构形限制的化合物，其作为用于治疗循环系统疾病的血管紧张素II拮抗剂是治疗有效的。 特别感兴趣的化合物是式I（I）其中W是N或CH 2; 其中X为N或CR 2; 其中Y为（CH 2）n且n为1至3; 其中Z为C = R 3或CR 4 R 5，或其中Y和Z一起形成-CR 6 = CR 7 - ，-CR 6 = CR 7 -CH 2或-CR 6 = CR 7 -CH 2 -CH 2 - ; 其中所述变量的其余部分如说明书中所定义; 或其药学上合适的盐或互变异构体。