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1. 发明申请

WO1991018888A1 N-SUBSTITUTED-1,2,4-TRIAZOLONE COMPOUNDS FOR TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
标题翻译：用于治疗心血管疾病的N-取代的1,2,4-三唑酮化合物
公开(公告)号：WO1991018888A1
公开(公告)日：1991-12-12
申请号：PCT/US1991003449
申请日：1991-05-23
申请人： G.D. SEARLE & CO. , MANNING, Robert, E. , REITZ, David, B. , HUANG, Horng-Chih
发明人： G.D. SEARLE & CO.
IPC分类号： C07D249/12
CPC分类号： C07D403/10 , C07D249/12
摘要： A class of N-substituted-1,2,4-triazolone compounds is described for use in treatment of cardiovascular disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein R is selected from 2-oxo-2-(tricyclo[3.3.1.1. ]dec-2-yl)ethyl, 3-phenylpropyl, 2-oxo-2-phenylethyl, 2-hyroxy-2-phenylethyl, 1,1-dimethylethyloxycarbonylmethyl, hexyl, ethoxycarbonylmethyl, carboxymethyl, 1-naphthalenylmethyl, 2-cyclohexylethyl, pentyl, ethoxycarbonylmethoxyethyl substituted with phenyl, carboxymethoxyethyl substituted with phenyl, 3,5,5-trimethylhexyl, (2-phenylmethoxy)-1-(phenylmethyl)-E-ethenyl, 1-benzoyl-2-phenylethyl, 1-oxobutyl, 2-(2,5-dimethyoxyphenyl)-2-oxoethyl, 2-phenyl-2-(phenylmethoxyethyl, 2-(2,5-dimethioxy-phenyl)-2-hydroxyethyl, 2-naphthalenylmethyl, methoxycarbonyl-butyl, ethoxycarbonylethyl substituted with benzoyl, 1-benzyoyl-1-methylethyl, 1-pentanoic acid, cyclopropylmethyl, 3-phenyl-2E-propenyl and 3-acetonitrile; wherein R is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neopentyl, 1-cyanobutyl, propylthio and butylthio; wherein each of R through R is hydrido with the proviso that at least one of R and R must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (a), (b) and (c), wherein each of R and R is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl. 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心血管疾病的N-取代的1,2,4-三唑酮化合物。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中R 1选自2-氧代-2-（三环[3.3.1.1.33.2]癸-2-基）乙基，3-苯基丙基，2-氧代-2-苯基乙基，2-羟基-2-苯基乙基，1,1-二甲基乙氧基羰基甲基，己基，乙氧基羰基甲基，羧甲基，1-萘基甲基，2-环己基乙基，戊基，被苯基取代的乙氧基羰基甲氧基乙基，被苯基取代的羧基甲氧基乙基，，5,5-三甲基己基，（2-苯基甲氧基）-1-（苯基甲基）-E-乙烯基，1-苯甲酰基-2-苯基乙基，1-氧代丁基，2-（2,5-二甲氧基苯基）-2-氧代乙基，2 - 苯基-2-（苯基甲氧基乙基，2-（2,5-二甲氧基 - 苯基）-2-羟乙基，2-萘基甲基，甲氧基羰基 - 丁基，苯甲酰基取代的乙氧基羰基乙基，1-苯甲酰基-1-甲基乙基，1-戊酸，环丙基甲基，3-苯基-2-丙烯基和3-乙腈;其中R 2选自乙基，正丙基，异丙基，正丁基，仲丁基，异丁基，4-甲基丁基，叔丁基，戊基，新戊基，1-氰基乙硫基，丁硫基; 其中R 3至R 11各自为氢，条件是R 5和R 9中的至少一个必须选自COOH，SH，PO 3 H 2，SO 3 H，CONHNH 2，CONHNHSO 2 CF 3，OH，（ a），（b）和（c），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。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。

2. 发明申请

WO1992011255A1 N-SUBSTITUTED N-('alpha'-TRIAZOLYL-TOLUYL)PYRROLE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译： N-取代的N-（α-三唑基 - 叔丁基）吡咯烷化合物，用于治疗循环障碍
公开(公告)号：WO1992011255A1
公开(公告)日：1992-07-09
申请号：PCT/US1991008726
申请日：1991-11-26
申请人： G.D. SEARLE & CO. , BOVY, Philippe, R. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D403/14
CPC分类号： C07D403/10 , C07D403/14
摘要： A class of N-substituted N-(α-triazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of formula (I), wherein m is one; wherein R1 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 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 R?3, R4, R5, R6, R7, R8, R9 and R10¿ is independently selected from hybrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R?5 and R8¿ must be selected from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, a), b) and c) wherein each of R?42 and R43¿ 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.

3. 发明申请

WO1994008990A1 N-ARYLHETEROARYLALKYL 1-PHENYL-IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的N-苯基二甲基-1-苯基咪唑-2-酮化合物
公开(公告)号：WO1994008990A1
公开(公告)日：1994-04-28
申请号：PCT/US1993005603
申请日：1993-06-16
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D401/10 , C07D401/14
摘要： A class of N-arylheteroarylalkyl 1-phenyl-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 formula (I) wherein A is selected from (a), (b), (c), (d), (e) and (f); wherein m is one; wherein each of R , R and R is independently selected from hybrido, alkyl, alkoxy, cyano, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; alkylcarbonyl and haloalkylcarbonyl; wherein R is hybrido; wherein R is alkyl; wherein R is an acidic group selected from COOH and (g); or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt.
摘要翻译：描述了一类N-芳基杂芳基烷基1-苯基 - 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式（I）的血管紧张素II拮抗剂，其中A选自（a），（b），（c），（d），（e）和（f）其中m为1; 其中R 1，R 2和R 3各自独立地选自杂环基，烷基，烷氧基，氰基，卤素，羟基，羧基，烷氧羰基，甲酰基和乙酰基。烷基羰基和卤代烷基羰基; 其中R 4是杂环基; 其中R 5是烷基; 其中R 6是选自COOH的酸性基团和（g）; 或其立体异构体或其互变异构体或药学上可接受的盐。

4. 发明申请

WO1994008989A1 N-ARYLHETEROARYLALKYL 1-CYCLOALKYL-IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：用于治疗循环障碍的N-亚油酰基胆碱1-环丙基咪唑烷-2-酮化合物
公开(公告)号：WO1994008989A1
公开(公告)日：1994-04-28
申请号：PCT/US1993005601
申请日：1993-06-16
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D401/06
CPC分类号： C07D401/14
摘要： A class of N-arylheteroarylalkyl 1-cycloalkyl-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 angiotension II antagonists of formula (A), wherein A is selected from (a), (b), (c), (d), (e) and (f); wherein each of R , R and R is independently selected from hydrido, alkyl, alkoxy, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; wherein R is hydrido; R is alkyl; wherein R is an acidic group selected from COOH and (g); or a stereoisomer 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-1-环烷基 - 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式（A）的血管紧张素II拮抗剂，其中A选自（a），（b），（c），（d），（e）和（f）其中R 1，R 2和R 3各自独立地选自氢，烷基，烷氧基，卤素，羟基，羧基，烷氧基羰基，甲酰基和乙酰基; 其中R 7是氢的; R 8是烷基; 其中R 9是选自COOH的酸性基团和（g）; 或其立体异构体或其互变异构体或其药学上可接受的盐。

5. 发明申请

WO1992004335A2 RENAL-SELECTIVE BIPHENYLALKYL 1H-SUBSTITUTED-1,2,4-TRIAZOLE ANGIOTENSIN II ANTAGONISTS FOR TREATMENT OF HYPERTENSION 审中-公开
标题翻译：肾选择性联苯基取代的1H-1,2,4-三唑血管紧张素II拮抗剂用于治疗高血压的
公开(公告)号：WO1992004335A2
公开(公告)日：1992-03-19
申请号：PCT/US1991005897
申请日：1991-08-26
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D249/08
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 is an example.
摘要翻译：描述了肾特异性化合物，其在一个实施方案中是前药，优选转化成肾，成为能够阻断血管紧张素II（AII）受体的化合物。这些前药是由两个部件，即通过AII拮抗剂的化合物和其可从第一组件当两个组件被化学结合到所述缀合物被分离的第二部件表示的第一组分形成的缀合物。两种组分通过在肾中选择性切割的链接化学连接，例如通过酶。这样释放的AII拮抗剂化合物可用于阻断肾脏中的AII受体。特别感兴趣的缀合物是联苯甲基取代的-1H-1,2,4-三唑，例如，N-乙酰谷氨酸，5的化合物的谷氨酰衍生物 - [[4“ - （3,5-二dibutyl1H-1 ，2,4-三唑-1-基）甲基] [1,1'-联苯] -2-基] carbonylhydrazide-。

6. 发明申请

WO1995021817A1 SUBSTITUTED SPIRO COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的替代性SPIRO化合物
公开(公告)号：WO1995021817A1
公开(公告)日：1995-08-17
申请号：PCT/US1995001385
申请日：1995-02-07
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E. , HUANG, Horng-Chi , LI, Jinglin
发明人： G.D. SEARLE & CO.
IPC分类号： C07C317/14
CPC分类号： C07D213/70 , C07C311/16 , C07C311/29 , C07C317/14 , C07C317/22 , C07C323/65 , C07D213/34 , C07D213/61 , C07D317/56
摘要： A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (III), wherein n is a number selected from 0, 1 and 2; wherein R is selected from hydrido and halo; wherein R is selected from hydrido and halo; wherein R is selected from hydrido, halo, lower alkyl, lower alkoxy, lower haloalkyl, lower haloalkoxy, and hydroxyl; wherein R is selected from hydrido, halo, and lower alkyl; or wherein R and R together form methylenedioxy; and wherein R is selected from lower alkyl and amino; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类取代的螺环化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式（III）定义，其中n是选自0,1和2的数; 其中R 6选自氢和卤素; 其中R 7选自氢和卤素; 其中R 8选自氢，卤素，低级烷基，低级烷氧基，低级卤代烷基，低级卤代烷氧基和羟基; 其中R 9选自氢，卤素和低级烷基; 或其中R 8和R 9一起形成亚甲二氧基; 并且其中R 11选自低级烷基和氨基; 或其药学上可接受的盐。

7. 发明申请

WO1992001667A1 RENAL-SELECTIVE PRODRUGS FOR CONTROL OF RENAL SYMPATHETIC NERVE ACTIVITY IN THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于控制高血压治疗中的晚期反应性神经活性的选择性预防措施
公开(公告)号：WO1992001667A1
公开(公告)日：1992-02-06
申请号：PCT/US1991000611
申请日：1991-01-28
申请人： G.D. SEARLE & CO. , REITZ, David, B. , KOEPKE, John, P. , BLAINE, Edward, H. , SCHUH, Joseph, R. , MANNING, Robert, E. , SMITS, Glenn, J.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C229/34
CPC分类号： C07D213/54 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/12 , C07C237/22 , C07C243/34 , C07C243/38 , C07D209/08 , C07D209/14 , C07D209/34 , C07D213/56 , C07D213/65 , C07D213/73 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/87 , C07D215/227 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D235/30 , C07D241/42 , C07D241/44 , C07D263/58 , C07D265/36 , C07D285/14 , C07D295/185 , C07D307/52 , C07D307/54 , C07D309/40 , C07D333/20 , C07D333/24 , C07D333/66
摘要： Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine- beta -hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine- beta -hydroxylase-inhibitors, of which N-acetyl- gamma -glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.
摘要翻译：描述了肾选择性前药，其优先在肾中转化成能够抑制参与肾交感神经活性的儿茶酚胺型神经递质合成的化合物。本文所述的前药衍生自能够抑制一种或多种参与儿茶酚胺合成的酶的抑制剂化合物，这些化合物可分类为酪氨酸羟化酶抑制剂，或作为多巴 - 脱羧酶抑制剂，或作为多巴胺-β-羟化酶抑制剂。这些抑制剂化合物通过可主要在尼克定位的酶选择性识别的可切割键与化学部分如谷氨酸衍生物连接。释放的抑制剂化合物然后可用于肾脏中以抑制参与儿茶酚胺合成的一种或多种酶。抑制肾脏儿茶酚胺合成可以抑制与钠滞留相关的疾病如高血压相关的增强的肾神经活动。特别感兴趣的缀合物是多巴胺-β-羟化酶抑制剂的谷氨酰衍生物，其中优选N-乙酰基-γ-谷氨酰镰孢酸酰肼[在式（a）中表示）。

8. 发明申请

WO1991001724A1 RENAL-SELECTIVE PRODRUGS FOR THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于治疗高血压的选择性预防药物
公开(公告)号：WO1991001724A1
公开(公告)日：1991-02-21
申请号：PCT/US1990004168
申请日：1990-07-25
申请人： G.D. SEARLE & CO. , REITZ, David, B. , KOEPKE, John, P. , BLAINE, Edward, H. , SCHUH, Joseph, R. , MANNING, Robert, E. , SMITS, Glenn, J.
发明人： G.D. SEARLE & CO.
IPC分类号： A61K31/12
CPC分类号： C07D213/73 , C07C59/64 , C07C59/90 , C07C237/12 , C07C237/22 , C07D209/08 , C07D209/20 , C07D209/34 , C07D213/50 , C07D213/65 , C07D213/80 , C07D213/81 , C07D213/86 , C07D215/227 , C07D233/64 , C07D233/88 , C07D233/90 , C07D235/30 , C07D241/42 , C07D241/44 , C07D263/58 , C07D265/36 , C07D285/14 , C07D307/46 , C07D307/52 , C07D333/20 , C07D333/22 , C07D333/66
摘要： Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine- beta -hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine- beta -hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
摘要翻译：描述了肾选择性前药，其优先在肾中转化成能够抑制参与肾交感神经活性的儿茶酚胺型神经递质合成的化合物。本文描述的前药衍生自能够抑制一种或多种参与儿茶酚胺合成的酶的抑制剂化合物，这些化合物可分类为酪氨酸羟化酶抑制剂，或作为脱羧脱羧酶抑制剂，或作为多巴胺-β-羟化酶抑制剂。这些抑制剂化合物通过被主要位于肾中的酶选择性识别的可切割键与化学部分如谷氨酸衍生物连接。释放的抑制剂化合物然后可用于肾脏中以抑制参与儿茶酚胺合成的一种或多种酶。抑制肾脏儿茶酚胺合成可以抑制与钠滞留相关的疾病如高血压相关的增强的肾神经活动。特别感兴趣的缀合物是多巴胺-β-羟化酶抑制剂的谷氨酰衍生物，其中N-乙酰基-Y-谷氨酰镰孢酸是优选的。

9. 发明申请

WO1994021629A1 1-PHENYL-IMIDAZOL-2-ONE BIPHENYLMETHYL COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译： 1-苯基咪唑-2-酮联苯甲基化合物治疗循环障碍
公开(公告)号：WO1994021629A1
公开(公告)日：1994-09-29
申请号：PCT/US1994002156
申请日：1994-03-08
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D403/00
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 formula (I) wherein each of R , R and R 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 R , R and R must be a substituent other than hydrido, and with the further proviso that when each of R and R is hydrido, then R cannot be chloro; wherein R is hydrido; wherein R is alkyl; and wherein R 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。特别感兴趣的化合物是式（I）的血管紧张素II拮抗剂，其中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。

10. 发明申请

WO1992017469A2 N-ARYLHETEROARYLALKYL IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS 审中-公开
标题翻译：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：WO1992017469A2
公开(公告)日：1992-10-15
申请号：PCT/US1992002439
申请日：1992-04-01
申请人： G.D. SEARLE & CO. , REITZ, David, B. , MANNING, Robert, E.
发明人： G.D. SEARLE & CO.
IPC分类号： 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 formula (I) wherein A is selected from (a), (b), (c), (d), (e) and (f), wherein m is one; R1 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, phenetyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R0 is hydrido; 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 R?3, R4, R6, R7, R8, R9, R10 and R11¿ is hydrido and R5 must be seleted from COOH, SH, PO¿3?H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, (g), (h) and (i) wherein each of R?42 and R43¿ is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.

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