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公开(公告)号：EP0211429A1
公开(公告)日：1987-02-25
申请号：EP86110772.0
申请日：1986-08-04
发明人： Atwal, Karnail S.
IPC分类号： C07D243/12 , C07D401/06 , C07D405/06 , C07D409/06 , A61K31/55
CPC分类号： C07D243/12
摘要： Compounds of formula
wherein
R 4 is aryl or hetero are disclosed. These compounds are useful as cardiovascular agents and especially as anti-hypertensive agents.-
2.发明公开Indole and benzimidazole-substituted dihydropyrimidine derivatives useful as A-II receptors antagonists 失效吲哚和苯并咪唑取代物二氢嘧啶二酮类化合物NützlichfürA-II-Rezeptoren-Antagonisten。
公开(公告)号：EP0547827A1
公开(公告)日：1993-06-23
申请号：EP92311202.3
申请日：1992-12-09
IPC分类号： C07D403/06 , C07D403/14 , A61K31/505
CPC分类号： C07D403/14
摘要： Novel compounds having the formula
and its isomer
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R s , R 7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.摘要翻译： 具有式CHEM的新型化合物及其异构体
其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和X如本文所定义。 这些化合物抑制血管紧张素II的作用，因此可用作例如抗高血压药。 -
3.发明公开Substituted indole and benzimidazole derivatives useful as A-II receptors antagonists 失效Substituierte Indole und Benzimidazolederivatenützlichals A-II-Rezeptoren-Antagonisten。
公开(公告)号：EP0547556A1
公开(公告)日：1993-06-23
申请号：EP92121316.1
申请日：1992-12-15
IPC分类号： C07D403/10 , C07D403/14 , A61K31/505
CPC分类号： C07D403/10 , C07D403/14
摘要： Novel compounds are disclosed having the formula
or its isomer
wherein R₁, R₂, R₃, R₄, R₅, R₆, R₇ and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.摘要翻译： 公开了具有式CHEM或其异构体CHEM的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和X如本文所定义。 这些化合物抑制血管紧张素II的作用，因此可用作例如抗高血压药。
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4.发明公开2-Thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxylic acid diesters and 3-acyl-5-pyrimidinecarboxylic acids and esters 失效2-硫代羰基-4-芳基杂环基-1,5（2H） - 嘧啶并碳酸酯和3-酰基-5-嘧啶羰基和酯。
公开(公告)号：EP0204317A2
公开(公告)日：1986-12-10
申请号：EP86107536.4
申请日：1986-06-03
IPC分类号： C07D239/22 , C07D401/04 , C07D413/04 , A61K31/505
CPC分类号： C07D239/22 , C07D401/04 , C07D413/04
摘要： Pyrimidine compounds of the formula
wherein X is sulfur or oxygen, Y is R 11 or-O-R 1 , and R 4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.摘要翻译： 公开了式CHEM的嘧啶化合物，其中X是硫或氧，Y是R 11或-O-R 1，R 4是芳基或杂环。 这些化合物由于其钙进入阻断血管扩张剂活性而可用作心血管药物，特别是抗高血压药。
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5.发明公开
公开(公告)号：EP0354553A3
公开(公告)日：1990-04-11
申请号：EP89114729.0
申请日：1989-08-09
IPC分类号： C07C279/28 , C07D217/24 , C07D295/192 , C07C317/42 , A61K31/44 , A61K31/275 , A61K31/40 , A61K31/455 , A61K31/505
CPC分类号： C07D295/18 , A61K31/40 , A61K31/44 , A61K31/455 , A61K31/505 , C07C279/28 , C07C317/42 , C07C2601/14 , C07C2602/10 , C07D217/24 , C07D405/04
摘要： Compounds of the formula I:
and tautomers thereof, wherein at least one of R 2 , R 3 and R4 is a strong electron withdrawing group, are disclosed. These compounds possess potassium channel activating activity and, as such, are useful as antihypertensive agents and show less cardiac effects than known potassium channel activators. Also disclosed is a process for preparing these and other compounds and the use of potassium channel activators for the preparation of drugs for the treatment of fibrillation of the heart wherein said potassium channel activators are selected from pinacidil, cromakalim, nicorandil, minoxidil and the compounds of formula I.摘要翻译： 式I化合物：
及其互变异构体，其中R 2，R 3和R 4中的至少一个是强吸电子基团。 这些化合物具有钾通道活化活性，因此可用作抗高血压药物，并且比已知钾通道激活剂显示更少的心脏效应。 还公开了一种制备这些和其它化合物的方法，以及使用钾通道激活剂来制备用于治疗心脏颤动的药物，其中所述钾通道激活剂选自哌拉西地尔，克罗卡明，尼可地尔，米诺地尔和 公式一 -
6.发明公开2-Thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxylic acid diesters and 3-acyl-5-pyrimidinecarboxylic acids and esters 失效2-硫代或邻 - 4-芳基或杂环基-1,5（2H） - 嘧啶二羧酸和三 - 乙基-5-吡啶甲酰氧基酸和酯
公开(公告)号：EP0204317A3
公开(公告)日：1987-12-16
申请号：EP86107536
申请日：1986-06-03
IPC分类号： C07D239/22 , C07D401/04 , C07D413/04 , A61K31/505
CPC分类号： C07D239/22 , C07D401/04 , C07D413/04
摘要： Pyrimidine compounds of the formula
wherein X is sulfur or oxygen, Y is R 11 or-O-R 1 , and R 4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.-
7.发明公开
公开(公告)号：EP0163458A1
公开(公告)日：1985-12-04
申请号：EP85303472.6
申请日：1985-05-17
发明人： Atwal, Karnail S.
IPC分类号： C07C93/14 , C07C91/23 , C07D209/16 , C07D277/64 , C07D235/14 , C07D263/56
CPC分类号： C07D263/56 , C07C2603/18 , C07D209/16 , C07D235/14 , C07D277/64
摘要： New compounds, useful for the treatment of hyperten- sion, have the formula
and pharmaceutically acceptable salts thereof, wherein
R, is hydrogen or methyl;
R 2 is hydrogen, alkyl, alkanoyl, or arylcarbonyl;
R 3 and R 4 are each aryl; R 3 and R 4 are each cycloalkyl; R 3 is hydrogen or alkyl and R 4 is cycloalkyl or 9H-fluoren-9-yl; or R 3 is hydrogen or alkyl and R 4 is heteroaryl;
R 5 and R 6 are the same or different and each is hydrogen, hydroxy, alkoxy or alkanoyl; and
n is 1, 2, 3 and 4.摘要翻译： 可用于治疗高血压的新化合物具有式
及其药学上可接受的盐，其中R 1是氢或甲基; R2是氢，烷基，烷酰基或芳基羰基; R3和R4各自为芳基; R3和R4各自为环烷基; R3是氢或烷基，R4是环烷基或9H-芴-9-基; 或R3是氢或烷基，R4是杂芳基; R5和R6相同或不同，各自为氢，羟基，烷氧基或烷酰基; n为1,2,3,4 -
8.发明公开Aryl cyanoguanidines: potassium channel activators and method of making same 失效芳基氰基胍：Kaliumkanal aktivierende Mittel sowie Verfahren zu ihrer Herstellung。
公开(公告)号：EP0354553A2
公开(公告)日：1990-02-14
申请号：EP89114729.0
申请日：1989-08-09
IPC分类号： C07C279/28 , C07D217/24 , C07D295/192 , C07C317/42 , A61K31/44 , A61K31/275 , A61K31/40 , A61K31/455 , A61K31/505
CPC分类号： C07D295/18 , A61K31/40 , A61K31/44 , A61K31/455 , A61K31/505 , C07C279/28 , C07C317/42 , C07C2601/14 , C07C2602/10 , C07D217/24 , C07D405/04
摘要： Compounds of the formula I:
and tautomers thereof, wherein at least one of R 2 , R 3 and R4 is a strong electron withdrawing group, are disclosed. These compounds possess potassium channel activating activity and, as such, are useful as antihypertensive agents and show less cardiac effects than known potassium channel activators.
Also disclosed is a process for preparing these and other compounds and the use of potassium channel activators for the preparation of drugs for the treatment of fibrillation of the heart wherein said potassium channel activators are selected from pinacidil, cromakalim, nicorandil, minoxidil and the compounds of formula I.摘要翻译： 式I化合物：
及其互变异构体，其中R 2，R 3和R 4中的至少一个是强吸电子基团。 这些化合物具有钾通道活化活性，因此可用作抗高血压药物，并且比已知钾通道激活剂显示更少的心脏效应。 还公开了一种制备这些和其它化合物的方法，以及使用钾通道激活剂来制备用于治疗心脏颤动的药物，其中所述钾通道激活剂选自哌拉西地尔，克罗卡明，尼可地尔，米诺地尔和 公式一
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