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公开(公告)号:EP0095666A2
公开(公告)日:1983-12-07
申请号:EP83104932.5
申请日:1983-05-19
申请人: ABBOTT LABORATORIES
IPC分类号: C07D209/62 , C07D405/06 , C07D209/66 , C07C121/48 , A61K31/40 , C07C121/75
CPC分类号: C07D405/06 , C07C255/00 , C07D209/62 , C07D209/66
摘要: DisGosed herein are tetrahydro-benzo [e] isoindolines useful in the treatment of hypertension, which are represented by the formula
wherein R, R,, and R 2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, benzyloxy, benzoyloxy, thiomethyl, halo, or
wherein R. and R 5 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula
wherein R 6 is loweralkyl of 1 to 4 carbon atoms; or R and R,, or R, and R 2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R, or R 2 must be other than hydrogen; and R 3 is hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula
wherein m is 0, 1 or 2, p is 0 or 1, R 7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R 8 and R 9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1. to 4 carbon atoms, or halo, or R, and R 9 can be taken together to form a methylendioxy or ethylenedioxy bridge; or 1,4-benzodioxan.摘要翻译: 本文公开的是可用于治疗高血压的四氢 - 苯并[e]异吲哚啉,其由式CHEM表示,其中R,R 1和R 2独立地选自氢,羟基,1至3个碳原子的低级烷氧基,低级链烯氧基 1至3个碳原子的苄基氧基,苯甲酰氧基,硫代甲基,卤素或CHEM,其中R 4和R 5独立地选自氢,1至4个碳原子的低级酰基或式CHEM的磺酰基,其中R 6是1的低级烷基 至4个碳原子; 或R和R 1,或R 1和R 2可以一起形成亚甲二氧基或亚乙二氧基桥; 条件是R,R 1或R 2中的至少一个必须不是氢; 并且R 3是氢; 1至4个碳原子的低级烷基; 1至4个碳原子的卤素取代的低级烷基; 其中m为0,1或2,p为0或1,R 7为氢或1至4个碳原子的低级烷基,R 8和R 9独立地选自氢,羟基,甲氧基,低级烷基1 至4个碳原子,或卤素,或R8和R9可以一起形成甲基二氧基或亚乙二氧基桥; 或1,4-苯并二恶烷。
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公开(公告)号:EP0095666A3
公开(公告)日:1985-01-16
申请号:EP83104932
申请日:1983-05-19
申请人: ABBOTT LABORATORIES
IPC分类号: C07D209/62 , C07D405/06 , C07D209/66 , C07C121/48 , A61K31/40 , C07C121/75
CPC分类号: C07D405/06 , C07C255/00 , C07D209/62 , C07D209/66
摘要: DisGosed herein are tetrahydro-benzo [e] isoindolines useful in the treatment of hypertension, which are represented by the formula
wherein R, R,, and R 2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, benzyloxy, benzoyloxy, thiomethyl, halo, or
wherein R. and R 5 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula
wherein R 6 is loweralkyl of 1 to 4 carbon atoms; or R and R,, or R, and R 2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R, or R 2 must be other than hydrogen; and R 3 is hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula
wherein m is 0, 1 or 2, p is 0 or 1, R 7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R 8 and R 9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1. to 4 carbon atoms, or halo, or R, and R 9 can be taken together to form a methylendioxy or ethylenedioxy bridge; or 1,4-benzodioxan.摘要翻译: 本发明公开了用于治疗高血压的四氢 - 苯并[e]异吲哚啉,其由下式表示:其中R 1,R 2和R 2独立地选自氢,羟基,1至3个碳原子的低级烷氧基,1的低级链烯氧基 苄氧基,苯甲酰氧基,硫代甲基,卤素,或者其中R和R 5独立地选自氢,1-4个碳原子的低级π-酰氨基或下式的磺酰基:其中R 6为1-4个碳原子的低级烷基; 或R 1和R 2或R 1和R 2可一起形成亚甲二氧基或亚乙二氧基桥; 条件是R 1,R 2或R 2中的至少一个必须不是氢; 和R3是氢; 具有1至4个碳原子的低级烷基; 卤素取代的1至4个碳原子的低级烷基; 其中m为0,1或2,p为0或1,R 7为氢或1-4个碳原子的低级烷基,R 8和R 9独立地选自氢,羟基,甲氧基,1-4低级烷基 碳原子或卤素,或R 1和R 9可一起形成亚甲基二氧基或亚乙基二氧桥; 或1,4-苯并二恶烷。
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公开(公告)号:EP0095666B1
公开(公告)日:1989-01-18
申请号:EP83104932.5
申请日:1983-05-19
申请人: ABBOTT LABORATORIES
IPC分类号: C07D209/62 , C07D405/06 , C07D209/66 , C07C121/48 , A61K31/40 , C07C121/75
CPC分类号: C07D405/06 , C07C255/00 , C07D209/62 , C07D209/66
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