![Tetrahydro-benzo(e) isoindolines](/ep/1985/01/16/EP0095666A3/abs.jpg.150x150.jpg)
基本信息:
- 专利标题: Tetrahydro-benzo(e) isoindolines
- 专利标题(中):四氢 - 苯并(e)异吲哚啉
- 申请号:EP83104932 申请日:1983-05-19
- 公开(公告)号:EP0095666A3 公开(公告)日:1985-01-16
- 发明人: DeBernardis, John Francis , Kerkman, Daniel Joseph , McClellan, William John
- 申请人: ABBOTT LABORATORIES
- 专利权人: ABBOTT LABORATORIES
- 当前专利权人: ABBOTT LABORATORIES
- 优先权: US383631 19820601
- 主分类号: C07D209/62
- IPC分类号: C07D209/62 ; C07D405/06 ; C07D209/66 ; C07C121/48 ; A61K31/40 ; C07C121/75
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(中):
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.
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。
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D209/00 | 杂环化合物,含五元环、与其他环稠合、带1个氮原子作为惟一的杂环原子 |
--------C07D209/02 | .与一个碳环稠合 |
----------C07D209/58 | ..[b]-或[c]-稠合 |
------------C07D209/62 | ...萘并[c]吡咯,氢化萘并[c]吡咯 |