发明公开
EP0174085A3 Bisarylamides of N,N'-di-[1-aminoalkyl-2]-alkylene diamines having a cardiovascular activity
失效
具有心血管活性的N,N'-二氨基亚氨基二烷基亚氨基二胺的双联体
- 专利标题: Bisarylamides of N,N'-di-[1-aminoalkyl-2]-alkylene diamines having a cardiovascular activity
- 专利标题(中): 具有心血管活性的N,N'-二氨基亚氨基二烷基亚氨基二胺的双联体
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申请号: EP85305285申请日: 1985-07-25
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公开(公告)号: EP0174085A3公开(公告)日: 1987-10-14
- 发明人: Jozic, Ljerka
- 申请人: BEECHAM - WUELFING GmbH & Co. KG
- 专利权人: BEECHAM - WUELFING GmbH & Co. KG
- 当前专利权人: BEECHAM - WUELFING GmbH & Co. KG
- 优先权: GB8419103 19840726
- 主分类号: C07C103/82
- IPC分类号: C07C103/82 ; C07C103/30 ; C07D211/58 ; C07D211/26 ; C07D213/82 ; C07C121/50 ; C07D317/60 ; C07C121/43 ; C07C87/20 ; C07C103/48 ; C07C91/08 ; C07C87/22 ; C07D211/74 ; C07D211/22 ; C07D211/18
摘要:
Disclosed are compounds of formula (1) and pharmaceutically acceptable salts thereof:
wherein:
R, and R 9 are independently phenyl, phenyl C 1-4 alkyl, phenyl C 2-4 alkenyl or pyridyl, the aromatic moiety optionally substituted by one, two or three of halogen, trifluoromethyl, C 1-4 alkoxy, C 1-4 alkyl, cyano, hydroxy, nitro, NR 10 R 11 or O 2 SNR 10 R 11 wherein R, o and R 11 are independently hydrogen or C 1-6 alkyl or together are C 3-6 polymethylene, or disubstituted at adjacent carbon atoms by C 1-2 alkylenedioxy; C 3-8 cycloalkyl; or aliphatic heterocyclyl having up to six ring atoms the heteroatom(s) being selected from oxygen, sulphur or nitrogen; m and n are independently integers of 0 to 3, such that m + n is 0 to 3; and R z and R 8 are independently hydrogen C 1-4 alkyl or phenyl C 1-4 alkyl, R 3 is C 1-4 alkyl optionally substituted by hydroxy or thiol or phenyl C 1-4 alkyl, or together with R 4 is C 3-6 polymethylene, R 4 is hydrogen, C 1-4 alkyl, phenyl C 1-4 alkyl or as defined with R 3 , or together with R 5 is -(CH 2 ) p -where p is an integer from 2 to 6 such that m + p is 3 to 6, R 6 is hydrogen, C 1-4 alkyl or as defined with R 4 , or together with R 6 is -(CH 2 ) q -where q is an integer from 2 to 6 such that n + q is 3 to 6, R 6 is hydrogen, C 1-4 alkyl, phenyl C 1-4 alkyl or as defined with R 5 , or together with R 7 is C 3-6 polymethylene, and R 7 is C 1-4 alkyl optionally substituted by hydroxy or thiol, phenyl C 1-4 alkyl or as defined with R 6 , in which any phenyl moiety in R 2 ,R 3 ,R 4 ,R 6 ,R 7 and R 8 is optionally substituted by one or two of halogen, trifluoromethyl, C 1-4 alkoxy or C 1-4 alkyl. Such compounds have been found to possess cardiovascular activity, in particular calcium antagonistic activity which indicates that they are of potential use in the treatment of angina.
wherein:
R, and R 9 are independently phenyl, phenyl C 1-4 alkyl, phenyl C 2-4 alkenyl or pyridyl, the aromatic moiety optionally substituted by one, two or three of halogen, trifluoromethyl, C 1-4 alkoxy, C 1-4 alkyl, cyano, hydroxy, nitro, NR 10 R 11 or O 2 SNR 10 R 11 wherein R, o and R 11 are independently hydrogen or C 1-6 alkyl or together are C 3-6 polymethylene, or disubstituted at adjacent carbon atoms by C 1-2 alkylenedioxy; C 3-8 cycloalkyl; or aliphatic heterocyclyl having up to six ring atoms the heteroatom(s) being selected from oxygen, sulphur or nitrogen; m and n are independently integers of 0 to 3, such that m + n is 0 to 3; and R z and R 8 are independently hydrogen C 1-4 alkyl or phenyl C 1-4 alkyl, R 3 is C 1-4 alkyl optionally substituted by hydroxy or thiol or phenyl C 1-4 alkyl, or together with R 4 is C 3-6 polymethylene, R 4 is hydrogen, C 1-4 alkyl, phenyl C 1-4 alkyl or as defined with R 3 , or together with R 5 is -(CH 2 ) p -where p is an integer from 2 to 6 such that m + p is 3 to 6, R 6 is hydrogen, C 1-4 alkyl or as defined with R 4 , or together with R 6 is -(CH 2 ) q -where q is an integer from 2 to 6 such that n + q is 3 to 6, R 6 is hydrogen, C 1-4 alkyl, phenyl C 1-4 alkyl or as defined with R 5 , or together with R 7 is C 3-6 polymethylene, and R 7 is C 1-4 alkyl optionally substituted by hydroxy or thiol, phenyl C 1-4 alkyl or as defined with R 6 , in which any phenyl moiety in R 2 ,R 3 ,R 4 ,R 6 ,R 7 and R 8 is optionally substituted by one or two of halogen, trifluoromethyl, C 1-4 alkoxy or C 1-4 alkyl. Such compounds have been found to possess cardiovascular activity, in particular calcium antagonistic activity which indicates that they are of potential use in the treatment of angina.
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