发明公开
EP0223598A2 Catecholamine derivatives, processes for their preparation and pharmaceutical compositions thereof
失效
的儿茶酚胺衍生物,它们的制备方法和它们的药物组合物。
- 专利标题: Catecholamine derivatives, processes for their preparation and pharmaceutical compositions thereof
- 专利标题(中): 的儿茶酚胺衍生物,它们的制备方法和它们的药物组合物。
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申请号: EP86309004.9申请日: 1986-11-18
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公开(公告)号: EP0223598A2公开(公告)日: 1987-05-27
- 发明人: Dixon, John , Ince, Francis , Springthorpe, Brian
- 申请人: FISONS plc
- 申请人地址: Fison House Princes Street Ipswich Suffolk IP1 1QH GB
- 专利权人: FISONS plc
- 当前专利权人: FISONS plc
- 当前专利权人地址: Fison House Princes Street Ipswich Suffolk IP1 1QH GB
- 代理机构: Craig, Christopher Bradberry
- 优先权: GB8528605 19851120; GB8616792 19860710; GB8616793 19860710; GB8616794 19860710
- 主分类号: C07C215/52
- IPC分类号: C07C215/52 ; C07D213/38 ; C07C317/02 ; C07C409/44 ; A61K31/135 ; A61K31/44
摘要:
There are described compounds of formula I,
in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O) n , wherein n is 0, 1 or 2;
Y represents O or NH,
l and m each independently represent 2, 3 or 4,
R₁₀ represents phenyl substituted by one or more substituents R₂₃, which may be the same or different; or R₁₀ represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,
R₁₅ represents hydrogen or together with R₂₃ forms a (CH₂) p chain, wherein p represents 0, 1 or 2;
R₂₀, R₂₁, R₂₂ and R₂₃, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR₂₅, SH, NO₂, halogen, CF₃, SO₂R₃₀, CH₂OH or OH, wherein R₂₅, represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO₂ alkyl C 1 to 6, and R₃₀ represents alkyl C 1 to 6 or NH₂,
provided that when X represents an uninterrupted C4 alkylene chain, Y represents NH, m represents 2, l represents 2, R₁₀ represents phenyl, R₁₅ represents hydrogen, and R₂₁, R₂₂ and R₂₃ represent hydrogen, then R₂₀ does not represent hydrogen or 4-OH,
and pharmaceutically acceptable salts and solvates thereof.
There are also described processes for the preparation of the compounds of formula I and pharmaceutical compositions containing them. The compounds of the invention may be used in the treatment or prophylaxis of renal failure or cardiovascular disorders.
in which X represents a C2 to 8 alkylene chain optionally interrupted by a double bond or by S(O) n , wherein n is 0, 1 or 2;
Y represents O or NH,
l and m each independently represent 2, 3 or 4,
R₁₀ represents phenyl substituted by one or more substituents R₂₃, which may be the same or different; or R₁₀ represents pyridyl, a saturated carbocyclic group, alkyl C 1 to 6 or hydrogen,
R₁₅ represents hydrogen or together with R₂₃ forms a (CH₂) p chain, wherein p represents 0, 1 or 2;
R₂₀, R₂₁, R₂₂ and R₂₃, which may be the same or different, independently represent hydrogen, alkyl C 1 to 6, NHR₂₅, SH, NO₂, halogen, CF₃, SO₂R₃₀, CH₂OH or OH, wherein R₂₅, represents hydrogen, alkyl C 1 to 6, alkanoyl C 1 to 6 or SO₂ alkyl C 1 to 6, and R₃₀ represents alkyl C 1 to 6 or NH₂,
provided that when X represents an uninterrupted C4 alkylene chain, Y represents NH, m represents 2, l represents 2, R₁₀ represents phenyl, R₁₅ represents hydrogen, and R₂₁, R₂₂ and R₂₃ represent hydrogen, then R₂₀ does not represent hydrogen or 4-OH,
and pharmaceutically acceptable salts and solvates thereof.
There are also described processes for the preparation of the compounds of formula I and pharmaceutical compositions containing them. The compounds of the invention may be used in the treatment or prophylaxis of renal failure or cardiovascular disorders.
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