发明公开
- 专利标题: Isatine derivatives, their preparation and use
- 专利标题(中): ISATINE衍生物,其制备和使用
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申请号: EP90123474.0申请日: 1990-12-06
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公开(公告)号: EP0432648A3公开(公告)日: 1991-09-25
- 发明人: Wätjen, Frank , Drejer, Jorgen , Jensen, Leif Helth
- 申请人: NEUROSEARCH A/S
- 申请人地址: Smedeland 26 DK-2600 Glostrup DK
- 专利权人: NEUROSEARCH A/S
- 当前专利权人: NEUROSEARCH A/S
- 当前专利权人地址: Smedeland 26 DK-2600 Glostrup DK
- 代理机构: Grünecker, Kinkeldey, Stockmair & Schwanhäusser Anwaltssozietät
- 优先权: DK6248/89 19891211; DK6470/89 19891219; DK85/90 19900112; DK86/90 19900112; DK363/90 19900212; DK2093/90 19900831
- 主分类号: C07D209/40
- IPC分类号: C07D209/40 ; A61K31/40
摘要:
A method of treatment with compounds having the formula
wherein
R¹ is hydrogen, C₁₋₆-alkyl which may be branched, C₃₋₇-cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C₁₋₆-alkoxy, CH₂CO₂R' wherein R' is hydrogen or C₁₋₆-alkyl which may be branched, CH₂CN, CH₂CONR IV R V wherein R IV and R V independently are hydrogen or C₁₋₆-alkyl, or CH₂C(=NOH)NH₂;
R² is hydrogen, benzyl, C₁₋₆-alkyl which may be branched, or C₃₋₇-cycloalkyl;
R⁴, R⁵, R⁶, R⁷ independently are hydrogen, C₁₋₆-alkyl which may be branched, phenyl, halogen, C₁₋₆-alkoxy, NO₂, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, or CF₃; or R⁶ and R⁷ together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO₂, CF₃, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, and R⁴ and R⁵ have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel. The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.
wherein
R¹ is hydrogen, C₁₋₆-alkyl which may be branched, C₃₋₇-cycloalkyl, benzyl, phenyl which may be substituted, acyl, hydroxy, C₁₋₆-alkoxy, CH₂CO₂R' wherein R' is hydrogen or C₁₋₆-alkyl which may be branched, CH₂CN, CH₂CONR IV R V wherein R IV and R V independently are hydrogen or C₁₋₆-alkyl, or CH₂C(=NOH)NH₂;
R² is hydrogen, benzyl, C₁₋₆-alkyl which may be branched, or C₃₋₇-cycloalkyl;
R⁴, R⁵, R⁶, R⁷ independently are hydrogen, C₁₋₆-alkyl which may be branched, phenyl, halogen, C₁₋₆-alkoxy, NO₂, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, or CF₃; or R⁶ and R⁷ together form an additional 4 to 7 membered ring which may be aromatic or partial saturated and which may be substituted with halogen, NO₂, CF₃, CN, SO₂NR''R''' wherein R'' and R''' independently are hydrogen or C₁₋₆-alkyl, and R⁴ and R⁵ have the meanings set forth above, are disclosed, as well as pharmaceutical compositions thereof. Certain of the compounds are novel. The compounds and pharmaceutical compositions containing the compounds are useful in the treatment of central nervous system disorders and especially conditions sensitive to excitatory amino acids.
公开/授权文献
- EP0432648B1 Isatine derivatives, their preparation and use 公开/授权日:1995-08-02
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