发明公开
- 专利标题： Benzodiazepines
- 专利标题（中）： 苯二氮。
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申请号： EP91114730.4申请日： 1991-09-02
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公开(公告)号： EP0475231A1公开(公告)日： 1992-03-18
- 发明人: Bellemin, Anne Roberte , Hsu, Ming-Chu , Keith, Dennis Dalton , Sim, Iain Stuart , Tam, Steve Yik-Kai
- 申请人： F. HOFFMANN-LA ROCHE AG
- 申请人地址： Postfach 3255 CH-4002 Basel CH
- 专利权人： F. HOFFMANN-LA ROCHE AG
- 当前专利权人： F. HOFFMANN-LA ROCHE AG
- 当前专利权人地址： Postfach 3255 CH-4002 Basel CH
- 代理机构： Mahé, Jean
- 优先权： US579526 19900910
- 主分类号： C07D403/04
- IPC分类号： C07D403/04 ; A61K31/55
摘要：
Benzodiazepines of formula
wherein
X is N(R,R¹), OR⁴ or SR⁵,
R and R¹ are N(R²,R³) or substituted lower alkyl or an optionally substituted C₃-C₇-cycloalkyl, aryl, aralkyl or C₂-C₆-aliphatic hydrocarbon group, this aliphatic group having one or more double or triple bond, or one of R and R¹ is hydrogen, or
N(R,R¹) is an optionally substitued heterocycle with one or more heteroatoms,
R² and R³ are H, lower alkyl, aryl or aralkyl,
R⁴ is lower alkyl or has one of the meanings of R or R¹ with the exception of H and of N(R²,R³),
R⁵ is H or lower alkyl or has one of the meanings of R or R¹ with the exception of N(R²,R³),
Y and Z are H, NO₂, N(R²,R³), halogen, CF₃, OH, CN or lower alkyl or alkoxy, and
A, B and C are H, CH₃, C₂H₅, F or Cl,
and pharmaceutically acceptable salts thereof are useful as medicaments especially for the treatment or prophylaxis of viral infections, particularly of retroviral infections, such as HIV 1 and/or HIV 2 infections, or for protecting cells against such infections.
wherein
X is N(R,R¹), OR⁴ or SR⁵,
R and R¹ are N(R²,R³) or substituted lower alkyl or an optionally substituted C₃-C₇-cycloalkyl, aryl, aralkyl or C₂-C₆-aliphatic hydrocarbon group, this aliphatic group having one or more double or triple bond, or one of R and R¹ is hydrogen, or
N(R,R¹) is an optionally substitued heterocycle with one or more heteroatoms,
R² and R³ are H, lower alkyl, aryl or aralkyl,
R⁴ is lower alkyl or has one of the meanings of R or R¹ with the exception of H and of N(R²,R³),
R⁵ is H or lower alkyl or has one of the meanings of R or R¹ with the exception of N(R²,R³),
Y and Z are H, NO₂, N(R²,R³), halogen, CF₃, OH, CN or lower alkyl or alkoxy, and
A, B and C are H, CH₃, C₂H₅, F or Cl,
and pharmaceutically acceptable salts thereof are useful as medicaments especially for the treatment or prophylaxis of viral infections, particularly of retroviral infections, such as HIV 1 and/or HIV 2 infections, or for protecting cells against such infections.
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