公开(公告)号：EP0475231A1

公开(公告)日：1992-03-18

申请号：EP91114730.4

申请日：1991-09-02

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Bellemin, Anne Roberte ,  Hsu, Ming-Chu ,  Keith, Dennis Dalton ,  Sim, Iain Stuart ,  Tam, Steve Yik-Kai

IPC分类号： C07D403/04 ,  A61K31/55

CPC分类号： C07D403/04

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.

摘要翻译： 其中X为N（R，R 1），OR 4或SR 5的式CHEM的苯并二氮杂，R和R 1为N（R 2，R 3）或取代的 低级烷基或任选取代的C 3 -C 7 - 环烷基，芳基，芳烷基或C 2 -C 6脂族烃基，该具有一个或多个双键或三键的脂族基团，或R和R 1之一是氢或N （R 1，R 1）是具有一个或多个杂原子的任选取代的杂环，R 2和R 3是H，低级烷基，芳基或芳烷基，R 4是低级烷基或具有 R或R 1的含义除H和N（R 2，R 3）外，R 5是H或低级烷基或具有R或R 1的含义之一， 除了N（R 2，R 3），Y和Z是H，NO 2，N（R 2，R 3），卤素，CF 3，OH，CN或低级烷基或烷氧基 A，B和C是H，CH 3，C 2 H 5，F或Cl，及其药学上可接受的盐可用作特别用于治疗或预防病毒感染，特别是HIV 1和/或HIV的逆转录病毒感染的药物 2感染 或用于保护细胞免受这种感染。

公开(公告)号：EP0462522A1

公开(公告)日：1991-12-27

申请号：EP91109785.5

申请日：1991-06-14

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Bellemin, Anne Roberte ,  Earley, James Valentine ,  Hsu, Ming-Chu ,  Tam, Steve Yik-Kai

IPC分类号： C07D403/04 ,  A61K31/55

CPC分类号： C07D403/04

摘要： Aminobenzodiazepines of formula

   wherein R¹ is H, NO₂, halogen, CF₃, lower alkyl, OH, lower alkoxy or CN, and R² is H or CH₃,
   and pharmaceutically acceptable salts thereof possess antiviral activity 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.
They can be prepared from corresponding benzodiazepinethiones.

摘要翻译： 式中R 1为H，NO 2，卤素，CF 3，低级烷基，OH，低级烷氧基或CN，且R 2为H或CH 3的氨基苯并二氮杂and及其药学上可接受的盐具有抗病毒活性，特别是用于治疗或预防病毒感染，特别是 逆转录病毒感染，如HIV 1和/或HIV 2感染，或用于保护细胞免受这种感染。 它们可以由相应的苯并二氮杂硫酮制备。