申请人:AMERICAN HOME PRODUCTS CORPORATION
公开号:EP0213935A2
公开(公告)日:1987-03-11
The invention disclosed herein relates to a method of treating an animal infected by hepatitis B virus by administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of
(a) 3-amino-O-deoxo-4-imino-rifamycin S,
(b) 3-amino-4-deoxo-4- [(4-aminophenyl) sulphonyl] -amino-rifamycin SV,
(c)4-O-n-butylsulphonyl-3- [(1-piperidinylimino)methyl] -rifamycin SV,
(d) 4-O-n-butylsulphonyl-3- [(4-morpholinylimino) methyl] rifamycin SV,
(e) 3-[(dimethylhydrazono) methyl]-4-O-[(3-phenylpropyl) sulphonyll-rifamycin SV and
(f) 4-deoxy-N,3-ethylidenimino-4- (methylsulphonyll- amino- rifamycin SV
said amount being effective to alleviate the effects of said hepatitis B virus. The invention particularly relates to the use of the above mentioned rifamycin derivatives for the manufacture of a medicament for treating or preventing hepatitis. Also disclosed is a method of inhibiting the viral polymerase of hepatitis B virus by subjecting said polymerase to an amount of one of the rifamycin derivatives (a) - (f) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase. Compounds (b) to (f) described above are novel compounds.
本发明涉及一种治疗受乙型肝炎病毒感染的动物的方法,该方法是向受感染的动物施用一定量的利福霉素衍生物,该衍生物选自以下组别
(a) 3-氨基-O-脱氧-4-亚氨基-利福霉素 S
(b) 3-氨基-4-脱氧-4-[(4-氨基苯基)磺酰基]-氨基-利福霉素 SV、
(c) 4-O-正丁基磺酰基-3-[(1-哌啶亚氨基)甲基]-利福霉素 SV、
(d) 4-O-正丁基磺酰基-3-[(4-吗啉基亚胺基)甲基]利福霉素 SV、
(e) 3-[(二甲基肼)甲基]-4-O-[(3-苯基丙基)磺酰-利福霉素 SV 和
(f) 4-脱氧-N,3-亚乙基亚氨基-4-甲磺酰氨基-利福霉素 SV
所述用量能有效减轻所述乙型肝炎病毒的影响。本发明特别涉及使用上述利福霉素衍生物制造治疗或预防肝炎的药物。本发明还公开了一种抑制乙型肝炎病毒聚合酶的方法,该方法是将上述聚合酶置于一定量的上述(a)至(f)的利福霉素衍生物中,所述量可有效阻止上述病毒聚合酶合成乙型肝炎病毒。上述化合物(b)至(f)为新型化合物。