专利号:US-4743619-A 优先权日:1985-08-29 标 题 :Method of treating hepatitis 发明人:HUNG PAUL P 权利人:AMERICAN HOME PROD 摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-deoxo-4-imino-rifamycin S, (b) 3-amino-4-deoxo-4-[(4-aminophenyl)sulfonyl]amino-rifamycin SV, (c) 4-O-(n-butylsulfonyl)-3-[(1-piperidinylimino)methyl]-rifamycin SV, (d) 4-O-(n-butylsulfonyl)-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV, and (f) 4-deoxo-N,3-ethylidenimino-4-(methylsulfonyl)amino-rifamycin SV, said amount being effective to alleviate the effects of said hepatitis B virus. 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)-(f) described above are novel compounds.
专利号:US-4631290-A 优先权日:1985-08-29 标 题 :Method of treating hepatitis 发明人:HUNG PAUL P 权利人:AMERICAN HOME PROD 摘要:The invention disclosed herein provides a method of treating an animal infected by hepatitis B virus comprising administering to such infected animal an amount of a rifamycin derivative selected from a group consisting of (a) 3-amino-4-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-butylsulfonyl-3-[(4-morpholinylimino)methyl]-rifamycin SV, (e) 3-[(dimethylhydrazono)methyl]-4-O-[(3-phenylpropyl)sulfonyl]-rifamycin SV said amount being effective to alleviate the effects of said hepatitis B virus. 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)-(e) above, said amount being effective to prevent the synthesis of hepatitis B virus by said viral polymerase.
参考文献:10.1021/acs.orglett.6b03619 摘要:Williams DE, Dalisay DS, Chen J, Polishchuck EA, Patrick BO, Narula G, Ko M, Av-Gay Y, Li H, Magarvey N, Andersen RJ. Aminorifamycins and Sporalactams Produced in Culture by a Micromonospora sp. Isolated from a Northeastern-Pacific Marine Sediment Are Potent Antibiotics. Org Lett. 2017 Feb 17;19(4):766–9. doi: 10.1021/acs.orglett.6b03619.