发明名称 ARYL NAPHTHALIDE LIGNANS AS ANTI-HIV AGENTS
摘要 Provided herein are glycosidic aryl naphthalide lignans compounds, such as justiprocumin A isolated from the plant Justicia gendarussa Burm f. (Acanthaceae), which are effective in the treatment of AIDS and HIV infections.
申请公布号 US2014357584(A1) 申请公布日期 2014.12.04
申请号 US201214235870 申请日期 2012.07.27
申请人 THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS 发明人 Zhang Hongjie;Soejarto Djaja;Rong Lijun;Fong Harry H.S.;Rumschlag-Booms Emily
分类号 C07H17/04 主分类号 C07H17/04
代理机构 代理人
主权项 1. A method of treating, preventing or delaying the progression of a HIV infection in a patient, comprising administering a therapeutically effective amount of a compound having the formula (I) or (II): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are each independently hydrogen, halogen or a moiety comprising 1 to 30 plural valence atoms selected from carbon, nitrogen, oxygen and sulphur, or R2 and R3, R3 and R4, R4 and R5, R6 and R7, R7 and R8, R8 and R9 or R9 and R10 may be taken together with the carbon atoms to which they are attached to form a cyclic group which is optionally substituted with halogen or a moiety comprising 1 to 30 plural valence atoms selected from carbon, nitrogen, oxygen and sulphur, or at least one of R1, R2, R3, R5, R6, R7, R8, R9 and R10 or a said cyclic group comprises a glycosidic group; R11 and R12 may be taken together to form oxo; or while one of R11 and R12 is hydrogen or halogen, the other one of R11 and R12 is selected from R15, —OR15, —C(O)R15 and —C(O)OR15; R13 and R14 may be taken together to form oxo; or while one of R13 and R14 is hydrogen or halogen, the other one of R13 and R14 is selected from R15, —OR15, —C(O)R5 and —C(O)OR15; R15 is independently selected from hydrogen, halogen, trifluoromethyl, cyano, nitro, hydrocarbyl optionally substituted with 1, 2, 3, 4 or 5 R16, —(CH2)k-heterocyclyl optionally substituted with 1, 2, 3, 4 or 5 R16, —OR17, —C(O)R18, —C(O)N(R17)R18, —C(O)OR17, —OC(O)R17, —S(O)2R17, —S(O)2N(R17)R18, —N(R17)R18, —N(R17)N(R17)R18, —N(R17)C(O)R18 and —N(R17)S(O)2R18; R16 is independently selected from halogen, trifluoromethyl, cyano, nitro, oxo, ═NR17, —OR17, —C(O)R18, —C(O)N(R17)R18, —C(O)OR17, —OC(O)R17, —S(O)2R17, —S(O)2N(R17)R18, —N(R17)R18, —N(R17)N(R17)R18, —N(R17)C(O)R18 and —N(R17)S(O)2R18; R17 and R18 are each independently hydrogen or selected from hydrocarbyl and —(CH2)k-heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from halogen, cyano, amino, hydroxy, C1-6 alkyl and C1-6 alkoxy; wherein k is an integer between 1 and 6; X is nitrogen, oxygen or sulphur; R is hydrogen or selected from hydrocarbyl and —(CH2)k-heterocyclyl, either of which is optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from halogen, cyano, amino, hydroxy, C1-6 alkyl and Ct alkoxy; wherein k is an integer between 1 and 6; or a pharmaceutically acceptable salt or prodrug thereof; while R1, R2, R5, R6, R9, R10, R11 and R12 are each independently hydrogen, X is oxygen, and R13 and R14 taken together to form oxo, R3, R4, R7 and R8 each should not be OCH3; while R1, R2, R5, R6, R9, R10, R11 and R12 are each independently hydrogen, X is oxygen, and R13 and R14 taken together to form oxo, R3, R4, R7 and R8 each should not be OH; while R1, R2, R5, R8, R9, R10, R11 and R12 are each independently hydrogen, X is oxygen, and R13 and R14 taken together to form oxo, R3 and R4 or R7 and R8 taken together with the carbon atoms to which they are attached should not form a [1,3]dioxolo group; while R1, R2, R5, R6, R9, R10, R11, R12, R13 and R14 are each independently hydrogen, and R3, R4, R7 and R8 are each independently OCH3, R should not be CH3, CH2CH2CH3, CH(CH3)CH3 or CH2CH2CH2CH3.
地址 Urbana IL US