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1. 发明授权

US06242461B1 Use of aryl substituted azabenzimidazoles in the treatment of HIV and AIDS related diseases 失效
标题翻译：芳基取代的氮杂苯并咪唑在治疗艾滋病毒和艾滋病相关疾病中的应用
公开(公告)号：US06242461B1
公开(公告)日：2001-06-05
申请号：US09578655
申请日：2000-05-25
申请人： Steven W. Goldstein , William G. Stirtan , Brian A. Sherer
发明人： Steven W. Goldstein , William G. Stirtan , Brian A. Sherer
IPC分类号： A61K31435
CPC分类号： A61K31/444 , A61K31/437 , A61K45/06
摘要： This invention relates to novel aryl substituted azabenzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof wherein n is an integer from 1 to 4 X is CH or N; R1 is H, (C1-C6)alkyl or (C1-C6) alkoxy; R2 is H, (C1-C6)alkyl or (C1-C6) alkoxy; each R3 is independently selected from H, (C1-C6)alkyl (C1-C6) alkyloxy, (C1-C6) alkylthio, halo, nitro, cyano, ethynyl, hydroxy and trifluoromethyl; R4 is H, (C1-C6)alkyl or (C1-C6) alkoxy; R5 is H, (C1-C6)alkyl or (C1-C6) alkyloxy, trifluoromethyl; and W is N or C; Y is N (R4), N, S or O Z is R4, NR4H, O, or OH; Provided that when Y═NR4, W═C, Z═O, there is a single bond between YW and a double bond between WZ; and when Y=O or S, W═C, Z═O, there is a single bond between YW and a double bond between WZ; and when Y═N, W═N, there is a double bond between YW and Z does not exist. when Y═N, W═C, Z═R4 or NHR4, there is a double bond between YW and a single bond between WZ; The methods of preparing these compounds and their use in the treatment of HIV, AIDS, and AIDS related diseases and in slowing the progression of HIV infection into AIDS is also disclosed.
摘要翻译：本发明涉及式（I）的新的芳基取代的氮杂苯并咪唑及其药学上可接受的盐。或其药学上可接受的盐，其中n是1至4X的整数是CH或N; R 1是H，（C 1 -C 6）烷基或（ C1-C6）烷氧基; R2是H，（C1-C6）烷基或（C1-C6）烷氧基;每个R3独立地选自H，（C1-C6）烷基（C1-C6）烷氧基，（C1-C6） R4是H，（C1-C6）烷基或（C1-C6）烷氧基; R5是H，（C1-C6）烷基或（C1-C6）烷氧基，三氟甲基并且W为N或C; Y为N（R4），N，S或OZ为R4，NR4H，O或OH;条件是当Y = NR4时，W = C，Z = O，YW 和WZ之间的双键; 当Y = O或S时，W = C，Z = O，WW之间的YW与双键之间存在单键; 当Y = N，W = N时，YW和Z之间不存在双键。当Y = N，W = C，Z = R4或NHR4时，YW与WZ之间的单键存在双键 ; 还公开了制备这些化合物及其用于治疗艾滋病毒，艾滋病和艾滋病相关疾病以及将艾滋病毒感染进一步减缓为艾滋病的方法。

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