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1.发明公开Indoles as inhibitors of HIV reverse transcriptase 失效Indole zur Inhibierung von HIV-reverse-Transkriptase。
公开(公告)号：EP0678508A1
公开(公告)日：1995-10-25
申请号：EP95201691.3
申请日：1992-08-29
申请人： MERCK & CO. INC.
发明人： Williams, Theresa M. , Ciccarone, Terrence M. , Saari, Walfred S. , Wai, John S. , Greenlee, William J. , Balani, Suresh K. , Goldman, Mark E., Signal Phamaceuticals , Theoharides, Anthony D.
IPC分类号： C07D209/42 , C07D209/30 , C07D401/12 , C07D405/12 , C07D403/12 , C07D401/06 , C07D405/06 , C07D413/06 , A61K31/40 , A61K31/44 , A61K31/41
CPC分类号： C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06
摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。
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公开(公告)号：EP0292256A3
公开(公告)日：1990-10-03
申请号：EP88304492.7
申请日：1988-05-18
申请人： Merck & Co., Inc.
摘要： Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with α-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.
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3.发明公开Indoles as inhibitors of HIV reverse transcriptase 失效Indole zur Inhibierung von HIV-Reverse-Transkriptase。
公开(公告)号：EP0530907A1
公开(公告)日：1993-03-10
申请号：EP92202628.1
申请日：1992-08-29
申请人： MERCK & CO. INC.
发明人： Williams, Theresa M. , Ciccarone, Terrence M. , Saari, Walfred S. , Wai, John S. , Greenlee, William J. , Balani, Suresh K. , Goldman, Mark E. , Theoharides, Anthony D.
IPC分类号： C07D209/42 , C07D209/30 , C07D401/12 , C07D405/12 , C07D403/12 , C07D401/06 , C07D405/06 , C07D413/06 , A61K31/40 , A61K31/44 , A61K31/41
CPC分类号： C07D231/12 , C07D209/12 , C07D209/30 , C07D209/42 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/06
摘要： Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 新型吲哚化合物抑制HIV逆转录酶，可用于预防或治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合，抗感染药物 ，免疫调节剂，抗生素或疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。
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公开(公告)号：EP0292256A2
公开(公告)日：1988-11-23
申请号：EP88304492.7
申请日：1988-05-18
申请人： Merck & Co., Inc.
摘要： Analogs of the 17-membered ring portion of ANF wherein the cysteine moiety is replaced with dipeptidyl moieties, specifically, Phe-Pro, NMP-Pro, Pro-Pro, Val-Pro, Lys-Pro, Ile-Pro, Arg-Pro, HAr-Pro, Dly-Pro, Arg-Pro, Lys-BAr, Arg-Pro, CyA-CyA, Cys-Cys, or with α-aminoheptanoic acid result in analogs of ANF having increased potencies and metabolic stability.
摘要翻译： ANF的17-元环部分的类似物，其中半胱氨酸部分被二肽部分，特别是Phe-Pro，NMP-Pro，Pro-Pro，Val-Pro，Lys-Pro，Ile-Pro，Arg-Pro， HAr-Pro，Dly-Pro，Arg-Pro，Lys-BAr，Arg-Pro，CyA-CyA，Cys-Cys或与α-氨基庚酸导致ANF的类似物具有增加的效力和代谢稳定性。
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