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公开(公告)号：EP0535730A2
公开(公告)日：1993-04-07
申请号：EP92202923.6
申请日：1992-09-23
申请人： MERCK & CO. INC.
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/0808
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制法呢基蛋白转移酶（FTase）和癌基因蛋白Ras的法呢基化的化合物。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶和癌基因蛋白Ras的法呢基化的方法。
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公开(公告)号：EP0356223A3
公开(公告)日：1991-08-21
申请号：EP89308555.5
申请日：1989-08-23
申请人： MERCK & CO. INC.
发明人： Desolms, S. Jane , Huff, Joel R. , Vacca, Joseph P. , Sigal, Irving S. , Darke, Paul L. , Young, Steven D.
IPC分类号： C07K5/02 , C07C125/065 , C07C143/74 , C07C153/057 , C07D213/40 , C07H13/04 , C07F9/28 , C07F9/09 , A61K37/64 , A61K31/16 , A61K31/395
CPC分类号： C07D295/185 , C07C237/22 , C07C271/22 , C07C307/06 , C07C311/05 , C07C311/06 , C07C2602/08 , C07D307/33 , C07K5/0207 , Y02P20/55
摘要： A-G-B-B-J wherein A is an amine protecting group not useful or commonly employed in peptide synthesis, G a dipeptide isostere, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of HIV protease, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译： 形式为A-G-B-B-J的化合物，其中A是肽合成中无用或通常使用的胺保护基，G二肽等排物，B为氨基酸或其类似物，J为小端基。 这些化合物可用于抑制HIV蛋白酶，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，免疫调节剂，抗生素或其他抗生素组合使用 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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3.发明公开HIV protease inhibitors useful for the treatment of aids 失效HIV-Protease-Inhibitoren zur Behandlung von AIDS。
公开(公告)号：EP0337714A2
公开(公告)日：1989-10-18
申请号：EP89303539.4
申请日：1989-04-11
申请人： MERCK & CO. INC.
发明人： Sigal, Irving S. , Huff, Joel R. , Darke, Paul L. , Vacca, Joseph P. , Young, Steven D. , Desolms, S. Jane , Thompson, Wayne J. , Lyle, Terry A. , Graham, Samuel L. , Ghosh, Arun K.
IPC分类号： C07K5/02 , C07C125/065 , C07C143/74 , C07C153/057 , C07D213/40 , C07H13/04 , C07F9/28 , C07F9/09 , A61K37/64 , A61K31/16 , A61K31/395
CPC分类号： C07D401/12 , C07C271/22 , C07C311/03 , C07C2601/08 , C07C2602/08 , C07D235/24 , C07D311/68 , C07F9/091 , C07F9/301 , C07H13/04 , C07H15/04 , C07K5/0205 , C07K5/0207 , C07K5/0227 , Y02P20/55
摘要： Compounds of the form
wherein A is an amine protecting group commonly employed in peptide synthesis, G a dipeptide isostere, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of HIV protease, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.摘要翻译： 形式A-G-B-B-J的化合物，其中A是通常用于肽合成的胺保护基，G二肽等排物，B是氨基酸或其类似物，J是小端基。 这些化合物可用于抑制HIV蛋白酶，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，免疫调节剂，抗生素或其他抗生素组合使用 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：EP0535730A3
公开(公告)日：1993-08-18
申请号：EP92202923.6
申请日：1992-09-23
申请人： MERCK & CO. INC.
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/0808
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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5.发明公开HIV protease inhibitors useful for the treatment of aids 失效HIV-Protease-Inhibitorenfürdie Behandlung von AIDS。
公开(公告)号：EP0356223A2
公开(公告)日：1990-02-28
申请号：EP89308555.5
申请日：1989-08-23
申请人： MERCK & CO. INC.
发明人： Desolms, S. Jane , Huff, Joel R. , Vacca, Joseph P. , Sigal, Irving S. , Darke, Paul L. , Young, Steven D.
IPC分类号： C07K5/02 , C07C125/065 , C07C143/74 , C07C153/057 , C07D213/40 , C07H13/04 , C07F9/28 , C07F9/09 , A61K37/64 , A61K31/16 , A61K31/395
CPC分类号： C07D295/185 , C07C237/22 , C07C271/22 , C07C307/06 , C07C311/05 , C07C311/06 , C07C2602/08 , C07D307/33 , C07K5/0207 , Y02P20/55
摘要： A-G-B-B-J
wherein A is an amine protecting group not useful or commonly employed in peptide synthesis, G a dipeptide isostere, B an amino acid or analog thereof, and J a small terminal group are described. These compounds are useful in the inhibition of HIV protease, 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, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.摘要翻译： 形式为A-G-B-B-J的化合物，其中A是肽合成中无用或通常使用的胺保护基，G二肽等排物，B为氨基酸或其类似物，J为小端基。 这些化合物可用于抑制HIV蛋白酶，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，免疫调节剂，抗生素或其他抗生素组合使用 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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6.发明公开Benzothiazole-2-sulfonamide derivatives for the topical treatment of elevated intraocular pressure 失效苯并噻唑-2-磺酰胺衍生物为升高的眼内压的局部治疗。
公开(公告)号：EP0122831A2
公开(公告)日：1984-10-24
申请号：EP84400524.9
申请日：1984-03-14
申请人： Merck & Co., Inc.
发明人： Desolms, S. Jane
IPC分类号： C07D277/80 , A61K31/425
CPC分类号： C07D277/70 , C07D277/80 , C07D277/82 , Y10S514/913
摘要： Novel 2-benzothiazolesulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
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公开(公告)号：EP0535731A3
公开(公告)日：1993-08-11
申请号：EP92202924.4
申请日：1992-09-23
申请人： MERCK & CO. INC.
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0207 , C07K5/06078
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号：EP0535731A2
公开(公告)日：1993-04-07
申请号：EP92202924.4
申请日：1992-09-23
申请人： MERCK & CO. INC.
CPC分类号： C07K5/0808 , A61K38/00 , C07K5/0207 , C07K5/06078
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制法呢基蛋白转移酶（FTase）和癌基因蛋白Ras的法呢基化的化合物。 本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶和癌基因蛋白Ras的法呢基化的方法。
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9.发明授权Benzothiazole-2-sulfonamide derivatives for the topical treatment of elevated intraocular pressure 失效用于局部治疗高压内压的苯并噻唑-2-磺酰胺衍生物
公开(公告)号：EP0122831B1
公开(公告)日：1990-04-18
申请号：EP84400524.9
申请日：1984-03-14
申请人： Merck & Co., Inc.
发明人： Desolms, S. Jane
IPC分类号： C07D277/80 , A61K31/425
CPC分类号： C07D277/70 , C07D277/80 , C07D277/82 , Y10S514/913
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10.发明公开Benzothiazole-2-sulfonamide derivatives for the topical treatment of elevated intraocular pressure 失效用于局部治疗高压内压的苯并噻唑-2-磺酰胺衍生物
公开(公告)号：EP0122831A3
公开(公告)日：1987-04-01
申请号：EP84400524
申请日：1984-03-14
申请人： MERCK & CO. INC.
发明人： Desolms, S. Jane
IPC分类号： C07D277/80 , A61K31/425
CPC分类号： C07D277/70 , C07D277/80 , C07D277/82 , Y10S514/913
摘要： Novel 2-benzothiazolesulfonamides are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.
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