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公开(公告)号：US5510375A
公开(公告)日：1996-04-23
申请号：US155728
申请日：1993-11-19
IPC分类号： C07D311/56 , A61K31/35
CPC分类号： C07D311/56
摘要： The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.
摘要翻译： 本发明涉及有效抑制HIV天冬氨酰蛋白酶阻断HIV感染性的新型香豆素衍生物和相关化合物。 香豆素衍生物可用于开发用于治疗病毒感染和疾病（包括AIDS）的治疗。 本发明还涉及多功能香豆素的合成方法和相关结构。
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公开(公告)号：US5081254A
公开(公告)日：1992-01-14
申请号：US538858
申请日：1990-06-15
IPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
CPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
摘要： A novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.
摘要翻译： 描述了可用作抗菌剂的新一系列喹啉，萘啶和苯并恶嗪羧酸。 还描述了制备化合物以及新型中间体的新方法，它们的制备方法及其在治疗细菌感染中的用途。
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公开(公告)号：US4920120A
公开(公告)日：1990-04-24
申请号：US280924
申请日：1988-12-09
申请人： John M. Domagala , Susan E. Hagen , John S. Kiely
发明人： John M. Domagala , Susan E. Hagen , John S. Kiely
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/46 , A61K31/47 , A61K31/495 , A61P31/04 , C07C51/00 , C07C51/06 , C07C51/363 , C07C63/70 , C07D215/56 , C07D263/10 , C07D401/04 , C07D403/04 , C07D451/02 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07D519/00 , C07F7/08
CPC分类号： C07D263/10 , C07D215/56 , C07D401/04 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07F7/0812
摘要： Novel naphthyridine-, and quinolinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
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公开(公告)号：US4840956A
公开(公告)日：1989-06-20
申请号：US144301
申请日：1988-01-14
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Disubstituted 7-pyrrolidinoquinoline- and -napthylridine-3-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.
摘要翻译： 描述作为抗菌剂的二取代的7-吡咯烷基喹啉 - 和 - 萘基-3-羧酸以及其制备，配制和用于治疗细菌感染的方法。
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5.发明授权7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-quinoline-carboxylic acids 失效7 - [[3-（氨基甲基）-3-烷基] -1-吡咯烷基] - 喹啉羧酸
公开(公告)号：US4771055A
公开(公告)日：1988-09-13
申请号：US39438
申请日：1987-04-21
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , A61P35/00 , C07D207/09 , C07D401/04 , C07D471/04 , C07D215/56
CPC分类号： C07D401/04 , C07D471/04
摘要： Novel, orally active antibacterial agents are described and characterized as 7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acids or corresponding 1,8-naphthyridine derivatives as well as methods for their manufacture.
摘要翻译： 描述了新型口服活性抗菌剂，并将其表征为7 - [[3-（氨基甲基）-3-烷基] -1-吡咯烷基] -6-氟-1,4-二氢-4-氧-3-喹啉羧酸 酸或相应的1,8-萘啶衍生物及其制备方法。
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公开(公告)号：US5585491A
公开(公告)日：1996-12-17
申请号：US527199
申请日：1995-09-12
申请人： John M. Domagala , Susan E. Hagen , John S. Kiely
发明人： John M. Domagala , Susan E. Hagen , John S. Kiely
IPC分类号： C07C63/70 , C07D215/56 , C07D263/10 , C07D401/04 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07D519/00 , C07F7/08 , A61K31/435 , C07D471/02
CPC分类号： C07D263/10 , C07D215/56 , C07D401/04 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07F7/0812
摘要： Novel naphthyridine-, and quinolinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
摘要翻译： 描述了新的萘啶和喹啉羧酸作为抗菌剂，以及用于制备，配制和用于治疗细菌感染的方法，包括描述用于制造抗菌剂的某些新型中间体。
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公开(公告)号：US4929613A
公开(公告)日：1990-05-29
申请号：US222608
申请日：1988-07-25
IPC分类号： A61K31/47 , A61P31/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/18 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04 , C07D405/02
CPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
摘要： The novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.
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8.发明授权4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivative as antibacterial agents 失效4-氧代-1,4-二氢喹啉-3-羧酸衍生物作为抗菌剂
公开(公告)号：US4822801A
公开(公告)日：1989-04-18
申请号：US920536
申请日：1986-10-20
IPC分类号： C07D215/56 , A61K31/435 , A61K31/47 , A61K31/535 , A61K31/5383 , A61P31/04 , C07D401/04 , C07D471/04 , C07D487/10 , C07D498/04 , C07D498/06 , C07D519/00 , C07D401/02
CPC分类号： C07D401/04 , C07D471/04 , C07D487/10
摘要： Novel naphthyridine-, quinoline- and benzoxazinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
摘要翻译： 描述了作为抗菌剂的新型萘啶，喹啉和苯并恶嗪羧酸以及其制备，配制和用于治疗细菌感染的方法，包括用于制备抗菌剂的某些新型中间体的描述。
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公开(公告)号：US4771054A
公开(公告)日：1988-09-13
申请号：US896917
申请日：1986-08-15
IPC分类号： C07C45/00 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06 , C07D498/06 , C07D519/00 , A61K31/495
CPC分类号： C07D207/08 , C07C205/45 , C07C45/00 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06
摘要： Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
摘要翻译： 描述了新的喹啉羧酸作为抗菌剂，以及其制备，配制和用于治疗细菌感染的方法，包括描述用于制造抗菌剂的某些新型中间体。
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公开(公告)号：US4578473A
公开(公告)日：1986-03-25
申请号：US723019
申请日：1985-04-15
申请人： John M. Domagala , Mel C. Schroeder
发明人： John M. Domagala , Mel C. Schroeder
IPC分类号： A61K31/47 , A61P31/04 , C07D215/56 , C07D401/04 , C07D471/08 , C07D487/08 , C07D487/10 , C07D215/22
CPC分类号： C07D401/04 , C07D471/08 , C07D487/08 , C07D487/10
摘要： An improved process for the preparation of 7-substituted amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where an alkyl ester of a 6,7,8-trifluoro precursor is converted to a trialkylsilyl ester which fluorine at C.sub.7 is directly displaced to the desired product.
摘要翻译： 描述了制备7-取代的氨基-1-环丙基-6,8-二氟-1,4-二氢-4-氧代-3-喹啉羧酸的改进方法，其中将6,7- 三氟前体转化为三烷基甲硅烷基酯，其中C7的氟直接置换为所需产物。
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