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公开(公告)号：US08343912B2
公开(公告)日：2013-01-01
申请号：US12644943
申请日：2009-12-22
申请人： Richard A. Leese
发明人： Richard A. Leese
摘要： Provided herein is an antibacterial compound of the following formula: or a pharmaceutically acceptable salt thereof. The antibacterial compound has antibacterial properties against a diverse range of gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin B. Also provided are antibacterial pharmaceutical compositions containing the antibacterial compound, as well as methods for preparing the antibacterial compound.
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公开(公告)号：US06750199B2
公开(公告)日：2004-06-15
申请号：US09904756
申请日：2001-07-13
IPC分类号： A61K3812
CPC分类号： C07K1/14 , A61K38/00 , C07K7/06 , C07K7/08 , C07K7/56 , C07K7/60 , C07K11/00 , C08L23/08 , C08L23/0869 , C08L51/06 , C08L2203/14 , C09K3/10 , C09K2003/1037 , C09K2200/06 , C09K2200/062 , C09K2200/0622 , C08L2666/04 , C08L2666/02
摘要： The present invention provides antimicrobial sulfonamide derivatives of lipopeptide antibiotics, pharmaceutical compositions of antimicrobial sulfonamide derivatives, methods for making antimicrobial sulfonamide derivatives, methods for inhibiting microbial growth with antimicrobial sulfonamide derivatives and methods for treating or preventing microbial infections in a subject with antimicrobial sulfonamide derivatives. Antimicrobial sulfonamide derivatives are generally an amino core antibiotic that has been further modified with a lipophilic sulfonyl group.
摘要翻译： 本发明提供了脂肽抗生素的抗微生物磺酰胺衍生物，抗微生物磺酰胺衍生物的药物组合物，抗微生物磺酰胺衍生物的制备方法，用抗微生物磺酰胺衍生物抑制微生物生长的方法以及用抗微生物磺酰胺衍生物治疗或预防受试者的微生物感染的方法。 抗微生物磺酰胺衍生物通常是已经用亲脂性磺酰基进一步修饰的氨基核心抗生素。
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公开(公告)号：US08889826B2
公开(公告)日：2014-11-18
申请号：US11630847
申请日：2005-07-01
CPC分类号： C07K5/0815 , A61K38/00 , C07K5/06086 , C07K7/62 , C07K7/64 , Y02A50/473 , Y02P20/55
摘要： Disclosed herein are novel peptides and protected peptides. These compounds can be derived from naturally occurring peptides, such as those selected from colistin, circulin A, polymyxin A, polymyxin B, polymyxin D, octapeptin B, octapeptin C, and [Ile7]polymyxin B1. Also disclosed are pharmaceutical compositions containing the new peptides, as well as methods for preparing the novel peptides and protected peptides.
摘要翻译： 本文公开了新型肽和保护肽。 这些化合物可以衍生自天然存在的肽，例如选自粘菌素，环状蛋白A，多粘菌素A，多粘菌素B，多粘菌素D，八肽蛋白B，八肽蛋白C和[Ile7]多粘菌素B1的肽。 还公开了含有新肽的药物组合物，以及制备新肽和保护肽的方法。
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公开(公告)号：US08415307B1
公开(公告)日：2013-04-09
申请号：US13167495
申请日：2011-06-23
申请人： William V. Curran , Christopher M. Liu , Amy C. D. Bombardier , Richard A. Leese , You Seok Hwang , Blaise S. Lippa , Yanzhi Zhang
发明人： William V. Curran , Christopher M. Liu , Amy C. D. Bombardier , Richard A. Leese , You Seok Hwang , Blaise S. Lippa , Yanzhi Zhang
IPC分类号： A61K38/08
CPC分类号： C07K7/62 , A01N43/713 , A61K38/12 , Y02A50/473 , Y10S930/19
摘要： Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.
摘要翻译： 本文提供了可衍生自多粘菌素（例如多粘菌素A）的新型化合物和新的受保护化合物。该新化合物对多种革兰氏阴性细菌具有抗菌性能，与多粘菌素如多粘菌素A相比具有降低的毒性。还提供 是含有新化合物和新型受保护化合物的抗菌药物组合物，以及制备抗菌化合物和受保护化合物的方法。
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公开(公告)号：US06737403B2
公开(公告)日：2004-05-18
申请号：US09904352
申请日：2001-07-13
申请人： Donald B Borders , William V Curran , Amedeo A Fantini , Noreen D Francis , Howard Jarolmen , Richard A Leese
发明人： Donald B Borders , William V Curran , Amedeo A Fantini , Noreen D Francis , Howard Jarolmen , Richard A Leese
IPC分类号： A61K3812
CPC分类号： C07K1/14 , A61K38/00 , C07K7/08 , C07K7/56 , C07K9/00 , C07K11/02 , C08L23/08 , C08L23/0869 , C08L51/06 , C08L2203/14 , C09K3/10 , C09K2003/1037 , C09K2200/06 , C09K2200/062 , C09K2200/0622 , C08L2666/04 , C08L2666/02
摘要： The present invention provides laspartomycin core peptides, laspartomycin core peptide derivatives, antimicrobial laspartomycin derivatives, methods for making laspartomycin core peptides, methods for making laspartomycin core peptide derivatives, methods for making antimicrobial laspartomycin derivatives, pharmaceutical compositions of antimicrobial laspartomycin derivatives, methods of inhibiting microbial growth and methods for treating and/or preventing microbial infections in a subject.
摘要翻译： 本发明提供了拉沙曲霉素核心肽，拉斯马霉素核心肽衍生物，抗菌蓝鲸霉素衍生物，制备拉沙曲霉素核心肽的方法，制备蓝鲸霉素核心肽衍生物的方法，制备抗菌蓝鲸霉素衍生物的方法，抗微生物蓝鲸霉素衍生物的药物组合物，抑制微生物的方法 用于治疗和/或预防受试者微生物感染的生长和方法。
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公开(公告)号：US20080207874A1
公开(公告)日：2008-08-28
申请号：US11630847
申请日：2005-07-01
IPC分类号： C07K7/64
CPC分类号： C07K5/0815 , A61K38/00 , C07K5/06086 , C07K7/62 , C07K7/64 , Y02A50/473 , Y02P20/55
摘要： Novel protected cyclopeptide intermediates are prepared from polymyxin B are used to synthesize new peptide antibiotics. Intermediates are readily derivatized and deprotected to provide new families of antibiotics, which have potent anti-bacterial activity against gram-negative bacteria; but also are useful and potent against gram-positive bacteria.
摘要翻译： 由多粘菌素B制备的新型受保护的环肽中间体用于合成新的肽抗生素。 中间体易于衍生化和去保护，以提供新的抗生素家族，其对革兰氏阴性细菌具有有效的抗菌活性; 而且对革兰氏阳性细菌也是有用和有效的。
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公开(公告)号：US06767718B2
公开(公告)日：2004-07-27
申请号：US10142303
申请日：2002-05-10
IPC分类号： A61K3815
摘要： Novel cyclodepsipeptide intermediates have been prepared from the A21978 complex and used to synthesize new lipodepsipeptide antibiotics. The three intermediates can be readily derivatized to give new families of antibiotics that have potent antibacterial activity against gram positive bacteria.
摘要翻译： 已经从A21978复合物制备了新的环缩酚肽中间体，并用于合成新的脂多糖肽抗生素。 三种中间体可以很容易地衍生化，以给新的抗革兰氏阳性菌抗菌活性家族。
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公开(公告)号：US06511962B1
公开(公告)日：2003-01-28
申请号：US09760328
申请日：2001-01-12
申请人： Donald B Borders , William V Curran , Amedeo A Fantini , Noreen D Francis , Howard Jarolmen , Richard A Leese
发明人： Donald B Borders , William V Curran , Amedeo A Fantini , Noreen D Francis , Howard Jarolmen , Richard A Leese
IPC分类号： A61K3812
CPC分类号： C09K3/10 , A61K38/00 , C07K1/14 , C07K7/08 , C07K7/56 , C07K9/00 , C07K11/02 , C08L23/08 , C08L23/0869 , C08L51/06 , C08L2203/14 , C09K2003/1037 , C09K2200/06 , C09K2200/062 , C09K2200/0622 , C08L2666/04 , C08L2666/02
摘要： The present invention provides a laspartomycin core peptide, a laspartomycin core peptide derivative, a antimicrobial laspartomycin derivative, a method for making laspartomycin core peptides, methods for making laspartomycin core peptide derivatives, methods for making antimicrobial laspartomycin derivatives, pharmaceutical compositions of antimicrobial laspartomycin derivatives, methods of inhibiting microbial growth and methods for treating and/or preventing microbial infections in a subject.
摘要翻译： 本发明提供了一种天蓝假单胞菌核心肽，一拉曲霉素核心肽衍生物，一种抗微生物蓝鲸霉素衍生物，一种制备蓝鲸霉素核心肽的方法，制备蓝鲸霉素核心肽衍生物的方法，制备抗菌蓝鲸霉素衍生物的方法，抗菌蓝鲸霉素衍生物的药物组合物， 抑制微生物生长的方法以及治疗和/或预防受试者微生物感染的方法。
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9.发明授权公开(公告)号：US07868135B2
公开(公告)日：2011-01-11
申请号：US10880442
申请日：2004-06-28
申请人： Dale R. Cameron , Vincent A. Boyd , Richard A. Leese , William V. Curran , Donald B. Borders , Paulo W. M. Sgarbi , Shirley A. Wacowich-Sgarbi , Matthew Nodwell , Yuchen Chen , Qi Jia , Dominique Dugourd
发明人： Dale R. Cameron , Vincent A. Boyd , Richard A. Leese , William V. Curran , Donald B. Borders , Paulo W. M. Sgarbi , Shirley A. Wacowich-Sgarbi , Matthew Nodwell , Yuchen Chen , Qi Jia , Dominique Dugourd
IPC分类号： A61K38/12
摘要： The present invention provides derivatives of lipopeptide antibiotics that display antimicrobial activity against microorganisms, methods and compounds for synthesizing such antimicrobial derivatives and analogues, and methods of using the compounds in a variety of contexts, including in the treatment and prevention of microbial infections.
摘要翻译： 本发明提供显示抗微生物抗微生物活性的脂肽抗生素衍生物，用于合成这种抗微生物衍生物和类似物的方法和化合物，以及在多种情况下使用该化合物的方法，包括在治疗和预防微生物感染中。
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10.发明授权Method for selective extracting a 7-(hydrogen or substituted amino)-9-�(substituted glycyl) amido!-6-demethyl-6-deoxytetracycline compound 失效选择性提取7-（氢或取代的氨基）-9 - [（取代的甘氨酰基）酰胺基] -6-脱甲基-6-脱氧四环素化合物的方法
公开(公告)号：US5675030A
公开(公告)日：1997-10-07
申请号：US340552
申请日：1994-11-16
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/26 , C07C2103/46
摘要： The invention provides a method for selectively extracting a compound of formula I: ##STR1## wherein: R is hydrogen or --NR.sub.3 R.sub.4 ; and when R=--NR.sub.3 R.sub.4, R.sub.3 and R.sub.4 may be the same or different and are selected from hydrogen and straight or branched (C.sub.1 -C.sub.4)alkyl; R.sub.1 and R.sub.2 may be the same or different and are selected from straight or branched (C.sub.1 -C.sub.6)alkyl; from an aqueous mixture containing a compound of Formula I, its C-4 epimer and its oxidative degradation by-products by adding methylene at a concentration of 2-4 ml of methylene chloride per gram of compound of Formula I and at a pH between pH 6.5-8.0; and obtaining an extract containing methylene chloride, a compound of Formula I, and its C-4 epimer, said epimer being present in an amount of less than 3% of the amount of the compound of Formula I.
摘要翻译： 本发明提供了选择性提取式I化合物的方法：其中：R是氢或-NR 3 R 4; 当R = -NR 3 R 4时，R 3和R 4可以相同或不同，并且选自氢和直链或支链（C 1 -C 4）烷基; R 1和R 2可以相同或不同，并且选自直链或支链（C 1 -C 6）烷基; 从含有式I化合物，其C-4差向异构体及其氧化降解副产物的含水混合物中加入浓度为2-4ml二氯甲烷/克式I化合物的亚甲基，pH在pH 6.5-8.0; 并得到含有二氯甲烷的提取物，式I化合物及其C-4差向异构体，所述差向异构体的存在量小于式I化合物的量的3％。
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