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1. 发明授权

US06380181B1 Synthetic catechol derivatives, method for production and use thereof 失效
标题翻译：合成儿茶酚衍生物，其制备方法和用途
公开(公告)号：US06380181B1
公开(公告)日：2002-04-30
申请号：US09202955
申请日：1999-09-10
申请人： Lothar Heinisch , Ute Moellmann , Matthias Schnabelrauch , Rolf Reissbrodt
发明人： Lothar Heinisch , Ute Moellmann , Matthias Schnabelrauch , Rolf Reissbrodt
IPC分类号： A61K3143
CPC分类号： C07D501/00 , A61K47/54 , A61K47/547 , C07C235/60 , C07C235/64 , C07C237/22 , C07C245/08 , C07C251/24 , C07C251/80 , C07C251/86 , C07D263/06 , C07D499/00
摘要： Catechol derivatives of general formula (I) in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.
摘要翻译：通式（I）的儿茶酚衍生物，其中R1表示O-酰基，R2表示作为铁载体的3-和/或4-位官能团中的氨基酸残基和/或作为革兰氏阴性细菌中铁的生物螯合剂。与抗生素结合可改善细菌的渗透，从而提高细胞的抗菌功效。

2. 发明授权

US6013647A Benzoxazinedione derivatives, method of producing them and uses thereof 失效
标题翻译：苯并恶嗪二酮衍生物，其制备方法和用途
公开(公告)号：US6013647A
公开(公告)日：2000-01-11
申请号：US35344
申请日：1998-03-05
申请人： Lothar Heinisch , Steffen Wittmann , Ute Moellmann , Rolf Reissbrodt
发明人： Lothar Heinisch , Steffen Wittmann , Ute Moellmann , Rolf Reissbrodt
IPC分类号： C07D499/70 , A61K31/535 , A61K31/536 , A61K31/538 , A61K38/00 , A61K47/48 , A61P3/00 , A61P31/04 , A61P43/00 , C07D265/24 , C07D265/26 , C07D413/06 , C07D413/12 , C07D499/00 , C07D499/68 , C07D501/20 , C07K5/02 , C07K5/06 , C07K5/103 , C07K7/06
CPC分类号： C07K7/06 , C07D265/26 , C07D499/00 , C07K5/02 , C07K5/06026 , C07K5/1008 , A61K38/00
摘要： This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams. In addition, said compounds, as potential prodrug forms for iron chelating agents, are suitable for use against diseases which are caused by a disorder of the iron metabolism. The invention can be employed in pharmaceutical research and in the pharmaceutical industry, and in agriculture.
摘要翻译：本发明涉及对应于式I的新的苯并恶嗪二酮衍生物：其中R1 = H或羧基烷基，R2 = H，烷基或苯基，R3代表衍生自氨基酸，二肽和腙的不同酸基或其与活性成分例如抗生素。化合物可以其盐形式或易裂解的酯的形式存在为游离酸。根据本发明的化合物构成了杂环保护的邻苯二酚衍生物，并且作为抗革兰氏阴性细菌菌株的铁载体是有效的，特别是对假单胞菌和大肠杆菌和沙门氏菌菌株有效。以它们与活性成分的缀合物的形式，例如抗生素（作为“铁载体 - 抗生素共轭物”），它们可以将后者转运到细菌细胞中，并且可以改善或延长其抗菌作用，有时甚至与对其它β-内酰胺酶有抗性的细菌菌株有关。此外，作为铁螯合剂的潜在前体药物形式的所述化合物适用于针对由铁代谢紊乱引起的疾病。本发明可用于制药研究，制药工业和农业领域。

3. 发明授权

US06124290A Polycyclic phthalazine compounds and their use 失效
标题翻译：多环酞嗪化合物及其用途
公开(公告)号：US06124290A
公开(公告)日：2000-09-26
申请号：US242295
申请日：2000-01-28
申请人： Lothar Heinisch , Ute Moellmann , Wolfgang Witte , Christiane Cuny , Ernst Roemer , Walter Werner , Udo Graefe
发明人： Lothar Heinisch , Ute Moellmann , Wolfgang Witte , Christiane Cuny , Ernst Roemer , Walter Werner , Udo Graefe
IPC分类号： C07D307/32 , A61K31/50 , A61K31/502 , A61P31/04 , C07D237/26 , C07D237/32 , A61K31/435
CPC分类号： C07D237/26
摘要： Polycyclic phthalazines, in particular 2-substituted maduraphthalazines (10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-1,9,14-trioxo-1,2,6,7,9,14-hexahydronaphthaceno-1,2-g-phthalazines), of formula I and their use against gram-positive bacterial strains, particularly against multi-resistant staphylococci (MRSA) and against glycopeptide-resistant, for example vancomycin-resistant, enterococci. The polycyclic phthalazines are thus suitable for preparing anti-bacterially effective pharmaceutical compositions. In formula I, R.sup.1 is carboxyalkyl or carboxyaryl, and R.sup.2 and R.sup.3 represent H or acyl (for example CO-alkyl or COO-alkyl), with R.sup.1 being different from optionally substituted carboxyphenyl when R.sup.3 represents C.sub.1-8 alkanoyl. The invention also relates to salts, amides and esters of compounds of formula I.
摘要翻译： PCT No.PCT / FI96 / 03632 Sec。 371日期2000年1月28日 102（e）日期2000年1月28日PCT 1997年7月9日PCT公布。公开号WO98 / 07706 日期1998年2月26日多环酞嗪，特别是2-取代的马卡波肼（10,12,15,16-四羟基-8-甲氧基-11-甲基-1,9,14-三氧杂-1,2,6,7,9 ，14-六氢萘并-1,2- -g-酞嗪），以及它们对革兰氏阳性细菌菌株，特别是针对多重耐药葡萄球菌（MRSA）和抗糖肽抗性（例如万古霉素抗性肠球菌）的用途。因此，多环酞嗪适于制备抗细菌有效的药物组合物。在式I中，R 1是羧基烷基或羧基芳基，R 2和R 3表示H或酰基（例如CO-烷基或COO-烷基），当R 3表示C 1-8烷酰基时，R 1不同于任选取代的羧基苯基。本发明还涉及式I化合物的盐，酰胺和酯。

4. 发明授权

US08440842B2 Antimicrobial compounds, their synthesis and their use for treatment of mammalian infections 有权
标题翻译：抗菌化合物，其合成及其用于治疗哺乳动物感染的用途
公开(公告)号：US08440842B2
公开(公告)日：2013-05-14
申请号：US12669748
申请日：2008-06-25
申请人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
发明人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
IPC分类号： A61K31/54 , C07D327/06 , C07D409/00
CPC分类号： C07D279/08
摘要： The present invention relates to compounds of Formula (I) or salts thereof wherein R1, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
摘要翻译：本发明涉及式（I）化合物或其盐，其中R1，R2，R3，R4，R5，R6和其一个或多个下列举的其它变量如本文所定义。式I的化合物具有作为抗微生物剂的活性。还公开了使用哺乳动物的微生物感染的药物组合物和方法，例如使用式（I）化合物或其盐的结核病或麻风病感染。

5. 发明授权

US07863268B2 Benzothiazinone derivatives and their use as antibacterial agents 有权
标题翻译：苯并噻嗪酮衍生物及其作为抗菌剂的用途
公开(公告)号：US07863268B2
公开(公告)日：2011-01-04
申请号：US12227655
申请日：2006-05-24
申请人： A. Vadim Makarov , Stewart T. Cole , Ute Moellmann
发明人： A. Vadim Makarov , Stewart T. Cole , Ute Moellmann
IPC分类号： C07D417/06 , A61K31/541
CPC分类号： C07D417/04 , C07D491/113
摘要： Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R1, R2, R3, R4, R5, and R6, and other variables enumerated under one or more of R1, R2, R3, R4, R5, and R6 are as defined.
摘要翻译：公开了式（I）的苯并噻嗪衍生物，其制备方法以及使用抗菌剂等化合物治疗由细菌引起的哺乳动物感染性疾病，特别是结核分枝杆菌和由分枝杆菌引起的麻风病的疾病的治疗方法：其中R1，R2，R3， R4，R5和R6以及R1，R2，R3，R4，R5和R6中的一个或多个下列举的其它变量如上所定义。

6. 发明申请

US20100286130A1 ANTIMICROBIAL COMPOUNDS, THEIR SYNTHESIS AND THEIR USE FOR TREATMENT OF MAMMALIAN INFECTIONS 有权
标题翻译：抗微生物化合物，其合成及其用于治疗哺乳动物感染的用途
公开(公告)号：US20100286130A1
公开(公告)日：2010-11-11
申请号：US12669748
申请日：2008-06-25
申请人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
发明人： Ute Moellmann , Vadim Makarov , Cole T. Stewart
IPC分类号： A61K31/5415 , C07D417/04 , A61P31/06 , A61P31/08
CPC分类号： C07D279/08
摘要： The present invention relates to compounds of Formula (I) or salts thereof wherein R′, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
摘要翻译：本发明涉及式（I）化合物或其盐，其中R 1，R 2，R 3，R 4，R 5，R 6和其一个或多个下列举的其它变量如本文所定义。式I的化合物具有作为抗微生物剂的活性。还公开了使用哺乳动物的微生物感染的药物组合物和方法，例如使用式（I）化合物或其盐的结核病或麻风病感染。

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