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1. 发明授权

US4585589A Water-soluble alkanoyloxy and alkoxycarbonyloxy rifampicin derivatives, process for its preparation, intermediates, and its pharmaceutical composition as antibacterials 失效
标题翻译：水溶性烷酰氧基和烷氧基羰氧基利福平衍生物，其制备方法，中间体及其作为抗菌剂的药物组合物
公开(公告)号：US4585589A
公开(公告)日：1986-04-29
申请号：US626358
申请日：1984-06-29
申请人： Adriano Malabarba , Bruno Cavalleri , Pietro Ferrari
发明人： Adriano Malabarba , Bruno Cavalleri , Pietro Ferrari
IPC分类号： A61K31/495 , A61P31/04 , C07D498/08
CPC分类号： C07D498/08
摘要： The present invention is directed to new water soluble rifampicin derivatives which are suitable for preparing aqueous solutions for oral or parenteral administration. The new derivatives of the invention are 4 and/or 8 alkanoyl or alkanoyloxyalkyl esters of rifampicin and possess essentially the same antibacterial activity of this widely known antibiotic substance.
摘要翻译：本发明涉及适用于制备用于口服或肠胃外给药的水溶液的新的水溶性利福平衍生物。本发明的新衍生物是利福平的4种和/或8种烷酰基或烷酰氧基烷基酯，并且具有与该广为人知的抗生素物质基本相同的抗菌活性。

2. 发明授权

US4629781A Chemical process for preparing L 17392 (deglucoteicoplanin) and its salts 失效
标题翻译：制备L 17392（脱葡萄糖可乐素）及其盐的化学方法
公开(公告)号：US4629781A
公开(公告)日：1986-12-16
申请号：US680435
申请日：1984-12-11
申请人： Paolo Strazzolini , Adriano Malabarba , Bruno Cavalleri
发明人： Paolo Strazzolini , Adriano Malabarba , Bruno Cavalleri
IPC分类号： C07D498/22 , C07D245/00 , C07K9/00 , C07K5/12
CPC分类号： C07K9/008 , Y10S930/19 , Y10S930/27
摘要： The present invention is directed to a chemical process for preparing antibiotic L 17392 (deglucoteicoplanin) and its salts with bases and acids by submitting a teicoplanin compound or a teicoplanin-like compound to controlled strong acidic hydrolysis conditions.
摘要翻译：本发明涉及通过将泰可菌素化合物或替考拉宁样化合物递送至受控强酸性水解条件来制备抗生素L 17392（脱葡萄糖可乐宁）及其与碱和酸的盐的化学方法。

3. 发明授权

US5041534A Process for preparing antibiotic L 17054 失效
标题翻译：制备抗生素L 17054的方法
公开(公告)号：US5041534A
公开(公告)日：1991-08-20
申请号：US929040
申请日：1986-11-10
申请人： Adriano Malabarba , Paolo Strazzolini , angelo Borghi , Bruno Cavalleri , Carolina Coronelli
发明人： Adriano Malabarba , Paolo Strazzolini , angelo Borghi , Bruno Cavalleri , Carolina Coronelli
IPC分类号： A61K38/00 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： The present invention is directed to the essentially pure preparation of an antibiotic substance arbitrarily designated antibiotic L 17054. This antibiotic substance is obtained from the known antibiotic substance named teicoplanin (formerly teichomycin) by chemical treatment. The new compound and the pharmaceutically acceptable salts possess antimicrobial activity.
摘要翻译：本发明涉及任意指定的抗生素L 17054的抗生素物质的基本上纯的制剂。该抗生素物质通过化学处理从已知的名称为替考拉宁（以下称为teichomycin）的抗生素物质获得。新化合物和药学上可接受的盐具有抗微生物活性。

4. 发明授权

US4954483A Carboxylic acid ester derivatives or deglucoteicoplanin 失效
标题翻译：羧酸酯衍生物或脱葡萄糖精蛋白
公开(公告)号：US4954483A
公开(公告)日：1990-09-04
申请号：US243168
申请日：1988-09-08
申请人： Adriano Malabarba , Paolo Strazzolini , Aldo Trani , Ambrogio Magni , Bruno Cavalleri
发明人： Adriano Malabarba , Paolo Strazzolini , Aldo Trani , Ambrogio Magni , Bruno Cavalleri
IPC分类号： C07K7/64 , A61K38/00 , C07K1/02 , C07K1/113 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： The present invention is directed to carboxylic acid esters of deglucoteicoplanin, i.e. of the aglycon moiety of the antibiotic teicoplanin. The compounds of the invention are conveniently prepared either by deglucoteicoplanin or by any of the glycopeptides of the teicoplanin group, such as teicoplanin itself, one of its components, antibiotic L 17054 and antibiotic L 17046.
摘要翻译： PCT No.PCT / EP85 / 00262 Sec。 371日期1986年2月6日 102（e）日期1986年2月6日PCT归档1985年6月2日PCT公布。出版物WO86 / 日本1986年1月3日。本发明涉及脱葡萄糖可乐碱的羧酸酯，即抗生素替考拉宁的糖苷配基部分。本发明的化合物可以方便地通过脱葡萄糖精蛋白或替考拉宁组的任何糖肽制备，例如替考拉宁本身，其组分之一，抗生素L 17054和抗生素L 17046。

5. 发明授权

US4684644A Basic monocarboxyamide derivatives of actagardine having antibiotic activity and compositions thereof 失效
标题翻译：具有抗生素活性的卡那定的基本单羧酰胺衍生物及其组合物
公开(公告)号：US4684644A
公开(公告)日：1987-08-04
申请号：US842523
申请日：1986-03-21
申请人： Adriano Malabarba , Bruno Cavalleri
发明人： Adriano Malabarba , Bruno Cavalleri
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , C12P1/06 , A61K35/00 , C07D295/14
CPC分类号： C12P1/06
摘要： The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine. More particularly, they are basic monoamide derivatives of actagardine which may be schematically represented by the following formula I: ##STR2## The compound of the invention possess improved antimicrobial activity in particular against gram positive bacteria.
摘要翻译：本发明涉及一类基本的单加酰胺酰胺衍生物。放线菌肽（INN）是一种抗生素，由Actinoplanes Sp。 ATCC 31048和Actinoplanes Sp。 ATCC 31049，其描述于美国专利No. 第4,022,884号。阿卡加丁显示抗革兰氏阳性生物的体外和体内活性。其完整的化学结构尚不清楚，但只有其化学功能和主要碎片的信息。特别地，已经发现，阿格达加胺具有两个羧基官能团和伯氨基官能团，因此可以表示如下：本发明的化合物是在加马丁的羧基官能团之一的单酰胺衍生物。更具体地说，它们是阿加豆苷的碱性单酰胺衍生物，其可以由下式I示意性地表示：式I本发明的化合物具有改善的抗菌活性，特别是抗革兰氏阳性细菌。

6. 发明授权

US4661470A Ester derivatives of antibiotic L 17046 失效
公开(公告)号：US4661470A
公开(公告)日：1987-04-28
申请号：US797295
申请日：1985-11-12
申请人： Adriano Malabarba , Ambrogio Magni , Paolo Strazzolini , Bruno Cavalleri , Aldo Trani
发明人： Adriano Malabarba , Ambrogio Magni , Paolo Strazzolini , Bruno Cavalleri , Aldo Trani
IPC分类号： A61K38/00 , A61P31/04 , C07K1/113 , C07K9/00 , C07K14/195 , C07K14/41 , A61K37/02 , C07K5/12
CPC分类号： C07K9/008 , Y10S930/19
摘要： The present invention is directed to ester derivatives at the carboxylic function of the glycopeptidic antibiotic substance called antibiotic L 17046 with antimicrobial activity mainly against gram-positive bacteria.

7. 发明授权

US5132286A Composition of antibiotic L 17054 and a method for the treatment of bacterial infections using the antibiotic 失效
标题翻译：抗生素L 17054的组合物和使用抗生素处理细菌感染的方法
公开(公告)号：US5132286A
公开(公告)日：1992-07-21
申请号：US702797
申请日：1991-05-17
申请人： Adriano Malabarba , Angelo Borghi , Paolo Strazzolini , Bruno Cavalleri , Carolina Coronelli
发明人： Adriano Malabarba , Angelo Borghi , Paolo Strazzolini , Bruno Cavalleri , Carolina Coronelli
IPC分类号： C12P17/18 , A23K20/195 , A61K35/74 , A61K38/00 , A61P31/04 , C07G11/00 , C07K1/113 , C07K9/00 , C12P1/06 , C12P21/02
CPC分类号： C07K9/008 , A61K38/00 , Y10S930/19 , Y10S930/27
摘要： The present invention is directed to the essentially pure preparation of an antibiotic substance arbitrarily designated antibiotic L 17054. This antibiotic substance is obtained from the known antibiotic substance named teicoplanin (formerly teichomycin) by chemical treatment. The new compound and the pharmaceutically acceptable salts possess antimicrobial activity.

8. 发明授权

US4914187A Ester derivatives of antibiotic L 17046 失效
标题翻译：抗生素L 17046的酯衍生物
公开(公告)号：US4914187A
公开(公告)日：1990-04-03
申请号：US373680
申请日：1989-06-23
申请人： Adriano Malabarba , Paolo Strazzolini , Ambrogio Magni , Bruno Cavalleri , Aldo Trani
发明人： Adriano Malabarba , Paolo Strazzolini , Ambrogio Magni , Bruno Cavalleri , Aldo Trani
IPC分类号： C07K9/00
CPC分类号： C07K9/008
摘要： The present invention is directed to ester derivatives at the carboxylic function of the glycopeptidic antibiotic substance called antibiotic L 17046 with antimicrobial activity mainly against gram-positive bacteria.
摘要翻译：本发明涉及称为抗生素L 17046的抗糖抗生素物质的羧酸官能团的酯衍生物，其具有主要抗革兰氏阳性菌的抗微生物活性。

9. 发明授权

US4698418A Process for preparing antibiotic L 17046 失效
标题翻译：制备抗生素L 17046的方法
公开(公告)号：US4698418A
公开(公告)日：1987-10-06
申请号：US778473
申请日：1985-09-20
申请人： Adriano Malabarba , Bruno Cavalleri
发明人： Adriano Malabarba , Bruno Cavalleri
IPC分类号： C07K1/113 , C07K9/00 , C07K14/195 , C07K14/41 , C07K5/12
CPC分类号： C07K9/008 , Y10S930/19 , Y10S930/27
摘要： This invention relates to a process for converting a teicoplanin-like compound into antibiotic L 17046 characterized in that a teicoplanin-like compound selected from teicoplanin complex, any further purified preparation thereof, teicoplanin factor A.sub.2, teicoplanin factor A.sub.3, each of the main components of teicoplanin factor A.sub.2, antibiotic L 17054 and a mixture of two or more of the above substances in any proportion is submitted to hydrolysis with a strong acid in the presence of a polar aprotic organic solvent selected from ethers, ketones and mixtures thereof that a room temperature are liquid.
摘要翻译：本发明涉及一种将替考拉宁样化合物转化为抗生素L 17046的方法，其特征在于，将替考拉宁类化合物选自替考拉宁复合物，其任何进一步纯化的制剂，替考拉宁因子A2，替考拉宁因子A3，每种主要成分替考拉宁因子A2，抗生素L 17054以及两种或更多种上述物质的任何比例的混合物，在极性非质子有机溶剂的存在下，用强酸进行水解，所述极性非质子有机溶剂选自醚，酮及其混合物，室温是液体的

10. 发明授权

US4594187A Process for preparing antibiotic L 17054 失效
标题翻译：制备抗生素L 17054的方法
公开(公告)号：US4594187A
公开(公告)日：1986-06-10
申请号：US680460
申请日：1984-12-11
申请人： Paolo Strazzolini , Adriano Malabarba , Bruno Cavalleri
发明人： Paolo Strazzolini , Adriano Malabarba , Bruno Cavalleri
IPC分类号： C07G11/00 , C07K1/113 , C07K1/20 , C07K9/00 , C07K14/195 , C07K14/41 , C07H15/26
CPC分类号： C07K9/008 , Y10S930/19 , Y10S930/27
摘要： The present invention is directed to a chemical process for preparing the antibiotic substance denominated antibiotic L 17054 and its pharmaceutically acceptable salts by selectively hydrolyzing teicoplanin or a factor or component thereof with a concentrated strong organic acid.
摘要翻译：本发明涉及通过用浓缩的强有机酸选择性水解替考拉宁或其因子或组分来制备称为抗生素物质的抗生素物质L 17054及其药学上可接受的盐的化学方法。

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