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1. 发明申请

US20130059005A1 BUPROPION HYDROBROMIDE POLYMORPHS 有权
标题翻译：支链淀粉多糖
公开(公告)号：US20130059005A1
公开(公告)日：2013-03-07
申请号：US13653503
申请日：2012-10-17
申请人： Stefano TURCHETTA , Maurizio ZENONI
发明人： Stefano TURCHETTA , Maurizio ZENONI
IPC分类号： A61K31/137 , A61K9/14 , A61K9/30 , A61P25/24 , A61P3/04 , A61P25/06 , A61P25/00 , A61P25/20 , A61P15/10 , A61P19/02 , A61P3/10 , A61P31/12 , C07C225/16 , A61P25/22
CPC分类号： C07C225/10 , A61K9/2886 , A61K31/137 , A61K45/06 , C07C225/16
摘要： Polymorphous and amorphous forms of bupropion hydrobromide are described.
摘要翻译：描述了安非他酮氢溴酸盐的多晶型和无定形形式。

2. 发明授权

US08058238B2 High purity lipopeptides 有权
标题翻译：高纯度脂肽
公开(公告)号：US08058238B2
公开(公告)日：2011-11-15
申请号：US11739180
申请日：2007-04-24
申请人： Thomas Kelleher , Jan-Ji Lai , Joseph P. DeCourcey , Paul Lynch , Maurizio Zenoni , Auro Tagliani
发明人： Thomas Kelleher , Jan-Ji Lai , Joseph P. DeCourcey , Paul Lynch , Maurizio Zenoni , Auro Tagliani
IPC分类号： C07K7/50 , C07K7/00
CPC分类号： A61K38/12 , A61K38/10 , C07K1/145 , C07K5/0821 , C07K7/08 , Y10S435/886 , A61K2300/00
摘要： The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
摘要翻译：本发明公开了高纯度的达托霉素和包含该化合物的药物组合物。本发明公开了一种纯化达托霉素的方法，其中包括阴离子交换层析，疏水相互作用色谱和阴离子交换层析的顺序步骤。本发明还公开了一种通过改良缓冲液增强的阴离子交换层析纯化达托霉素的方法。本发明还公开了通过发酵乳链霉菌生产达托霉素的改进方法。本发明还公开了用于分析达托霉素纯度的高压液相色谱法。本发明还公开了脂肽胶束和制备胶束的方法。本发明还公开了使用脂肽胶束来纯化脂肽抗生素如达托霉素的方法。本发明还公开了使用脂肽胶束治疗。

3. 发明申请

US20110207658A1 High Purity Lipopeptides 有权
标题翻译：高纯度脂肽
公开(公告)号：US20110207658A1
公开(公告)日：2011-08-25
申请号：US12888233
申请日：2010-09-22
申请人： Thomas J. Kelleher , Jan-Ji Lai , Joseph P. DeCourcey , Paul D. Lynch , Maurizio Zenoni , Auro R. Tagliani
发明人： Thomas J. Kelleher , Jan-Ji Lai , Joseph P. DeCourcey , Paul D. Lynch , Maurizio Zenoni , Auro R. Tagliani
IPC分类号： A61K38/12 , C07K7/64 , A61P31/04 , C12P21/04
CPC分类号： A61K38/12 , A61K38/10 , C07K1/145 , C07K5/0821 , C07K7/08 , Y10S435/886 , A61K2300/00
摘要： The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
摘要翻译：本发明公开了高纯度的达托霉素和包含该化合物的药物组合物。本发明公开了一种纯化达托霉素的方法，其中包括阴离子交换层析，疏水相互作用色谱和阴离子交换层析的顺序步骤。本发明还公开了一种通过改良缓冲液增强的阴离子交换层析纯化达托霉素的方法。本发明还公开了通过发酵乳链霉菌生产达托霉素的改进方法。本发明还公开了用于分析达托霉素纯度的高压液相色谱法。本发明还公开了脂肽胶束和制备胶束的方法。本发明还公开了使用脂肽胶束来纯化脂肽抗生素如达托霉素的方法。本发明还公开了使用脂肽胶束治疗。

4. 发明授权

US07615631B2 Crystalline solvate of cefuroxime acid 有权
标题翻译：头孢呋辛酸的结晶溶剂化物
公开(公告)号：US07615631B2
公开(公告)日：2009-11-10
申请号：US11379132
申请日：2006-04-18
申请人： Maurizio Zenoni , Angelo Giovanni Cattaneo
发明人： Maurizio Zenoni , Angelo Giovanni Cattaneo
IPC分类号： C07D501/34
CPC分类号： C07D501/00
摘要： Crystalline acetonitrile solvate of cefuroxime acid, useful for preparing the antibiotic cefuroxime sodium salt.
摘要翻译：头孢呋辛酸的结晶乙腈溶剂化物，可用于制备抗生素头孢呋辛钠盐。

5. 发明授权

US07560545B2 Process for obtaining cefotetan with high yield 失效
标题翻译：以高产量获得头孢替坦的方法
公开(公告)号：US07560545B2
公开(公告)日：2009-07-14
申请号：US11383075
申请日：2006-05-12
申请人： Maurizio Zenoni , Antonio Manca , Riccardo Monguzzi
发明人： Maurizio Zenoni , Antonio Manca , Riccardo Monguzzi
IPC分类号： C07D501/57 , C07D501/12
CPC分类号： C07D501/48
摘要： The invention relates to a method for obtaining cefotetan acid substantially free of tautomer, by treating crude cefotetan with Al3+ ions which cause the tautomer to precipitate. The precipitate is eliminated by filtration to provide a solution from which practically tautomer-free cefotetan is obtained.
摘要翻译：本发明涉及通过用导致互变异构体沉淀的Al 3+离子处理粗头孢替坦来获得基本上不含互变异构体的头孢替坦的方法。通过过滤除去沉淀物，得到几乎不含互变异构头孢替丹的溶液。

6. 发明申请

US20050009747A1 High purity lipopeptides 审中-公开
标题翻译：高纯度脂肽
公开(公告)号：US20050009747A1
公开(公告)日：2005-01-13
申请号：US10747485
申请日：2003-12-29
申请人： Thomas Kelleher , Jan-Ji Lai , Joseph DeCourcey , Paul Lynch , Maurizio Zenoni , Auro Tagliani
发明人： Thomas Kelleher , Jan-Ji Lai , Joseph DeCourcey , Paul Lynch , Maurizio Zenoni , Auro Tagliani
IPC分类号： C12P21/02 , A61K38/00 , A61K38/10 , A61K38/12 , A61K45/00 , A61K45/06 , A61P29/00 , A61P31/04 , A61P31/10 , C07K20060101 , C07K1/18 , C07K1/20 , C07K1/34 , C07K1/36 , C07K5/097 , C07K7/00 , C07K7/08 , C12P17/16 , C12R1/465 , A61K38/16 , A61K38/17
CPC分类号： A61K38/12 , A61K38/10 , C07K1/145 , C07K5/0821 , C07K7/08 , Y10S435/886 , A61K2300/00
摘要： The invention discloses highly purified daptomycin and to pharmaceutical compositions comprising this compound. The invention discloses a method of purifying daptomycin comprising the sequential steps of anion exchange chromatography, hydrophobic interaction chromatography and anion exchange chromatography. The invention also discloses a method of purifying daptomycin by modified buffer enhanced anion exchange chromatography. The invention also discloses an improved method for producing daptomycin by fermentation of Streptomyces roseosporus. The invention also discloses high pressure liquid chromatography methods for analysis of daptomycin purity. The invention also discloses lipopeptide micelles and methods of making the micelles. The invention also discloses methods of using lipopeptide micelles for purifying lipopeptide antibiotics, such as daptomycin. The invention also discloses using lipopeptide micelles therapeutically.
摘要翻译：本发明公开了高纯度的达托霉素和包含该化合物的药物组合物。本发明公开了一种纯化达托霉素的方法，其中包括阴离子交换层析，疏水相互作用色谱和阴离子交换层析的顺序步骤。本发明还公开了一种通过改良缓冲液增强的阴离子交换层析纯化达托霉素的方法。本发明还公开了通过发酵乳链霉菌生产达托霉素的改进方法。本发明还公开了用于分析达托霉素纯度的高压液相色谱法。本发明还公开了脂肽胶束和制备胶束的方法。本发明还公开了使用脂肽胶束来纯化脂肽抗生素如达托霉素的方法。本发明还公开了使用脂肽胶束治疗。

7. 发明授权

US06255480B1 Aminothiazole derivatives useful in the preparation of &bgr;-lactam antibiotics 有权
标题翻译：用于制备β-内酰胺抗生素的氨基噻唑衍生物
公开(公告)号：US06255480B1
公开(公告)日：2001-07-03
申请号：US09331702
申请日：1999-06-24
申请人： Maurizio Zenoni , Mario Leone , Maurizio Serra , Mauro Filippi
发明人： Maurizio Zenoni , Mario Leone , Maurizio Serra , Mauro Filippi
IPC分类号： C07D27738
CPC分类号： C07D277/587 , C07D417/12 , C07D501/00
摘要： Aminothiazole derivatives having the carboxyl activated by means of thioesters, said derivatives being condensable with &bgr;-lactam nuclei to yield &bgr;-lactam antibiotics
摘要翻译：具有通过硫酯活化的羧基的氨基噻唑衍生物，所述衍生物与β-内酰胺核可缩合以产生β-内酰胺抗生素

8. 发明授权

US5654425A Method for the acylation of the 7-amino group of the cephalosporanic ring 失效
标题翻译：头孢菌素环的7-氨基酰化方法
公开(公告)号：US5654425A
公开(公告)日：1997-08-05
申请号：US432072
申请日：1995-05-01
申请人： Maurizio Zenoni , Claudio Fuganti
发明人： Maurizio Zenoni , Claudio Fuganti
IPC分类号： C07D501/20 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/34 , C07D501/36 , C12P35/00 , C12P35/04 , C07D501/24
CPC分类号： C12P35/04 , C07D501/00 , Y02P20/55
摘要： A method for the acylation of the 7-amino group of the cephalosporanic ring, according to which a 7-ACA amino thiazolyl protected adduct is prepared by acylating said amino group by an aminothiazolyl acetic acid whose amino group has been protected by a phenyl acetyl or a phenoxy acetyl group, the amino group being then deprotected by aqueous hydrolysis in the presence of penicillin G amidase or respectively penicillin V amidase.
摘要翻译：酰基化头孢菌素环的7-氨基的方法，根据该方法，通过用氨基噻唑乙酸酰化所述氨基来制备7-ACA氨基噻唑基保护的加合物，其氨基已被苯基乙酰基或苯氧基乙酰基，然后在青霉素G酰胺酶或分别为青霉素V酰胺酶的存在下，通过水解水解脱氨基。

9. 发明授权

US5574153A Oxime derivatives of cephalosporanic structure 失效
标题翻译：肟衍生物的头孢菌素结构
公开(公告)号：US5574153A
公开(公告)日：1996-11-12
申请号：US281170
申请日：1994-07-27
申请人： Maurizio Zenoni , Mario Leone , Riccardo Colombo
发明人： Maurizio Zenoni , Mario Leone , Riccardo Colombo
IPC分类号： C07D213/63 , A61K31/435 , A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07C59/70 , C07C229/34 , C07C251/16 , C07C251/24 , C07C251/40 , C07C251/48 , C07C251/52 , C07C251/60 , C07C255/13 , C07C307/02 , C07C311/08 , C07C317/44 , C07C323/62 , C07D213/74 , C07D463/00 , C07D501/00 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/26 , C07D501/30 , C07D501/36 , C07D501/38 , C07D501/40 , C07D501/48 , C07D501/50 , C07D501/59 , C07D501/60 , C07D505/00 , C07D501/34 , C07D501/32
CPC分类号： C07D501/00 , C07D463/20 , C07D463/22 , C07D505/00
摘要： The invention relates to oxime derivatives of cephalosporanic structure, possessing antibacterial activity.
摘要翻译：本发明涉及头孢菌素结构的肟衍生物，具有抗菌活性。

10. 发明授权

US09266863B2 Process for the synthesis of azacitidine and decitabine 有权
标题翻译：合成阿扎胞苷和地西他滨的方法
公开(公告)号：US09266863B2
公开(公告)日：2016-02-23
申请号：US13073014
申请日：2011-03-28
申请人： Lorenzo De Ferra , Maurizio Zenoni , Stefano Turchetta , Mauro Anibaldi , Ettore Ammirati , Paolo Brandi , Giorgio Berardi
发明人： Lorenzo De Ferra , Maurizio Zenoni , Stefano Turchetta , Mauro Anibaldi , Ettore Ammirati , Paolo Brandi , Giorgio Berardi
IPC分类号： C07H19/12 , C07H1/00 , C07D405/04
CPC分类号： C07D405/04 , C07H1/00 , C07H19/12
摘要： Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
摘要翻译：本文描述的是在N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺的存在下合成氮杂胞苷或地西他滨的方法，其包括氮代胞嘧啶的甲硅烷基化。这种反应在有机溶剂中进行，优选非质子性，甚至更优选选自二氯甲烷，二氯乙烷和/或乙腈。根据该方法的另一方面，每摩尔氮杂胞嘧啶使用2至3摩尔N，O-双 - 三甲基甲硅烷基 - 三氟乙酰胺，优选2.2至2.5。

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