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1. 发明申请

WO2008084411A2 MODIFIED SACCHARIDES 审中-公开
标题翻译：改良的SACCHARIDES
公开(公告)号：WO2008084411A2
公开(公告)日：2008-07-17
申请号：PCT/IB2008/001116
申请日：2008-01-11
申请人： NOVARTIS AG , BARDOTTI, Angela , BERTI, Francesco , COSTANTINO, Paolo
发明人： BARDOTTI, Angela , BERTI, Francesco , COSTANTINO, Paolo
CPC分类号： C08B37/00 , A61K39/095 , A61K47/646 , A61K2039/55505 , A61K2039/6037 , C07H13/00 , C08B37/006
摘要： Modified capsular saccharides comprising a blocking group at a hydroxyl group position on at least one of the monosaccharide units of the corresponding native capsular saccharide, wherein the blocking group is of the formula (Ia) or (Ib): -OX-Y (Ia) or -0-R 1 (Ib) wherein X is C(O), S(O) or SO 2 ; Y is NR 1 R 2 or R 3 ; R 1 is C 1-6 alkyl substituted with 1, 2 or 3 groups independently selected from hydroxyl, sulphydryl and amine; R 2 is H or C 1-6 alkyl; and R3 is C 1-6 alkyl; processes for modifying a capsular saccharide with the blocking groups; saccharide-protein conjugates comprising the modified capsular saccharide; processes for making the saccharide-protein conjugates, pharmaceutical compositions comprising the modified capsular saccharides and/or saccharide-protein conjugates; and methods and uses of the same.
摘要翻译：在相应的天然荚膜糖的至少一个单糖单元上的羟基位置上含有封闭基团的改性荚膜糖，其中所述封闭基团为式（Ia）或（Ib）：-OX-Y（Ia）或者-O-R 1（Ib）其中X是C（O），S（O）或SO 2; Y是NR 1，R 2或R 3; R 1是被独立地选自羟基，巯基和胺的1,2或3个基团取代的C 1-6烷基; R 2是H或C 1-6烷基; 且R 3为C 1-6烷基; 用阻聚基修饰荚膜糖的方法; 包含修饰的荚膜糖的糖 - 蛋白质缀合物; 制备糖 - 蛋白质缀合物的方法，包含改性荚膜糖和/或糖 - 蛋白质缀合物的药物组合物; 以及相同的方法和用途。

2. 发明申请

WO2012085668A3 COMPOUNDS 审中-公开
公开(公告)号：WO2012085668A3
公开(公告)日：2012-06-28
申请号：PCT/IB2011/003244
申请日：2011-12-23
申请人： NOVARTIS AG , COSTANTINO, Paolo , ADAMO, Roberto , ROMANO, Maria Rosaria , DANIEL, Elisa , BERTI, Francesco , CAPPELLITTI, Emilia , LAY, Luigi
发明人： COSTANTINO, Paolo , ADAMO, Roberto , ROMANO, Maria Rosaria , DANIEL, Elisa , BERTI, Francesco , CAPPELLITTI, Emilia , LAY, Luigi
IPC分类号： C07H15/04 , C07H15/18 , A61K39/08 , C08B37/00 , C08L5/00 , C12P19/04 , A61P1/12 , A61P31/04 , A61K39/40 , A61K39/44 , A61K47/48
摘要： The invention provides a synthetic C. difficile PS-II cell wall saccharide. The invention also provides a process for purifying C. difficile PS-II saccharide from C. difficile bacterial cells resulting in reduced contamination. The saccharides may be used in vaccines, particularly as conjugates with carrier proteins.

3. 发明申请

WO2011138636A1 CONJUGATION OF STAPHYLOCOCCUS AUREUS TYPE 5 AND TYPE 8 CAPSULAR POLYSACCHARIDES 审中-公开
标题翻译： US US US US US US US US ES ES ES ES ES ES ES ES ES ES ES ES ES ES ES ES
公开(公告)号：WO2011138636A1
公开(公告)日：2011-11-10
申请号：PCT/IB2010/002565
申请日：2010-09-30
申请人： NOVARTIS AG , BERTI, Francesco , COSTANTINO, Paolo , ROMANO, Maria, Rosaria
发明人： BERTI, Francesco , COSTANTINO, Paolo , ROMANO, Maria, Rosaria
IPC分类号： A61K47/48
CPC分类号： A61K39/385 , A61K39/085 , A61K47/6415 , A61K47/646 , A61K2039/6037 , A61K2039/627 , Y10S424/831 , Y10S530/807
摘要： The invention provides a process for preparing a conjugate of a S.aurens type 5 or type 8 capsular polysaccharide and a carrier molecule, comprising the steps of: (a) depolymerising the capsular polysaccharide, to give a polysaccharide fragment; (b) oxidising the fragment in order to introduce an aldehyde group into at least one saccharide residue in the fragment, to give an oxidised saccharide residue; and (c) coupling the oxidised saccharide residue to a carrier molecule via the aldehyde group, thereby giving the conjugate. The coupling in step (c) may be direct, or may be via a linker molecule. The invention also provides a conjugate obtained or obtainable by this process.
摘要翻译：本发明提供了一种制备5型或5型葡萄球菌荚膜多糖和载体分子的缀合物的方法，包括以下步骤：（a）解聚荚膜多糖，得到多糖片段; （b）氧化该片段以将醛基引入片段中的至少一个糖残基中，得到氧化的糖残基; 和（c）通过醛基将氧化的糖残基偶联到载体分子上，从而得到缀合物。步骤（c）中的偶联可以是直接的，或可以通过连接体分子。本发明还提供通过该方法获得或可获得的缀合物。

4. 发明申请

WO2011051917A1 PURIFICATION OF STAPHYLOCOCCUS AUREUS TYPE 5 AND TYPE 8 CAPSULAR SACCHARIDES 审中-公开
标题翻译： US US US US US US US US ES ES ES ES ES ES ES ES ES ES ES ES ES ES
公开(公告)号：WO2011051917A1
公开(公告)日：2011-05-05
申请号：PCT/IB2010/054934
申请日：2010-11-01
申请人： NOVARTIS AG , COSTANTINO, Paolo , ROMANO, Maria Rosaria , BERTI, Francesco
发明人： COSTANTINO, Paolo , ROMANO, Maria Rosaria , BERTI, Francesco
IPC分类号： A61K39/085 , A61K39/385
CPC分类号： C07H1/08 , A61K39/085 , A61K2039/55505 , A61K2039/6037 , C12P19/04
摘要： The invention provides a method for releasing capsular polysaccharide from S.aureus type 5 or type 8 cells, comprising the step of treating the cells with acid. The invention further provides a process for purifying capsular polysaccharide from S.aureus type 5 or type 8 cells comprising this method. Other processing steps may be included in the process, such as enzymatic treatment, e.g. to remove nucleic acid, protein and/or peptidoglycan contaminants; diafiltration, e.g. to remove low molecular weight contaminants; anion exchange chromatography, e.g. to remove residual protein; and concentration.
摘要翻译：本发明提供一种从金黄色葡萄球菌5型或8型细胞中释放荚膜多糖的方法，包括用酸处理细胞的步骤。本发明还提供了一种从包括该方法的5型金黄色葡萄球菌或8型细胞中纯化荚膜多糖的方法。其他处理步骤可以包括在该方法中，例如酶处理，例如，去除核酸，蛋白质和/或肽聚糖污染物; 渗滤，例如去除低分子量污染物; 阴离子交换层析，例如去除残留蛋白质; 和集中。

5. 发明申请

WO2010049806A1 PURIFICATION METHOD 审中-公开
标题翻译：净化方法
公开(公告)号：WO2010049806A1
公开(公告)日：2010-05-06
申请号：PCT/IB2009/007346
申请日：2009-10-27
申请人： NOVARTIS AG , COSTANTINO, Paolo , BERTI, Francesco , KABANOVA, Anna , ROMANO, Maria, Rosaria
发明人： COSTANTINO, Paolo , BERTI, Francesco , KABANOVA, Anna , ROMANO, Maria, Rosaria
IPC分类号： B01D15/36 , B01D61/14 , C07K1/34 , A61K39/09 , C07K1/18 , C12P19/00
CPC分类号： A61K39/092 , A61K2039/55505 , A61K2039/6037 , B01D15/34 , B01D15/363 , B01D61/145
摘要： A process for purifying a Streptococcus pyogenes GAS carbohydrate comprising a step of anionic exchange chromatography. The process provides a good yield of GAS carbohydrate. The saccharides of the invention have low levels of hyaluronic acid, protein and nucleic acid contamination.
摘要翻译：一种用于纯化化脓性链球菌GAS碳水化合物的方法，其包括阴离子交换层析步骤。该方法提供了良好的GAS碳水化合物产量。本发明的糖类具有低水平的透明质酸，蛋白质和核酸污染。

6. 发明申请

WO2009150543A2 CONJUGATED VI SACCHARIDES 审中-公开
标题翻译：结合六味
公开(公告)号：WO2009150543A2
公开(公告)日：2009-12-17
申请号：PCT/IB2009/006285
申请日：2009-06-12
申请人： NOVARTIS AG , MICOLI, Francesca , COSTANTINO, Paolo , BERTI, Francesco
发明人： MICOLI, Francesca , COSTANTINO, Paolo , BERTI, Francesco
IPC分类号： A61K47/48 , A61P43/00
CPC分类号： C07K14/195 , A61K39/0275 , A61K47/6415 , A61K47/646
摘要： Two Vi conjugates have been prepared by carbodiimide-mediated synthesis, using adipic acid dihydrazide derivatized CRM 197 (a non-toxic variant of diphtheria toxin) and tetanus toxoid, as carrier proteins.
摘要翻译：已经通过碳二亚胺介导的合成制备了两种Vi缀合物，其使用衍生化的CRM197（一种白喉毒素的无毒变体）和破伤风类毒素的己二酸二酰肼作为载体蛋白。

7. 发明申请

WO2009077854A2 ADJUVANTED GLUCANS 审中-公开
公开(公告)号：WO2009077854A2
公开(公告)日：2009-06-25
申请号：PCT/IB2008/003582
申请日：2008-11-26
申请人： NOVARTIS AG , BERTI, Francesco , COSTANTINO, Paolo , ROMANO, Maria, Rosaria
发明人： BERTI, Francesco , COSTANTINO, Paolo , ROMANO, Maria, Rosaria
IPC分类号： A61K39/00 , C08B37/00 , A61P31/10
CPC分类号： A61K39/0002 , A61K47/6415 , A61K47/646 , A61K2039/55505 , A61K2039/55555 , A61K2039/55561 , A61K2039/55566 , A61K2039/55583 , A61K2039/6037 , C08B37/0024
摘要： The use of beta-glucans as antigens for immunising against fungi is known. According to the invention, the beta-glucans are administered together with an adjuvant. The adjuvant improves the immune response. The glucan will usually be conjugated to a carrier. Suitable glucans include laminarin and curdlan.
摘要翻译：使用β-葡聚糖作为抗真菌免疫的抗原是已知的。根据本发明，β-葡聚糖与佐剂一起施用。佐剂改善免疫反应。葡聚糖通常与载体结合。合适的葡聚糖包括昆布兰和凝胶多糖。

8. 发明申请

WO2011080595A2 POLYSACCHARIDE IMMUNOGENS CONJUGATED TO E. COLI CARRIER PROTEINS 审中-公开
标题翻译：多糖免疫调节蛋白与大肠杆菌载体蛋白结合
公开(公告)号：WO2011080595A2
公开(公告)日：2011-07-07
申请号：PCT/IB2010/003484
申请日：2010-12-30
申请人： NOVARTIS AG , COSTANTINO, Paolo , SERINO, Laura , ROMANO, Maria, Rosaria , TONTINI, Marta , BERTI, Francesco , MICOLI, Francesca , KABANOVA, Anna
发明人： COSTANTINO, Paolo , SERINO, Laura , ROMANO, Maria, Rosaria , TONTINI, Marta , BERTI, Francesco , MICOLI, Francesca , KABANOVA, Anna
IPC分类号： A61K47/48 , A61K39/02
CPC分类号： A61K47/4833 , A61K39/0002 , A61K39/0258 , A61K39/39 , A61K47/646 , A61K2039/6068 , Y02A50/401 , Y02A50/403 , Y02A50/41 , Y02A50/478 , Y02A50/484
摘要： E. coli proteins have been identified that are useful as carrier proteins to improve a response to a polysaccharide immunogen conjugated to such protein. In particular, AcfD precursor protein (orf3526 polypeptide), Flu antigen 43 protein (orf1364 polypeptide), and Sell repeat-containing protein (upec-5211 polypeptide) have been shown to be effective. Additionally, these E. coli proteins can enhance the immune response to glucans, particularly fungal glucans.
摘要翻译：已经鉴定出大肠杆菌蛋白质可用作载体蛋白，以改善对与这种蛋白质缀合的多糖免疫原的反应。特别地，已证明AcfD前体蛋白（orf3526多肽），Flu抗原43蛋白（orf1364多肽）和含Sell重复蛋白（upec-5211多肽）是有效的。此外，这些大肠杆菌蛋白质可增强对葡聚糖，特别是葡萄糖葡萄糖的免疫应答。

9. 发明申请

WO2012035519A1 IMMUNOGENIC COMPOSITIONS 审中-公开
标题翻译：免疫组化
公开(公告)号：WO2012035519A1
公开(公告)日：2012-03-22
申请号：PCT/IB2011/054069
申请日：2011-09-16
申请人： NOVARTIS AG , BERTI, Francesco , CONTORNI, Mario , COSTANTINO, Paolo , FINCO, Oretta , GRANDI, Guido , MAIONE, Domenico , TELFORD, John
发明人： BERTI, Francesco , CONTORNI, Mario , COSTANTINO, Paolo , FINCO, Oretta , GRANDI, Guido , MAIONE, Domenico , TELFORD, John
IPC分类号： A61K39/385 , A61P31/04
CPC分类号： A61K39/385 , A61K39/092 , A61K47/646 , A61K2039/6037 , A61K2039/627
摘要： The invention provides an immunogenic composition comprising: a) a conjugate that is a capsular saccharide from GBS serotype la conjugated to a carrier protein; b) a conjugate that is a capsular saccharide from GBS serotype lb conjugated to a carrier protein; and c) a conjugate that is a capsular saccharide from GBS serotype III conjugated to a carrier protein. The invention also provides a method for immunising a patient against infection by GBS comprising the step of administering to the patient a conjugate that is a capsular saccharide from GBS conjugated to a diphtheria toxoid or derivative thereof, wherein the patient has been pre-immunised with a diphtheria toxoid or derivative thereof.
摘要翻译：本发明提供免疫原性组合物，其包含：a）缀合物，其是来自与载体蛋白质缀合的GBS血清型1a的荚膜糖; b）缀合物，其是与载体蛋白缀合的GBS血清型1b的荚膜糖; 和c）缀合物，其是与载体蛋白质缀合的GBS血清型III的荚膜糖。本发明还提供了一种用于免疫患者免受GBS感染的方法，包括向患者施用作为与白喉类毒素或其衍生物缀合的GBS的荚膜糖的缀合物的步骤，其中所述患者已经用白喉类毒素或其衍生物。

10. 发明申请

WO2009081276A3 FERMENTATION PROCESSES FOR CULTIVATING STREPTOCOCCI AND PURIFICATION PROCESSES FOR OBTAINING CPS THEREFROM 审中-公开
公开(公告)号：WO2009081276A3
公开(公告)日：2009-07-02
申请号：PCT/IB2008/003729
申请日：2008-12-19
申请人： NOVARTIS AG , COSTANTINO, Paolo , NORELLI, Francesco , BERTI, Francesco , CICALA, Concetta, Maria , BAZZOCCHI, Giulia , FONTANI, Silvia , OLIVIERI, Roberto
发明人： COSTANTINO, Paolo , NORELLI, Francesco , BERTI, Francesco , CICALA, Concetta, Maria , BAZZOCCHI, Giulia , FONTANI, Silvia , OLIVIERI, Roberto
IPC分类号： C12N1/20 , A61K39/04 , C12P19/04
摘要： This invention is in the field of bacterial cultures, and specifically relates to the optimization of culture conditions to improve the production of bacterial capsular polysaccharides from Streptococcus strains in fed batch culture and to novel purification methods suitable for production scale purification of bacterial capsular polysaccharides from Streptococcus strains resulting in higher levels of purity than previously obtained for production scale.

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