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公开(公告)号:US20190233459A1
公开(公告)日:2019-08-01
申请号:US16215349
申请日:2018-12-10
发明人: Jian YIN , Jing HU , Peter Seeberger , Chunjun QIN
摘要: The present disclosure discloses the chemical synthesis method of the Plesiomonas shigelloides serotype O51 O-antigen oligosaccharide, belonging to the field of chemistry. Source-abundant D-glucose, L-fucose, D-glucosamine and the like are used as raw materials to prepare three glycosylation building blocks, the synthetic route composed of 11 reaction modules is designed, and through the optimization of protecting group and the optimization of the time of introducing functional group, the preparation of the target oligosaccharide chain is successfully achieved. The oligosaccharide chain prepared in the present disclosure has the advantages of cheap and easy-to-get raw materials, and simple and easy-to-repeat preparation method. The present disclosure will have good application prospects in the aspects of development of new drugs and vaccines of Plesiomonas shigelloides, and the like.
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公开(公告)号:US20190211333A1
公开(公告)日:2019-07-11
申请号:US16363108
申请日:2019-03-25
发明人: David B. Rozema , Darren H. Wakefield , Andrei V. Blokhin , Jonathan D. Benson , Zhen Li , Tao Pei , Fred Fleitz
IPC分类号: C12N15/113 , C07H15/04 , A61K31/713 , A61K47/54
CPC分类号: C12N15/113 , A61K31/713 , A61K47/549 , C07H15/04 , C12N2310/14 , C12N2310/317 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/351 , C12N2310/3515 , C12N2310/3521 , C12N2310/3533 , C12N2310/3525
摘要: Described are novel targeting ligands that may be linked to compounds, such therapeutic compounds, that are useful in directing the compounds to the target in vivo. The targeting ligands disclosed herein can serve to target expression-inhibiting oligomeric compounds, such as RNAi agents, to liver cells to modulate gene expression. The targeting ligands disclosed herein, when conjugated to an expression-inhibiting oligomeric compound, may be used in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Compositions including the targeting ligands disclosed herein when linked to expression-inhibiting oligomeric compounds are capable of mediating expression of target nucleic acid sequences in liver cells, such as hepatocytes, which may be useful in the treatment of diseases or conditions that respond to inhibition of gene expression or activity in a cell, tissue, or organism.
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公开(公告)号:US20180170956A1
公开(公告)日:2018-06-21
申请号:US15900544
申请日:2018-02-20
发明人: Andre BENATTAR , Andrey BONNARDEL , Jerome GUILBOT , Sebastien KERVERDO , Herve ROLLAND , Guy TABACCHI
IPC分类号: C07H15/04 , A61Q1/14 , A61Q5/02 , C07D307/20 , A61Q19/10 , C07H1/00 , A61K8/60 , C07D493/04 , A61Q17/04 , A61Q19/00 , A61Q19/08 , A61Q19/04
CPC分类号: C07H15/04 , A61K8/602 , A61Q1/14 , A61Q5/02 , A61Q17/04 , A61Q19/00 , A61Q19/04 , A61Q19/08 , A61Q19/10 , C07D307/20 , C07D493/04 , C07H1/00
摘要: A process for preparing a composition (C1) represented by the formula (I): HO—CH2—(CHOH)n—CH2—O-(G)x-H, in which G represents the remainder of a reducing sugar, n is an integer equal to 2, 3 or 4 and x, which indicates the mean degree of polymerization of the remainder G, represents a decimal number greater than 1 and less than or equal to 5, characterized in that the process includes at least one step a) of reacting a polyol of formula (A1): HO—CH2—(CHOH)n—CH2—OH, in which n is an integer equal to 2, 3 or 4, with a reducing sugar of formula (II): HO-G-H, in which G represents the remainder of a reducing sugar, in the presence of an acid catalyst (Ca), and in that the acid catalyst (Ca) is chosen from phosphorous acid, phosphoric acid and polyphosphoric acid.
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公开(公告)号:US20180116939A1
公开(公告)日:2018-05-03
申请号:US15560879
申请日:2016-03-14
发明人: Jae Won YOU , Tae Hun PARK , Yong-Jin KIM , Jon Hwan LEE
IPC分类号: A61K8/68 , A61K8/60 , A61Q19/00 , A61K31/133 , A61P17/10 , A61P31/04 , C07H15/04 , C07C215/10
CPC分类号: A61K8/68 , A61K8/60 , A61K31/133 , A61P17/10 , A61P31/04 , A61Q19/00 , C07C215/10 , C07H15/04 , C07H15/12
摘要: The present invention relates to a phytospingosine derivative generated by a condensation reaction of phytospingosine and maltose or lactose, which is an aldose-based disaccharide, and to a composition containing the same. The phytospingosine derivative of the present invention has high solubility in water compared with phytospingosine, is easy to formulate since the stabilization problem in a solution is solved, and maintains or further enhances the antibacterial effect of phytospingosine.
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公开(公告)号:US09902751B2
公开(公告)日:2018-02-27
申请号:US15105620
申请日:2014-12-29
IPC分类号: C07H7/06 , C07H1/00 , C07H7/04 , C07H15/04 , C07D407/12 , C07H23/00 , C07D307/20
CPC分类号: C07H7/06 , C07D307/20 , C07D407/12 , C07H1/00 , C07H7/04 , C07H15/04 , C07H23/00 , Y02P20/55
摘要: An improved process for the preparation of empagliflozin is disclosed. Novel intermediates of formulas (13) and (14) for the preparation of empagliflozin are also disclosed, wherein R1 and R2 are independently hydrogen or hydroxyl protecting groups.
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公开(公告)号:US09884883B2
公开(公告)日:2018-02-06
申请号:US14992995
申请日:2016-01-11
发明人: Nattaporn Lohitharn , Daniel Derr
摘要: Provided are organic solvent free methods for obtaining compositions comprising one or more rhamnolipids as well as compositions obtainable from said methods.
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公开(公告)号:US09856283B2
公开(公告)日:2018-01-02
申请号:US14847439
申请日:2015-09-08
IPC分类号: C07H15/04 , C07H5/04 , A61K31/7028 , A61K31/70 , A61K31/7016 , A61K31/702 , C07D309/10 , C07H13/04
CPC分类号: C07H15/04 , A61K31/70 , A61K31/7016 , A61K31/702 , A61K31/7028 , C07D309/10 , C07H5/04 , C07H13/04
摘要: There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods.
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公开(公告)号:US20170333545A1
公开(公告)日:2017-11-23
申请号:US15534676
申请日:2015-05-15
IPC分类号: A61K39/09 , A61K39/385 , G01N33/569 , C07H15/18 , C07H15/04 , A61K39/00
CPC分类号: A61K39/092 , A61K31/715 , A61K39/385 , A61K2039/575 , A61K2039/627 , C07H15/02 , C07H15/04 , C07H15/18 , C08B37/006 , G01N33/56944 , G01N2333/3156 , G01N2400/00 , G01N2469/20
摘要: The present invention relates to synthetic saccharides of general formula (I) that are related to Streptococcus pneumoniae serotype 4 capsular polysaccharide and conjugates thereof. Said conjugate and a pharmaceutical composition containing said conjugate are useful for prevention and/or treatment of diseases associated with Streptococcus pneumoniae, and more specifically of diseases associated with Streptococcus pneumoniae serotype 4. Furthermore, the synthetic saccharides of general formula (I) are useful as marker in immunological assays for detection of antibodies against Streptococcus pneumoniae bacteria.
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公开(公告)号:US09816122B2
公开(公告)日:2017-11-14
申请号:US14430930
申请日:2013-09-25
申请人: Glycom A/S
发明人: Pauline Peltier-Pain , Gyula Dekany , Christophe Pain , Pierre Chassagne , Nicolas Fierfort , Dóra Molnàr-Gàbor
摘要: The invention relates to a method for producing a glycoconjugate comprising an oligosaccharide part covalently linked to a non-sugar moiety selected from the group consisting of amino acids, peptides, proteins, lipids, longer alkyl groups, polyethylene glycols, α,β-unsaturated amido group and polyvinyl alcohols, using a genetically modified cell.
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公开(公告)号:US09782466B2
公开(公告)日:2017-10-10
申请号:US12321418
申请日:2009-01-20
申请人: Paolo Constantino
发明人: Paolo Constantino
IPC分类号: A61K39/385 , A61K45/00 , A61K47/00 , A61K39/00 , A61K39/095 , A61K39/102 , A61K39/09 , A61K39/08 , C09F1/02 , A23J1/00 , C07K1/00 , C07K14/00 , C07K16/00 , C07K17/00 , C07K1/06 , C07K1/08 , C09F1/00 , A23J1/04 , A61K38/00 , A23J1/20 , C07H15/04 , C07K14/22 , C07K14/285 , A61K38/48
CPC分类号: A61K39/095 , A23J1/04 , A23J1/205 , A61K38/00 , A61K38/4893 , A61K39/092 , A61K39/102 , A61K39/39 , A61K2039/545 , A61K2039/55505 , A61K2039/6037 , C07H15/04 , C07K14/22 , C07K14/285 , C09F1/00 , C09G1/00 , Y02A50/466 , Y10S424/831
摘要: Precipitated bacterial capsular polysaccharides can be efficiently re-solubilized using alcohols as solvents. The invention provides a process for purifying a bacterial capsular polysaccharide, comprising the steps of (a) precipitation of said polysaccharide, followed by (b) solubilization of the precipitated polysaccharide using ethanol. CTAB can be used for step (a). The material obtained, preferably following hydrolysis and sizing, can be conjugated to a carrier protein and formulated as a vaccine. Also, in vaccines comprising saccharides from both serogroups A and C, the invention provides that the ratio (w/w) of MenA saccharide:MenC saccharide is >1.
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