公开(公告)号：US11993627B2

公开(公告)日：2024-05-28

申请号：US16625342

申请日：2018-07-03

申请人： The University of North Carolina at Chapel Hill

发明人： Jian Liu ,  Jine Li ,  Guowei Su

IPC分类号： C07H3/06 ,  C07H11/00 ,  C08B37/00 ,  C12N9/10 ,  C12P19/26

CPC分类号： C07H3/06 ,  C07H11/00 ,  C08B37/0063 ,  C08B37/0069 ,  C12N9/1048 ,  C12N9/13 ,  C12P19/26

摘要： Methods of synthesizing chondroitin sulfate oligosaccharides are provided. Enzymatic schematic approaches to synthesizing structurally defined homogenous chondroitin sulfate oligosaccharides at high yields are provided. Synthetic chondroitin sulfate oligosaccharides ranging from 3-mers to 15-mers are provided.

公开(公告)号：US20220354873A1

公开(公告)日：2022-11-10

申请号：US17665724

申请日：2022-02-07

申请人： Gilead Sciences, Inc.

发明人： Steven Donald Axt ,  Pavel Robertovich Badalov ,  Katrien Brak ,  Silvio Campagna ,  Andrei Chtchemelinine ,  Edward Doerffler ,  Morin Mae Frick ,  Detian Gao ,  Lars V. Heumann ,  Brittanie Hoang ,  Willard Lew ,  Robert Ronald Milburn ,  Sean Timothy Neville ,  Bruce Ross ,  Erik Rueden ,  Robert William Scott ,  Dustin Siegel ,  Andrew C. Stevens ,  Clarissa Tadeus ,  Tiago Vieira ,  Andrew W. Waltman ,  Xianghong Wang ,  Mark Charles Whitcomb ,  Lydia Wolfe ,  Chia-Yun Yu

IPC分类号： A61K31/685 ,  A61K31/706 ,  A61K31/7056 ,  A61K31/53 ,  C07H1/00 ,  C07H1/02 ,  C07H11/00 ,  C07H15/18 ,  A61K31/6615 ,  A61K31/665 ,  A61K31/683 ,  C07D487/04 ,  C07D519/00 ,  C07F9/24 ,  C07F9/6561 ,  A61K31/675 ,  A61K45/06 ,  A61K31/00

摘要： Provided are methods of preparing compounds and pharmaceutical compositions for treating Filoviridae virus infections The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

公开(公告)号：US11344565B2

公开(公告)日：2022-05-31

申请号：US14926063

申请日：2015-10-29

申请人： Gilead Sciences, Inc.

发明人： Steven Donald Axt ,  Pavel Robertovich Badalov ,  Katrien Brak ,  Silvio Campagna ,  Andrei Chtchemelinine ,  Edward Doerffler ,  Morin Mae Frick ,  Detian Gao ,  Lars V. Heumann ,  Brittanie Hoang ,  Willard Lew ,  Robert Ronald Milburn ,  Sean Timothy Neville ,  Bruce Ross ,  Erik Rueden ,  Robert William Scott ,  Dustin Siegel ,  Andrew C. Stevens ,  Clarissa Tadeus ,  Tiago Vieira ,  Andrew W. Waltman ,  Xianghong Wang ,  Mark Charles Whitcomb ,  Lydia Wolfe ,  Chia-Yun Yu

IPC分类号： C07H5/06 ,  C07H7/06 ,  A61K31/685 ,  A61K31/706 ,  A61K31/7056 ,  A61K31/53 ,  C07H1/00 ,  C07H1/02 ,  C07H11/00 ,  C07H15/18 ,  A61K31/6615 ,  A61K31/665 ,  A61K31/683 ,  C07D487/04 ,  C07D519/00 ,  C07F9/24 ,  C07F9/6561 ,  A61K31/675 ,  A61K45/06 ,  A61K31/00

摘要： Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl3-2LiCl, LaCl3, CeCl3, NdCl3, or YCl3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

公开(公告)号：US20190185503A1

公开(公告)日：2019-06-20

申请号：US16325940

申请日：2017-08-14

申请人： OPKO Pham-iaceutica!s, LLC.

发明人： Tahir AHMED ,  ARIE GUTMAN ,  IRINA FEDOTEV ,  IGOR RUKHMAN ,  OLGA GROSSMAN

IPC分类号： C07H11/00 ,  A61P37/08 ,  A61K9/00 ,  C07H1/00

摘要： Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.

公开(公告)号：US09796999B2

公开(公告)日：2017-10-24

申请号：US14706794

申请日：2015-05-07

申请人： BIOMARIN PHARMACEUTICAL INC.

发明人： Brett E. Crawford ,  Jillian R. Brown ,  Charles A. Glass

IPC分类号： C12Q1/527 ,  C07H3/06 ,  C07H3/04 ,  C07H13/04 ,  C07H5/06 ,  A61K31/702 ,  G01N33/66 ,  C07H7/033 ,  C07H11/00

CPC分类号： C12Q1/527 ,  A61K31/702 ,  C07H3/04 ,  C07H3/06 ,  C07H5/06 ,  C07H7/033 ,  C07H11/00 ,  C07H13/04 ,  G01N33/66 ,  G01N2333/988 ,  G01N2400/40 ,  G01N2800/042 ,  G01N2800/52 ,  G01N2800/7071

摘要： Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation.

公开(公告)号：US09605019B2

公开(公告)日：2017-03-28

申请号：US14233579

申请日：2012-07-13

申请人： Gregory L. Verdine ,  Meena ,  Naoki Iwamoto ,  David Charles Donnell Butler

发明人： Gregory L. Verdine ,  Meena ,  Naoki Iwamoto ,  David Charles Donnell Butler

IPC分类号： C07H21/02 ,  C07H21/04 ,  C07H21/00 ,  C07H11/00 ,  C07H13/12 ,  C07D265/30 ,  C07D295/00 ,  C07C69/96 ,  C07C315/00 ,  C07C317/00 ,  C07C331/00 ,  C07C381/00 ,  A61K31/66 ,  A61K31/70 ,  C07C309/66 ,  C07D295/108 ,  C07H13/04

CPC分类号： C07H21/04 ,  A61K31/66 ,  A61K31/70 ,  C07C309/66 ,  C07D295/108 ,  C07H13/04

摘要： The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.

公开(公告)号：US20150307915A1

公开(公告)日：2015-10-29

申请号：US14706794

申请日：2015-05-07

申请人： BIOMARIN PHARMACEUTICAL INC.

发明人： Brett E. CRAWFORD ,  Jillian R. BROWN ,  Charles A. GLASS

IPC分类号： C12Q1/527 ,  C07H7/033 ,  C07H11/00

CPC分类号： C12Q1/527 ,  A61K31/702 ,  C07H3/04 ,  C07H3/06 ,  C07H5/06 ,  C07H7/033 ,  C07H11/00 ,  C07H13/04 ,  G01N33/66 ,  G01N2333/988 ,  G01N2400/40 ,  G01N2800/042 ,  G01N2800/52 ,  G01N2800/7071

摘要： Provided herein are processes for detecting oligosaccharides in a biological sample. In specific instances, the biological sample is provided from an individual suffering from a disorder associated with abnormal glycosaminoglycan accumulation.

摘要翻译： 本文提供了检测生物样品中寡糖的方法。 在具体情况下，生物样品由患有与异常糖胺聚糖累积相关的病症的个体提供。

公开(公告)号：US20120088909A1

公开(公告)日：2012-04-12

申请号：US13138557

申请日：2010-03-02

申请人： André Lehmann ,  Bert Volkert

发明人： André Lehmann ,  Bert Volkert

IPC分类号： C08B3/00 ,  C07H11/00 ,  B01J19/12 ,  C08B31/02

CPC分类号： C08B31/04 ,  C08B3/02 ,  C08B3/06 ,  C08B15/05 ,  C08B31/12

摘要： Process for esterifying, etherifying or silylating polysaccharide or derivatives thereof by means of an esterifying reagent, etherifying reagent or silylating reagent in the presence of an ionic liquid, in which(a) the process is carried out under heterogeneous reaction conditions, and (b) the amount of ionic liquid is 2% to 25% by weight, based on the polysaccharide or derivatives thereof.

摘要翻译： 和（b）在离子液体存在下，通过酯化试剂，醚化试剂或甲硅烷基化试剂酯化，醚化或甲硅烷基化多糖或其衍生物的方法，其中（a）该方法在非均相反应条件下进行， 基于多糖或其衍生物，离子液体的量为2重量％至25重量％。

公开(公告)号：US07973145B2

公开(公告)日：2011-07-05

申请号：US12322151

申请日：2009-01-29

申请人： Keisuke Ohta ,  Masahiko Miura ,  Kengo Sakaguchi ,  Fumio Sugawara ,  Noriyuki Sato ,  Hiroeki Sahara ,  Nobuaki Takahashi ,  Yoko Mori ,  Takayuki Yamazaki ,  Kazuyoshi Masaki ,  Hiroshi Murata

发明人： Keisuke Ohta ,  Masahiko Miura ,  Kengo Sakaguchi ,  Fumio Sugawara ,  Noriyuki Sato ,  Hiroeki Sahara ,  Nobuaki Takahashi ,  Yoko Mori ,  Takayuki Yamazaki ,  Kazuyoshi Masaki ,  Hiroshi Murata

IPC分类号： C07G3/00 ,  C07H11/00 ,  C07H15/00 ,  C07H17/00 ,  C07H1/00 ,  A01N43/04 ,  A61K31/70

CPC分类号： C07H15/06 ,  A61K31/7028 ,  A61K41/0038 ,  C07H15/10

摘要： Sulfoquinovosylacyl propanediol compounds represented by formula (I): wherein R1 is an acyl residue of a fatty acid, Y is a number of 1, 2 or 3, and M represents a cation having a positive charge equal to Y and pharmaceutically acceptable salts thereof are effective for treating tumors.

摘要翻译： 由式（I）表示的磺基奎诺糖基酰基丙二醇化合物：其中R1是脂肪酸的酰基残基，Y是1,2或3的数，M表示正电荷等于Y的阳离子及其药学上可接受的盐是 有效治疗肿瘤。

公开(公告)号：US20110130354A1

公开(公告)日：2011-06-02

申请号：US12960145

申请日：2010-12-03

申请人： Vito Ferro ,  Jon Krueger Fairweather ,  Tomislav Karoli ,  Ligong Liu

发明人： Vito Ferro ,  Jon Krueger Fairweather ,  Tomislav Karoli ,  Ligong Liu

IPC分类号： A61K31/7034 ,  C07H11/00 ,  C07H15/08 ,  C07H15/18 ,  C07H15/26 ,  A61K31/7028 ,  A61K31/7056 ,  A61P35/00 ,  A61P35/04 ,  A61P29/00 ,  A61P7/02 ,  A61P3/00 ,  A61P31/00 ,  A61P9/00 ,  A61P19/02 ,  A61P25/00 ,  A61P11/06 ,  A61P9/10

CPC分类号： C07H15/04 ,  C07H3/04 ,  C07H3/06 ,  C07H11/00

摘要： The invention relates to compounds which are polysulfated oligosaccharide derivatives having activity as inhibitors of heparan sulfate-binding proteins and inhibitors of the enzyme heparanase; methods for the preparation of the compounds; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment, lowering of blood triglyceride levels and inhibition of cardiovascular disease of a mammalian subject.

摘要翻译： 本发明涉及具有作为硫酸乙酰肝素结合蛋白的抑制剂和乙酰肝素酶的抑制剂的活性的多硫酸化寡糖衍生物的化合物; 化合物的制备方法; 包含该化合物的组合物，以及其用于抗血管生成，抗转移，抗炎，抗微生物，抗凝血和/或抗血栓形成治疗的化合物及其组合物的用途，降低血液甘油三酯水平和抑制哺乳动物受试者的心血管疾病。