公开(公告)号：US11891413B2

公开(公告)日：2024-02-06

申请号：US16768350

申请日：2018-11-30

申请人： Idorsia Pharmaceuticals Ltd

发明人： Arun Naini ,  Daniel Knopp ,  Bopanna Monnanda ,  Arne Von Bonin ,  Claney Lebev Pereira

IPC分类号： C07H3/06 ,  A61K47/54 ,  A61K31/33 ,  A61K31/335 ,  A61K31/702 ,  A61K39/108 ,  C07H15/20 ,  G01N33/569 ,  A61K39/00 ,  C07H15/04 ,  C07H15/08

CPC分类号： C07H3/06 ,  A61K31/33 ,  A61K31/335 ,  A61K31/702 ,  A61K39/0266 ,  A61K47/549 ,  C07H15/20 ,  G01N33/56916 ,  A61K2039/6037 ,  C07H15/04 ,  C07H15/08 ,  G01N2333/26

摘要： The present invention relates to a synthetic oligosaccharide of general formula (I): T*-[(—Ux+4—Ux+3—Ux+2—Ux+1—Ux)m—(Vx+2—Vx+1—Vx)1-m-T-O-L-E that is related to Klebsiella pneumoniae serotype O3, O3b and/or O5 lipopolysaccharide and conjugate thereof. Said synthetic oligosaccharide, said conjugate and pharmaceutical composition containing said synthetic oligosaccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic oligosaccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae serotype O3, O3b and/or O5 bacteria.

公开(公告)号：US20210171563A1

公开(公告)日：2021-06-10

申请号：US16762724

申请日：2018-11-08

申请人： Washington University

发明人： Vasilios Kalas ,  James W. Janetka ,  Scott Hultgren ,  Jerry Pinkner ,  Amarendar Maddirala ,  Vishnu Damalanka

IPC分类号： C07H15/203 ,  A61K45/06 ,  A61K31/7034 ,  C07H15/20 ,  C07H17/02 ,  A61K31/706 ,  C07H17/04 ,  A61K31/7048 ,  A61K31/7056 ,  C07H15/26

摘要： The present invention is directed to various compounds, compositions, and methods for treating bacterial infections such as urinary tract infections.

公开(公告)号：US09938562B2

公开(公告)日：2018-04-10

申请号：US15035152

申请日：2014-11-03

申请人： Glycosynth Limited

发明人： Hayley Jane Turner ,  Michael Burton

IPC分类号： C12Q1/34 ,  C07H15/20 ,  C07H15/203

CPC分类号： C12Q1/34 ,  C07H15/20 ,  C07H15/203 ,  G01N2333/938

摘要： Conjugates of 2,3-dihydroxynaphthalene and its derivatives with enzyme cleavable groups are chromogenic substrates that form colored compounds when complexed with metal ions, e.g. iron ions, on cleavage by enzymes, and are useful in microbial detection and identification. The cleavage products form purple or red-brown colored complexes, that can easily be observed by the naked eye. Microbes can be grown in the presence of the substrates and the metal salts that provide the metal ion for complexing with the 2,3-dihydroxynaphthalene product. Substituents in the naphthalene ring may affect the solubility of the substrates and also the diffusibility and color of the metal complexes. Some of the substrates yield soluble complexes on cleavage and are of particular value in liquid growth media. Other substrates produce less soluble complexes that are more suitable for use in solid agar media. Methods of synthesizing the substrates are described.

公开(公告)号：US09834575B2

公开(公告)日：2017-12-05

申请号：US14191331

申请日：2014-02-26

申请人： TriAct Therapeutics, Inc.

发明人： Thomas F. White ,  Steven Smith

IPC分类号： A61K31/7012 ,  A61K31/7034 ,  C07H15/20 ,  C07F9/12 ,  A61K31/662 ,  A61K45/06 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/661 ,  C07H15/203

CPC分类号： C07H15/20 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/661 ,  A61K31/662 ,  A61K31/7012 ,  A61K31/7034 ,  A61K45/06 ,  C07F9/12 ,  C07H15/203 ,  A61K2300/00

摘要： The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor metabolite. Catecholic butane metabolites can serve as dual kinase inhibitors for purposes of methods described herein.

公开(公告)号：US09822058B2

公开(公告)日：2017-11-21

申请号：US14390190

申请日：2013-03-13

申请人： CHDI FOUNDATION, INC.

发明人： Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Michael Prime ,  William Leonard Mitchell ,  Peter Johnson ,  Naomi Went

IPC分类号： C07C62/38 ,  C07D307/94 ,  C07D309/10 ,  C07D215/18 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D233/64 ,  C07D235/26 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07C317/44 ,  C07D413/08 ,  C07D413/10 ,  C07C323/62 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07D257/04 ,  C07D203/08 ,  C07D263/58 ,  C07C235/82 ,  C07D207/08 ,  C07D271/07 ,  C07D207/337 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/80 ,  C07C69/757 ,  C07D203/10 ,  C07D307/79 ,  C07D413/12 ,  C07H15/20

CPC分类号： C07C62/38 ,  C07C69/757 ,  C07C229/22 ,  C07C229/46 ,  C07C229/48 ,  C07C235/82 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2602/50 ,  C07D203/08 ,  C07D203/10 ,  C07D207/08 ,  C07D207/337 ,  C07D215/18 ,  C07D233/64 ,  C07D235/26 ,  C07D257/04 ,  C07D263/58 ,  C07D271/07 ,  C07D295/155 ,  C07D305/06 ,  C07D305/08 ,  C07D307/54 ,  C07D307/79 ,  C07D307/80 ,  C07D307/94 ,  C07D309/10 ,  C07D311/58 ,  C07D317/46 ,  C07D317/60 ,  C07D319/18 ,  C07D403/10 ,  C07D405/08 ,  C07D405/10 ,  C07D405/12 ,  C07D413/08 ,  C07D413/10 ,  C07D413/12 ,  C07H15/20

摘要： Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US20170247401A1

公开(公告)日：2017-08-31

申请号：US15373260

申请日：2016-12-08

申请人： Washington University

发明人： James W. Janetka ,  Zhenfu Han ,  Scott Hultgren ,  Jerome S. Pinkner ,  Corinne Cusumano

IPC分类号： C07H15/20 ,  C07H15/26

CPC分类号： C07H15/20 ,  A01N43/10 ,  A01N43/16 ,  A01N43/38 ,  A01N43/42 ,  A01N43/52 ,  A01N43/54 ,  A01N43/76 ,  A01N43/78 ,  A01N47/36 ,  A01N55/08 ,  A61K31/505 ,  A61K31/7034 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61K31/706 ,  C07D309/10 ,  C07H15/203 ,  C07H15/207 ,  C07H15/22 ,  C07H15/26 ,  C07H19/056

摘要： The present invention encompasses compounds and methods for treating urinary tract infections.

公开(公告)号：US09422325B2

公开(公告)日：2016-08-23

申请号：US14505808

申请日：2014-10-03

申请人： Trustees of Tufts College

发明人： Clay S. Bennett ,  An-Hsiang A. Chu

IPC分类号： C07J17/00 ,  C07H15/20 ,  C07H3/06 ,  C07H3/04 ,  C07H1/00 ,  C07H15/02 ,  C08B37/00 ,  C07H3/02 ,  C07H15/18 ,  C07H15/203 ,  C07J41/00

CPC分类号： C07J17/005 ,  C07H1/00 ,  C07H3/02 ,  C07H3/04 ,  C07H3/06 ,  C07H15/18 ,  C07H15/203 ,  C07J41/0055 ,  C07J41/0088 ,  C08B37/00

摘要： Provided are methods for the preparation of glycosylation products, including those represented by formula I: Sugar-O—R′  I comprising the step of combining R′—OH, a glycosyl sulfide glycosyl donor (“thioglycoside donor”), a hypervalent iodine alkyl-transfer activating reagent, and a base. In an embodiment, the hypervalent iodine alkyl-transfer activating reagent is (phenyl(trifluoroethyl)iodonium triflimide).

摘要翻译： 提供制备糖基化产物的方法，包括由式I表示的糖基化产物：糖-O-R'I包括将R'-OH，糖硫基糖苷供体（“硫代糖苷供体”），高价烷基烷基 转移活化试剂和碱。 在一个实施方案中，高价烷基转移活化剂是（苯基（三氟乙基）碘鎓三氟甲磺酰亚胺）。

公开(公告)号：US09399656B2

公开(公告)日：2016-07-26

申请号：US14264361

申请日：2014-04-29

申请人： Microbial Chemistry Research Foundation

发明人： Koichi Nakae ,  Fukiko Kojima

IPC分类号： C07H15/22 ,  C07H15/20 ,  C12P17/06 ,  C12R1/01 ,  C12P19/48

CPC分类号： C07H15/22 ,  C07H15/20 ,  C12P17/06 ,  C12P19/48 ,  C12R1/01

摘要： A compound represented by the following Structural Formula (A) or a salt thereof. The compound or the salt thereof is suitably produced from a microorganism belonging to the genus Saccharothrix and can be suitably used as a prostaglandin production inhibitor.

摘要翻译： 由以下结构式（A）表示的化合物或其盐。 化合物或其盐适宜地由属于蔗糖属属的微生物产生，可以适当地用作前列腺素产生抑制剂。

公开(公告)号：US09249171B2

公开(公告)日：2016-02-02

申请号：US14402231

申请日：2013-05-22

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Adrian Ortiz ,  Tamas Benkovics ,  Zhongping Shi ,  Prashant P. Deshpande ,  Zhiwei Guo ,  David R. Kronenthal ,  Chris Sfouggatakis

IPC分类号： C07H15/20 ,  C07H19/06 ,  C12P19/38 ,  C07D309/10 ,  C07D407/04 ,  C07D307/20

CPC分类号： C07H15/20 ,  C07D307/20 ,  C07D309/10 ,  C07D407/04 ,  C07H19/06 ,  C12P19/385

摘要： A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and sulfoxide process steps later on.

摘要翻译： 制备式I化合物的方法利用起始化合物以及稍后的亚硫酰亚胺和亚砜工艺步骤。

公开(公告)号：US09238669B2

公开(公告)日：2016-01-19

申请号：US14236620

申请日：2012-07-30

申请人： Peter H. Seeberger ,  Christopher E. Martin ,  Felix Broecker ,  Chakkumkal Anish

发明人： Peter H. Seeberger ,  Christopher E. Martin ,  Felix Broecker ,  Chakkumkal Anish

IPC分类号： C07H15/04 ,  C07H3/06 ,  C07H5/04 ,  C07H3/08 ,  C07H13/08 ,  C07H15/20 ,  C07K16/12 ,  G01N33/569

CPC分类号： C07H3/06 ,  C07H3/08 ,  C07H5/04 ,  C07H13/08 ,  C07H15/04 ,  C07H15/20 ,  C07K16/1282 ,  G01N33/56911

摘要： The invention relates to a synthetic oligosaccharide representing part of the repeating unit of the Clostridium difficile glycopolymer PS-I and having the sequence of the pentasaccharide a-L-Rhap-(1→3)-β-D-Glcp-(1→4)-[a-L-Rhap-(1→3]-a-D-Glcp-(1→2)-a-D-Glcp or a synthetic fragment or derivative thereof. Preferably, the claimed synthetic oligosaccharide bears at least one linker L for conjugation to a carrier protein or for immobilization on a surface. Further aspects of the invention relate to advantageous methods for synthesizing said synthetic oligosaccharide and oligosaccharide-protein conjugate as well as to uses thereof, in particular as vaccines and diagnostic tools.

摘要翻译： 本发明涉及代表艰难梭菌聚糖聚合物PS-1的重复单元的一部分的合成寡糖，其具有五糖aL-Rhap-（1→3） - ＆amp; Gr-D-Glcp-（1→4） - [aL-Rhap-（1→3）-aD-Glcp-（1→2）-aD-Glcp或其合成片段或衍生物。优选地，所要求保护的合成寡糖至少具有一个连接体L， 本发明的其它方面涉及用于合成所述合成寡糖和寡糖 - 蛋白质结合物的有利方法以及其用途，特别是疫苗和诊断工具。