公开(公告)号：US20180208620A1

公开(公告)日：2018-07-26

申请号：US15872270

申请日：2018-01-16

申请人： The United States of America, as represented by the Secretary of Agriculture

发明人： Neil P. Price

IPC分类号： C07H19/06 ,  A61K31/7072 ,  A61K45/06 ,  A61P31/04 ,  A01N43/54 ,  C07H15/207 ,  A61K31/7034 ,  A01N43/16 ,  C07H19/16 ,  A61K31/7076 ,  A01N43/90

CPC分类号： C07H19/06 ,  A01N43/16 ,  A01N43/54 ,  A01N43/90 ,  A01N57/16 ,  A61K31/7034 ,  A61K31/7072 ,  A61K31/7076 ,  A61K45/06 ,  A61P31/04 ,  C07H15/207 ,  C07H19/16

摘要： Tunicamycin related compounds having an acyl chain double bond reduced and/or having an acyl chain double bond and an uracil ring double bond reduced are described as well as methods of making these tunicamycin related compounds. These tunicamycin related compounds are not toxic to eukaryotic cells and can be used to kill Gram-positive bacteria, alone or in combination with other antibiotics. Use of these tunicamycin related compounds to kill Gram-positive bacteria, treat Gram-positive bacterial diseases, and disinfect objects or surfaces are described. In addition, naturally-occurring streptovirudin compounds are not toxic to eukaryotic cells and can be used to kill Gram-positive bacteria, alone or in combination with other antibiotics.

公开(公告)号：USRE46955E1

公开(公告)日：2018-07-17

申请号：US15261470

申请日：2016-09-09

申请人： Progen PG500 Series Pty Ltd

发明人： Vito Ferro ,  Tomislav Karoli ,  Ligong Liu ,  Paul Newton Handley ,  Kenneth David Johnstone ,  Norbert Wimmer ,  Edward Timothy Hammond

IPC分类号： A61K31/70 ,  C07H15/00 ,  C07H17/02 ,  C07J43/00 ,  C07H5/02 ,  C07H5/04 ,  C07H5/06 ,  C07H11/00 ,  C07H15/04 ,  C07H15/207 ,  C07H15/24 ,  C07H15/26 ,  C07J17/00 ,  C07J41/00 ,  C07J31/00 ,  C07H3/04 ,  C07H3/06

CPC分类号： C07J43/003 ,  C07H3/04 ,  C07H3/06 ,  C07H5/02 ,  C07H5/04 ,  C07H5/06 ,  C07H11/00 ,  C07H15/04 ,  C07H15/207 ,  C07H15/24 ,  C07H15/26 ,  C07H17/02 ,  C07J17/005 ,  C07J31/006 ,  C07J41/0088 ,  C07J41/0094

摘要： The invention relates to novel compounds that have utility as inhibitors of heparan sulfate-binding proteins; compositions comprising the compounds, and use of the compounds and compositions thereof for the antiangiogenic, antimetastatic, anti-inflammatory, antimicrobial, anticoagulant and/or antithrombotic treatment of a mammalian subject.

公开(公告)号：US09994605B2

公开(公告)日：2018-06-12

申请号：US15124913

申请日：2015-03-12

申请人： UNIVERSITAET BASEL

发明人： Beat Ernst ,  Ruben Herrendorff ,  Andreas Steck ,  Fan Yang

IPC分类号： C07H15/207 ,  C07H15/203 ,  C08F2/00 ,  C08G69/10 ,  C08G69/48 ,  G01N33/68 ,  C08F120/36

CPC分类号： C07H15/207 ,  C07H15/203 ,  C08F2/00 ,  C08F120/36 ,  C08G69/10 ,  C08G69/48 ,  G01N33/6896 ,  G01N2400/02 ,  G01N2800/285

摘要： The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substituents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone.

公开(公告)号：US09890176B2

公开(公告)日：2018-02-13

申请号：US14206303

申请日：2014-03-12

申请人： Vertex Pharmaceuticals Incorporated

发明人： Evelyne Dietrich ,  Carl Poisson ,  Michel Gallant ,  Stephanie Lessard ,  Bingcan Liu ,  Sanjoy Kumar Das ,  Yeeman Ramtohul ,  Thumkunta Jagadeeswar Reddy ,  Julien Martel ,  Frederic Vallee ,  Jean-Francois Lévesque

IPC分类号： C07H15/203 ,  C07H15/20 ,  C07H15/207 ,  C07H15/22 ,  C07D493/10 ,  C07H15/18

CPC分类号： C07D493/10 ,  C07H15/18 ,  C07H15/20 ,  C07H15/203 ,  C07H15/207 ,  C07H15/22

摘要： The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

公开(公告)号：US20170369519A1

公开(公告)日：2017-12-28

申请号：US15488603

申请日：2017-04-17

申请人： POSTECH ACADEMY-INDUSTRY FOUNDATION

发明人： Young Ho RHEE ,  Mijin KIM ,  Soyeong KANG

IPC分类号： C07H17/04 ,  C07H15/04 ,  C07H3/06 ,  C07H3/04 ,  C07D407/12 ,  C07D309/10 ,  C07D307/32 ,  C07H15/207 ,  C07C43/215

CPC分类号： C07H17/04 ,  C07C43/215 ,  C07C43/315 ,  C07C2601/14 ,  C07D307/32 ,  C07D309/10 ,  C07D407/12 ,  C07H3/04 ,  C07H3/06 ,  C07H15/04 ,  C07H15/207

摘要： The present invention relates to a method for the stereoselective preparation of apiose derivatives from allylic alcohol compounds and allene compounds using catalytic asymmetric synthesis. The method for the stereoselective preparation of apiose derivatives of the present invention is based on the catalytic asymmetric synthesis from allylic alcohol compounds and allene compounds in the presence of a metal catalyst, so that apiose derivatives can be produced stereoselectively, with high yield, with high optical purity regardless of the types of substituents of the compounds. The method of the invention can also be used for the preparation of oligosaccharides including monosaccharides, disaccharides, and polysaccharides or various compounds including apiose derivatives because the method can minimize the production of by-products without using an activating group, unlike the conventional method for the preparation of adipose derivatives.

公开(公告)号：US20170296566A9

公开(公告)日：2017-10-19

申请号：US15025730

申请日：2014-09-29

申请人： GLYCOMIMETICS, INC.

发明人： John L. MAGNANI ,  John M. PETERSON ,  Ingrid G. WINKLER

IPC分类号： A61K31/7034 ,  A61K38/18 ,  A61K31/7048 ,  A61K31/7056 ,  C07H15/207 ,  A61K45/06

CPC分类号： A61K31/7034 ,  A61K31/7048 ,  A61K31/7056 ,  A61K38/1825 ,  A61K45/06 ,  C07H15/207 ,  A61K2300/00

摘要： Methods for treating and/or preventing mucositis comprising administering to a subject in need thereof an effective amount of at least one compound chosen from E-selectin antagonists, pharmaceutically acceptable salts of E-selectin antagonists, prodrugs of E-selectin antagonists, and pharmaceutically acceptable salts of prodrugs of E-selectin antagonists, and compositions comprising at least one of such compound.

公开(公告)号：US20160194667A1

公开(公告)日：2016-07-07

申请号：US15076830

申请日：2016-03-22

申请人： Asahi Kasei Chemicals Corporation

发明人： Kazunobu Konishi ,  Shinichi Imazu ,  Mayumi Sato

IPC分类号： C12P7/02 ,  C07H15/207 ,  C12N9/16 ,  C12N9/90

CPC分类号： C12P7/02 ,  C07H15/207 ,  C12N9/16 ,  C12N9/90 ,  C12N15/70 ,  C12P19/46 ,  C12Y301/03025 ,  C12Y505/01004 ,  Y02P20/52

摘要： To impart significantly improved myo-inositol producing capability, suitable for use in recombinant DNA techniques and synthetic biology methods, to a host microorganism that does not possess an endogenous myo-inositol biosynthesis pathway, such as Escherichia coli. Inositol monophosphatase activity is strengthened in a transformant obtained by introducing a myo-inositol biosynthesis pathway into a host microorganism that does not possess an endogenous myo-inositol biosynthesis pathway.

摘要翻译： 赋予不具有内源性肌醇 - 肌醇生物合成途径的宿主微生物如大肠杆菌显着改善适用于重组DNA技术和合成生物学方法的肌醇产生能力。 在通过将肌醇生物合成途径引入不具有内源肌内肌醇生物合成途径的宿主微生物获得的转化体中，肌醇单磷酸酶活性得到加强。

公开(公告)号：US20150025030A1

公开(公告)日：2015-01-22

申请号：US14383557

申请日：2013-06-08

申请人： ZHEJIANG YONGNING PHARMACEUTICAL CO LTD

发明人： Fengqi Ye ,  Ben Cai ,  Min Lu ,  Yongling Chen

IPC分类号： C07H15/207

CPC分类号： C07H15/207 ,  C07D309/04 ,  C07H7/04

摘要： A hydroxysafflor yellow A sodium compound as shown in a formula (I) and preparation as well as medicinal application thereof are provided. According to the present invention, the safflower is utilized as a raw material. A monomer pharmaceutical compound, the hydroxysafflor yellow A sodium, is obtained by sufficient processes, and a purity thereof is surely above 98.5%. Therefore, the hydroxysafflor yellow A sodium is a monomer compound, which is safer, more effective, more stable and more controllable than hydroxysafflor yellow A, for treating blood circulation disorders such as platelet aggregation, coronary heart disease, angina pectoris and acute cerebral ischemia. Furthermore, the hydroxysafflor yellow A sodium has sufficient solubility and human tolerance.

摘要翻译： 提供了式（I）所示的羟基花青黄A钠化合物及其制备方法及其药用。 根据本发明，红花被用作原料。 通过充分的方法获得单体药物化合物羟基红花黄A钠，其纯度肯定在98.5％以上。 因此，羟基红花黄A钠是一种单体化合物，其用于治疗血液循环障碍如血小板聚集，冠心病，心绞痛和急性脑缺血，比羟基红花黄A更安全，更有效，更稳定和更可控。 此外，羟基花青黄A钠具有足够的溶解度和人的耐受性。

公开(公告)号：US20140303096A1

公开(公告)日：2014-10-09

申请号：US14242916

申请日：2014-04-02

申请人： Dania Birte REICHE ,  Laura JOHNSTON ,  Nicole MOHREN

发明人： Dania Birte REICHE ,  Laura JOHNSTON ,  Nicole MOHREN

IPC分类号： C07H15/207

CPC分类号： A61K31/7034 ,  A61K9/0019 ,  A61K9/0031 ,  A61K9/0053 ,  A61K9/02 ,  A61K9/20 ,  A61K9/2018 ,  A61K9/48 ,  A61K9/4866 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61K47/545 ,  C07H15/207

摘要： The present invention relates to SGLT2 inhibitor or a pharmaceutically acceptable form thereof for use in the treatment and/or prevention of a metabolic disorder of an equine animal. In particular, the present invention relates the SGLT2 inhibitor or a pharmaceutically acceptable form thereof for use in the treatment and/or prevention of insulin resistance, hyperinsulinemia, impaired glucose tolerance, dyslipidemia, dysadipokinemia, subclinical inflammation, systemic inflammation, low grade systemic inflammation, obesity, and/or regional adiposity in an equine animal.

摘要翻译： 本发明涉及用于治疗和/或预防马动物代谢紊乱的SGLT2抑制剂或其药学上可接受的形式。 特别地，本发明涉及用于治疗和/或预防胰岛素抵抗，高胰岛素血症，葡萄糖耐量异常，血脂异常，血管兴奋素血症，亚临床炎症，全身性炎症，低度全身性炎症的SGLT2抑制剂或其药学上可接受的形式， 肥胖和/或马类动物中的局部肥胖。

公开(公告)号：US08846880B2

公开(公告)日：2014-09-30

申请号：US12994059

申请日：2009-05-20

申请人： Valérie Quesniaux Ryffel ,  Olivier Martin ,  Sophie Front

发明人： Valérie Quesniaux Ryffel ,  Olivier Martin ,  Sophie Front

IPC分类号： C07H15/00 ,  C07H21/00 ,  C07H15/207

CPC分类号： C07H15/207

摘要： The present invention relates to novel synthetic analogs of phosphatidyl-myo-inositol mannosides (hereinafter referred to as PIMs) of general formula (I): or a pharmaceutically acceptable salt thereof, to the method for preparing same and to the use thereof in the prevention or treatment of a disease associated with the overexpression of cytokines or of chemokines, in particular of TNF and/or of IL-12. The invention also relates to a pharmaceutical composition comprising at least one synthetic derivative of PIM.

摘要翻译： 本发明涉及通式（I）所示的磷脂酰肌醇甘露糖苷（以下称为PIM）的新型合成类似物或其药学上可接受的盐及其制备方法及其在预防中的应用 或治疗与细胞因子或趋化因子特别是TNF和/或IL-12的过度表达相关的疾病。 本发明还涉及包含PIM的至少一种合成衍生物的药物组合物。