公开(公告)号：US20240180945A1

公开(公告)日：2024-06-06

申请号：US18493421

申请日：2023-10-24

Applicant: SyneuRx International (Taiwan) Corp.

Inventor： Guochuan Emil Tsai ,  Yi-Wen Mao ,  Lu-Ping Lu ,  Wei-Hua Chang ,  Han-Yi Hsieh ,  Jhe Wei Hu ,  Tsai-Miao Shih ,  ChanHui Huang

IPC: A61K31/7048 ,  A23L33/00 ,  A23L33/10 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  A61P25/18 ,  C07C69/90 ,  C07D207/34 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26

CPC classification number: A61K31/7048 ,  A23L33/10 ,  A23L33/40 ,  A61K31/235 ,  A61K31/36 ,  A61K31/40 ,  A61K31/415 ,  A61K31/7034 ,  A61P25/18 ,  C07C69/90 ,  C07D207/34 ,  C07D231/14 ,  C07D317/68 ,  C07H15/22 ,  C07H15/26 ,  A23V2002/00

Abstract: A compound of Formula (I):




or a pharmaceutically acceptable salt thereof, in which Ring X is a 3 to 7 membered monocyclic ring, at least one of R1, R2, R3, and R4 is OR5 or CH2OR5 and the other R1, R2, R3, and R4 each independently are halogen, OH, OR5, CH2OR5, CO2H, OC═OR6, (C═O)R6, R6, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, H, or absent. Also provided herein are therapeutic uses of the compound of Formula (I).

公开(公告)号：US20190117748A1

公开(公告)日：2019-04-25

申请号：US16092137

申请日：2017-04-06

Applicant: BRANDEIS UNIVERSITY

Inventor： Isaac J. KRAUSS ,  Joel Sebastian TEMME

IPC: A61K39/00 ,  C12N15/117 ,  C07H15/22 ,  A61K39/39 ,  C12N15/115 ,  A61P31/18

CPC classification number: A61K39/0005 ,  A61K39/39 ,  A61K2039/51 ,  A61K2039/545 ,  A61P31/18 ,  C07H15/22 ,  C07H21/04 ,  C12N15/10 ,  C12N15/115 ,  C12N15/117 ,  C12N2310/13 ,  C12N2310/16 ,  C12N2310/351 ,  C12N2320/30

Abstract: Disclosed are oligonucleotides that binds specifically to HIV neutralizing monoclonal antibody 2G12 with a K4 value lower than 20 nM, the oligonucleotide comprising a predicted structure, at 37° C., having exactly one stem-loop whereby the loop comprises the nucleotide sequence of AACCNACGGANAAA (SEQ ID NO: 1), where N is a modified nucleoside base, and the stem includes at least 3 nucleotide base-pairs and one of the nucleotides in the stem includes a modified nucleoside base, wherein the modified nucleoside base has the structure -B-L-A where A is a branched-chain Man9 oligosaccharide, L is a linker molecule, and B is independently a pyrimidine or pyridine base linked to the sugar-phosphate backbone of the oligonucleotide. Immunogenic conjugates that include the oligonucleotide, and pharmaceutical compositions that include the oligonucleotide or the immunogenic conjugate are also disclosed. Various method of using the oligonucleotides, immunogenic conjugates, and pharmaceutical compositions are also disclosed.

公开(公告)号：US09890176B2

公开(公告)日：2018-02-13

申请号：US14206303

申请日：2014-03-12

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： 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: C07H15/203 ,  C07H15/20 ,  C07H15/207 ,  C07H15/22 ,  C07D493/10 ,  C07H15/18

CPC classification number: C07D493/10 ,  C07H15/18 ,  C07H15/20 ,  C07H15/203 ,  C07H15/207 ,  C07H15/22

Abstract: 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：US20160040206A1

公开(公告)日：2016-02-11

申请号：US14831519

申请日：2015-08-20

Applicant: iNtRON Biotechnology, Inc.

Inventor： Yeo Joon Yoon ,  Sung Ryeol Park ,  Je Won Park ,  Jae Kyung Sohng

IPC: C12P19/48 ,  C12N15/76 ,  C07H15/234 ,  C12N15/52

CPC classification number: C12P19/485 ,  A61K31/351 ,  A61K31/7036 ,  C07H15/22 ,  C07H15/234 ,  C12N15/52 ,  C12N15/76 ,  C12R1/61 ,  Y02A50/473

Abstract: Vectors expressing kanA-kanB-kanK and other kanamycin production-related genes, Streptomyces species recombinant bacteria transformed with the vectors, a method of producing kanamycin antibiotics by the bacteria, and a new kanamycin compound produced by the bacterium are provided. With the use of the recombinant bacteria of the present invention, the direct fermentative biosynthesis of amikacin and tobramycin as semi-synthetic kanamycins is possible, and the yield of kanamycin B as a precursor of the semi-synthetic kanamycin is improved.

Abstract translation: 表达kanA-kanB-kanK和其他卡那霉素生产相关基因的载体，用载体转化的链霉菌属重组细菌，细菌产生卡那霉素抗生素的方法和由细菌产生的新的卡那霉素化合物。 通过使用本发明的重组细菌，可以直接发酵生物合成作为半合成的卡那霉素的阿米卡星和妥布霉素作为半合成卡那霉素的前体的卡那霉素B的产率。

公开(公告)号：US09080169B2

公开(公告)日：2015-07-14

申请号：US13701849

申请日：2011-06-10

Applicant: Isaac Jonathan Krauss ,  Lizbeth K. Hedstrom ,  Iain S. MacPherson

Inventor： Isaac Jonathan Krauss ,  Lizbeth K. Hedstrom ,  Iain S. MacPherson

IPC: C12Q1/68 ,  C12P19/34 ,  C07H21/04 ,  C12N15/10 ,  C07H15/22

CPC classification number: C07H21/04 ,  A61K39/21 ,  A61K47/549 ,  A61K47/646 ,  A61K2039/55505 ,  A61K2039/55511 ,  A61K2039/6068 ,  A61K2039/6081 ,  A61K2039/627 ,  C07H15/22 ,  C12N7/00 ,  C12N15/1048 ,  C12N15/1058

Abstract: Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative.

Abstract translation: 本文描述了可用作针对一种或多种人或兽医治疗适应症的疫苗的寡糖 - 寡核苷酸缀合物，以及合成和鉴定它们的方法。 可以使用非人抗体作为结合靶标鉴定缀合物，从而扩大本发明的功能和范围。 有效的缀合物可以通过迭代来鉴定。

公开(公告)号：US08895510B2

公开(公告)日：2014-11-25

申请号：US12418774

申请日：2009-04-06

Applicant: John L. Magnani

Inventor： John L. Magnani

IPC: A61K31/7064 ,  C07H15/22 ,  A61P9/10

CPC classification number: C07H15/26 ,  A61K31/7034 ,  A61K31/7036 ,  A61K31/7064 ,  C07H15/22

Abstract: Compounds, compositions and methods are provided for treatment of diseases or complications associated therewith, in which a selectin plays a role. More specifically, particular glycomimetics and uses thereof are described. For example, use of particular glycomimetics for treating sickle cell disease or a cancer involving a selectin, or complications associated with either, is described.

Abstract translation: 提供化合物，组合物和方法用于治疗与其相关的疾病或并发症，其中选择素起作用。 更具体地，描述了特定的糖模拟物及其用途。 例如，描述了使用特定的糖模拟物来治疗镰状细胞病或涉及选择蛋白的癌症，或与之有关的并发症。

公开(公告)号：US20130116417A1

公开(公告)日：2013-05-09

申请号：US13701849

申请日：2011-06-10

Applicant: Isaac J. Krauss ,  Lizbeth K. Hedstrom ,  Iain S. MacPherson

Inventor： Isaac J. Krauss ,  Lizbeth K. Hedstrom ,  Iain S. MacPherson

IPC: C12N15/10 ,  C07H15/22 ,  C07H21/04

CPC classification number: C07H21/04 ,  A61K39/21 ,  A61K47/549 ,  A61K47/646 ,  A61K2039/55505 ,  A61K2039/55511 ,  A61K2039/6068 ,  A61K2039/6081 ,  A61K2039/627 ,  C07H15/22 ,  C12N7/00 ,  C12N15/1048 ,  C12N15/1058

Abstract: Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative.

Abstract translation: 本文描述了可用作针对一种或多种人或兽医治疗适应症的疫苗的寡糖 - 寡核苷酸缀合物，以及合成和鉴定它们的方法。 可以使用非人抗体作为结合靶标鉴定缀合物，从而扩大本发明的功能和范围。 有效的缀合物可以通过迭代来鉴定。

公开(公告)号：US08410066B2

公开(公告)日：2013-04-02

申请号：US12768173

申请日：2010-04-27

Applicant: John L. Magnani ,  Arun K. Sarkar

Inventor： John L. Magnani ,  Arun K. Sarkar

IPC: A61K31/7036 ,  C07H17/02 ,  C07H15/207 ,  C07H3/06

CPC classification number: C07H15/26 ,  A61K31/7034 ,  A61K31/7052 ,  A61K31/7064 ,  C07H15/207 ,  C07H15/22

Abstract: Compounds, compositions and methods are provided for treating cancer and inflammatory diseases, and for releasing cells such as stem cells (e.g., bone marrow progenitor cells) into circulating blood and enhancing retention of the cells in the blood. More specifically, heterobifunctional compounds that inhibit both E-selectins and CXCR4 chemokine receptors are described.

Abstract translation: 提供化合物，组合物和方法用于治疗癌症和炎性疾病，以及用于将细胞例如干细胞（例如骨髓祖细胞）释放到循环血液中并增强细胞在血液中的保留。 更具体地，描述了抑制E-选择蛋白和CXCR4趋化因子受体的异双功能化合物。

公开(公告)号：US08198419B2

公开(公告)日：2012-06-12

申请号：US13018811

申请日：2011-02-01

Applicant: Jon Thorson

Inventor： Jon Thorson

IPC: C07H17/08 ,  C07H15/00 ,  C07H17/00 ,  C07G11/00 ,  A01N43/04 ,  A61K31/70

CPC classification number: C07H1/00 ,  C07H15/207 ,  C07H15/22 ,  C07H17/08

Abstract: The present invention provides glycorandomaized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.

Abstract translation: 本发明提供了用于快速产生多糖化结构化文库的糖多糖结构和组合方法，包括在糖基转移酶存在下孵育一种或多种糖苷和一组NDP-糖。 糖基转移酶可以是与天然次生代谢产物相关或参与生产天然次生代谢产物，或与天然次生代谢产物相关或参与生产天然次生代谢产物相关或相关的糖基转移酶。 糖基转移酶对于其NDP-糖供体和/或其糖苷酸可显示出显着的灵活性。 NDP-糖供体可以是可商购的，或者可以通过利用相对于其底物具有显着柔性的突变体或野生型核苷酸转移酶来产生。

公开(公告)号：US08071535B2

公开(公告)日：2011-12-06

申请号：US10571510

申请日：2004-09-10

Applicant: Yitzhak Tor ,  Nathan Luedtke

Inventor： Yitzhak Tor ,  Nathan Luedtke

IPC: A61K31/70 ,  A61K38/00 ,  C07H15/22 ,  C08B5/10 ,  C08B11/00

CPC classification number: A61K31/7034 ,  A61K31/704 ,  A61K31/7048 ,  A61K47/552 ,  A61K49/0043 ,  A61K49/0052 ,  C07H15/22

Abstract: Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.

Abstract translation: 提供了可用于合成包含胍基化的环状缩醛的缀合物的试剂和方法。 还提供了增加各种治疗化合物的细胞摄取和使用这些缀合物的治疗方式的方法。