公开(公告)号：US20230348365A1

公开(公告)日：2023-11-02

申请号：US18156226

申请日：2023-01-18

Applicant: HORITZONTS TECNOLOGICS HUNGARY KORLÁTOLT FELELOSSÉGU TÁRSASÁG

Inventor： Alfredo HERNÁNDEZ CABANILLAS ,  Santiago MADERUELO CORRAL ,  Montserrat ORTEGA DOMÉNECH ,  Diego Fernando ROSERO VALENCIA ,  Ángel RUMBERO SÁNCHEZ ,  Victor TENA PÉREZ

IPC: C07C243/34 ,  A61P31/10 ,  C07C243/28 ,  C07C259/06

CPC classification number: C07C243/34 ,  A61P31/10 ,  C07C243/28 ,  C07C259/06

Abstract: The invention relates to hydrazide compounds and their use in medicine, particularly in treating and/or preventing infections caused by a fungus.

公开(公告)号：US20220016253A1

公开(公告)日：2022-01-20

申请号：US17311338

申请日：2019-12-05

Applicant: B. G. Negev Technologies and Applications Ltd., at Ben-Gurion University

Inventor： Eliahu HELDMAN ,  Moshe KUSHNIR ,  Eleonora SHAUBI

IPC: A61K47/54 ,  C07C235/34 ,  C07C243/28 ,  C07C243/34 ,  C07C231/12

Abstract: The present invention provides conjugates comprising a sugar such as mannitol and one or more L-DOPA and/or DOPA decarboxylse inhibitors including, inter alia, L-DOPA, carbidopa, benserazide, or a combination thereof, wherein the sugar is conjugated to the carboxyl group of the L-DOPA and/or DOPA decarboxylse inhibitor/ s) via a hydroxyl group of the sugar. The present invention further provides related pharmaceutical compositions and methods of producing the conjugates, as well as methods of use for treating medical disorders responsive to dopamininergic stimulation such as movement disorders including, inter alia, Parkinson's Disease.

公开(公告)号：US20210163424A1

公开(公告)日：2021-06-03

申请号：US17248924

申请日：2021-02-12

Applicant: NDSU RESEARCH FOUNDATION

Inventor： Jayaraman Sivaguru ,  Akila Iyer ,  Mukund Sibi ,  Dean Webster ,  Saravana Kumar Rajendran ,  Ramya Raghunathan ,  Ravichandanath Singathi ,  Retheesh Krishnan ,  Anthony Clay

IPC: C07D239/88 ,  C07C243/34 ,  C07D207/24 ,  C08F120/14 ,  C07C243/30 ,  C07C243/28 ,  C07D209/48 ,  C07C243/38 ,  C08F2/48

Abstract: The invention relates to novel hydrazide-based templates, methods of making the same, and methods of using the hydrazide-based templates as molecular scaffolds for asymmetric light driven transformations, light driven material synthesis, and biological applications. Furthermore, the present invention relates to photoinitiators, monomers, and polymers derived from biomass, together with methods and methods of using the same.

公开(公告)号：US20210059966A1

公开(公告)日：2021-03-04

申请号：US16923396

申请日：2020-07-08

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Adam D. Hughes ,  Erik Fenster ,  Melissa Fleury ,  Roland Gendron ,  Edmund J. Moran

IPC: A61K31/197 ,  C07C243/26 ,  C07C271/22 ,  C07D317/40 ,  C07C231/02 ,  C07D319/06 ,  C07D207/263 ,  C07C233/56 ,  C07C243/30 ,  A61K31/24 ,  A61K31/27 ,  A61K31/365 ,  A61K45/06 ,  C07C243/28

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US10704076B2

公开(公告)日：2020-07-07

申请号：US16224006

申请日：2018-12-18

Applicant: University of Cincinnati ,  Government of the United States as Represented by the Secretary of the Air Force

Inventor： Daniel J. Hassett ,  Thomas J. Lamkin ,  Warunya Panmanee ,  Deborah E. Taylor ,  Chloe J. A. Shea

IPC: C12Q1/18 ,  A61K31/175 ,  A61K31/18 ,  A61K31/343 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/435 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A01N37/10 ,  A01N37/28 ,  A01N41/06 ,  A01N43/12 ,  A61K31/216 ,  A01N43/38 ,  A01N43/42 ,  A01N43/44 ,  A01N43/52 ,  A01N43/54 ,  A01N43/56 ,  A01N43/80 ,  A01N43/82 ,  A01N43/90 ,  A01N47/38 ,  C07C69/738 ,  C07C243/28 ,  C07C311/21 ,  C07D209/08 ,  C07D215/52 ,  C07D215/56 ,  C07D231/20 ,  C07D235/18 ,  C07D271/12 ,  C07D275/03 ,  C07D307/92 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D471/04 ,  C07D491/052

Abstract: A high through-put screening method for identifying agents effective for inhibiting biofilm formation and/or killing established biofilm are disclosed. The method includes three tiers, and each tier includes three specific biological process assays. The tier levels are a primary screen, a confirmation screen, and a dose-response screen, and the biological process assays include assays for total bacterial growth, bacterial metabolic activity, and biofilm formation. The series of assays may be run once or more than once at each tier. A library of compounds is subject to tier A and only compounds meeting a primary parameter advance to tier B, and only tier B compounds meeting a confirmation parameter advance to tier C, and only tier C compounds meeting a dose-response parameter are identified as putative agents effective for inhibiting and/or eradicating a biofilm, further wherein the assays are conducted for each compound subject to the respective tier. The method is effective and validated for identifying agents which inhibit and/or kill Staphylococcus epidermidis, Pseudomonas aeruginosa, and Acinetobacter baumannii biofilms. Agents identified according to the high through-put screen and validated in follow-up experiments as effective for inhibiting and/or killing bacterial biofilms are also disclosed.

公开(公告)号：US20190054083A1

公开(公告)日：2019-02-21

申请号：US15895883

申请日：2018-02-13

Applicant: CASE WESTERN RESERVE UNIVERSITY

Inventor： Chris Dealwis

IPC: A61K31/496 ,  C07D209/48 ,  C07C243/28 ,  C07C237/22 ,  A61K31/223 ,  A61K31/495 ,  A61K45/06 ,  A61K31/165 ,  A61K31/166 ,  A61K31/4035 ,  A61K31/4152 ,  C07D295/088

Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.

公开(公告)号：US09889129B2

公开(公告)日：2018-02-13

申请号：US14387151

申请日：2013-03-21

Applicant: Case Western Reserve University

Inventor： Chris Dealwis

IPC: A61K31/496 ,  A61K31/495 ,  A61K45/06 ,  A61K31/165 ,  A61K31/166 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/223 ,  C07C237/22 ,  C07C243/28 ,  C07D209/48 ,  C07D295/088

CPC classification number: A61K31/496 ,  A61K31/165 ,  A61K31/166 ,  A61K31/223 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/495 ,  A61K45/06 ,  C07C237/22 ,  C07C243/28 ,  C07D209/48 ,  C07D295/088 ,  A61K2300/00

Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.

公开(公告)号：US20160052871A1

公开(公告)日：2016-02-25

申请号：US14781242

申请日：2014-04-18

Applicant: ADESSO ADVANCED MATERIALS WUXI CO., LTD.

Inventor： Bing Qin ,  Xin Li ,  Bo Liang

IPC: C07C243/38 ,  C08K7/06 ,  C07C241/02 ,  C07C243/28 ,  C07C213/02 ,  C07C201/12 ,  C08G59/14 ,  C07C217/84

CPC classification number: C07C243/38 ,  C07C201/12 ,  C07C213/02 ,  C07C217/84 ,  C07C241/02 ,  C07C243/28 ,  C08G59/1477 ,  C08G59/50 ,  C08J5/24 ,  C08J11/16 ,  C08J11/26 ,  C08K7/06 ,  Y02W30/705 ,  Y02W30/706

Abstract: The present invention provides, among others, compounds of Formula (I) or a salt thereof, methods for making these compounds, degradable polymers and reinforced composites made therefrom, and methods for degrading and/or recycling the degradable polymers and reinforced composites.

Abstract translation: 本发明尤其提供了式（I）化合物或其盐，制备这些化合物的方法，可降解聚合物和由其制备的增强复合材料，以及降解和/或再循环可降解聚合物和增强复合材料的方法。

公开(公告)号：US20150314017A1

公开(公告)日：2015-11-05

申请号：US14799712

申请日：2015-07-15

Applicant: Dr. Robert Yongxin Zhao ,  SUZHOU M-CONJ BIOTECH CO., LTD

Inventor： Robert Yongxin Zhao

IPC: A61K47/48 ,  C07C243/28 ,  C07D207/452 ,  C07D403/14 ,  C07C311/55 ,  C07D213/71 ,  C07K5/065 ,  A61K45/06 ,  C07C275/50

CPC classification number: A61K31/337 ,  A61K31/404 ,  A61K31/5365 ,  A61K31/551 ,  A61K31/5513 ,  A61K45/06 ,  A61K47/6803 ,  A61K47/6889 ,  A61K49/0002 ,  C07C243/28 ,  C07C275/50 ,  C07C311/55 ,  C07D207/452 ,  C07D213/71 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D493/08 ,  C07D498/14 ,  C07D519/00 ,  C07K5/06078 ,  C07K5/06139 ,  Y02A50/385 ,  Y02A50/402 ,  Y02A50/414 ,  Y02A50/415 ,  Y02A50/463 ,  Y02A50/473 ,  Y02A50/49

Abstract: The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

Abstract translation: 本发明涉及含有肼的新型二硫桥连接体，其通过将细胞结合分子上的一对硫醇连接起来将化合物/细胞毒性剂与细胞结合分子的特异性缀合用于肼。 本发明还涉及制备这种接头的方法，以及使用这种连接体制备均相共轭物的方法，以及缀合物在治疗癌症，感染和自身免疫疾病中的应用。

公开(公告)号：US20150266812A1

公开(公告)日：2015-09-24

申请号：US14730994

申请日：2015-06-04

Applicant: Usher Ill Initiative, Inc.

Inventor： Roland Werner BÜRLI ,  William Rameshchandra Krishna ESMIEU ,  Christopher James LOCK ,  Karine Fabienne MALAGU ,  Andrew Pate OWENS ,  William E. HARTE

IPC: C07C243/28

CPC classification number: A61K31/5025 ,  A61K31/165 ,  A61K31/167 ,  A61K31/40 ,  C07C243/28 ,  C07C251/86 ,  C07C2602/08 ,  C07D487/04 ,  C07D495/04 ,  C07D519/00 ,  G01N33/502 ,  G01N33/6848 ,  G01N33/6893 ,  G01N2333/4703 ,  G01N2400/40 ,  G01N2500/04 ,  G01N2500/10

Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.

Abstract translation: 本文描述了用于治疗视网膜退行性疾病的化合物，组合物和方法，例如色素性视网膜炎，Leber先天性黑素瘤，综合性视网膜变性，年龄相关性黄斑变性和Usher综合征，以及与Usher综合征相关的听力损失。