公开(公告)号：US20230114875A1

公开(公告)日：2023-04-13

申请号：US17786089

申请日：2020-12-18

申请人： Oxford Drug Design Limited

发明人： Grace EDMUND ,  Michael H. CHARLTON ,  Paul William FINN ,  Aigars JIRGENSONS ,  Marija SKVORCOVA ,  Janis VELIKS ,  Liene GRIGORJEVA

IPC分类号： C07C381/10 ,  C07C313/06 ,  C07D277/16 ,  C07D213/71 ,  C07D333/34 ,  C07D333/52 ,  C07D307/79 ,  C07D215/36 ,  C07D231/18 ,  C07D495/04 ,  C07D317/50

摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(amino-oxo-aryl-λ6-sulfanylidene)acetamide compounds (referred to herein as ANASIA compounds) that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-tRNA synthetase, LeuRS). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.

公开(公告)号：US20230041576A1

公开(公告)日：2023-02-09

申请号：US17778492

申请日：2020-11-20

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Beibei Chen ,  Toren Finkel ,  Yuan Liu

IPC分类号： C07D215/36 ,  C07D311/12 ,  C07D213/71 ,  C07D471/04 ,  C07D215/40 ,  C07D217/24 ,  C07D265/36 ,  C07D487/04 ,  C07D267/14 ,  C07D263/46 ,  C07D277/36 ,  C07D241/42 ,  C07D403/04 ,  C07D401/12 ,  C07D403/12

摘要： This document provides compounds that are inhibitors of NF-κB activity, as well as the methods of using such compounds for treating diseases and conditions such as cancer, inflammatory conditions, or autoimmune diseases.

公开(公告)号：US20220251043A1

公开(公告)日：2022-08-11

申请号：US17627692

申请日：2020-07-22

申请人： Taipei Medical University

发明人： Shiow-Lin PAN ,  Chia-Ron YANG ,  Han-Li HUANG ,  Huang-Ju TU ,  Jing-Ping LIOU

IPC分类号： C07D215/40 ,  C07D215/36 ,  C07D215/26 ,  C07D217/22 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00

摘要： Disclosed herein are hydroxamic acid compounds. Also disclosed is a method of using the hydroxamic acid compounds for treating a condition associated with histone deacetylase 6.

公开(公告)号：US20220213041A1

公开(公告)日：2022-07-07

申请号：US17554086

申请日：2021-12-17

申请人： AbbVie Global Enterprises Ltd.

发明人： Andrew Bogdan ,  David J. Hardee ,  Timothy R. Hodges ,  Henry Korman ,  Huan-Qiu Li ,  Michael R. Schrimpf

IPC分类号： C07D215/36 ,  C07D401/12

摘要： The present invention provides for compounds of Formula (I) wherein R1 has any of the values defined in the specification, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

公开(公告)号：US11261170B2

公开(公告)日：2022-03-01

申请号：US16879204

申请日：2020-05-20

申请人： Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd.

发明人： Jiawang Zhu ,  Zhiquan Song ,  Dong Long ,  Lichun Wang ,  Jingyi Wang

IPC分类号： C07D401/04 ,  A61P1/16 ,  C07D215/14 ,  C07D215/227 ,  C07D215/36 ,  C07D215/38 ,  C07D333/56 ,  C07D413/04

摘要： The invention relates to an aromatic compound, pharmaceutical composition comprising the same, and a method for preparing the compound and an intermediate thereof. The invention also relates to use of the compound for the manufacture of a medicament for the prevention or treatment of a PPAR-related disease.

公开(公告)号：US20210353571A1

公开(公告)日：2021-11-18

申请号：US17265402

申请日：2019-08-02

申请人： Pharmaxis Ltd.

发明人： Alison Dorothy FINDLAY ,  Craig Ivan TURNER ,  Mandar DEODHAR ,  Jonathan Stuart FOOT ,  Wolfgang JAROLIMEK ,  Wenbin ZHOU ,  Alberto BUSON ,  Angelique Elsa GRECO

IPC分类号： A61K31/18 ,  A61P17/02 ,  A61P35/00 ,  A61P19/04 ,  A61P35/04 ,  C07C311/29 ,  C07C317/32 ,  C07D213/71 ,  C07D215/36 ,  C07D277/64 ,  C07D209/08 ,  A61K31/145 ,  A61K31/4409 ,  A61K31/47

摘要： The present invention relates to novel compounds which are capable of inhibiting certain amine oxidase enzymes. These compounds are useful for treatment of a variety of indications, e.g., fibrosis, cancer and/or angiogenesis in human subjects as well as in pets and livestock. In addition, the present invention relates to pharmaceutical compositions containing these compounds, as well as various uses thereof.

公开(公告)号：US11161831B2

公开(公告)日：2021-11-02

申请号：US16848661

申请日：2020-04-14

申请人： Baylor College of Medicine

发明人： David J. Tweardy ,  Moses M. Kasembeli ,  Marvin X. Xu ,  Thomas Kristian Eckols

IPC分类号： C07D333/34 ,  A61K31/47 ,  A61K31/4406 ,  A61K31/415 ,  A61K31/381 ,  A61K31/357 ,  A61K31/145 ,  C07D215/36 ,  C07D213/71 ,  C07D231/18 ,  C07D319/18 ,  C07C311/08 ,  C07C311/10 ,  C07C311/13 ,  C07C311/31 ,  C07C311/24 ,  C07C311/29 ,  C07C311/44 ,  C07C311/49 ,  C07C311/06 ,  A61K31/06 ,  A61K31/18 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/428 ,  A61K31/45 ,  A61K31/454 ,  A61K31/4704 ,  A61K31/4709 ,  A61K31/513 ,  C07C311/21 ,  C07C323/49 ,  C07C381/06 ,  A61K45/06

摘要： Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

公开(公告)号：US11123316B2

公开(公告)日：2021-09-21

申请号：US16843215

申请日：2020-04-08

申请人： The University of Melbourne

发明人： Paul Stephen Donnelly ,  Stacey Erin Rudd ,  Spencer John Williams

IPC分类号： A61K31/18 ,  C07K17/06 ,  A61K51/10 ,  C07C259/06 ,  C07C309/14 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07C311/46 ,  C07C323/60 ,  C07D207/48 ,  C07D211/60 ,  C07D211/96 ,  C07D213/42 ,  C07D213/74 ,  C07D213/89 ,  C07D215/36 ,  C07D223/06 ,  C07D277/06 ,  C07D277/80 ,  C07D279/12 ,  C07D295/13 ,  C07D309/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D453/06 ,  C07D471/08 ,  C07D487/08

摘要： The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

公开(公告)号：US20210171477A1

公开(公告)日：2021-06-10

申请号：US16632849

申请日：2018-07-23

申请人： NOVARTIS INFLAMMASOME RESEARCH, INC.

发明人： Luigi FRANCHI ,  Shomir GHOSH ,  Gary GLICK ,  Jason KATZ ,  Anthony William OPIPARI, Jr. ,  William ROUSH ,  Hans Martin SEIDEL ,  Dong-Ming SHEN ,  Shankar VENKATRAMAN ,  David Guenther WINKLER

IPC分类号： C07D277/36 ,  C07C307/06 ,  C07D307/64 ,  C07D333/34 ,  C07D263/46 ,  C07D213/71 ,  C07D231/18 ,  C07D487/04 ,  C07D215/36 ,  C07D317/62 ,  C07D307/79 ,  C07D239/26

摘要： In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured. The variables shown in Formula AA are as defined in the claims. The compounds of formula AA are NLRP3 activity modulators and, as such, can be used in the treatment of metabolic disorders (e.g. Type 2 diabetes, atherosclerosis, obesity or gout), a disease of the central nervous system (e.g. Alzheimer's disease, multiple sclerosis, Amyotrophic Lateral Sclerosis or Parkinson's disease), lung disease (e.g. asthma, COPD or pulmonary idiopathic fibrosis), liver disease (e.g. NASH syndrome, viral hepatitis or cirrhosis), pancreatic disease (e.g. acute pancreatitis or chronic pancreatitis), kidney disease (e.g. acute kidney injury or chronic kidney injury), intestinal disease (e.g. Crohn's disease or Ulcerative Colitis), skin disease (e.g. psoriasis), musculoskeletal disease (e.g. scleroderma), a vessel disorder (e.g. giant cell arteritis), a disorder of the bones (e.g. osteoarthritis, osteoporosis or osteopetrosis disorders), eye disease (e.g. glaucoma or macular degeneration), a disease caused by viral infection (e.g. HIV or AIDS), an autoimmune disease (e.g. Rheumatoid Arthritis, Systemic Lupus Erythematosus or Autoimmune Thyroiditis), cancer or aging.

公开(公告)号：US10995070B2

公开(公告)日：2021-05-04

申请号：US16239946

申请日：2019-01-04

申请人： Monsanto Technology LLC

发明人： Urszula Slomczynska ,  Matthew W. Dimmic ,  William P. Haakenson, Jr. ,  Jennifer L. Bennett ,  Barry J. Shortt ,  Christina M. Taylor ,  Deryck Jeremy Williams

IPC分类号： C07D215/14 ,  A01N25/00 ,  A61K31/095 ,  A61K31/04 ,  A61K31/395 ,  A61K31/045 ,  A61K31/335 ,  A01N43/42 ,  A61K31/47 ,  A01N43/713 ,  A01N43/76 ,  A01N43/78 ,  A01N43/82 ,  A01N57/24 ,  A01N63/30 ,  C07D257/04 ,  A01N35/06 ,  A01N37/10 ,  A01N37/22 ,  A01N41/10 ,  A01N41/12 ,  A01N43/16 ,  A01N43/18 ,  A01N43/54 ,  A01N43/60 ,  A01N43/84 ,  A01N57/20 ,  A01N63/00 ,  A01N65/08 ,  C07D215/18 ,  C07D215/26 ,  C07D215/36 ,  C07D409/04

摘要： Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants.