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：US20230096670A1

公开(公告)日：2023-03-30

申请号：US17799054

申请日：2021-02-26

申请人： Daewoong Pharmaceutical Co., Ltd.

发明人： Youn Jung YOON ,  Hee Kyoon YOON

IPC分类号： C07D407/04 ,  C07D307/79

摘要： An intermediate useful for the synthesis of an SGLT inhibitor and a method for preparing an SGLT inhibitor are provided. By employing an intermediate having Chemical Formula 5, the difficulty of purification with existing processes can be solved, the quality requirements for related substances can be achieved with only one purification step, and the quality control problem in each step can be solved by performing several steps in situ. A method for synthesizing a compound of Chemical Formula 1 by using a compound of Chemical Formula 5 enables purification in an earlier step, thereby solving the problems of existing synthesis processes, in which the quality requirements for related substances were difficult to control step-by-step due to a continuous process, thereby minimizing the amount of related substances in the final product. In addition, the yield of a diphenylmethane derivative according to Chemical Formula 1 is increased.

公开(公告)号：US20220326230A1

公开(公告)日：2022-10-13

申请号：US17678512

申请日：2022-02-23

申请人： Firmenich Incorporated

发明人： Catherine TACHDJIAN ,  Andrew P. PATRON ,  Sara L. ADAMSKI-WERNER ,  Farid BAKIR ,  Qing CHEN ,  Vincent DARMOHUSODO ,  Stephen Terrence HOBSON ,  Xiaodong LI ,  Ming QI ,  Daniel H. ROGERS ,  Marketa RINNOVA ,  Guy SERVANT ,  Xiao-Qing TANG ,  Mark ZOLLER ,  David WALLACE ,  Amy XING ,  Klaus GUBERNATOR

IPC分类号： G01N33/543 ,  C07C233/65 ,  C07C235/54 ,  C07C275/30 ,  C07C275/34 ,  C07D307/84 ,  C07D317/68 ,  G01N33/566 ,  G01N33/74 ,  A23L27/20 ,  C07D263/56 ,  C07D213/81 ,  C07D213/85 ,  C07D215/48 ,  C07D217/06 ,  C07D231/14 ,  C07D333/24 ,  C07D333/38 ,  C07D401/04 ,  C07D409/12 ,  C07D417/12 ,  C07D261/18 ,  C07D271/12 ,  C07D275/03 ,  C07D209/08 ,  C07D277/64 ,  C07D209/42 ,  C07D285/135 ,  C07D213/40 ,  C07D307/52 ,  C07D307/68 ,  C07D307/79 ,  C07D307/82 ,  G01N33/50 ,  A23L2/56 ,  A61K8/49 ,  A61K8/55 ,  A61K47/22 ,  A61K47/24 ,  C07D405/12 ,  C07F9/655 ,  A23L27/00

摘要： The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

公开(公告)号：US20220204449A1

公开(公告)日：2022-06-30

申请号：US17548288

申请日：2021-12-10

申请人： ILDONG PHARMACEUTICAL CO., LTD.

发明人： Woojin JEON ,  Do Sup LEE ,  Suh-Youn SHON ,  Junsu BAN ,  Sungjun HONG ,  Jin Hee LEE ,  Jaeho HEO ,  Jungwoo LEE ,  JoonTae PARK ,  Kyung Mi AN ,  Hongchul YOON

IPC分类号： C07D209/08 ,  C07D307/79 ,  C07D319/18

摘要： The present disclosure provides pharmaceutical compositions and compounds having dual agonist activity at the μ and δ opioid receptors. The agonist compounds of this disclosure can also provide GPCR functional selectivity, including selective activity in the Gi pathway. In some embodiments, the compounds of this disclosure are biased μ-opioid and/or δ-opioid receptor agonists that do not significantly recruit β-arrestins, but can activate G-protein-dependent pathways, and thus can be administered without risk of significant undesirable side effects exhibited by conventional opioid receptor agonists. In some embodiments there is provided a substantially optically pure compound having dual agonist activity at the μ and δ opioid receptors.

公开(公告)号：US11374044B2

公开(公告)日：2022-06-28

申请号：US16318240

申请日：2017-07-18

申请人： Nippon Kayaku Kabushiki Kaisha

发明人： Kazuki Niimi ,  Yusuke Tone ,  Hidenori Yakushiji

IPC分类号： C07D495/04 ,  C07D277/66 ,  C07D307/79 ,  C07D307/87 ,  C07D333/54 ,  C07D333/72 ,  H01L27/146 ,  H01L51/00 ,  H01L31/10 ,  H01L51/42 ,  H01L27/30 ,  H01L29/786 ,  H01L51/44

摘要： The present invention pertains to a material for a photoelectric conversion element for use in an imaging element, the material containing a compound represented by formula (1) (in formula (1), R1 and R2 independently represent a substituted or unsubstituted fused heterocyclic aromatic group). The material can provide a photoelectric conversion element having excellent hole and electron leakage preventing properties, hole and electron transport properties, heat tolerance to processing temperatures, and visible light transparency.

公开(公告)号：US11242317B2

公开(公告)日：2022-02-08

申请号：US16519590

申请日：2019-07-23

申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY

发明人： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Venkata Velvadapu

IPC分类号： A61K31/405 ,  A61K31/41 ,  A61K31/42 ,  A61K31/415 ,  A61K31/40 ,  C07D515/02 ,  C07D209/44 ,  C07D295/04 ,  C07D261/06 ,  C07D233/02 ,  C07D233/00 ,  C07D207/327 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/192 ,  A61K31/44 ,  C07C229/56 ,  C07C255/54 ,  C07C255/55 ,  C07C211/27 ,  C07C217/84 ,  C07C233/11 ,  C07C233/64 ,  C07C233/65 ,  C07C235/58 ,  C07C311/08 ,  C07C311/16 ,  C07C311/17 ,  C07C317/14 ,  C07D235/06 ,  C07D403/10 ,  C07D239/26 ,  C07D409/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D209/08 ,  C07D295/155 ,  C07D213/55 ,  C07C53/18 ,  C07C63/66 ,  C07C65/19 ,  C07C65/28 ,  C07C229/64 ,  C07C317/44 ,  C07D207/08 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D211/70 ,  C07D213/64 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D249/06 ,  C07D277/30 ,  C07D307/79 ,  C07D333/54 ,  C07D401/04 ,  C07D401/10

摘要： Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

公开(公告)号：US11161824B2

公开(公告)日：2021-11-02

申请号：US16326453

申请日：2017-08-18

申请人： University College Dublin, National University of Ireland, Dublin

发明人： Patrick Guiry ,  Catherine Godson ,  Monica De Gaetano ,  Eibhlin Butler ,  Claire Wilson ,  Catherine Tighe ,  Denise Moran ,  Andrea Zanetti ,  Kevin Gahan

IPC分类号： C07D239/26 ,  C07D215/14 ,  C07D217/02 ,  C07D239/74 ,  C07D241/42 ,  C07D231/12 ,  C07D307/36 ,  C07D307/79 ,  C07D333/06 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/47 ,  A61K31/472 ,  A61P11/06 ,  A61P13/12 ,  C07D215/18 ,  C07D217/22 ,  C07D233/68 ,  C07D263/32 ,  C07D263/34 ,  C07D307/80 ,  C07D333/56 ,  C07D405/06 ,  C07D407/06 ,  C07D409/06 ,  C07D413/06

摘要： The present invention relates to a compound of formula (I): wherein L is an optionally substituted heterocyclic group excluding unsubstituted monocyclic pyridine groups; wherein a is 0, 1 or 2; wherein R1 is H or with R2 is a bond; wherein R2 is an optionally substituted alkoxy or aryloxy group, or with R1 forms a bond; wherein R3 is an optionally substituted alkyl group; and wherein R4 is CH2, CMe2 or O. Such compounds may be used in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis.

公开(公告)号：US11124524B2

公开(公告)日：2021-09-21

申请号：US16374571

申请日：2019-04-03

申请人： Solutia Canada Inc.

发明人： Neil Robin Branda ,  Jeremy Graham Finden ,  Simon James Gauthier ,  Ali Hayek ,  Kyle Andrew Hope-Ross ,  James Daniel Senior ,  Andreea Spantulescu ,  Serguei Sviridov

IPC分类号： C07D495/04 ,  C07F7/18 ,  C07D409/14 ,  C07D493/14 ,  C07D333/22 ,  C07D333/38 ,  C07D495/14 ,  C07D519/00 ,  C07F7/08 ,  C07D493/22 ,  C07D333/18 ,  C07D513/14 ,  G02B5/22 ,  C07D493/04 ,  C07D513/04 ,  C09K9/02 ,  G02B1/04 ,  C07D333/12 ,  C07D277/22 ,  C07D307/79 ,  G02B5/20 ,  G02B5/23

摘要： A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R1 is independently selected from the group consisting of H, or halo; each R2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R2 together form —CH═CH— and form part of a polymer backbone; each R3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R4 is aryl; and each R5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.

公开(公告)号：US20210277051A1

公开(公告)日：2021-09-09

申请号：US17255074

申请日：2018-06-22

申请人： ZHEJIANG PEPTITES BIOTECH CO., LTD.

发明人： Haiying XING ,  Zhiguo LIU ,  Xinyou YU ,  Xiaohang CHEN ,  Huiping WANG

IPC分类号： C07K1/10 ,  C07D307/79 ,  C07C217/90 ,  C07K1/06 ,  C07K7/23

摘要： The invention relates to a compound or a salt thereof, a method for preparation thereof, and use thereof, wherein the compound has the structure of Formula (1): the substituents in Formula (1) are as defined in the specification. The compound of Formula (1) or a salt thereof can be attached to a solid-phase resin, on which solid-phase synthesis may be performed.

公开(公告)号：US20210188793A1

公开(公告)日：2021-06-24

申请号：US17195351

申请日：2021-03-08

申请人： Lundbeck La Jolla Research Center, Inc. ,  THE SCRIPPS RESEARCH INSTITUTE

发明人： Justin S. CISAR ,  Cheryl A. GRICE ,  Todd K. JONES ,  Micah J. NIPHAKIS ,  Jae Won CHANG ,  Kenneth M. LUM ,  Benjamin F. CRAVATT

IPC分类号： C07D295/205 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D307/79 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  A61P25/22 ,  C07D295/26 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

摘要： This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.