公开(公告)号：US20240327418A1

公开(公告)日：2024-10-03

申请号：US18293840

申请日：2022-08-01

申请人： OCEAN UNIVERSITY OF CHINA ,  QINGDAO HIGENE BIOPHARMACEUTICAL CO., LTD ,  MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD

发明人： Xiaoyang LI ,  Zhongren ZHOU ,  Yuqi JIANG ,  Kairui YUE ,  Wenfang XU

IPC分类号： C07D491/048 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/655 ,  A61P35/00 ,  A61P35/02 ,  C07C247/12 ,  C07D209/42 ,  C07D213/40 ,  C07D213/56 ,  C07D307/85 ,  C07D333/70 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04

CPC分类号： C07D491/048 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/655 ,  A61P35/00 ,  A61P35/02 ,  C07C247/12 ,  C07D209/42 ,  C07D213/40 ,  C07D213/56 ,  C07D307/85 ,  C07D333/70 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04

摘要： A compound targeting HDAC and NAD synthesis and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof, as well as preparation and application thereof. Specifically, a compound shown in structural general formula (I) and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof are provided. The compound of the structural general formula (I) is a multi-target inhibitor, targeting HDAC and NAD targets, and exhibiting significant HDAC inhibitory activity, while representative compounds exhibit certain NAD inhibitory activity.


Ring E-B-L-C (O)—(NH)r-R   (General formula I)

公开(公告)号：US11976075B2

公开(公告)日：2024-05-07

申请号：US18356923

申请日：2023-07-21

申请人： Isosterix, Inc.

发明人： Roopa Rai ,  Mark Bures

IPC分类号： C07D487/04 ,  A61P35/00 ,  C07D213/56 ,  C07D307/85 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D213/46 ,  C07D231/12 ,  C07D231/38 ,  C07D413/08 ,  C07D413/10 ,  C07D413/14 ,  C07D471/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07D213/56 ,  C07D307/85 ,  C07D401/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12

摘要： Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.

公开(公告)号：US20230373947A1

公开(公告)日：2023-11-23

申请号：US18229277

申请日：2023-08-02

申请人： MITSUI CHEMICALS, INC.

发明人： Kei Yoshida ,  Takeo Wakita ,  Hiroyuki Katsuta ,  Akiyoshi Kai ,  Yutaka Chiba ,  Kiyoshi Takahashi ,  Hiroko Kato ,  Nobuyuki Kawahara ,  Michikazu Nomura ,  Hidenori Daido ,  Junji Maki ,  Shinichi Banba

IPC分类号： C07D333/38 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/30 ,  C07D241/24 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D309/08 ,  C07D309/28 ,  C07D317/62 ,  C07D333/68 ,  A01N43/40 ,  A01N37/22 ,  A01N43/60 ,  C07C237/48 ,  C07D207/34 ,  C07D239/28 ,  C07D261/18 ,  C07D307/85 ,  C07D317/46

CPC分类号： C07D333/38 ,  A01N37/44 ,  A01N43/08 ,  A01N43/10 ,  A01N43/12 ,  A01N43/16 ,  A01N43/30 ,  A01N43/42 ,  A01N43/54 ,  A01N43/56 ,  A01N43/58 ,  A01N43/78 ,  A01N43/80 ,  C07C237/42 ,  C07C317/40 ,  C07C323/42 ,  C07C327/48 ,  C07D207/416 ,  C07D213/64 ,  C07D213/73 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D215/52 ,  C07D231/14 ,  C07D231/16 ,  C07D239/30 ,  C07D241/24 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D307/24 ,  C07D307/68 ,  C07D307/84 ,  C07D309/08 ,  C07D309/28 ,  C07D317/62 ,  C07D333/68 ,  A01N43/40 ,  A01N37/22 ,  A01N43/60 ,  C07C237/48 ,  C07D207/34 ,  C07D239/28 ,  C07D261/18 ,  C07D307/85 ,  C07D317/46

摘要： A compound represented by Formula (1):




The compound can be used as insecticides.

公开(公告)号：US20210380539A1

公开(公告)日：2021-12-09

申请号：US17204206

申请日：2021-03-17

申请人： CANCER RESEARCH TECHNOLOGY LIMITED

发明人： Alison E. MCGONAGLE ,  Allan M. JORDAN ,  Bohdan WASZKOWYCZ ,  Colin P. HUTTON ,  Ian D. WADDELL ,  James R. HITCHIN ,  Kate M. SMITH ,  Niall M. HAMILTON

IPC分类号： C07D235/26 ,  C07D413/14 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/14 ,  C07D417/06 ,  A61P35/00 ,  C07D307/85 ,  C07D403/04

摘要： The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.

公开(公告)号：US20210323941A1

公开(公告)日：2021-10-21

申请号：US16093365

申请日：2017-04-14

申请人： The United States of America, as represented by the Secretary, Department of Health and Human ,  The University of Kansas

发明人： David R. Sibley ,  Amy Elizabeth Moritz ,  R. Benjamin Free ,  Joseph P. Steiner ,  Noel Terrence Southall ,  Marc Ferrer ,  Xin Hu ,  Warren S. Weiner ,  Jeffrey Aubé ,  Kevin Frankowski

IPC分类号： C07D401/12 ,  C07D209/42 ,  C07D471/04 ,  C07D409/12 ,  C07D235/24 ,  C07D405/12 ,  C07D295/185 ,  C07D213/65 ,  C07D213/81 ,  C07D317/64 ,  C07D307/85 ,  C07D333/70 ,  A61P25/28

摘要： The disclosure of a compound of Formula (I) or a pharmaceutically acceptable salt thereof (I) The variables W, R1, R2, R3, and R4 are defined in the disclosure. The disclosure provides a compound or salt of Formula (I) together with a pharmaceutically acceptable carrier. The disclosure also provides methods of treating a patient for Parkinson's disease and related syndromes, dyskinesia, especially dyskinesias secondary to treating Parkinson's disease with L-DOPA, neurodegenerative disorders such as Alzheimer's disease and dementia, Huntington's disease, restless legs syndrome, bipolar disorder and depression, schizophrenia, cognitive dysfunction, or substance use disorders, the methods comprising administering a compound of Formula I or salt thereof to the patient. The disclosure provides combination methods of treatment in which the compound of Formula (I) is administered to the patient together with one or more additional active agents.

公开(公告)号：US20210093619A1

公开(公告)日：2021-04-01

申请号：US16619985

申请日：2018-06-07

申请人： GlaxoSmithKline Intellectual Property Development Limited

发明人： Jeffrey Michael AXTEN ,  Michael P. DEMARTINO ,  Karen Anderson EVANS ,  Biswajit KALITA ,  Jeffrey M. RALPH

IPC分类号： A61K31/4439 ,  A61K45/06 ,  C07C233/41 ,  A61K31/165 ,  A01N1/02 ,  C07D213/65 ,  A61K31/44 ,  A61K31/444 ,  C07D401/12 ,  C07D305/08 ,  A61K31/337 ,  A61K31/4166 ,  C07D233/36 ,  C07D207/12 ,  A61K31/40 ,  C07D401/04 ,  A61K31/397 ,  C07D205/04 ,  A61K31/343 ,  C07D307/85 ,  C07D311/58 ,  A61K31/353 ,  A61K31/4035 ,  C07D209/44 ,  A61K31/451 ,  C07D211/18 ,  C07D401/14 ,  C07D207/273 ,  C07D211/46 ,  A61K9/48 ,  A61K9/00 ,  A61K9/20

摘要： The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula IIIQ: wherein X6′, a, b, C8′, D8′, L82′, L83′, R81′, R82′, R83′, R84′, R85′, R86′, z82′, z84′, z85′, and z86′ are as defined herein; or salts thereof.
The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

公开(公告)号：US20190177310A1

公开(公告)日：2019-06-13

申请号：US16219805

申请日：2018-12-13

申请人： Praxis Biotech LLC

发明人： Sebastian BERNALES ,  Luz Marina DELGADO OYARZO ,  Gonzalo Esteban NÚÑEZ VASQUEZ ,  Gonzalo Andrés URETA DÍAZ ,  Brahmam PUJALA ,  Dayanand PANPATIL ,  Bhawana BHATT ,  Sarvajit CHAKRAVARTY

IPC分类号： C07D413/12 ,  C07D265/36 ,  C07D263/24 ,  C07D307/85 ,  C07D401/12 ,  C07D405/12 ,  C07D215/18 ,  C07D211/58 ,  C07D491/048 ,  C07D277/68 ,  C12N5/00

摘要： The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.

公开(公告)号：US10100027B2

公开(公告)日：2018-10-16

申请号：US15514389

申请日：2015-09-23

申请人： CHANGZHOU YINSHENG PHARMACEUTICAL CO., LTD. ,  SICHUAN UNIVERSITY

发明人： Yang Zhang ,  Zhifei Fu ,  Jianfei Wang ,  Jian Li ,  Shuhui Chen ,  Yuquan Wei ,  Luoting Yu ,  Xin Tao

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D405/00 ,  C07D307/85 ,  C07D405/14 ,  C07D405/12 ,  C07D413/14 ,  C07D413/12 ,  C07D405/06

摘要： Provided is a benzofuran analog having a structure represented by formula (I) and used as an NS4B inhibitor, or a pharmaceutically acceptable salt of the benzofuran analog. The benzofuran analog has anti-hepatitis C virus activity.

公开(公告)号：US09918959B2

公开(公告)日：2018-03-20

申请号：US15502117

申请日：2015-08-05

申请人： The Scripps Research Institute ,  Board of Regents of the University of Texas System, Austin

发明人： Dale Boger ,  Bruce Beutler

IPC分类号： C07D307/79 ,  C07D333/50 ,  A61K31/343 ,  A61K31/167 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4439 ,  C07D307/85 ,  A61K39/39 ,  C07D209/42 ,  C07D405/12 ,  C07D401/12 ,  C07D409/12 ,  A61K31/498 ,  C07D403/12 ,  A61K31/506 ,  C07C237/44

CPC分类号： A61K31/343 ,  A61K31/167 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/498 ,  A61K31/506 ,  A61K39/39 ,  C07C237/44 ,  C07C2601/14 ,  C07D209/18 ,  C07D209/42 ,  C07D307/85 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： A TLR-independent adjuvant compound that corresponds in structure to Formula I, below, or its pharmaceutically acceptable salt is disclosed in which X, Y, Z, n, R1, R2, R3, R4 and W are defined within. Also disclosed are a method of its preparation and use, as well as a pharmaceutical composition containing the same.

公开(公告)号：US20170044100A1

公开(公告)日：2017-02-16

申请号：US15305725

申请日：2015-04-22

申请人： THE JOHNS HOPKINS UNIVERSITY ,  UNIVERSITY OF ILLINOIS AT CHICAGO

发明人： William R. Bishai ,  Shichun Lun ,  Haidan Guo ,  Alan Kozikowski ,  Oluseye Onajole ,  Jozef Stec

IPC分类号： C07D209/42 ,  C07D403/12 ,  C07D307/85 ,  C07D235/24 ,  C07D487/04 ,  C07D277/68 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/55 ,  A61K31/343 ,  A61K31/407 ,  A61K31/428 ,  A61K31/4409 ,  A61K31/496 ,  C07D401/12

CPC分类号： C07D209/42 ,  A61K31/343 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06 ,  C07D235/24 ,  C07D277/68 ,  C07D307/85 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  C07D487/04 ,  A61K2300/00

摘要： The present invention provides novel indoleamide compounds for treating tuberculosis, including drug-resistant M-tuberculosis, compositions comprising the indoleamides and methods of using the indoleamides in conjunction with other biologically active agents for the treatment of tuberculosis in a subject in need thereof.

摘要翻译： 本发明提供了用于治疗结核病的新型吲哚酰胺化合物，包括耐药性结核分枝杆菌，包含吲哚胺的组合物和使用吲哚胺与其它生物活性剂联合用于治疗有此需要的受试者的结核病的方法。