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：US20230382870A1

公开(公告)日：2023-11-30

申请号：US18227325

申请日：2023-07-28

申请人： SHENZHEN EDK PHARMACEUTICAL TECHNOLOGY CO., LTD.

发明人： Guohong Yang ,  Lijun Yu ,  Junze He ,  Meijuan Duan

IPC分类号： C07D231/16 ,  A61K9/00 ,  A61K9/20 ,  A61K47/10 ,  A61K47/26 ,  C07D209/18 ,  C07D209/42 ,  C07D231/12

CPC分类号： C07D231/16 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K47/10 ,  A61K47/26 ,  C07D209/18 ,  C07D209/42 ,  C07D231/12

摘要： An N-aromatic amide compounds with formula (I) is disclosed. The definitions of R1, R2, R3, R4, R5, R6, W1, W2 and W3 in the formula are the same as those in the description.

公开(公告)号：US20230365546A1

公开(公告)日：2023-11-16

申请号：US18025638

申请日：2021-09-02

申请人： ORIGIANT PHARMACEUTICAL CO., LTD

发明人： Shengyong YANG ,  Linli LI

IPC分类号： C07D417/04 ,  C07D471/04 ,  C07D417/14 ,  C07D401/04 ,  C07D209/42 ,  C07D405/14 ,  C07D487/04 ,  C07D513/04 ,  C07D403/04 ,  C07D519/00 ,  A61P1/00

CPC分类号： C07D417/04 ,  C07D471/04 ,  C07D417/14 ,  C07D401/04 ,  C07D209/42 ,  C07D405/14 ,  C07D487/04 ,  C07D513/04 ,  C07D403/04 ,  C07D519/00 ,  A61P1/00

摘要： Provided are a 5-substituted indole 3-amide derivative, a preparation method and a use thereof, belonging to the field of medicine. A compound represented by formula I or a pharmaceutically acceptable salt thereof is provided. This type of compound can significantly inhibit the activity of RIPK1 kinase, has high selectivity and excellent safety, serves as a RIPK1 kinase inhibitor, and can be used as a potential therapeutic drug for inflammation, immune diseases, tumors and neurodegenerative diseases. TNFα-induced SIRS model experiments proved that the compound can inhibit a RIPK1 kinase in vivo. Pharmacokinetic results showed that this series of compounds has excellent pharmacokinetic properties, thus providing a novel strategy and means for disease treatments targeting RIPK1.

公开(公告)号：US11760727B2

公开(公告)日：2023-09-19

申请号：US17214834

申请日：2021-03-27

申请人： Shenzhen EDK Pharmaceutical Technology Co., Ltd.

发明人： Guohong Yang ,  Lijun Yu ,  Junze He ,  Meijuan Duan

IPC分类号： C07D231/16 ,  C07D231/12 ,  A61K9/00 ,  A61K9/20 ,  A61K47/10 ,  A61K47/26 ,  C07D209/18 ,  C07D209/42

CPC分类号： C07D231/16 ,  A61K9/0019 ,  A61K9/2018 ,  A61K9/2059 ,  A61K47/10 ,  A61K47/26 ,  C07D209/18 ,  C07D209/42 ,  C07D231/12

摘要： The present invention relates to N-aromatic amide compounds with formula (I) and/or (II) and preparation methods therefor, pharmaceutical compositions and pharmaceutical formulations containing the compounds with formula (I) and/or (II), and use of the compounds with formula (I) and/or (II) in preparing a medicament for the treatment of diseases related to androgens. The definitions of R1, R2, R3, R4, R5, R6, W1, W2, W3, W4 and W5 in the formula are the same as those in the description. The compounds with the formula (I) and/or (II) are capable of binding to the androgen receptors and have activity for anti-androgen and degrading androgen receptor. The compounds can be used alone or as compositions for the treatment of various androgen-related diseases such as prostate cancer, prostate hyperplasia, breast cancer, bladder cancer, ovarian cancer and the like, and also for the treatment of acne, hirsutism, psilosis and other diseases.

公开(公告)号：US11667640B2

公开(公告)日：2023-06-06

申请号：US16803628

申请日：2020-02-27

申请人： LUNELLA BIOTECH, INC.

发明人： Michael P. Lisanti ,  Federica Sotgia

IPC分类号： C07D487/04 ,  C07D209/42 ,  G16C20/50 ,  C07D265/36 ,  C07D417/12 ,  C40B30/06 ,  C40B40/14

CPC分类号： C07D487/04 ,  C07D209/42 ,  C07D265/36 ,  C07D417/12 ,  C40B30/06 ,  C40B40/14 ,  G16C20/50

摘要： The present disclosure relates to compounds that bind to at least one of ACAT1/2 and OXCT1/2 and inhibit mitochondrial ATP production, referred to herein as mitoketoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoketoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoketoscins to provide anti-aging benefits. Specific mitoketoscin compounds are also disclosed.

公开(公告)号：US20190031692A1

公开(公告)日：2019-01-31

申请号：US16148622

申请日：2018-10-01

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Avinash S. Phadke ,  Xiangzhu Wang ,  Dawei Chen ,  Akihiro Hashimoto ,  Venkat Rao Gadhachanda ,  Godwin Pais ,  Qiuping Wang ,  Atul Agarwal ,  Milind Deshpande

IPC分类号： C07F9/572 ,  A61K31/4709 ,  C07F5/02 ,  A61K9/00 ,  C07D209/30 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/444 ,  A61K31/501 ,  A61K31/675 ,  A61K31/683 ,  A61K31/4184 ,  A61K31/55 ,  C07D209/88 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/404 ,  A61K31/549 ,  C07D209/44 ,  C07D209/12 ,  A61K31/506 ,  C07F9/6558 ,  C07D471/08 ,  A61K31/437 ,  A61K31/519 ,  C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D417/06 ,  C07D209/42 ,  C07D487/04 ,  C07D417/12 ,  C07D513/04 ,  C07F9/6561 ,  C07D209/40 ,  C07D413/14 ,  C07B59/00 ,  C07D487/14 ,  C07D403/08 ,  C07D413/06 ,  C07D417/14 ,  C07D403/06 ,  C07D405/14 ,  C07D209/14 ,  C07D495/04 ,  C07D405/12 ,  C07D491/113 ,  C07F7/08

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07B2200/05 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US20180334678A1

公开(公告)日：2018-11-22

申请号：US15969374

申请日：2018-05-02

申请人： THE SCRIPPS RESEARCH INSTITUTE

发明人： Matthew D. Disney

IPC分类号： C12N15/63 ,  C12N15/113 ,  C07H21/02 ,  C07D471/04

CPC分类号： C12N15/63 ,  A61K31/404 ,  A61K31/7105 ,  A61K38/00 ,  A61K48/00 ,  C07D209/14 ,  C07D209/42 ,  C07D471/04 ,  C07H21/02 ,  C12N15/113 ,  C12N2310/14

摘要： A repeat expansion in C9ORF72 causes frontotemporal dementia and amyotrophic lateral sclerosis (c9FTD/ALS). RNA of the expanded repeat (r(GGGGCC)exp) forms nuclear foci or undergoes repeat-associated non-ATG (RAN) translation producing “c9RAN proteins”. Since neutralizing r(GGGGCC)exp could inhibit these potentially toxic events, we sought to identify small molecule binders of r(GGGGCC)exp. Chemical and enzymatic probing of r(GGGGCC)8 indicate it adopts a hairpin structure in equilibrium with a quadruplex structure. Using this model, bioactive small molecules targeting r(GGGGCC)exp were designed and found to significantly inhibit RAN translation and foci formation in cultured cells expressing r(GGGGCC)66 and neurons trans-differentiated from fibroblasts of repeat expansion carriers. Finally, we show that poly(GP) c9RAN proteins are specifically detected in c9ALS patient cerebrospinal fluid. Our findings highlight r(GGGGCC)exp-binding small molecules as a possible c9FTD/ALS therapeutic, and suggest c9RAN proteins could potentially serve as a pharmacodynamic biomarker to assess efficacy of therapies that target r(GGGGCC)exp.

公开(公告)号：US10081645B2

公开(公告)日：2018-09-25

申请号：US15711794

申请日：2017-09-21

申请人： Achillion Pharmaceuticals, Inc.

发明人： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC分类号： A61K31/4025 ,  A61K31/4184 ,  A61K31/4427 ,  A61K31/496 ,  A61K31/4188 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/506 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  C07F9/572 ,  C07D417/06 ,  C07F7/08 ,  C07D403/12 ,  C07D209/42 ,  A61K31/675 ,  C07B59/00 ,  C07D209/14 ,  C07D209/40 ,  C07D405/12 ,  C07D417/12 ,  C07D487/14 ,  C07D491/113 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/549 ,  A61K31/55 ,  C07D495/04 ,  A61K31/683 ,  C07D413/06 ,  C07D403/08 ,  C07D487/04 ,  C07D403/06 ,  C07F9/6561 ,  C07F9/6558 ,  C07F5/02

CPC分类号： C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07B2200/05 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616

摘要： Compounds, methods of use, and processes for making inhibitors of complement factor D comprising formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US20180185364A1

公开(公告)日：2018-07-05

申请号：US15675000

申请日：2017-08-11

申请人： Vertex Pharmaceuticals Incorporated

发明人： Mark Thomas Miller ,  Corey Anderson ,  Vijayalaksmi Arumugam ,  Brian Richard Bear ,  Hayley Marie Binch ,  Jeremy J. Clemens ,  Thomas Cleveland ,  Erica Conroy ,  Timothy Richard Coon ,  Bryan A. Frieman ,  Peter Diederik Jan Grootenhuis ,  Raymond Stanley Gross ,  Sara Sabina Hadida-Ruah ,  Haripada Khatuya ,  Pramod Virupax Joshi ,  Paul John Krenitsky ,  Chun-Chieh Lin ,  Gulin Erdogan Marelius ,  Vito Melillo ,  Jason McCartney ,  Georgia McGaughey Nicholls ,  Fabrice Jean Denis Pierre ,  Alina Silina ,  Andreas P. Termin ,  Johnny Uy ,  Jinglan Zhou

IPC分类号： A61K31/506 ,  C07D417/12 ,  C07D405/14 ,  C07D401/14 ,  C07D401/12 ,  C07D231/14 ,  C07D231/12 ,  C07D213/84 ,  C07D213/82 ,  C07D209/42 ,  A61K31/497 ,  A61K31/496 ,  A61K31/4709 ,  A61K31/4545 ,  A61K31/4525 ,  A61K31/444 ,  A61K31/4439 ,  A61K31/4418 ,  A61K31/44 ,  A61K31/415 ,  A61K31/404 ,  A61J1/03

CPC分类号： A61K31/506 ,  A61J1/035 ,  A61K31/404 ,  A61K31/415 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  C07D209/18 ,  C07D209/42 ,  C07D209/49 ,  C07D213/64 ,  C07D213/73 ,  C07D213/82 ,  C07D213/84 ,  C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D235/24 ,  C07D239/34 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D413/14 ,  C07D417/12

摘要： The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

公开(公告)号：US09988380B2

公开(公告)日：2018-06-05

申请号：US14762770

申请日：2014-03-10

申请人： Nanyang Technological University ,  National University of Singapore

发明人： Michael Givskov ,  Liang Yang ,  Yang Yi Sean Tan

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P31/04 ,  C07D471/04 ,  C07D209/42 ,  C07C229/36 ,  A01N37/44 ,  A01N43/38 ,  A01N43/90

CPC分类号： C07D471/04 ,  A01N37/44 ,  A01N43/38 ,  A01N43/90 ,  A61K31/519 ,  C07C229/36 ,  C07D209/42 ,  C07D487/04

摘要： The invention relates to compounds for use as quorum sensing inhibitors, and in particular, to quorum sensing inhibitors of Pseudomonas aeruginosa.