公开(公告)号：US20240317709A1

公开(公告)日：2024-09-26

申请号：US18588717

申请日：2024-02-27

申请人： Lakehead University

发明人： Jinqiang Hou ,  Wenjie Liu

IPC分类号： C07D401/12 ,  C07D249/06

CPC分类号： C07D401/12 ,  C07D249/06

摘要： Fluorine-containing triazole derivatives as potent LPA1 antagonists were successfully discovered. Among them, one compound demonstrated great inhibition activity of LPA-induced cell proliferation, migration, and invasion on a breast cancer cell line. Our findings further support the role LPA plays in breast cancer. These results provide a new alternative for the development of novel targeted therapy for the treatment of breast cancer.

公开(公告)号：US20240300968A1

公开(公告)日：2024-09-12

申请号：US18291809

申请日：2022-07-26

申请人： The University of Manchester

发明人： Samuel Butterworth ,  Miguel Garzon Sanz

IPC分类号： C07D491/08 ,  A61K31/17 ,  A61K31/4035 ,  A61K31/4192 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/5386 ,  C07C317/42 ,  C07D211/34 ,  C07D211/96 ,  C07D249/06 ,  C07D401/12 ,  C07D405/12

CPC分类号： C07D491/08 ,  A61K31/17 ,  A61K31/4035 ,  A61K31/4192 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/5386 ,  C07C317/42 ,  C07D211/34 ,  C07D211/96 ,  C07D249/06 ,  C07D401/12 ,  C07D405/12

摘要： This invention relates to therapeutic 6-substituted naphthalene-1,3-disulfonic acid derivatives of formula (I) (Formula (I)). More specifically, the invention relates to compounds of formula (I) useful as modulators of extracellular nicotinamide phosphoribosyl transferase (eNAMPT) that stabilize the protein in its dimeric form. In addition the invention contemplates pharmaceutical compositions comprising the compounds, processes to prepare the compounds and the compounds for use in methods of medical treatment of e.g. (i) diabetes; (ii) cardiovascular disease; (iii) inflammatory bowel condition; (iv) cancer; (v) liver disease; (vi) inflammatory skin conditions; (vii) lung conditions; (viii) arthritis; (ix) kidney disease (e.g. chronic kidney disease); or (x) sepsis. An exemplary compound is e.g. 6-(2-fluoro-5-((3-(4-(piperidin-1-ylsulfonyl) phenyl) ureido)methyl)phenyl)-4-(trioxidaneylthio) naphthalene-2-sulfonic acid (example 1).

公开(公告)号：US12054478B2

公开(公告)日：2024-08-06

申请号：US17944757

申请日：2022-09-14

申请人： China Pharmaceutical University

发明人： Qidong You ,  Xiaoke Guo ,  Dongdong Li ,  Weilin Chen ,  Zhihui Wang

IPC分类号： C07D405/12 ,  C07D249/06 ,  C07D401/12 ,  C07D403/10

CPC分类号： C07D405/12 ,  C07D249/06 ,  C07D401/12 ,  C07D403/10

摘要： The present disclosure relates to the field of medicinal chemistry, in particular to a phenyl triazole MLL1-WDR5 protein-protein interaction inhibitor (I) and a preparation method thereof, and pharmacodynamics experiments prove that the compound of the present disclosure has relatively strong MLL1-WDR5 protein-protein interaction inhibition activity.

公开(公告)号：US20240254079A1

公开(公告)日：2024-08-01

申请号：US18239892

申请日：2023-08-30

申请人： ARCUS BIOSCIENCES, INC.

发明人： Joel Worley BEATTY ,  Samuel Lawrie DREW ,  Matthew EPPLIN ,  Jeremy Thomas Andre FOURNIER ,  Balint GAL ,  Tezcan GUNEY ,  Karl T. HAELSIG ,  Clayton HARDMAN ,  Steven Donald JACOB ,  Jenna Leigh JEFFREY ,  Jaroslaw KALISIAK ,  Kenneth Victor LAWSON ,  Manmohan Reddy LELETI ,  Erick Allen LINDSEY ,  Artur Karenovich MAILYAN ,  Debashis MANDAL ,  Guillaume MATA ,  Hyunyoung MOON ,  Jay Patrick POWERS ,  Brandon Reid ROSEN ,  Yongli SU ,  Anh Thu TRAN ,  Zhang WANG ,  Xuelei YAN ,  Kai YU

IPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/395 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/3955 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07C2602/08 ,  C07C2602/10

摘要： Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

公开(公告)号：US20240245673A1

公开(公告)日：2024-07-25

申请号：US18532424

申请日：2023-12-07

申请人： Pfizer Inc.

发明人： James Matthew Frick ,  Michelle Renee Garnsey ,  Brian Stephen Gerstenberger ,  Xinjun Hou ,  Magdalena Korczynska ,  Alpha Albert Lee ,  Luong Tien Nguyen ,  Usa Reilly ,  Matthew Christopher Robinson ,  Alexandria Paige Taylor ,  Thomas Reynold Vargo ,  Lei Zhang

IPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

CPC分类号： A61K31/4709 ,  A61K31/415 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/427 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D215/38 ,  C07D231/12 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

摘要： The invention relates to compounds of Formula (I)




and pharmaceutically acceptable salts thereof as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may inhibit the activity of papain-like protease (PLpro) and may be useful in the treatment of viral infections, in particular viral infections associated with PLpro activity and/or expression such as coronaviruses infections.

公开(公告)号：US12043600B2

公开(公告)日：2024-07-23

申请号：US17285155

申请日：2019-10-17

申请人： SYNGENTA CROP PROTECTION AG

发明人： Farhan Bou Hamdan ,  Matthias Weiss ,  Atul Mahajan ,  Jagadeesh Prathap Kilaru ,  Ramya Rajan ,  Laura Quaranta ,  Stefano Rendine ,  Mathias Blum ,  Martin Pouliot ,  Simon Williams ,  Thomas James Hoffman

IPC分类号： C07D231/16 ,  A01N43/56 ,  A01N43/647 ,  C07D231/12 ,  C07D231/22 ,  C07D249/06

CPC分类号： C07D231/16 ,  A01N43/56 ,  A01N43/647 ,  C07D231/12 ,  C07D231/22 ,  C07D249/06

摘要： Compounds of the formula (I), wherein the substituents are as defined in claim 1, useful as a pesticides, especially as fungicides.

公开(公告)号：US11939303B2

公开(公告)日：2024-03-26

申请号：US17252703

申请日：2018-08-20

申请人： POLITECHNIKA GDANSKA

发明人： Sebastian Demkowicz ,  Mateusz Dasko ,  Janusz Rachon

IPC分类号： C07D249/06 ,  A61P35/00 ,  G01N33/573 ,  A61K31/4192

CPC分类号： C07D249/06 ,  A61P35/00 ,  G01N33/573 ,  A61K31/4192

摘要： The present invention relates to 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives and derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol as new compounds. The subject of the invention is the medical use of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives and the medical use of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol derivatives. The subject of the invention is the use of new compounds as an agent with the properties of a steroid sulfatase inhibitor and/or an estrogen receptor modulator. The present invention relates to the medical use of novel compounds for use as an antimicrobial medicament and/or estrogen receptor modulator. In particular, 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenyl sulfamate derivatives are for use as medicament in cancer therapy. The invention also relates to a process for the preparation of these new compounds, wherein the derivatives of 4-(1-phenyl-1H-[1,2,3]triazol-4-yl)-phenol are the intermediate product from which the sulfamate derivatives are obtained.

公开(公告)号：US20240025858A1

公开(公告)日：2024-01-25

申请号：US18257373

申请日：2021-12-15

申请人： GW Research Limited

发明人： Alan James SILCOCK ,  Antoine MILLET ,  Karen Ka-Yen TSE ,  Paul Stuart HINCHLIFFE ,  Andrew SHARPE ,  Iain David SIMPSON ,  Joanne PEACH ,  Stefano LEVANTO

IPC分类号： C07D231/12 ,  C07C39/23 ,  C07D249/06 ,  C07D239/34 ,  C07D213/65 ,  C07D213/74 ,  C07D213/16 ,  C07D213/14 ,  C07D405/04 ,  C07D263/32 ,  C07D249/08 ,  C07D261/08 ,  C07D233/64 ,  C07D271/10 ,  C07D213/64 ,  C07D405/06 ,  C07C215/50 ,  C07C213/08 ,  C07C43/23 ,  C07C41/30 ,  C07D271/06 ,  A61P25/08

CPC分类号： C07D231/12 ,  C07C39/23 ,  C07D249/06 ,  C07D239/34 ,  C07D213/65 ,  C07D213/74 ,  C07D213/16 ,  C07D213/14 ,  C07D405/04 ,  C07D263/32 ,  C07D249/08 ,  C07D261/08 ,  C07D233/64 ,  C07D271/10 ,  C07D213/64 ,  C07D405/06 ,  C07C215/50 ,  C07C213/08 ,  C07C43/23 ,  C07C41/30 ,  C07D271/06 ,  A61P25/08

摘要： The present invention relates to a group of novel compounds, methods for their manufacture and the use of these compounds as research tools and as pharmaceuticals. The novel compounds are analogues of cannabidiol (CBD). CBD is a non-psychoactive cannabinoid which has been used to treat various diseases and disorders. While such treatments hold promise, there remains a need in the art for more effective treatments and this has been brought about by way of novel cannabidiol compounds.

公开(公告)号：US20230373985A1

公开(公告)日：2023-11-23

申请号：US18030723

申请日：2021-07-12

申请人： Origenis Gmbh ,  Neuron23, Inc.

发明人： Roland KOESTLER ,  Nasser Yehia ,  Jean Tassel ,  Marcus Wegmann ,  Federico Medda ,  Patricia Perez-Gallan ,  Christiane Gilch ,  Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Zhonghua Pei ,  Scott Savage

IPC分类号： C07D417/12 ,  C07D401/14 ,  C07D491/052 ,  C07D487/04 ,  C07D413/12 ,  C07D249/06 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D405/12 ,  C07D231/38 ,  C07D498/04

CPC分类号： C07D417/12 ,  C07D401/14 ,  C07D491/052 ,  C07D487/04 ,  C07D413/12 ,  C07D249/06 ,  C07D401/12 ,  C07D413/14 ,  C07D417/14 ,  C07D405/12 ,  C07D231/38 ,  C07D498/04

摘要： The present invention relates to novel compounds that modulate the activity of one or more kinases, such as TYK2 or mutants thereof. The compounds, which may be kinase inhibitors or activators, are useful for treating autoimmune diseases, such as, such as psoriasis, lupus, multiple sclerosis, and inflammatory bowel disease.

公开(公告)号：US20230339884A1

公开(公告)日：2023-10-26

申请号：US18321092

申请日：2023-05-22

申请人： Bristol-Myers Squibb Company

发明人： Yan Shi ,  Peter Tai Wah Cheng ,  Ying Wang ,  Jun Shi ,  Shiwei Tao ,  Jun Li ,  Lawrence J. Kennedy ,  Robert F. Kaltenbach, III ,  Hao Zhang ,  James R. Corte

IPC分类号： C07D403/04 ,  C07D249/06 ,  A61P35/00 ,  C07C249/06 ,  C07D401/04 ,  C07C403/04

CPC分类号： C07D401/04 ,  A61P35/00 ,  C07C249/06 ,  C07C403/04 ,  C07D249/06 ,  C07D403/04 ,  A61P1/16

摘要： The present invention provides compounds of Formula (I):





or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.