公开(公告)号：US20240246951A1

公开(公告)日：2024-07-25

申请号：US17928746

申请日：2022-07-14

Applicant: NATIONAL CENTER FOR GLOBAL HEALTH AND MEDICINE

Inventor： Hiroaki MITSUYA ,  Hirokazu TAMAMURA ,  Nobuyo KUWATA

IPC: C07D417/14 ,  A61K31/428 ,  A61P31/14

CPC classification number: C07D417/14 ,  A61K31/428 ,  A61P31/14

Abstract: A compound represented by the following general formula (1) that has an activity of suppressing a virus protease and an antiviral activity and has a low toxicity to a host cell:

公开(公告)号：US12043621B2

公开(公告)日：2024-07-23

申请号：US17206542

申请日：2021-03-19

Applicant: Trustees of Boston University ,  Massachusetts Institute of Technology

Inventor： Arturo Vegas ,  Sean Quinnell ,  Daniel Sheehy ,  Kelly Tan ,  Luke Ceo ,  Stephen Thomas Nestor ,  Angela Nicole Koehler ,  Becky Leifer ,  Shelby Doyle

IPC: C07D471/14 ,  A61K45/06 ,  C07D207/09 ,  C07D211/96 ,  C07D213/85 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07K16/28

CPC classification number: C07D417/14 ,  A61K45/06 ,  C07D207/09 ,  C07D211/96 ,  C07D213/85 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/06 ,  C07D471/04 ,  C07D495/04 ,  C07K16/2866

Abstract: The technology described herein is directed to IL-4 and/or IL-13 inhibitors and uses thereof.

公开(公告)号：US20240239807A1

公开(公告)日：2024-07-18

申请号：US18365919

申请日：2023-08-04

Applicant: Gilead Sciences, Inc.

Inventor： Stephen E. Ammann ,  Xinpei Cai ,  Eda Y. Canales ,  Weng K. Chang ,  Gregory F. Chin ,  Henok H. Kinfe ,  Scott E. Lazerwith ,  Jessica L. McKinley ,  Michael R. Mish ,  Devan Naduthambi ,  Jason K. Perry ,  Kevin X. Rodriguez ,  Scott D. Schroeder ,  Christopher J. Swank ,  Joshua J. Van Veldhuizen

IPC: C07D495/04 ,  A61P31/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D495/04 ,  A61P31/14 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

Abstract: The present disclosure relates to compounds of Formula I:




and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, useful in the treatment of treating viral infections, for example, coronaviridae infections.

公开(公告)号：US20240239786A1

公开(公告)日：2024-07-18

申请号：US18555112

申请日：2022-04-11

Applicant: Yale University

Inventor： Z Ping Lin ,  Elena Ratner ,  Yong-Lian Zhu

IPC: C07D417/14 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/502 ,  A61P35/00 ,  C07D249/12 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D417/14 ,  A61K31/4196 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/502 ,  A61P35/00 ,  C07D249/12 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

Abstract: The present invention relates to compounds represented by Formulae (I) to (V), or a racemate, enantiomer, diastereomer, pharmaceutically acceptable salt, solvate, hydrate, or derivative thereof, and compositions thereof. In various aspects, the present invention also relates to methods of reducing or inhibiting ribonucleotide reductase (RNR), poly ADP-ribose polymerase (PARP), and/or homologous recombination (HR) repair using said compounds. In some aspects, the present invention relates to methods of inducing at least one double strand break (DSB) using said compounds. In another aspect, the present invention relates to methods of treating or preventing cancer (e.g., ovarian cancer, BRCA-wild type cancer, etc.) using said compounds.

公开(公告)号：US20240239772A1

公开(公告)日：2024-07-18

申请号：US18556564

申请日：2022-04-21

Applicant: The Cleveland Clinic Foundation

Inventor： Shaun R. Stauffer ,  Sang Hoon Han ,  Alice Hooper ,  Joshua Maw ,  Dhiraj P. Sonawane ,  Matthew R. Porter ,  Steven Martinez ,  Joseph Alvarado ,  Jonathan D. Macdonald

IPC: C07D403/12 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/496 ,  A61P31/14 ,  C07D249/04 ,  C07D249/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

CPC classification number: C07D403/12 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/496 ,  A61P31/14 ,  C07D249/04 ,  C07D249/18 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: Disclosed herein are compounds that inhibit 3C-like protease and inhibit replication of viruses, including SARS-CoV-2. Also disclosed herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds, e.g., in a method of treating a viral infection, such as a coronavirus infection.

公开(公告)号：US12036209B2

公开(公告)日：2024-07-16

申请号：US17196695

申请日：2021-03-09

Applicant: Arvinas Operations, Inc.

Inventor： Andrew P. Crew ,  Erika Araujo

IPC: A61K31/437 ,  A61K31/422 ,  A61K31/427 ,  A61K31/551 ,  A61K38/20 ,  A61K38/53 ,  A61K47/64 ,  A61P21/04 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04

CPC classification number: A61K31/437 ,  A61K31/422 ,  A61K31/427 ,  A61K31/551 ,  A61K38/2006 ,  A61K38/53 ,  A61K47/642 ,  A61P21/04 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D401/14 ,  C07D417/14 ,  C07D487/04

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240228464A9

公开(公告)日：2024-07-11

申请号：US18383949

申请日：2023-10-26

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Guoqiang Wang ,  Ruichao Shen ,  Brett Granger ,  Jing He ,  Xuechao Xing ,  Yong He ,  Jiang Long ,  Jun Ma ,  Bin Wang ,  Yat Sun Or

IPC: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof:




which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which is associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).

公开(公告)号：US12030875B2

公开(公告)日：2024-07-09

申请号：US17273878

申请日：2019-09-06

Applicant: PIC Therapeutics, Inc.

Inventor： Ashis Saha

IPC: C07D417/04 ,  A61P35/00 ,  C07D277/30 ,  C07D277/42 ,  C07D417/10 ,  C07D417/14

CPC classification number: C07D417/04 ,  A61P35/00 ,  C07D277/30 ,  C07D277/42 ,  C07D417/10 ,  C07D417/14

Abstract: The present invention provides compounds inhibiting eIF4E activity, and compositions and methods of using thereof. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful for treating a variety of diseases, disorders or conditions, associated with eIF4E. Such diseases, disorders, or conditions include cellular proliferative disorders (e.g., cancer) such as those described herein.

公开(公告)号：US12030872B2

公开(公告)日：2024-07-09

申请号：US17286870

申请日：2019-10-25

Applicant: Merck Sharp & Dohme LLC

Inventor： Vladimir Simov ,  William P. Kaplan ,  John J. Acton, III ,  Michael J. Ardolino ,  Joanna L Chen ,  Peter H. Fuller ,  Hakan Gunaydin ,  Derun Li ,  Ping Liu ,  Kaitlyn Marie Logan ,  Joey Methot ,  Gregori J. Morriello ,  Santhosh F. Neelamkavil ,  Luis Torres ,  Xin Yan ,  Hua Zhou

IPC: C07D405/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D403/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of diseases, such as Parkinson's disease, in which LRRK-2 kinase is involved.

公开(公告)号：US20240217963A1

公开(公告)日：2024-07-04

申请号：US18549923

申请日：2022-03-17

Applicant: SIRONAX LTD.

Inventor： Yaning SU ,  Zhaolan ZHANG ,  Yanping XU ,  Zhiyuan ZHANG

IPC: C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

Abstract: It provides compounds of Formula I, compositions comprising the same, and methods of using the same, including use in treating various diseases and conditions, including those mediated by receptor-interacting protein 1 (RIP1) signaling.