公开(公告)号：US20240317767A1

公开(公告)日：2024-09-26

申请号：US18670264

申请日：2024-05-21

Applicant: AstraZeneca AB

Inventor： Johan Olof BRODDEFALK ,  Hans Fredrik EMTENÂS ,  Kenneth Lars GRANBERG ,  Malin Anita LEMURELL ,  Daniel Tor PETTERSEN ,  Alleyn Thomas PLOWRIGHT ,  Lars Johan Andreas ULANDER

IPC: C07D487/04 ,  A61K31/4155 ,  A61K31/4985 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  C07D231/40 ,  C07D231/44 ,  C07D231/50 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/4155 ,  A61K31/4985 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  C07D231/40 ,  C07D231/44 ,  C07D231/50 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04

Abstract: The present application relates to novel compounds of formula (I)




to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.

公开(公告)号：US20240018113A1

公开(公告)日：2024-01-18

申请号：US18372771

申请日：2023-09-26

Applicant: Astellas Pharma, Inc. ,  Mitobridge, Inc.

Inventor： Junko Maeda ,  Ikumi Kuriwaki ,  Kai Kitamura ,  Yumi Yamashita ,  Kenichi Kakefuda ,  Akio Kamikawa ,  Kenji Negoro ,  Wataru Hamaguchi ,  Ryushi Seo ,  Jeffrey Ciavarri

IPC: C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

CPC classification number: C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

Abstract: [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

公开(公告)号：US11787766B2

公开(公告)日：2023-10-17

申请号：US16639949

申请日：2018-08-17

Applicant: SHANGHAI ENNOVABIO PHARMACEUTICALS CO., LTD.

Inventor： Lei Jiang ,  Jianwen Deng ,  Xiaoli Lu ,  Ke Shang ,  Jianyong Shou ,  Bing Wang ,  Danyi Wu ,  Xueli Xu ,  Yuan Xu ,  Yi Zhang ,  Mingwei Zheng

IPC: C07D213/69 ,  C07D213/73 ,  C07D213/84 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D519/00 ,  A61K31/137 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4545 ,  A61K39/12 ,  A61K39/245 ,  A61K39/29 ,  A61K45/06 ,  C07C211/03 ,  C07C223/02 ,  C07D231/40

CPC classification number: C07D213/69 ,  A61K31/137 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4545 ,  A61K39/12 ,  A61K39/245 ,  A61K39/29 ,  A61K45/06 ,  C07C211/03 ,  C07C223/02 ,  C07D213/73 ,  C07D213/84 ,  C07D231/40 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D519/00

Abstract: Provided are a compound for the prevention and treatment of diseases associated with PD-L1, a preparation method therefor and use thereof. Specifically, provided are the compound of formula I, the stereoisomer and the racemate thereof, or pharmaceutically acceptable salts thereof, and also provided is an application thereof in the preparation of a drug for the prevention and treatment of diseases associated with PD-L1.

公开(公告)号：US20230242548A1

公开(公告)日：2023-08-03

申请号：US18058655

申请日：2022-11-23

Applicant: The Regents of the University of California

Inventor： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC: C07D495/04 ,  A61K38/17 ,  C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D207/14 ,  C07D211/62 ,  C07D295/185 ,  C07D295/26 ,  C07D211/58 ,  C07D487/04 ,  C12N9/14 ,  C07C235/20 ,  C07C317/08 ,  C12Q1/6886

CPC classification number: C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/26 ,  C07D295/185 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US11667648B2

公开(公告)日：2023-06-06

申请号：US16813295

申请日：2020-03-09

Applicant: Promega Corporation

Inventor： Sergiy Levin ,  Rachel Friedman Ohana ,  Thomas Kirkland ,  Keith V. Wood

IPC: C07D491/22 ,  C07D231/40 ,  C07D487/04

CPC classification number: C07D491/22 ,  C07D231/40 ,  C07D487/04

Abstract: Provided herein are cell-permeable, cell-compatible, and chemoselectively-cleavable linkers for tethering (e.g., covalently) functional elements (e.g., a cellular interaction element and a capture element), and methods of use (e.g., intracellular capture and extracellular release of cellular targets) therewith.

公开(公告)号：US11247987B2

公开(公告)日：2022-02-15

申请号：US16753439

申请日：2018-10-05

Applicant: FORMA Therapeutics, Inc.

Inventor： Justin Caravella ,  Bingsong Han ,  Cuixian Liu ,  Stephanos Ioannidis ,  Alexandre Joseph Buckmelter ,  David James Richard ,  Matthew W. Martin ,  Steven Mischke ,  Scot Mente

IPC: C07D417/04 ,  C07D417/12 ,  C07C261/04 ,  C07D231/40 ,  C07D241/04 ,  C07D265/30 ,  C07D277/46 ,  C07D277/56

Abstract: The present disclosure relates to chemical entities useful as inhibitors of Ubiquitin Specific Protease 30 (USP30), pharmaceutical compositions comprising the chemical entities, and methods of using the chemical entities. The chemical entities as disclosed herein can be useful in the treatment of a disease, disorder, or condition involving mitochondrial dysfunction, including neurodegenerative diseases, motor neuron diseases, metabolic disorders, and cancers, among other ailments. Chemical entities disclosed herein include compounds of Formula (II): wherein A, R2, R3, R4, Ra, Rc, Rd, Re, Rf, and m are defined herein.

公开(公告)号：US11225469B2

公开(公告)日：2022-01-18

申请号：US15543643

申请日：2016-01-15

Applicant: Whitehead Institute for Biomedical Research ,  Dana-Farber Cancer Institute, Inc. ,  The United States of America, as represented by the Secretary, Department of Health and Human Services

Inventor： David M. Sabatini ,  Michael Pacold ,  Matthew B. Boxer ,  Jason M. Rohde ,  Kyle R. Brimacombe ,  Min Shen ,  Ganesha Bantukallu ,  Li Liu

IPC: C07D401/12 ,  C07D213/75 ,  C07D213/40 ,  A61K45/06 ,  C07D233/88 ,  C07D213/78 ,  C07D235/30 ,  C07D249/14 ,  C07D231/40 ,  A61P43/00 ,  A61P35/00

Abstract: The present invention provides compounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both.

公开(公告)号：US11186596B2

公开(公告)日：2021-11-30

申请号：US17047787

申请日：2019-04-26

Applicant: ADT PHARMACEUTICALS, LLC

Inventor： Michael Boyd ,  Xi Chen

IPC: C07F5/02 ,  C07C235/32 ,  C07D213/40 ,  C07D213/56 ,  C07D231/40 ,  C07D261/08 ,  C07D277/28 ,  C07D307/52 ,  C07D317/12 ,  C07D327/04

Abstract: Disclosed are compounds for medical uses, for example, compounds of formula (Ia), wherein A1, A2, A3, A4, A5, A6, A7, R6, R7 and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.

公开(公告)号：US20210221778A1

公开(公告)日：2021-07-22

申请号：US16501272

申请日：2017-09-12

Applicant: Nuria Vilaboa ,  Richard W. Voellmy

Inventor： Nuria Vilaboa ,  Richard W. Voellmy

IPC: C07D277/46 ,  C07D277/82 ,  C07D333/36 ,  C07D417/04 ,  C07D417/12 ,  C07D277/56 ,  C07D417/14 ,  C07D263/48 ,  C07D261/14 ,  C07D231/40 ,  C07D285/135 ,  C07D213/75 ,  C07D215/42 ,  A61P35/00

Abstract: The present disclosure relates to a class of mammalian heat shock factor (HSF) inhibitors, to pharmaceutical compositions comprising these inhibitors as well as to methods for using the inhibitors. The inhibitors inhibit stress-induced expression from heat shock gene promoters. Furthermore, the inhibitors are cytotoxic to a variety of human cancer cells types.

公开(公告)号：US11008334B2

公开(公告)日：2021-05-18

申请号：US16720526

申请日：2019-12-19

Applicant: The Regents of the University of California

Inventor： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC: C12Q1/6886 ,  C12N9/14 ,  C07D495/04 ,  A61K38/17 ,  C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D207/14 ,  C07D211/62 ,  C07D295/185 ,  C07D295/26 ,  C07D211/58 ,  C07D487/04 ,  C07C235/20 ,  C07C317/08

Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.