Abstract: The invention relates to quinazoline compounds, the preparation method, use, and the pharmaceutical composition thereof. The said quinazoline compounds, which are represented by Formula (I), are phosphatidylinositol 3-kinase (PI3K) inhibitors, and can be applied to prevent and/or treat PI3K activity-related diseases, such as cancer, immune diseases, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders or neurological diseases.
Type:
Grant
Filed:
December 26, 2017
Date of Patent:
December 27, 2022
Assignee:
INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
Inventors:
Heng Xu, Xiaoguang Chen, Songwen Lin, Ming Ji, Jing Jin, Deyu Wu, Chunyang Wang, Yuanhao Lv
Abstract: Disclosed are novel dioxoisoquinolinone derivative compounds, pharmaceutically acceptable salts thereof, optical isomers, hydrates, and solvates thereof as well as uses thereof. More specifically, the novel dioxoisoquinolinone derivative compounds, pharmaceutically acceptable salts, optical isomers, hydrates, solvates show inhibition activity of EZH1 (Enhancer of zeste homolog 1) and/or EZH2 (Enhancer of zeste homolog 2) activity. Pharmaceutical compositions containing the compound is also disclosed.
Type:
Grant
Filed:
May 20, 2021
Date of Patent:
December 27, 2022
Assignee:
HANMI PHARMACEUTICAL CO., LTD.
Inventors:
Seung Hyun Jung, Dong Jin Hong, Ji Young Hwang, Seo Hee Kim, So Min Park, Shin Mee Mah, Young Gil Ahn
Abstract: Histone deacetylases (HDACs) inhibitors are disclosed according to the following structural formula. The moiety A is a benzene ring, optionally substituted. The moiety B is a benzene ring attached at the 1,4 or 1,3 position, or a cyclohexane ring attached at the 1,4 position, optionally substituted. R and Z are further substituents. The HDACs inhibitors possess cytotoxicities to various cancer cell lines. They are useful for treating a tumor associated with deregulation of the activity of histone deacetylases in a subject in need thereof, in one embodiment, the HDACs inhibitors of the invention are useful for treating glioma, breast cancer, colon cancer, target cell lung cancer, adenocarcinoma of the lung, small cell lung cancer, stomach cancer, liver cancer, ovary adenocarcinoma, pancreas carcinoma, prostate carcinoma, promyiocytic leukemia, chronic myelocytic leukemia, or acute lymphocytic leukemia in a subject in need thereof.
Abstract: Disclosed is a pyrimidine compound acting on an EGFR exon 20 insertion mutation and an ERBB2 exon 20 insertion mutation or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
July 24, 2020
Date of Patent:
December 20, 2022
Assignee:
CHINA RESOURCES PHARMACEUTICAL HOLDINGS COMPANY LIMITED
Inventors:
Charles Z. Ding, Lu Zhang, Xile Liu, Lihong Hu, Wen Jiang, Jian Li, Shuhui Chen
Abstract: The present invention relates to novel compounds having the general formula: and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for suppressing tumor cell growth, ameliorating the pathogenesis of systemic lupus erythematosus, and the treatment of various other disorders, including Noonan syndrome, diabetes, neutropenia, neuroblastoma, melanoma, juvenile leukemia, juvenile myelomonocytic leukemia, chronic myelomonocytic leukemia, acute myeloid leukemia, and other cancers associated with SHP2 deregulation with the compounds and compositions of the invention, alone or in combination with other treatments.
Type:
Grant
Filed:
September 22, 2017
Date of Patent:
December 20, 2022
Assignees:
Relay Therapeutics, Inc., D. E. Shaw Research, LLC
Inventors:
Brian K. Albrecht, Fabrizio Giordanetto, Jack Benjamin Greisman, Paul Maragakis, Alexander M. Taylor, W. Patrick Walters
Abstract: The present invention relates to a triazine compound according to formula 1: suitable for use as a layer material for electronic devices, and to an organic semiconductor layer comprising at least one compound according to formula 1, as well as to an organic electronic device comprising at least one organic semiconductor layer, and a method of manufacturing the same.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
December 20, 2022
Assignees:
Novaled GmbH, Samsung SDI Co. Ltd.
Inventors:
Benjamin Schulze, Ansgar Werner, Elena Galan, Regina Luschtinetz, Qiang Huang, Kipo Jang, Hyungsun Kim
Abstract: Disclosed are a compound selected from novel pyrimido[4,5-d]pyrimidin-2-one derivative compounds having excellent anti-proliferative activity against cancer cells, pharmaceutically acceptable salts thereof, hydrates thereof and stereoisomers thereof, a method for preparing the compound, a pharmaceutical composition for preventing, alleviating or treating cancer metastasis and proliferative diseases containing the compound as an active ingredient, and an anticancer composition against cancer cells, containing the compound as an active ingredient. The compounds of this invention exhibit most excellent selective inhibitory activity against LCK and anti-proliferative activity against cancer cells, thus being useful for inhibiting cancer cells, and for preventing or treating cancer metastasis and proliferative diseases.
Type:
Grant
Filed:
August 25, 2020
Date of Patent:
December 20, 2022
Assignee:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
Inventors:
Seo Jung Han, Tae Bo Sim, Do Hee Oh, Jae Eun Cheong, Dong Keon Hwang
Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 3, 2022
Date of Patent:
December 20, 2022
Assignee:
Deciphera Pharmaceuticals, LLC
Inventors:
Rodrigo Ruiz Soto, Oliver Rosen, Jama Pitman
Abstract: The present invention relates to compounds of Formulae (I) and (II) as defined herein, and salts and solvates thereof. The present invention also relates to pharmaceutical compositions comprising compounds of Formulae (I) and (II), and to the use of compounds of Formulae (I) and (II) in the treatment or prevention of filarial worm infection, as well as other diseases or conditions in which filarial worm infection is implicated.
Type:
Grant
Filed:
January 17, 2018
Date of Patent:
December 6, 2022
Assignees:
Liverpool School of Tropical Medicine, The University of Liverpool, Eisai R&D Management Co., Ltd.
Inventors:
Stephen A. Ward, Mark J. Taylor, Paul M. O'Neill, Weiqian David Hong, Farid Benayoud
Abstract: The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I) to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
November 8, 2022
Assignee:
Mirati Therapeutics, Inc.
Inventors:
Thomas P. Bobinski, Christopher Ronald Smith, Matthew Arnold Marx, John Michael Ketcham, Aaron Craig Burns, John David Lawson, Svitlana Kulyk, Jon Kuehler, Anthony Ivetac
Abstract: Methods of inducing apoptosis of cancer cells by contacting the cancer cells with a pyridine derivative are provided. Methods of treating a subject suffering from a hyperproliferative disease or complications thereof comprising the step of administering a therapeutically effective amount of a composition to the subject, wherein the composition comprises pyridine derivatives are provided.
Type:
Grant
Filed:
February 17, 2022
Date of Patent:
November 8, 2022
Assignee:
King Abdulaziz University
Inventors:
Khadijah M. Al-Zaydi, Meaad Bagazi, Tamer Said Saleh
Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
Type:
Grant
Filed:
February 13, 2018
Date of Patent:
November 8, 2022
Assignee:
PRAXIS PRECISION MEDICINES, INC.
Inventors:
Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
Abstract: The present disclosure provides compounds having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein X1, X2, X11, X12, R1, R3, R5, R5?, R6, and R7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to inhibit a USP1 protein and/or to treat a disorder responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
November 1, 2022
Assignee:
KSQ Therapeutics, Inc.
Inventors:
Jehrod Burnett Brenneman, Elsa Beyer Krall, Michael Schlabach, Andrew Alistair Wylie
Abstract: A problem is presented in that conventional photochromic compounds cannot be considered adequate in terms of the colorizing/decolorizing rate and durability, and the production process therefore has many steps. The present invention provides an industrially applicable photochromic compound that has both a rapid colorizing/decolorizing reaction and high durability and can also be synthesized at a low cost. This compound is characterized in that etheric oxygen atoms are bonded to the carbon atoms at position 1 of a pyranoquinazoline (8H-pyrano[3,2-f]quinazoline) skeleton and position 10 of a naphthopyran (3H-naphtho[2,1-b]pyran) skeleton, said compound having photochromic properties and being a photochromic compound that has both a rapid colorizing/decolorizing reaction and high durability. Also provided is an industrially applicable photochromic compound that can be synthesized at a low cost.
Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Type:
Grant
Filed:
February 11, 2020
Date of Patent:
October 25, 2022
Assignee:
National Institute of Biological Sciences, Beijing
Inventors:
Zhiyuan Zhang, Xiaodong Wang, Yaning Su, Hanying Ruan, Yan Ren
Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Type:
Grant
Filed:
September 4, 2020
Date of Patent:
October 25, 2022
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor
Abstract: The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds of Formula (I) to pharmaceutical compositions comprising compounds of Formula (I) and to methods of use thereof, such as methods of treating cancer using the compounds of Formula (I) and pharmaceutical compositions comprising those compounds.
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
October 25, 2022
Assignee:
Mirati Therapeutics, Inc.
Inventors:
Thomas P. Bobinski, Christopher Ronald Smith, Matthew Arnold Marx, John Michael Ketcham, Aaron Craig Burns, John David Lawson, Svitlana Kulyk, Jon Kuehler, Anthony Ivetac
Abstract: Disclosed herein are serine threonine kinase (AKT) degradation/disruption compounds including an AKT ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of AKT-mediated diseases.
Type:
Grant
Filed:
March 6, 2019
Date of Patent:
October 18, 2022
Assignee:
Icahn School of Medicine at Mount Sinai
Inventors:
Jian Jin, Jing Liu, Ramon E. Parsons, Jia Xu, Xufen Yu
Abstract: The compounds of formula (I) where the group —R may represent ?O or —H, are new anti-proliferative agents with remarkable anti-tumour effects in-vivo, showing in particular a wide spectrum of activities in respect of lymphomas of different origin.
Type:
Grant
Filed:
March 26, 2018
Date of Patent:
October 18, 2022
Assignee:
FONDAZIONE PER L'ISTITUTO ONCOLOGICO DI RICERCA (IOR)
Inventors:
Eugenio Gaudio, Francesco Bertoni, Natalina Pazzi, Matilde Guala