Abstract: In a preferred embodiment, there is provided a protecting group for protecting the thiol side chain of a cysteine residue, the protecting group comprising a Diels-Alder cycloadduct of a furan and a maleimide, and optionally, a linker interposed between the thiol side chain and the Diels-Alder cycloadduct.
Type:
Grant
Filed:
September 7, 2021
Date of Patent:
January 24, 2023
Inventors:
John Frederick Trant, Daniel Meister, Sarah Nasri, Anthony Emanuel Chifor, John James Hayward, Seyedeh Maryamdokht Taimoory, Mohadeseh Dashti-Pour
Abstract: Methods of treating cancer, such as leukemia, via administration of therapeutically effective amounts of artemisinins and one or more additional therapeutic agents are detailed herein. The artemisinins include artesunate, dihydroartemisinin, artemether, arteether, artelinate, ART-631, and ART-838. The one or more additional therapeutic agents include BCL-2 inhibitors such as ABT-199, ABT-263, and ABT-737; kinase inhibitors such as lestaurtinib, midostaurin, and sorafenib; and anti-neoplastic agents such as cytarabine, doxorubicin, etoposide, cyclophosphamide, triplotide, vinorelbine, cisplatin, and rituximab.
Abstract: Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
January 17, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Robert M. Garbaccio, Jeffrey C. Kern, James J. Mulhearn, Philip E. Brandish
Abstract: Disclosed herein are compounds of formula I and/or a stereoisomer, stable isotopologue, and/or pharmaceutically acceptable salts thereof; and therapeutic uses of these compounds, which are inhibitors of tryptophan 2, 3-dioxygenase 2 (TDO2) and/or indoleamine 2, 3-dioxygenase 1 (IDO1), potentially useful in the treatment of diseases treatable, such as cancers.
Type:
Grant
Filed:
October 19, 2018
Date of Patent:
January 10, 2023
Assignee:
JS Innopharm (Shanghai) Ltd.
Inventors:
Jintao Zhang, Wen Xu, Shanzhong Jian, Ao Li, Qun Li
Abstract: The present disclosure provides methods for producing N-(fluorosulfonyl)azoles, sulfonyldiazoles, or related derivatives thereof, and the related products including N-(fluorosulfonyl)azoles, sulfonyldiazoles, and related derivatives thereof. For example, an N-(fluorosulfonyl)azole is obtained by reaction of sulfuryl fluoride with an azoles, an azolate salt, an N-silylazole, or a combination thereof. Symmetric and asymmetric sulfonyldiazoles are obtained by further reaction of such an N-(fluorosulfonyl)azole with azoles, azolate salts, or N-silylazoles. A sulfonyldiazole can be also produced by reacting sulfuryl fluoride with an azole, an N-silylazole, or a combination thereof in one pot.
Abstract: The present invention relates to substituted imidazolidin-2-one derivatives of formula (I) or pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and utility as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions and disorders mediated by PRMT5, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.
Abstract: Described herein are trehalose analogues. Also described herein are methods of making the trehalose analogues and uses of the analogues. For example, the disclosed trehalose analogues may be useful in the detection of bacteria.
Abstract: The disclosure relates to USP30 Inhibitor Compounds I, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising same, and medical uses involving same.
Type:
Grant
Filed:
October 4, 2019
Date of Patent:
December 27, 2022
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Alex J. Buckmelter, Justin Andrew Caravella, Hongbin Li, Matthew W. Martin, Steven Mischke, David James Richard, Angela V. West
Abstract: A heterocyclic compound and an organic light-emitting device including the same are provided. The heterocyclic compound is represented by Formula 1: Details of R1, R2, R3, X1, L1, and a1 and b1 are provided in the disclosure.
Type:
Grant
Filed:
June 16, 2017
Date of Patent:
December 27, 2022
Assignee:
SAMSUNG DISPLAY CO., LTD.
Inventors:
Soobyung Ko, Haejin Kim, Mieun Jun, Youngkook Kim, Seokhwan Hwang
Abstract: Provided are a novel tetracarboxylic acid dianhydride and a method for preparing the same. According to an exemplary embodiment of the present invention, a novel tetracarboxylic acid dianhydride appropriate for providing a polyimide film having high transparency and thermal resistance and having excellent thermal dimensional stability due to a substrate of which the stress is not increased even with a heat treatment at a high temperature and a method for preparing the same may be provided.
Type:
Grant
Filed:
July 9, 2021
Date of Patent:
December 20, 2022
Assignees:
SK Innovation Co., Ltd., SK ie technology Co., Ltd.
Abstract: Disclosed are a class of pyrazole compounds and applications thereof in the preparation of a medicament for treating related diseases. Specifically, related are a compound represented by formula (II) and a pharmaceutically acceptable salt thereof.
Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
Type:
Grant
Filed:
August 27, 2020
Date of Patent:
November 29, 2022
Assignee:
Epizyme, Inc.
Inventors:
Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kerren Kalai Swinger
Abstract: Hydrophilic Linkers, Drug-Linker compounds, Drug-Ligand Conjugate compounds and Ligand-Linkers and methods of making and using the same are provided.
Type:
Grant
Filed:
January 27, 2021
Date of Patent:
November 29, 2022
Assignee:
Seagen Inc.
Inventors:
Svetlana Doronina, Robert Lyon, Peter Senter
Abstract: Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
Type:
Grant
Filed:
October 30, 2020
Date of Patent:
November 29, 2022
Assignee:
Pfizer Inc.
Inventors:
Gary Erik Aspnes, Scott W. Bagley, John M. Curto, Matthew S. Dowling, David Edmonds, Mark E. Flanagan, Kentaro Futatsugi, David A. Griffith, Kim Huard, Gajendra Ingle, Wenhua Jiao, Chris Limberakis, Alan M. Mathiowetz, David W. Piotrowski, Roger B. Ruggeri
Abstract: The present invention relates to salt forms of the Pim kinase inhibitor N-{(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of Pim kinase-related diseases such as cancer.
Type:
Grant
Filed:
January 13, 2021
Date of Patent:
November 22, 2022
Assignee:
Incyte Corporation
Inventors:
Zhongjiang Jia, Ganfeng Cao, Qiyan Lin, Yongchun Pan, Lei Qiao, Vaqar Sharief, Chongsheng Eric Shi, Michael Xia, Changsheng Zheng, Qun Li
Abstract: Described herein are epinephrine salts, specifically the epinephrine malonate salt; the epinephrine malonate salt in crystalline form; a pharmaceutical composition comprising epinephrine malonate; a sublingual or buccal pharmaceutical composition comprising epinephrine malonate in crystalline form; and a method for treating a patient comprising administering a pharmaceutical composition of epinephrine malonate in crystalline form.
Abstract: Compositions of pro-chelator compounds are described herein. The pro-chelators may be activated in reducing conditions, such as in the intracellular space, so as to sequester metals such as iron. The pro-chelators may be used to target malignant cells or in the treatment in a condition associated with metal ion disregulation.
Type:
Grant
Filed:
November 26, 2018
Date of Patent:
November 22, 2022
Assignee:
ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
Inventors:
Elisa Tomat, Tsuhen Chang, Eman A. Akam
Abstract: Described herein in part are silanol based therapeutic payloads comprising a silanol terminus, a divalent spacer moiety, and a drug moiety capable of effecting a target cell or tissue.
Type:
Grant
Filed:
June 29, 2020
Date of Patent:
November 15, 2022
Assignee:
BlinkBio, Inc.
Inventors:
Hanh N. Nguyen, Leslie O. Ofori, Jutta Wanner, Douglas S. Werner
Abstract: Chemical compositions, and related methods for synthesizing furan, such as oleo-furan, surfactants, include calcium, magnesium, ammonium and/or lithium cations and one of a number of furan derivatives. Methods for synthesizing such furan surfactants containing calcium, magnesium, ammonium and/or lithium cations can include chemical reagents and purification procedures to prepare furan surfactants containing calcium, magnesium, ammonium and/or lithium cations. These furan surfactant compositions can be free of dioxane and ethoxylate.
Type:
Grant
Filed:
May 3, 2021
Date of Patent:
November 8, 2022
Assignee:
SIRONIX RENEWABLES, INC.
Inventors:
Shawn Eady, Sabrina Conrad, Trenton Wilke, Christoph Krumm
Abstract: Certain embodiments are directed hydrophilic redox substrates for leukocyte esterase (LE). In certain aspects a hydrophilic redox leukocyte esterase substrate or a small molecule enzyme substrate for use in methods and/or devices to electrochemically detect and/or measure LE activity in a sample.
Type:
Grant
Filed:
November 8, 2018
Date of Patent:
November 8, 2022
Assignee:
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Waldemar Gorski, Stanton McHardy, Douglas Hanson, Travis Menard, Andrew Fleischman