Abstract: A novel class of inhibitors of protein kinases that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of one or more CDK enzyme and/or by one or more aberrant CDK activity, including certain cancers of lung, breast, brain, ovary, prostate, colorectal cancer and leukaemias. The inhibitors have the general structure (I).
Type:
Grant
Filed:
February 1, 2018
Date of Patent:
September 7, 2021
Assignee:
Aucentra Therapeutics Pty Ltd
Inventors:
Shudong Wang, Sarah Al Haj Diab, Yi Long
Abstract: Provided are a sultam compound having isocitrate dehydrogenase 1 (IDH1) inhibitory activity as represented by formula I or pharmaceutically-acceptable salts, solvates or hydrates thereof, a preparation method thereof, and a pharmaceutical composition containing the compound. The compound or the pharmaceutically-acceptable salts, solvates or hydrates thereof, and the pharmaceutical composition containing the compound can be used to treat IDH1 mutation-induced cancers.
Type:
Grant
Filed:
March 22, 2017
Date of Patent:
September 7, 2021
Assignees:
Chai Tai Tianqing Pharmaceutical Group Co., Ltd., Lianyungang Runzhong Pharmaceutical Co., Ltd., Centaurus Biopharma Co., Ltd.
Abstract: Formula III compound, its products and pharmaceutical compositions containing them for the treatment of central nervous and vascular system diseases, particularly neurodegenerative disorders with cognitive deterioration, diseases associated with oxidative stress, diseases taking in mitochondrial dysfunction, Parkinson's disease and neuropathic pain, as well as the pathological processes associated with aging.
Type:
Grant
Filed:
May 3, 2017
Date of Patent:
August 24, 2021
Assignees:
UNIVERSIDAD DE LA HABANA, CENTRO DE INVESTIGACIÓN Y DESARROLLO DE MEDICAMENTOS CIDEM
Abstract: The present disclosure describes novel TRK kinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such TRK kinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.
Type:
Grant
Filed:
October 11, 2018
Date of Patent:
August 24, 2021
Assignee:
ANGEX PHARMACEUTICAL, INC.
Inventors:
Wen-Lian Wu, Zhiqiang Yang, Francis Lee, John Qiang Tan
Abstract: Novel compounds and pharmaceutically acceptable salts capable of modulating the activity of kinases, including Akt, ERK and MEK. Such modulation affects biological functions, for example, by inhibiting cell proliferation and/or inducing apoptosis. Also provided are pharmaceutical compositions and medicaments, comprising the compounds or salts of the invention, alone or in combination with other therapeutic agents or palliative agents.
Abstract: Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.
Type:
Grant
Filed:
February 12, 2021
Date of Patent:
August 10, 2021
Assignee:
IDEAYA BIOSCIENCES, INC.
Inventors:
Muzaffar Alam, Leah Cleary, Melissa Fleury, Zhonghua Pei, Richard Steel, James Sutton, John E. Knox, Zachary E. R. Newby
Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.
Type:
Grant
Filed:
December 27, 2018
Date of Patent:
August 10, 2021
Assignee:
eFFECTOR Therapeutics Inc.
Inventors:
Justin T. Ernst, Paul A. Sprengeler, Siegfried H. Reich, Samuel Sperry
Abstract: The present invention provides pyrazole derivatives of Formula (I), and in particular N1-(4-(5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl) pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as casein kinase 1 (CK1) and/or interleukin 1 receptor associated kinase 1 (IRAKI) inhibitors for treating cancer, inflammatory and immune related disorders.
Abstract: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
Abstract: Disclosed are crystalline forms of sepiapterin free base selected from polymorphs A, B, C, D, E, F, and G, and combinations thereof, as well as crystalline polymorphs of salts of sepiapterin. Also disclosed are pharmaceutical compositions containing one or more such polymorphs and methods for preparing such polymorphs. Sepiapterin is useful in the treatment of a number diseases associated with low cellular levels of BH4, for example, phenylketonuria.
Abstract: Provided are compounds that target the nucleotide-binding oligomerization domain, leucine rich repeat containing X1 (NLRX1) pathway. The compounds can be used to treat multiple conditions, including inflammatory, immune-mediated, and/or chronic inflammatory gastrointestinal diseases; systemic immune-mediated diseases; cancers; and infectious diseases.
Type:
Grant
Filed:
May 1, 2020
Date of Patent:
July 20, 2021
Assignee:
LANDOS BIOPHARMA, INC.
Inventors:
Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas
Abstract: The present application provides dihydropyrido[2,3-d]pyrimidone inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
Type:
Grant
Filed:
October 10, 2019
Date of Patent:
July 20, 2021
Assignee:
Incyte Corporation
Inventors:
Alexander Sokolsky, Liangxing Wu, Wenqing Yao
Abstract: Crystalline forms of seletalisib, designated as Form B and Form F and characterized herein, being selective inhibitors of PI3 kinase enzymes, in particular of the human PBK? isoform, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
July 13, 2021
Assignee:
UCB Biopharma SPRL
Inventors:
Luc Lambert Jozef Jan Aerts, Georges Assaf, Nicolas Edmond Carly, Vincent Adolphe Carol Cool, Jean-Pierre Delatinne, Laurent Jacques Willy Delhaye, Jean Paul Kestemont, Sarah Le Meur
Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation, pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
Type:
Grant
Filed:
April 26, 2018
Date of Patent:
July 6, 2021
Assignee:
AstraZeneca AB
Inventors:
Tudor Grecu, Jason Grant Kettle, Martin John Packer, Stuart Eric Pearson, James Michael Smith
Abstract: Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.
Type:
Grant
Filed:
December 14, 2017
Date of Patent:
June 29, 2021
Assignees:
ONO PHARMACEUTICAL CO., LTD., VANDERBILT UNIVERSITY
Inventors:
Craig W Lindsley, Joshua M. Wieting, Kevin M. McGowan, Jerod S. Denton, Kentaro Yashiro, Haruto Kurata, Yoko Sekioka, Takahiro Mori, Yuzo Iwaki
Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
June 29, 2021
Assignees:
Daiichi Sankyo Company, Limited, Sanford Burnham Prebys Medical Discovery Institute
Abstract: Disclosed herein, inter alia, are piperazinyl norbenzom orphan compounds and uses thereof, including, for example, methods for treating a CNS disease, treating traumatic brain injury, improving cognition, or diagnosing and treating cancer.
Type:
Grant
Filed:
October 19, 2016
Date of Patent:
June 29, 2021
Assignee:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Stephen F. Martin, James J. Sahn, Timothy R. Hodges
Abstract: The present invention provides methods for obtaining purified rapamycin derivatives, including purified Biolimus A9. A crystalline form of Biolimus A9 is also described.
Type:
Grant
Filed:
March 2, 2020
Date of Patent:
June 29, 2021
Assignee:
Biosensors International Group, Ltd.
Inventors:
Margaret W. Kayo, Richard S. Fornicola, Ivan Kovacik, Leelakrishna Kondaveti, Aniruddh Singh
Abstract: The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
Type:
Grant
Filed:
March 13, 2018
Date of Patent:
June 22, 2021
Assignee:
Assembly Biosciences, Inc.
Inventors:
Leping Li, Lee D. Arnold, Sreenivasa Reddy Mundla