Abstract: The invention provides 3-deuterium-enriched 3-(6-, 7-, or 8-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
Abstract: The present invention relates to a composition for use in the treatment of onychomycosis and/or tinea pedis, the composition comprising a polymer capable of forming nanoparticles and terbinafine, or derivative or salt thereof, wherein the nanoparticles are formed with and/or in the presence of terbinafine, or derivative or salt thereof and wherein the composition is administered topically to provide a daily dose to an infected area in the range of about 5 ?g to about 50 ?g of terbinafine. The invention also relates to a combination of the composition and a liquid dispensing device for dispensing a pre-defined quantity of the composition to a user's toes and/or inter-digital spaces and/or front of the foot.
Type:
Grant
Filed:
June 28, 2018
Date of Patent:
November 1, 2022
Assignee:
Blueberry Therapeutics Limited
Inventors:
John Ridden, Christine Caroline Ridden, David Cook, Julie Cook
Abstract: Provided is a compound for inhibiting and degrading anaplastic lymphoma kinase ALK. Specifically provided is a compound as represented by the following formula I, wherein the definition of each group is as stated in the description. The compound has excellent anaplastic lymphoma kinase (ALK) inhibitory activity, and can be used for preparing drugs for treatment of ALK activity-related diseases.
Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Type:
Grant
Filed:
July 31, 2020
Date of Patent:
November 1, 2022
Assignees:
Valo Health, Inc., Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Peter Dragovich, Xiongcai Liu, Snahel Patel, Po-Wai Yuen, Mark Zak, Guiling Zhao, Yamin Zhang, Xiaozhang Zheng
Abstract: Novel quinazolinones useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.
Type:
Grant
Filed:
December 18, 2017
Date of Patent:
October 18, 2022
Assignee:
Oligomerix, Inc.
Inventors:
Eliot J. Davidowitz, James G. Moe, Allen B. Reitz, Haiyan Bian, Charles Gluchowski, James Hendrix, Albert S. Yehaskel, Mark E. McDonnell, H. Marie Loughran
Abstract: The present application provides pyrazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.
Type:
Grant
Filed:
March 4, 2020
Date of Patent:
October 18, 2022
Assignee:
Incyte Corporation
Inventors:
Joshua Hummel, Jingwei Li, Zhenwu Li, Ding-Quan Qian, Liangxing Wu, Kaijiong Xiao, Meizhong Xu, Jeffrey C. Yang, Wenqing Yao, Fenglei Zhang, Min Ye, Yingnan Chen, Margaret Favata, Yvonne Lo
Abstract: The present invention relates to a CPT-bound compound or a pharmaceutically acceptable salt thereof, the CPT-bound compound being obtained by binding CPT (or a CPT derivative) and guanidine to a reduced monosaccharide. The CPT-bound compound enhances solubility and cell permeability of the CPT drug, which makes it possible to effectively deliver CPT to target cells. Therefore, a pharmaceutical composition comprising, as an active ingredient, the CPT-bound compound or a pharmaceutically acceptable salt thereof is expected to be able to effectively treat cancer, in particular, colorectal cancer, even with a low dose of CPT.
Type:
Grant
Filed:
November 7, 2019
Date of Patent:
October 11, 2022
Assignee:
SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
Abstract: The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.
Type:
Grant
Filed:
September 29, 2018
Date of Patent:
October 11, 2022
Assignees:
SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Lei Li, Meiyu Geng, Ying Huang, Jian Ding, Qiong Zhang, Min Huang, Shuai Tang, Ning Shen, Yi Chen
Abstract: The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of filovirus infection in humans and other mammals. A new class of small molecules is disclosed that inhibits the interaction of naturally processed (i.e., proteolytically cleaved) filovirus glycoprotein (GPCL) with its host receptor Niemann-Pick C1 (NPC1) protein and thus block infection of host cells by filoviruses. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of filovirus infection.
Type:
Grant
Filed:
December 5, 2017
Date of Patent:
October 4, 2022
Assignees:
Microbiotix, Inc., Albert Einstein College of Medicine, The Government of the United States as Represented by the Secretary of the Army
Inventors:
Terry L. Bowlin, Donald T. Moir, Kartik Chandran, John M. Dye, Jr., John D. Williams, Zachary D. Aron, Jay P. Barbor, Kelly N. Lively, Peter J. Nash, Debra M. Mills, Arnab Basu
Abstract: A method for producing an aromatic dianhydride includes reacting an aromatic diimide with a substituted or unsubstituted phthalic anhydride in an aqueous medium in the presence of an amine exchange catalyst to provide an aqueous reaction mixture including an N-substituted phthalimide, an aromatic tetraacid salt, and at least one of an aromatic triacid salt and an aromatic imide diacid salt. The method further includes removing the phthalimide from the aqueous reaction mixture by extracting the aqueous reaction mixture with an organic solvent using a sieve tray extraction column. The aromatic tetraacid salt is converted to the corresponding aromatic dianhydride. Aromatic dianhydrides prepared according to the method are also described.
Type:
Grant
Filed:
May 6, 2019
Date of Patent:
October 4, 2022
Assignee:
SHPP GLOBAL TECHNOLOGIES B.V.
Inventors:
Gregory L. Hemmer, Sivakumar Periyasamy, Simon Padmanabhan, Robert Werling, Ravi Gautam
Abstract: The present technology relates to methods of treating one or more behavioral symptoms (for example, anxiety) of 22q11.2 deletion syndrome in a subject by administering, e.g., transdermally, an effective amount of cannabidiol (CBD) to the subject wherein one or more behavioral symptoms of 22q11.2 deletion syndrome are treated in the subject.
Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
Abstract: The present invention provides novel compounds having the general formula: wherein R1, R2, X, Y and A are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
September 20, 2022
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Xingchun Han, Min Jiang, Yongguang Wang, Song Yang
Abstract: The present invention relates to a series of substituted purine derivatives capable of inhibiting CDC7 kinase activity and, as such, suitable for use in the treatment of neurological diseases such as, inter alia, Alzheimer's disease, amyotrophic lateral sclerosis or frontotemporal dementia, involving hyperphosphorylation of TDP-43 and the subsequent formation of aggregates, induced by CDC7.
Type:
Grant
Filed:
March 21, 2018
Date of Patent:
September 20, 2022
Assignee:
CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS (CSIC)
Inventors:
Ana Martinez Gil, Daniel I. Perez, Carmen Gil Ayuso-Gontán, Angeles Martin-Requero, Elisa Rojas Prats, Loreto Martinez-Gonzalez, Concepción Perez
Abstract: Described herein are crystalline forms of compounds that are deoxycytidine kinase (dCK) inhibitors, methods of making such crystalline forms, pharmaceutical compositions and medicaments comprising such crystalline forms, and methods of using such crystalline forms in the treatment of conditions, diseases, or disorders that would benefit from modulation of deoxycytidine kinase (dCK) activity.
Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
July 2, 2020
Date of Patent:
September 13, 2022
Assignee:
ADVERIO PHARMA GMBH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
Abstract: Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments.
Type:
Grant
Filed:
February 13, 2020
Date of Patent:
August 30, 2022
Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
Inventors:
Weiping Tang, Gabrielle N. Winston-McPherson, Haibo Xie, Alan D. Attie, Mark Patrick Keller, Ka Yang
Abstract: Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
Type:
Grant
Filed:
August 30, 2021
Date of Patent:
August 30, 2022
Assignee:
Janssen Pharmaceutica NV
Inventors:
J. Kent Barbay, Wenying Chai, Gavin C. Hirst, Kevin D. Kreutter, David A. Kummer, Kelly J. McClure, Rachel T. Nishimura, Amy Y. Shih, Jennifer D. Venable, Hariharan Venkatesan, Jianmei Wei
Abstract: Provided is a novel technique for improving storage stability of a pharmaceutical composition containing pemafibrate, a salt thereof or a solvate thereof and a cellulose species. A pharmaceutical preparation obtained by storing a pharmaceutical composition containing the following components (A) and (B) in a tight package: (A) pemafibrate, a salt thereof or a solvate thereof; and (B) a cellulose species.