Abstract: This invention relates to a liquid pharmaceutical composition comprising cabozantinib to treat locally advanced or metastatic solid tumors, particularly advanced urothelial cancer or renal cell carcinoma in patients in need thereof.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
November 22, 2022
Assignee:
Exelixis, Inc.
Inventors:
Khalid Shah, Gisela Schwab, Steven Lacy
Abstract: A diastereoselective method of preparing benzofuran-based 4,5-spirocycles via metal catalyzed alkenylation is described. The method can be used to provide compounds containing the benzofuranone-4,5-spirocyclic motif of the phainanoids, a class a natural products having immunosuppressive activity. Synthetic analogs of phainanoids, e.g., compounds that mimic the structure of the “western” part of the structure of the phainanoids and that contain the benzofuranone-4,5-spirocycle are described, as well as their synthetic intermediates, and their methods of synthesis.
Abstract: The present invention relates to: a 4-benzopyranone derivative and a pharmaceutically acceptable salt, solvate, racemate, or stereoisomer thereof; a composition for preventing, alleviating or treating TNF-related diseases, containing the same as an active ingredient; and a method for treating TNF-related diseases, a reagent composition for inhibiting TNF, and a method for inhibiting TNF, all of which use the same. The compositions can be orally administered so as not to cause injection side effects, do not cause immunological tolerance, and can effectively inhibit a TNF activity by being directly bound to TNF while facilitating co-administering with a conventional oral preparation and dosage control.
Abstract: Provided herein are methods for preparing ketone-containing organic molecules. The methods are based on novel iron/copper-mediated (“Fe/Cu-mediated”) coupling reactions. The Fe/Cu-mediated coupling reaction can be used in the preparation of complex molecules, such as halichondrins and analogs thereof. In particular, the Fe/Cu-mediated ketolization reactions described herein are useful in the preparation of intermediates en route to halichondrins.
Type:
Grant
Filed:
May 9, 2018
Date of Patent:
November 15, 2022
Assignee:
President and Fellows of Harvard College
Abstract: A composition for inhibiting skin cell proliferation and/or anti-inflammation is provided. The composition for inhibiting skin cell proliferation and/or anti-inflammation includes: apigenin and luteolin, wherein a weight ratio of the apigenin to the luteolin is about 1.5-25:1, or a mole ratio of the apigenin to the luteolin is about 1.5-25:1. Moreover, the apigenin and the luteolin have a synergistic effect on inhibiting skin cell proliferation and/or anti-inflammation.
Type:
Grant
Filed:
December 31, 2019
Date of Patent:
November 8, 2022
Assignee:
INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTE
Abstract: The present invention provides: a method for producing an epoxyalkane capable of obtaining an epoxide in a high yield while attaining a high olefin conversion rate and a high selectivity for epoxides even when an olefin includes a long carbon chain, and a solid oxidation catalyst. The method for producing an epoxyalkane of the present invention comprises reacting an olefin with an oxidant in the presence of a solid oxidation catalyst, wherein the solid oxidation catalyst comprises a transition metal and a carrier that supports the transition metal, and the carrier is a composite of a metal oxide with a phosphonic acid.
Abstract: The present disclosure provides the compound having inhibitory property against TNIK having a specific chemical structure or its pharmaceutically acceptable salt. The present disclosure also provides a composition comprising the compound or its pharmaceutically acceptable salt. The present disclosure also provides a medical use of the compound, its salt or the composition comprising the compound or its pharmaceutically acceptable salt for treating or preventing cancer. The present disclosure also provides a method of treatment or prevention of cancer comprising administering the compound, its salt or the composition comprising the compound or its salt to a subject in need of such treatment or prevention.
Type:
Grant
Filed:
January 31, 2019
Date of Patent:
November 1, 2022
Assignees:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY, INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Inventors:
Sung Youn Chang, Hyuk Lee, Ki Young Kim, Bum Tae Kim, Sung Soo Kim, Seong Hwan Kim, Hwan Jung Lim, Jung Nyoung Heo, Sang Joon Shin, Sang Youn Park
Abstract: The invention provides a method for producing an epoxy compound by hydrogen peroxide using an organic compound having a carbon-carbon double bond as a raw material, wherein a by-product is suppressed from being generated and the epoxy compound is produced in a high yield. In particular, the invention provides a method for producing an epoxy compound involving oxidizing a carbon-carbon double bond in an organic compound with hydrogen peroxide in the presence of a catalyst, wherein the catalyst comprises a tungsten compound; a phosphoric acid, a phosphonic acid or salts thereof; and an onium salt having an alkyl sulfate ion represented by formula (I) as an anion: wherein R1 is a linear or branched aliphatic hydrocarbon group having 1 to 18 carbons, which may be substituted with 1 to 3 phenyl groups.
Abstract: Large ring silacrown ethers having at least fourteen ring atoms with at least one lipophilic or hydrophobic substituent on the ring and/or on the silicon atom are provided. Pharmaceutical compositions containing these silacrown ethers and the use of these materials as therapeutic agents are also described.
Abstract: This disclosure is related to aromatic compounds of formula (I), and methods of their use in treating medical conditions associated with Heat Shock Protein-90 (HSP90), e.g., cancer. Compounds of formula (I) have the following structure: Also disclosed are pharmaceutical compositions comprising compounds of formula (I).
Type:
Grant
Filed:
March 20, 2018
Date of Patent:
October 25, 2022
Assignee:
TAIPEI MEDICAL UNIVERSITY
Inventors:
Jing-ping Liou, Che-ming Teng, Shiow-lin Pan
Abstract: The present disclosure relates to solid forms of N-{[2?-(2,6-difluoro-3,5-dimethoxyphenyl)-3?-oxo-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-[2,7]naphthyridin]-6?-yl]methyl}acrylamide, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.
Type:
Grant
Filed:
February 6, 2020
Date of Patent:
October 18, 2022
Assignee:
Incyte Corporation
Inventors:
Yongchun Pan, Chongsheng Eric Shi, Ming Tao, Wayne Han, Michael Xia, Dengjin Wang, Zhongjiang Jia, Jiacheng Zhou, Qun Li
Abstract: This disclosure relates to synthetic coupling methods using catalytic molecules. In certain embodiments, the catalytic molecules comprise heterocyclic thiolamide, S-acylthiosalicylamide, disulfide, selenium containing heterocycle, diselenide compound, ditelluride compound or tellurium containing heterocycle.
Type:
Grant
Filed:
October 9, 2020
Date of Patent:
October 18, 2022
Assignee:
Emory University
Inventors:
Lanny Steven Liebeskind, Pavan Kumar Reddy Gangireddy
Abstract: Systems and methods for producing ethylene oxide (EO) are disclosed. Ethylene oxide is produced by direct oxidizing ethylene with oxygen in a reactor. The effluent from the reactor is processed to produce (a) a product stream comprising water and ethylene oxide, (b) a reabsorber overhead stream comprising ethylene, methane, argon, and carbon dioxide, and (c) a carbonate flash gas stream comprising carbon dioxide, ethylene, methane, and water. The reabsorber overhead stream and the carbonate flash gas stream are combined to form a reclaim gas stream. The reclaimed gas stream is separated in a membrane separation unit to remove carbon dioxide and argon, forming a recycle stream comprising primarily ethylene and methane, collectively.
Abstract: The present application relates to 3-cyclic amine-indole derivatives of general Formula (I), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. The diseases, disorders or conditions include, for example, psychosis, mental illnesses, and other neurological diseases, disorders and conditions.
Abstract: The present invention belongs to the field of biomedicine and relates to use of cannabidiol in the preparation of anti-influenza drugs. Specifically, the present invention relates to use of any one of (1) to (3) below in the preparation of drugs for treating or preventing influenza or drugs for relieving an influenza symptom: (1) cannabidiol or a pharmaceutically acceptable salt or ester thereof; (2) a plant extract containing cannabidiol; preferably, a cannabis extract containing cannabidiol; preferably, an industrial cannabis extract containing cannabidiol; and (3) a pharmaceutical composition, containing an effective amount of cannabidiol or a pharmaceutically acceptable salt or ester thereof, and one or more pharmaceutically acceptable auxiliary materials. The cannabidiol can effectively inhibit influenza viruses, and has the potential to prepare or be used as a drug for treating or preventing influenza.
Abstract: Disclosed are methods for treating an ethylene oxide stream suitable for use in carbonylation reactions. Such treatment uses an inorganic solid to remove water from the ethylene oxide stream. Discloses are also systems to carry out the methods herein.
Type:
Grant
Filed:
January 18, 2018
Date of Patent:
September 20, 2022
Assignee:
Novomer, Inc.
Inventors:
Konstantin A. Pokrovski, John B. Ruhl, Alexander Tseitlin, Kyle Sherry
Abstract: In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
Type:
Grant
Filed:
April 18, 2017
Date of Patent:
September 20, 2022
Assignee:
Novartis AG
Inventors:
Gary Glick, Shomir Ghosh, William R. Roush, Dong-Ming Shen
Abstract: Disclosed are a compound represented by Chemical Formula 1A or 1B, an organic thin film including the same, a thin film transistor, and an electronic device. In Chemical Formulae 1A and 1B, X1, X2, R1 to R4, and n1 are the same as described in the detailed description.
Type:
Grant
Filed:
August 21, 2019
Date of Patent:
September 20, 2022
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Eun Kyung Lee, Don-Wook Lee, Jeong Il Park
Abstract: The invention relates to medicine and concerns the treatment of diseases related to the aberrant activity of fractalkine and monocyte chemoattractant proteins 1-4 (CCL2, CCL7, CCL8, CCL13), preferably the treatment of pain, fever, pneumonia, bronchitis, bronchiolitis, alveolitis, rheumatoid arthritis, psoriasis and other diseases, using the compound 1-(2-(1H-imidazol-4-yl)ethyl)piperidine-2,6-dione or a pharmaceutically acceptable salt or solvate thereof The present invention also relates to pharmaceutical compositions that contain a therapeutically effective amount of the claimed compound according to the invention. The present compound and pharmaceutically acceptable salts thereof are highly effective in inhibiting the activity of the glutaminyl cyclase enzyme, which is involved in particular in processes of post-translational modification of the above-mentioned cytokines.
Type:
Grant
Filed:
March 6, 2018
Date of Patent:
September 13, 2022
Assignee:
“CHEMIMMUNE THERAPEUTICS” LIMITED LIABILITY COMPANY
Inventors:
Vladimir Evgenievich Nebolsin, Anastasia Vladimirovna Rydlovskaya
Abstract: The present invention directs to provide a novel compound for treating and/or preventing pain, having excellent skin permeation and reduced skin irritation.