Abstract: Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
Type:
Grant
Filed:
August 18, 2016
Date of Patent:
June 16, 2020
Assignees:
SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., JINAN UNIVERSITY, SHANGHAI INTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, comprising (i) a CB1 receptor mediating scaffold conjugated to (ii) a second therapeutic scaffold.
Type:
Grant
Filed:
August 10, 2017
Date of Patent:
June 16, 2020
Assignee:
The United States of America as represented by the Secretary, Department of Health and Human Services
Inventors:
George Kunos, Malliga Iyer, Resat Cinar, Kenner C. Rice
Abstract: Diaryl-azo derivatives are efficient fluorescence quenchers as well as nucleic acid duplex-stabilizing agents and are useful in oligonucleotide conjugates and probes. The oligonucleotide-quencher conjugates may be used in detection methods for nucleic acid targets.
Abstract: The present disclosure provides provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
June 2, 2020
Assignee:
EPIZYME, INC.
Inventors:
Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Jennifer C. Petter, Carl Eric Schwartz
Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, fibrotic disorders, cartilage (chondral) defects, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, and neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
Type:
Grant
Filed:
July 19, 2017
Date of Patent:
June 2, 2020
Assignee:
Samumed, LLC
Inventors:
John Hood, Sunil Kumar KC, David Mark Wallace, Gopi Kumar Mittapalli, Brian Joseph Hofilena, Chi Ching Mak, Venkataiah Bollu, Brian Eastman
Abstract: The present invention relates to novel compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
Abstract: Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
Abstract: This invention is directed to methods of preparing benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy.
Type:
Grant
Filed:
February 28, 2019
Date of Patent:
May 26, 2020
Assignee:
Xenon Pharmaceuticals Inc.
Inventors:
Jean-Christophe Andrez, Kristen Nicole Burford, Sultan Chowdhury, Charles Jay Cohen, Christoph Martin Dehnhardt, Robert Joseph Devita, James Roy Empfield, Thilo Focken, Michael Edward Grimwood, Syed Abid Hasan, James Philip Johnson, Jr., Alla Yurevna Zenova
Abstract: The present invention relates to an improved process for the preparation of amorphous (1S)-1,5-anhydro-1-[3-[[5 -(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol compound of formula-1, represented by the following structural formula.
Abstract: The present invention provides methods for the diagnosis and/or treatment of chronic kidney disease, immune complex-mediated GN, rheumatoid arthritis, and pulmonary fibrosis, and methods for identifying compounds for such therapeutic use.
Type:
Grant
Filed:
April 12, 2017
Date of Patent:
April 28, 2020
Assignee:
University of Valencia
Inventors:
Juan Saus, Fernando Revert, Ramón Merino Pérez, Jesús Merino Pérez, Francisco Revert-Ros
Abstract: Provided is an organic light-emitting element having high luminous efficiency and a long lifetime. The organic light-emitting element includes a pair of electrodes and an organic compound layer placed between the pair of electrodes, in which the organic compound layer includes an iridium complex having a benzo[f]isoquinoline of a specific structure as a ligand and a metal complex compound of a specific structure.
Abstract: The present disclosure provides conjugate structures and hydrazinyl-pyrrolo compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
Type:
Grant
Filed:
June 7, 2019
Date of Patent:
March 31, 2020
Assignee:
Redwood Bioscience, Inc.
Inventors:
David Rabuka, Aaron Edward Albers, Romas Alvydas Kudirka, Albert W. Garofalo
Abstract: A DDS preparation of a platinum complex, which selectively releases a highly active platinum complex in cells that are under reducing conditions, and exhibits high antitumor activity that is required from a medicine, is still not available, and there is a demand for a novel DDS preparation of a platinum complex that may be used in clinical fields. There is provided a polymer conjugate of a hexa-coordinated platinum complex, the polymer conjugate comprising a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; and a hexa-coordinated platinum complex having a halogen atom and a hydroxyl group at the axial positions, the hexa-coordinated platinum complex being bonded, directly or via a spacer, to a side-chain carboxyl group of the block copolymer.
Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
Type:
Grant
Filed:
June 17, 2019
Date of Patent:
March 24, 2020
Assignee:
Celgene Corporation
Inventors:
Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
Abstract: The present disclosure relates to: a) solid state forms of hydrobromide salts of Compound 1; b) pharmaceutical compositions comprising one or more solid state forms of hydrobromide salts of Compound 1, and, optionally, a pharmaceutically acceptable carrier; c) methods of treating tumors or cancers by administering one or more solid state forms of hydrobromide salts of Compound 1 to a subject in need thereof; and d) methods for the preparation of solid state forms of Compound 1.
Type:
Grant
Filed:
August 9, 2019
Date of Patent:
March 17, 2020
Assignee:
Pfizer Inc.
Inventors:
Elaine Greer, Stephen Anderson, Mark Maloney, Shu Yu, Ekaterina Albert, Emily Rigsbee
Abstract: The present application discloses 2-phenyl benzofuran derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
Type:
Grant
Filed:
November 10, 2016
Date of Patent:
March 17, 2020
Assignee:
AMBIENT PHOTONICS, INC.
Inventors:
John C. Warner, Srinivasa R. Cheruku, Jeffery A. Gladding
Abstract: An organic electroluminescence device including: an anode; a cathode; two or more emitting units that are disposed between the anode and the cathode, each unit having an emitting layer; and a charge-generating layer that is disposed between the emitting units, wherein the charge-generating layer includes an N layer nearer to the anode and a P layer nearer to the cathode, and the N layer includes a compound represented by the following formula (I) or (II):
Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of using these chemical entities, e.g., for treatment of cancer are described.
Abstract: This invention relates to compounds that are agonists of the muscarinic M4 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1a or a salt thereof, wherein n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.
Type:
Grant
Filed:
August 3, 2016
Date of Patent:
February 4, 2020
Assignee:
Heptares Therapeutics Limited
Inventors:
Giles Albert Brown, Miles Stuart Congreve, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan
Abstract: The present invention relates to pyrazolopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-1H-pyrazolo[3,4-c]pyridazine derivatives of formula (I), and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined in the description. The pyrazolopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They may useful in the treatment of a number of conditions, including pain and epilepsy.
Type:
Grant
Filed:
November 22, 2016
Date of Patent:
January 21, 2020
Assignee:
PFIZER LIMITED
Inventors:
Kevin Neil Dack, Robert McKenzie Owen, David Cameron Pryde