Abstract: Metal-assisted delayed fluorescent (MADF) emitters including cyclic tetradentate platinum (II) and palladium (II) complexes employing 8H-pyrido[3?,2?:4,5]-pyrrolo[3,2,1-de]acridine and its analogues. These complexes provide improved color purity and enhanced operational stability and are suitable for luminescent labels, emitters for organic light emitting diodes (OLEDs), and lighting applications.
Type:
Grant
Filed:
January 26, 2018
Date of Patent:
July 25, 2023
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: The present invention relates to the field of display technologies, and particularly to a fused polycyclic compound, a preparation method and use thereof. The fused polycyclic compound provided in the present invention has a structure of General Formula IV. The structure of the compound has ambipolarity, and the HOMO level and the LUMO level of the host material are respectively located on different electron donating group and electron withdrawing group, such that the transport of charges and holes in the host material becomes more balanced, thereby expanding the area where holes and electrons are recombined in the light emitting layer, reducing the exciton concentration, preventing the triplet-triplet annihilation of the device, and improving the efficiency of the device.
Abstract: The present disclosure is directed to novel compounds of Formula I and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g. controlling, alleviating, or slowing the progression of) of cancer, including glioblastoma, bone cancer, head and neck cancer, melanoma, basal cell carcinoma, squamous cell carcinoma, adenocarcinoma, oral cancer, esophageal cancer, gastric cancer, intestinal cancer, colon cancer, bladder cancer, hepatocellular carcinoma, renal cell carcinoma, pancreatic cancer, ovarian cancer, cervical cancer, lung cancer, breast cancer, and prostate cancer. The compounds of the disclosure are selective antagonists of the EP4 receptor and useful treatment of various diseases that may be ameliorated with blockade of PGE2-mediated signaling.
Type:
Grant
Filed:
June 22, 2021
Date of Patent:
May 2, 2023
Assignee:
TEMPEST THERAPEUTICS, INC.
Inventors:
Yalda Bravo, Jason David Burch, Austin Chih-Yu Chen, Joe Fred Nagamizo
Abstract: The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exhibits an opioid ? receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid ? receptor-related diseases (for example, headache) can be treated or prevented.
Abstract: Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.
Type:
Grant
Filed:
October 29, 2021
Date of Patent:
April 18, 2023
Assignee:
Tesaro, Inc.
Inventors:
Alistair Stewart, Anthony Joseph Toto, Frank Xing Chen, George Wu
Abstract: In some aspects, the present disclosure provides compounds of the formula: wherein the variables are as defined herein. In some embodiments, these compounds may be used to reduce the pain of a patient. These compounds may be used in pain relief and show an improved pharmaceutical profile relative to other commonly used opiates and opioid derivatives.
Type:
Grant
Filed:
July 8, 2020
Date of Patent:
March 28, 2023
Assignees:
University of Health Sciences & Pharmacy in St. Louis, University of Southern California, The University of North Carolina at Chapel Hill, Memorial Sloan Kettering Cancer Center, University of Florida Research Foundation, Incorporated
Inventors:
Susruta Majumdar, Vsevolod Katritch, Bryan Roth, Jay McLaughlin, Saheem Zaidi, Gavril W. Pasternak, Rajendra Uprety
Abstract: Disclosed herein are novel carborane hydroxamic acid matrix metalloproteinase (“MMP”) inhibitors and agents bearing borane-containing moieties and methods for their use in treating or preventing a disease, such as cancer and rheumatoid arthritis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: Formula (I) wherein the substituents are as described.
Type:
Grant
Filed:
June 28, 2019
Date of Patent:
February 28, 2023
Assignee:
LOYOLA UNIVERSITY OF CHICAGO
Inventors:
Daniel Paul Becker, Marlon Ray Lutz, Jr.
Abstract: Disclosed herein are compounds that can act as inhibitors of nicotinamide phosphoribosyltransferase (“NAMPT”), and methods for their use in treating or preventing diseases, such as pulmonary arterial hypertension (“PAH”). The compounds described herein can include compounds of Formula (II) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
Type:
Grant
Filed:
February 5, 2019
Date of Patent:
February 21, 2023
Assignees:
THE TRUSTEES OF INDIANA UNIVERSITY, THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Inventors:
Tom G. Driver, Roberto F. Machado, Najing Su, Xinyu Guan, Wrickban Mazumdar, Kira Ratia, Jason Ralph Hickok, Angelia Denise Lockett
Abstract: The disclosure provides compounds of formula (I): said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Type:
Grant
Filed:
November 2, 2021
Date of Patent:
February 21, 2023
Assignee:
AUTIFONY THERAPEUTICS LIMITED
Inventors:
Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large, Agostino Marasco
Abstract: The present invention provides a maleate, phosphate, sulfate, hydrochloride of a cyclohexane derivative, N?-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea, as shown in Formula I and crystal forms thereof. The crystal forms have low hygroscopicity and good stability and are convenient for long-term storage and transportation; or the crystal forms have a long half-life in vivo, high bioavailability and small individual difference, and thus have obvious clinical application advantages.
Abstract: The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.
Type:
Grant
Filed:
December 1, 2020
Date of Patent:
February 14, 2023
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, David Scott Carter, Jason S. Halladay, Robert T. Jacobs, Yang Liu, Jacob J. Plattner, Yong-Kang Zhang, Michael John Witty
Abstract: The present invention relates to compounds of formula (I). The compounds maybe used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.
Abstract: The invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Type:
Grant
Filed:
February 15, 2022
Date of Patent:
February 7, 2023
Assignee:
Albireo AB
Inventors:
Per-Göran Gillberg, Ingemar Starke, Santosh S. Kulkarni
Abstract: The present invention is directed to compounds having the Formulae (Ia), (Ib), (Ic), or (Id); or the Formulae (II), (IIa), (IIb), or (IIc); or the Formulae (III), (IIIa), (IIIb), (IIIc), (IIId), or (IIIe), and pharmaceutically acceptable salts, solvates, clathrates and prodrugs of any Formula thereof, compositions thereof, and methods for the treatment of a condition associated with a dysfunction in proteostasis.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
January 24, 2023
Assignee:
Proteostasis Therapeutics, Inc.
Inventors:
Matthew Cullen, Cecilia M. Bastos, Daniel Parks, Benito Munoz
Abstract: Provided is a method of manufacturing a trifluoropyruvyl fluoride dimer, including a reaction step of reacting hexafluoropropylene oxide and aldehyde.
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which q, R11, R12, R13 and R14 are as defined in the specification, for use in therapy.
Type:
Grant
Filed:
December 9, 2019
Date of Patent:
November 29, 2022
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Colm Carroll, Anne Goldby, Martin Teall
Abstract: A novel process for preparation of Deutetrabenazine ((RR, SS)-1,3,4,6,7-11b-Hexahydro-9,10-di(methoxy-d6)-3-(2-methylpropyl)-2H-benzo [a] quinolizin-2-one) of formula I comprises of methylation of N-(2-(3,4-dihydroxy-phenyl)-ethyl)-formamide compound of formula III with deuteriated methanol (CD3OD or CD3OH) to obtain d6-N-(2-(3,4-dimethoxy-phenyl)-ethyl)-formamide compound of formula IV; cyclization of d6-N-(2-(3,4-dimethoxy-phenyl)-ethyl)-formamide in presences of dehydrating agent to obtain d6-6,7-Dimethoxy-3,4-dihydroisoquinoline compound of formula V; reacting d6-6,7-Dimethoxy-3,4-dihydroisoquinoline compound of formula V with 2-acetyl-N,N,N,4-tetramethyl-1-pentanaminium iodide compound of formula VI.