Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
June 3, 2020
Date of Patent:
February 1, 2022
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Yao-Ling Qiu, Xuri Gao, Xiaowen Peng, Wei Li, Jorden Kass, Hui Cao, Byung-Chul Suh, Jiajun Zhang, Yat Sun Or
Abstract: The present disclosure relates to thiazole- or diathiazole-substituted aryl and heteroaryl compounds (I), pharmaceutical compositions containing them, and methods of using them, including treatment of disorders or disease related to regulation of the Vps34/PI3K III signaling pathway.
Type:
Grant
Filed:
April 9, 2019
Date of Patent:
February 1, 2022
Assignee:
Neuropore Therapies, Inc.
Inventors:
Emily M. Stocking, Wolfgang J. Wrasidlo
Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.
Type:
Grant
Filed:
August 8, 2018
Date of Patent:
February 1, 2022
Assignee:
Denali Therapeutics Inc.
Inventors:
Robert A. Craig, II, Javier de Vicente Fidalgo, Anthony A. Estrada, Jianwen A. Feng, Brian M. Fox, Christopher R. H. Hale, Katrina W. Lexa, Maksim Osipov, Travis Remarchuk, Zachary K. Sweeney
Abstract: A chemical compound is provided according to general formula (1):
Type:
Grant
Filed:
December 21, 2017
Date of Patent:
January 18, 2022
Assignee:
TECHNISCHE UNIVERSITÄT BERLIN
Inventors:
Roderich Suessmuth, Dennis Kerwat, Stefan Graetz, Iraj Behroz, Leonard Von Eckardstein, Patrick Michael Durkin, Marius Morkunas, John Weston
Abstract: The present invention relates to novel methods for the preparation of 1,3-benzodioxole heterocyclic compounds of formula (I). The compounds are useful as PDE4 inhibitors.
Type:
Grant
Filed:
June 19, 2018
Date of Patent:
January 11, 2022
Assignee:
UNION therapeutics A/S
Inventors:
Allan Carsten Dahl, Johan Eriksson Bajtner, Esben Paul Krogh Olsen, Bjørn Metzler
Abstract: Crystalline solid forms of methyl {(2S)-1-[(2S,5S)-2-(9-{2-[(2S,4S)-1-{(2R)-2-[(methoxycarbonyl)amino]-2-phenylacetyl}-4-(methoxymethyl)pyrrolidin-2-yl]-1H-imidazol-5-yl}-1,11-dihydroisochromeno[4?,3?:6,7]naphtho[1,2-d]imidazol-2-yl)-5-methylpyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl}carbamate (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using these crystalline forms.
Type:
Grant
Filed:
February 21, 2020
Date of Patent:
December 21, 2021
Assignee:
Gilead Pharmasset LLC
Inventors:
Olga Viktorovna Lapina, Bing Shi, Fang Wang, Scott Alan Wolckenhauer
Abstract: The invention provides compounds and compositions comprising compounds that modulate histone acyl transferase (HAT). The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a compound that modulates HAT to a subject.
Type:
Grant
Filed:
December 2, 2019
Date of Patent:
December 7, 2021
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
Ottavio Arancio, Shixian Deng, Donald W. Landry, Jole Fiorito, Rosa Purgatorio, Owen Anthony O'Connor, Jennifer Effie Amengual
Abstract: The present disclosure provides processes for the preparation of a compound of formula: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates.
Type:
Grant
Filed:
January 16, 2020
Date of Patent:
December 7, 2021
Assignee:
Gilead Pharmasset LLC
Inventors:
Kevin M. Allan, Shinji Fujimori, Lars V. Heumann, Grace May, Katie Ann Brown, Christopher M. Levins, Ganapati Reddy Pamulapati, Benjamin James Roberts, Keshab Sarma, Martin Gerald Teresk, Xiang Wang, Scott Alan Wolckenhauer
Abstract: The present disclosure provides pharmaceutical compositions comprising Gamma-glutamyl cycle inhibitors (GGCI) and certain pharmaceutically acceptable salts thereof, and methods of use.
Abstract: Disclosed herein are compounds of formula I and salts thereof. Also disclosed are compositions comprising compounds of formula I and methods using compounds of formula I.
Type:
Grant
Filed:
March 9, 2018
Date of Patent:
November 23, 2021
Assignee:
RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Inventors:
Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Yi Yuan, Yangsheng Sun
Abstract: Small molecules comprised of spiroindolinone analogues are provided. Some spiroindolinones are provided with a particular relative stereochemistry in which the indolone carbonyl and all three hydrogens are on the same face of the central pyrrolidine ring. A stereoselective method of synthesis is provided for making some of the spiroindolinones described above. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, fungal infections. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.
Type:
Grant
Filed:
June 13, 2016
Date of Patent:
November 16, 2021
Assignee:
The Regents of the University of California
Inventors:
David Lee Van Vranken, Haoping Liu, Ilandari Dewage Udara Anulal Premachandra, Fuqiang Wang, Chengtian Shen, Kevin Andre Scott, Shelley Ren-An Lane, Aaron David Mood, Stanley Chungsing Hiew
Abstract: The present disclosure provides compounds represented by Formula I and II: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, X, W, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I and II for use to treat a condition or disorder responsive to LSD1 inhibition such as cancer.
Type:
Grant
Filed:
May 15, 2018
Date of Patent:
November 9, 2021
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Shaomeng Wang, Dengyou Zhang, Canhui Zheng, Zhuo Chen, Liu Liu, Liyue Huang, Chao-Yie Yang
Abstract: Provided is a CCR2/CCR5 receptor antagonist and the use thereof in the preparation of a drug for treating diseases associated with the CCR2/CCR5. In particular, disclosed are a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.
Abstract: The present invention discloses a class of anti-influenza virus compounds, and the use thereof in the preparation of a drug for treating diseases associated with influenza viruses. In particular, the present invention discloses a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.
Abstract: Thiazolide compounds, such as nitazoxanide and/or tizoxanide, may be used against viruses belonging to the Picornaviridae family or the Paramyxoviridae family.
Type:
Grant
Filed:
March 30, 2017
Date of Patent:
October 5, 2021
Assignee:
Romark Laboratories L.C.
Inventors:
Jean-Francois Rossignol, Maria Gabriella Santoro
Abstract: A drug or agent containing a compound having an agonistic activity to STING as an active ingredient, where the compound is represented by the following general formula (I-1): wherein all symbols represent the same meanings as described in the specification, and the compound can be used as an active ingredient of an agent for suppressing the progression of, suppressing the recurrence of and/or treating cancer or infectious disease.
Abstract: The present disclosure provides novel ATX inhibitors, and pharmaceutical compositions comprising said inhibitors, as well as methods of treatment comprising administration of said inhibitors.
Type:
Grant
Filed:
June 2, 2017
Date of Patent:
September 21, 2021
Assignees:
UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, UNIVERSITY OF MEMPHIS
Inventors:
Duane D. Miller, Gabor G. Tigyi, Souvik Banerjee, Abby L. Parrill-Baker
Abstract: Embodiments are directed to a series of novel EPAC antagonists that are designed, synthesized and evaluated in an effort to develop diversified analogues based on the scaffold of the previously identified high-throughput (HTS) hit ESI-09.
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
September 21, 2021
Assignee:
Board of Regents, the University of Texas System
Inventors:
Jia Zhou, Zhiqing Liu, Na Ye, Fang Mei, Xiaodong Cheng
Abstract: Small molecule compounds having aggregation-induced emission (AIE) characteristics. The compounds include organic, aromatic salts having anion-?+ interactions. In some embodiments, the anion-?+ interactions can include heavy-atom-anion-?+ interactions. The heavy atom anions can include bromine or iodide, for example. The compounds can be water-soluble. The compounds can be useful as probes for bioimaging, as room temperature luminogens for electroluminescent devices, and white organic light-emitting applications.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
September 14, 2021
Assignee:
THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY