Abstract: Disclosed herein, inter alia, are piperazinyl norbenzom orphan compounds and uses thereof, including, for example, methods for treating a CNS disease, treating traumatic brain injury, improving cognition, or diagnosing and treating cancer.
Type:
Grant
Filed:
October 19, 2016
Date of Patent:
June 29, 2021
Assignee:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Stephen F. Martin, James J. Sahn, Timothy R. Hodges
Abstract: The present invention provides methods for obtaining purified rapamycin derivatives, including purified Biolimus A9. A crystalline form of Biolimus A9 is also described.
Type:
Grant
Filed:
March 2, 2020
Date of Patent:
June 29, 2021
Assignee:
Biosensors International Group, Ltd.
Inventors:
Margaret W. Kayo, Richard S. Fornicola, Ivan Kovacik, Leelakrishna Kondaveti, Aniruddh Singh
Abstract: The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
Type:
Grant
Filed:
March 13, 2018
Date of Patent:
June 22, 2021
Assignee:
Assembly Biosciences, Inc.
Inventors:
Leping Li, Lee D. Arnold, Sreenivasa Reddy Mundla
Abstract: Provided is a compound selected from compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: (I) wherein R1, R2, R3 and R4 are as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, neurological and psychiatric diseases and disorders. Also disclosed are compositions containing such compounds in combination with a pharmaceutically acceptable carrier, as well as methods relating to their use in subjects in need thereof.
Type:
Grant
Filed:
April 17, 2018
Date of Patent:
June 22, 2021
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Nicole Harriott, Donald Hettinger, Shawn Branum, Jeffrey C. Culhane
Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
Type:
Grant
Filed:
December 14, 2018
Date of Patent:
June 15, 2021
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
Abstract: The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
Type:
Grant
Filed:
May 6, 2020
Date of Patent:
June 8, 2021
Assignees:
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN, FORSCHUNGSVERBUND BERLIN E.V.
Inventors:
Michael Bader, Edgar Specker, Susann Matthes, Anja Schütz, Keven Mallow, Maik Grohmann, Marc Nazaré
Abstract: A method of preparing a tricyclic compound of formula (I), comprising the step of converting a compound of formula (II) into a compound of formula (III); and hydrogenating the compound of formula (III) in the presence of hydrogenation catalyst and hydrogen to form the tricyclic compound of formula (I); wherein R1 is H or a C1-3 alkyl group; and R2 is H, a halogen element or a C1-3 alkyl group.
Type:
Grant
Filed:
August 1, 2019
Date of Patent:
June 1, 2021
Assignee:
Formosa Laboratories, Inc.
Inventors:
Wen-Chieh Yang, Mei-Jing Lee, Hsueh-Chen Lee, Lung-Hsiang Li
Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
May 25, 2021
Assignees:
Daiichi Sankyo Company, Limited, Sanford Burnham Prebys Medical Discovery Institute
Abstract: Methods for treating a tumor, such as a benign or malignant tumor, are disclosed herein. The methods include administering a therapeutically effective amount of a small molecule that selectively binds to and stabilizes G-quadruplex DNA in the promoter of the c-MYC gene to the subject. The methods are also of use to decrease the size and/or number of metastases. Compounds for use in the disclosed methods are also provided.
Type:
Grant
Filed:
March 30, 2020
Date of Patent:
May 25, 2021
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
John Schneekloth, Jr., John Simmons, Kenneth Felsenstein, Beverly Mock, Lindsey Saunders, David Calabrese, Elena Leon
Abstract: The present invention relates to compounds of the formula I or II: (I) (II) processes for their preparation and their use as pharmaceutical agents or compositions in the treatment, of neurological disorders.
Type:
Grant
Filed:
June 24, 2020
Date of Patent:
May 18, 2021
Assignee:
Prana Biotechnology Limited
Inventors:
Penelope Jane Huggins, Jack Gordon Parsons, Kevin Jeffrey Barnham, Elisabeth Colette Louise Gautier, Antony Vincent Robinson
Abstract: The present disclosure provides, in part, a process for preparing compounds (I) having allosteric effector properties against Hepatitis B virus Cp.
Type:
Grant
Filed:
March 13, 2018
Date of Patent:
May 18, 2021
Assignee:
Assembly Biosciences, Inc.
Inventors:
Leping Li, Lee D. Arnold, Sreenivasa Reddy Mundla
Abstract: The present invention encompasses compounds of formula (I), wherein the groups R1 to R5, X, Y and W have the meanings given in the claims and specification, their use as inhibitors of BCL6, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
Type:
Grant
Filed:
December 7, 2017
Date of Patent:
May 11, 2021
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Steffen Steurer, Georg Dahmann, Nina Kerres, Manfred Koegl
Abstract: Provided herein are compounds of formula (IA) and (III) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
Type:
Grant
Filed:
April 23, 2020
Date of Patent:
April 27, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Hang Chu, Juan A. Guerrero, Anna E. Hurtley, Tae H. Hwang, Lan Jiang, Darryl Kato, Tetsuya Kobayashi, John E. Knox, Scott E. Lazerwith, Xiaofen Li, David W. Lin, Jonathan W. Medley, Michael L. Mitchell, Devan Naduthambi, Zachary Newby, Neil H. Squires, Vickie H. Tsui, Chandrasekar Venkataramani, William J. Watkins, Hong Yang
Abstract: This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.
Abstract: The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
Type:
Grant
Filed:
March 26, 2020
Date of Patent:
April 20, 2021
Assignee:
REVOLUTION MEDICINES, INC.
Inventors:
Jennifer Pitzen, Micah James Evans Gliedt, G. Leslie Burnett, James Bradley Aggen, Gert Kiss, Christopher Michael Semko, Walter Won, Gang Wang, Julie Chu-Li Lee, Arun P. Thottumkara, Adrian Liam Gill, Kevin T. Mellem
Abstract: Provided herein are compounds of formula (I) and (V) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.