Abstract: Syntheses of compounds of Formula III from compounds of Formula I via compounds of Formula II are described, as well as particular compounds of Formula III, or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and uses thereof. For example, certain of these compounds and compositions of Formula III have uses in the treatment of psychiatric or neurological disorders.
Type:
Grant
Filed:
August 26, 2021
Date of Patent:
May 9, 2023
Assignee:
Small Pharma Ltd
Inventors:
Peter Rands, George Knight, Richard Chubb, Derek Londesbrough, Tiffanie Benway, Zelah Joel
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
Type:
Grant
Filed:
August 16, 2022
Date of Patent:
May 9, 2023
Inventors:
Robert B. Perni, Glenn Short, Srinivas G. Rao, Tanweer A. Khan
Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.
Type:
Grant
Filed:
August 21, 2018
Date of Patent:
May 9, 2023
Assignees:
Drexel University, The Government of the United States of America, as represented by The Secretary of the Army
Inventors:
Giuseppe R. Palmese, Santosh K. Yadav, John J. LaScala
Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.
Type:
Grant
Filed:
August 11, 2022
Date of Patent:
April 18, 2023
Assignee:
Compass Pathfinder Limited
Inventors:
Derek John Londesbrough, Christopher Brown, Julian Scott Northen, Gillian Moore, Hemant Kashinath Patil, David E. Nichols
Abstract: The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.
Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.
Type:
Grant
Filed:
June 13, 2018
Date of Patent:
March 28, 2023
Assignee:
Kadmon Corporation, LLC
Inventors:
Eduardas Skucas, Kevin G. Liu, Ji-In Kim, Masha V. Poyurovsky, Rigen Mo
Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
March 19, 2020
Date of Patent:
March 14, 2023
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Nadia M. Ahmad, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Joanne Louise Camp, Lev Tyler Dewey Fanning, Sara Sabina Hadida Ruah, Dennis Hurley, Yvonne Schmidt, David Shaw, Urvi Patel, Stephen Andrew Thomson, Lidio Marx Carvalho Meireles
Abstract: The present application relates to psilocin derivatives of 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.
Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
Abstract: Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
March 7, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Michael K. Ameriks, Gang Chen, Chaofeng Huang, Brian Ngo Laforteza, Suchitra Ravula, Wei Zhang
Abstract: The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, as well as compositions comprising such compounds. These compounds and compositions have uses in the treatment of psychiatric or neurological disorders. Compounds of formula I comprise at least one deuterium atom at the ?-position and consequently have improved oral bioavailability relative to ?-diprotic analogues.
Type:
Grant
Filed:
May 6, 2022
Date of Patent:
February 14, 2023
Assignee:
Small Pharma Ltd.
Inventors:
Peter Rands, George Knight, Richard Chubb, Derek Londesbrough, Tiffanie Benway, Zelah Joel
Abstract: This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.
Type:
Grant
Filed:
September 1, 2021
Date of Patent:
February 14, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Thomas Fleck, Florian Paul Christian Binder, Georg Dahmann, Joerg P. Hehn, Annekatrin Charlotte Heimann, Uta Friederike Lessel, Jens Willwacher
Abstract: The present disclosure relates to 2-(3-indoyl)indolin-3-one derivatives of the natural product isatisine A, synthesized from dual catalytic synthesis on metallocarbene-azide cascade chemistry, useful for treating a subject having or suspected of having an infectious disease, wherein the infection disease is caused by a virus, wherein the virus is from the family flaviviridae or paramyxoviridae.
Type:
Grant
Filed:
March 27, 2019
Date of Patent:
January 31, 2023
Assignee:
The Governors of the University of Alberta
Inventors:
Frederick Glenn West, David J. Marchant, Bren Jordan P. Atienza, Lionel D. Jensen
Abstract: The present invention provides new prodrugs of therapeutically active compounds, including oligomeric prodrugs, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.
Type:
Grant
Filed:
September 20, 2019
Date of Patent:
January 10, 2023
Assignee:
Graybug Vision, Inc.
Inventors:
Ming Yang, John G. Bauman, Jeffrey L. Cleland, Nu Hoang, Emmett Cunningham
Abstract: There are provided new heterobifunctional agents designed to mediated formation of protein-protein dimers and promote ubiquitination of a protein of the dimer. Also provided are methods of synthesizing the agents, pharmaceutical formulations including the agents, and methods of using the agents to treat, ameliorate or cure diseases characterized by protein over-expression or malfunction.
Type:
Grant
Filed:
September 23, 2021
Date of Patent:
January 3, 2023
Assignee:
Agency for Science, Technology and Research (A*STAR)
Inventors:
Wei Hung, Thomas Hugo Keller, Wei Ling Wang, Gang Wang, Congbao Kang
Abstract: Provided are a compound superior in a cytotoxic action on cancer cells, an action inducing degradation of BET protein in cancer cells, and an inhibitory action on the binding of BET protein and acetylated histone, and useful as an anticancer agent, a BET protein degradation inducer or a BET protein inhibitor. A compound represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
Abstract: The present invention relates to heterobicyclic amides and related compounds which are inhibitors of CD38 and are useful in the treatment of cancer.
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
December 27, 2022
Assignee:
Ribon Therapeutics, Inc.
Inventors:
Laurie B. Schenkel, Melissa Marie Vasbinder, Kevin Wayne Kuntz, Nicholas Robert Perl, Jennifer Downing
Abstract: The present invention relates to a method for preparing Asenapine. In particular, the present invention relates to a method for preparing pharmaceutically acceptable Asenapine free base and new crystal form thereof, and also relates to methods for preparing the intermediate compounds used in said method.
Abstract: Disclosed are inhibitors for the ?-catenin/T-cell factor interaction. The inhibitors are selective for ?-catenin/T-cell factor over ?-catenin/cadherin and ?-catenin/APC interactions. Methods of using the disclosed compounds to treat cancer are also disclosed.
Type:
Grant
Filed:
March 28, 2019
Date of Patent:
December 20, 2022
Assignee:
H. Lee Moffitt Cancer Center and Research Center Institute, Inc.
Abstract: The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
Type:
Grant
Filed:
April 1, 2019
Date of Patent:
December 13, 2022
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Lei Zhu, John Daniel Bailey, Landon Durak, Joshua David Waetzig, Masahiro Mizuno, Kazuhiro Maeda, Tsuneo Yasuma, Hiroshi Yamaguchi, Koichiro Fukuoka, Kazuyuki Akiyama