Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.
Type:
Grant
Filed:
July 6, 2020
Date of Patent:
November 1, 2022
Assignees:
The Regents of the University of California, Friedrich-Alexander-Universität Erlangen-Nürnberg, The Board of Trustees of the Leland Stanford Junior University, The University of North Carolina at Chapel Hill
Inventors:
Brian K. Shoichet, Henry Lin, Peter Gmeiner, Aashish Manglik, Brian Kobilka, Bryan L. Roth, Daniela Gisela Dengler
Abstract: Provided are compositions and methods for promoting osteogenic differentiation of undifferentiated cells, such as stem cells. An example of a compound useful in the present method is 6,8-dimethyl-3-(4-phenyl-1H-imidazol-5-yl)quinolin-2(1H)-one (DIPQUO). The present methods can be used for treatment and prevention of bone disorders.
Inventors:
Dominique Amans, Stephen John Atkinson, Lee Andrew Harrison, David Jonathan Hirst, Robert Peter Law, Matthew Lindon, Alexander Preston, Jonathan Thomas Seal, Christopher Roland Wellaway
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
Type:
Grant
Filed:
June 26, 2020
Date of Patent:
October 11, 2022
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Zhiyong Yu, Fenglei Zhang, Wenqing Yao
Abstract: The disclosure provides processes for preparing a compound of Formula (I).
Type:
Grant
Filed:
December 7, 2018
Date of Patent:
October 11, 2022
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Paul T. Angell, Cristian Harrison, Robert M. Hughes, Berenice Lewandowski, Benjamin J. Littler, Vito Melillo, William A. Nugent, David Andrew Siesel, David Smith, John Studley
Abstract: Disclosed are a biaryl derivative having a structure represented by Formula (I) and inhibitory activity against PD-1/PD-L1 interaction, a preparation method thereof, and a pharmaceutical application thereof. The series of compounds of the can be widely applied to the preparation of a medicament for preventing and/or treating cancer or tumors, immune-related diseases and disorders, contagious diseases, infectious diseases or metabolic diseases that are mediated by a PD-1/PD-L1 signaling pathway, and shows promise for the development of a new generation of PD-1/PD-L1 inhibitors.
Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compostions thereof, which are useful for treating a variety of conditions associated with methyl modifying enzymes.
Type:
Grant
Filed:
November 8, 2018
Date of Patent:
October 4, 2022
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Jehrod B. Brenneman, Alexandre Côté, Victor S. Gehling, Avinash Khanna, Julian R. Levell, Ludivine Moine
Abstract: Novel thiazole- and isoquinoline-containing compounds are presented that are useful for treating and/or preventing broad-spectrum viral infections. Methods of treating and/or preventing broad-spectrum viral infections are also presented. These compounds have shown inhibition of HCMV, influenza viruses, Zika virus, BK Virus and RSV replication in cell-based assays.
Type:
Grant
Filed:
October 17, 2018
Date of Patent:
October 4, 2022
Assignee:
Evrys Bio, LLC
Inventors:
Stacy Remiszewski, Lillian W. Chiang, Eain Anthony Murphy, Qun Sun, Frank Kayser, Sarah Jocelyn Fink
Abstract: Described herein are compounds represented by formula (I?) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of preparing and using the same. The variables Ar, Ra, Rb, m, n, Y1, Y2, R3 and R4 are defined herein.
Type:
Grant
Filed:
March 13, 2019
Date of Patent:
October 4, 2022
Assignee:
BIOGEN MA INC.
Inventors:
Nathan Genung, Kevin M. Guckian, Jeffrey Vessels, Lei Zhang, Ryan Gianatassio, Edward Yin Shiang Lin, Zhili Xin
Abstract: The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as prostaglandin EP4 receptor antagonists, and are useful in the treatment or alleviation of pain and inflammation and other inflammation-associated disorders, such as arthritis, treating or preventing disorders or medical conditions selected from pain, inflammatory diseases and the like. Also described herein are methods of treating pain by administering the compounds of the disclosure, which are EP4 receptor antagonists.
Type:
Grant
Filed:
January 29, 2020
Date of Patent:
October 4, 2022
Assignee:
Avista Pharma Solutions, Inc.
Inventors:
Jason D. Speake, Brent Christopher Beck, Bharathi Pandi, Jennifer C. Freeman
Abstract: Provided are a heterocyclic compound, a preparation method and the use thereof in medicine, and particularly involved are a heterocyclic compound for preventing and/or treating hypemricemia and gout, a preparation method and the use thereof in medicine. In particular, provided are a compound as shown in formula (I) and/or formula (II) or a tautomer thereof and a pharmaceutically acceptable salt thereof, a preparation method therefor and a method and the use thereof for treating hypemricemia and gout.
Type:
Grant
Filed:
January 18, 2019
Date of Patent:
September 27, 2022
Assignee:
EVOPOINT BIOSCIENCES CO., LTD.
Inventors:
Yuchuan Wu, Xi Chen, Shaoqiang Huang, Yonghan Hu, Linhai Qu, Jinlian Zhu, Xiao Liu
Abstract: Novel compounds having a D3 receptor antagonistic activity are provided. The compound represented by Formula (I): wherein Ring A is a non-aromatic heterocycle or the like substituted with substituted or unsubstituted aromatic heterocyclyl or the like; R2a to R2d are each independently a hydrogen atom or the like; n is an integer of 0 to 3; Ring B is a non-aromatic carbocycle or the like; R3 is each independently halogen or the like; r is an integer of 0 to 4; -L- is —N(R10)—C(?O), or the like; R10 is a hydrogen atom or the like; R4 is substituted or unsubstituted aromatic heterocyclyl or the like, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 25, 2019
Date of Patent:
September 20, 2022
Assignee:
SHIONOGI & CO., LTD.
Inventors:
Yusuke Ichihashi, Masanao Inagaki, Koji Masuda
Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer or a deuterated analog thereof, wherein A1, A2, A3, A4, R4, X1, X2, and X3 are as described in any of the embodiments described in this disclosure; compositions thereof; and uses thereof.
Type:
Grant
Filed:
April 8, 2020
Date of Patent:
September 20, 2022
Assignee:
Opna Immuno-Oncology SA
Inventors:
Wayne Spevak, John Buell, Zuojun Guo, Hiroaki Inagaki, Yongil Jin, Phuongly Pham, Songyuan Shi, Jack Walleshauser, Jeffrey Wu, Guoxian Wu, Chao Zhang, Jiazhong Zhang, Ying Zhang
Abstract: Disclosed are methods and compositions for treating diabetes mellitus and non-alcoholic fatty liver disease by administering a therapeutic agent that inhibits the biological activity of B cell lymphoma 6 protein (BCL6).
Type:
Grant
Filed:
July 30, 2020
Date of Patent:
September 13, 2022
Assignee:
NORTHWESTERN UNIVERSITY
Inventors:
Grant D. Barish, Meredith A. Sommars, Madhavi D. Senagolage
Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.
Abstract: The application is directed to compounds of formula (I):(I), and formula (IA):(IA) and their salts and solvates, wherein R1, R2, R3, R4, R5, n, A1, A2, A3, and Y are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of ?-galactosidase, specially galactosidase beta-1 or GLB 1, including GM 1 gangliosidoses and Morquio syndrome, type B.
Type:
Grant
Filed:
December 27, 2017
Date of Patent:
September 13, 2022
Assignee:
Minoryx Therapeutics S.L.
Inventors:
Ana Maria García Collazo, Marc Martinell Pedemonte, Elena Cubero Jordà, Xavier Barril Alonso, Laura Pilar Rodriguez Pascau
Abstract: The invention relates to a CXCR4 receptor-binding compound for use for increasing or restoring interferon (IFN) level in an individual, wherein the interferon is a type-I interferon (IFN-I).
Type:
Grant
Filed:
June 16, 2017
Date of Patent:
September 6, 2022
Inventors:
Nicolas Pietrancosta, Nikaïa Smith, Jean-Philippe Herbeuval
Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
Type:
Grant
Filed:
January 10, 2020
Date of Patent:
September 6, 2022
Assignee:
ChemoCentryx, Inc.
Inventors:
Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang