Abstract: Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.
Type:
Grant
Filed:
July 1, 2020
Date of Patent:
February 21, 2023
Assignee:
NUVATION BIO INC.
Inventors:
Son Minh Pham, Sarvajit Chakravarty, Jayakanth Kankanala, Jiyun Chen, Chris P. Miller, Jeremy D. Pettigrew, Anjan Kumar Nayak, Anup Barde
Abstract: Disclosed herein are compounds, compositions, and methods for modulating the Cannabinoid receptor 2 (CB2) with the compounds and compositions disclosed herein. Also described are methods of treating diseases or conditions that are mediated by the action of Cannabinoid receptor 2 (CB2) or that we benefit from modulating the Cannabinoid receptor 2 (CB2).
Abstract: The present invention relates to naphthalene diimides, NDIs, and methods of synthesising them. The NDIs have DNA-quadruplex binding and stabilising activity, and potential in treatment of pancreatic, prostate, and other human cancers. The NDIs are a compound of Formula I.
Type:
Grant
Filed:
May 15, 2020
Date of Patent:
January 24, 2023
Assignee:
UCL Business Ltd
Inventors:
Stephen Neidle, Richard Angell, Sally Oxenford
Abstract: Provided are compositions and methods for treating osteoarthritis including intra-articular administration of a compound of Formula (I) including amorphous and polymorph forms thereof.
Type:
Grant
Filed:
December 1, 2020
Date of Patent:
January 24, 2023
Assignee:
BioSplice Therapeutics, Inc.
Inventors:
John Hood, David Mark Wallace, Sunil Kumar KC, Yusuf Yazici, Christopher Swearingen, Luis A Dellamary
Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
Type:
Grant
Filed:
September 11, 2020
Date of Patent:
January 10, 2023
Assignees:
Valo Health, Inc., Genentech, Inc.
Inventors:
Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
Type:
Grant
Filed:
May 20, 2022
Date of Patent:
January 10, 2023
Assignee:
Sitari Pharma, Inc.
Inventors:
David Campbell, Justin Chapman, Thomas R. Diraimondo, Sergio G. Duron
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
Type:
Grant
Filed:
July 12, 2021
Date of Patent:
January 10, 2023
Assignee:
Nimbus Saturn, Inc.
Inventors:
Neelu Kaila, Ian Linney, Stuart Ward, Grant Wishart, Ben Whittaker, Alexandre Cote, Jeremy Robert Greenwood, Abba Leffler, Steven K. Albanese, Daniel L. Severance
Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
July 7, 2020
Date of Patent:
January 10, 2023
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Daniel D. Long, John R. Jacobsen, Lan Jiang
Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
Type:
Grant
Filed:
September 9, 2020
Date of Patent:
December 27, 2022
Assignee:
Vitae Pharmaceuticals, LLC
Inventors:
David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Zhijie Liu, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
Abstract: Anti-tubercular compounds include trisubstituted indolizines having the following structural formula: wherein R1 is selected from the group consisting of 4-OCH3, 4-Cl, 4-Br, 4-F, 2-NO2, 3,5-CF3, CN, CH3, R2 is COOCH3, COOC2H5, and R3 is H and COOCH3.
Type:
Grant
Filed:
June 29, 2022
Date of Patent:
December 20, 2022
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Mohamed A. Morsy, Sandeep Chandrashekharappa, Melendran Pillay, Pran Kishore Deb
Abstract: Provided herein are compounds that interrupt the function of SALL4. Also described are pharmaceutical compositions and medical uses of these compounds.
Type:
Grant
Filed:
October 4, 2018
Date of Patent:
December 20, 2022
Assignees:
DANA-FARBER CANCER INSTITUTE, INC., THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
Abstract: Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
Type:
Grant
Filed:
December 30, 2020
Date of Patent:
December 20, 2022
Assignee:
H. Lee Moffitt Cancer Center and Research Institute, Inc.
Inventors:
Srikumar Chellappan, Nicholas J. Lawrence, Sujeewa Ranatunga Mahanthe Mudiyanselage
Abstract: The invention concerns a scalable, large-scale castanospermine preparation method that yields levels of purity greater than 98% from castanospermine-containing plant sources, such as Castanospermum australe seed material.
Type:
Grant
Filed:
June 4, 2021
Date of Patent:
December 6, 2022
Assignee:
Florida State University Research Foundation, Inc.
Abstract: A compound represented by formula (I), an optical isomer thereof and a pharmaceutically acceptable salt thereof, as well as an application of said compound as an FXIa inhibitor.
Abstract: A macrocycle represented by formula (I) and a pharmaceutical composition comprising the macrocycle, or a crystalline form, pharmaceutically acceptable salt, hydrate or solvent compound, stereoisomer, prodrug, or isotopic variant of the macrocycle. The macrocycle and the composition thereof inhibit a protein kinase.
Abstract: Provided is a method for preparing an epoxy compound having an alkoxysilyl group effectively by using a mild catalyst as well as an aromatic alcohol ring-opening agent. The preparation method for an epoxy compound having an alkoxysilyl group includes: performing a ring opening step by reacting an epoxy compound having an epoxide group, which is a starting material, with an aromatic alcohol ring-opening agent in the presence of a phosphine-based catalyst and an optional solvent so as to obtain an intermediate having a partially ring-opened epoxide group; and performing an alkoxysilylation step by reacting the intermediate having a partially ring-opened epoxide with isocyanate alkoxysilane.
Type:
Grant
Filed:
July 1, 2020
Date of Patent:
November 29, 2022
Assignee:
KOREA INSTITUTE OF INDUSTRIAL TECHNOLOGY
Inventors:
Yun Ju Kim, Hyun Aee Chun, Su Jin Park, Sook Yeon Park
Abstract: The invention provides novel azaindolylpyridone and diazaindolylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory diseases, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R2, R3 and X are as defined in the specification.
Type:
Grant
Filed:
August 23, 2018
Date of Patent:
November 15, 2022
Assignee:
Sprint Bioscience AB
Inventors:
Johan Lindström, Rickard Forsblom, Fredrik Rahm, Jenny Viklund