Abstract: The present invention covers 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
Inventors:
Norbert Schmees, Ilona Gutcher, Horst Irlbacher, Benjamin Bader, Na Zhao, Michael Platten, Ulrike Röhn, Ludwig Zorn, Lars Röse, Detlef Stöckigt
Abstract: Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Type:
Grant
Filed:
September 7, 2018
Date of Patent:
June 22, 2021
Assignee:
PHASEBIO PHARMACEUTICALS, INC.
Inventors:
Steven Sparks, Christopher M. Yates, Sammy R. Shaver, William J. Hoekstra
Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like mu opioid receptor agonists of Formula I. Compounds of the present technology demonstrate remarkable potency and selectivity for the mu opioid receptor, while also exhibiting a significant reduction (or, essentially, absence) of the negative side effects of many morphine-derived compounds.
Type:
Grant
Filed:
November 14, 2018
Date of Patent:
June 15, 2021
Assignees:
UNIVERSITY OF KANSAS, VICTORIA LINK LIMITED
Inventors:
Thomas E. Prisinzano, Rachel Saylor Crowley, Bronwyn Maree Daken Kivell
Abstract: The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).
Type:
Grant
Filed:
April 17, 2020
Date of Patent:
June 15, 2021
Assignee:
Black Diamond Therapeutics, Inc.
Inventors:
Alexander Flohr, Alexander Mayweg, George Trainor, David M. Epstein, Matthew O'Connor, Elizabeth Buck, Luca Arista
Abstract: Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.
Type:
Grant
Filed:
October 4, 2018
Date of Patent:
June 8, 2021
Assignee:
The Johns Hopkins University
Inventors:
Jun O. Liu, Yingjun Li, Kalyan Kumar Pasunooti, Wukun Liu, Wei Shi, Ruojing Li, Sarah Head
Abstract: Disclosed are a class of coumarin-like cyclic compounds as MEK inhibitors and pharmaceutical compositions comprising the compounds, and the use of same in the preparation of a drug for treating MEK-related diseases. Particularly disclosed are compounds as shown in formula (I) and pharmaceutically acceptable salts thereof or tautomers thereof.
Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for a method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.
Type:
Grant
Filed:
December 17, 2019
Date of Patent:
June 1, 2021
Assignees:
LUNDBECK LA JOLLA RESEARCH CENTER, INC., THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
Abstract: Substituted pyrimidine and pyridines as NR2B receptor ligands, for example Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity.
Type:
Grant
Filed:
April 3, 2019
Date of Patent:
May 18, 2021
Assignee:
JANSSEN PHARMACEUTICA NV
Inventors:
Jeannie M. Ziff, Cathy Preville, Brock T. Shireman
Abstract: This invention relates to 4-substituted isoquinoline compounds and their derivatives and uses thereof for treatment of cancer, for example, acute myeloid leukemia.
Abstract: The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as a cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
Type:
Grant
Filed:
January 20, 2017
Date of Patent:
May 11, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Ian Stansfield, Olivier Alexis Georges Querolle, Gerhard Max Gross, Edgar Jacoby, Lieven Meerpoel, Janusz Jozef Kulagowski, Calum Macleod, Samuel Edward Mann, Simon Richard Green, George Hynd
Abstract: RNA polymerase I (Pol I) is a dedicated polymerase for the transcription of the 47S ribosomal RNA precursor subsequently processed into the mature 5.8S, 18S and 28S ribosomal RNAs and assembled into ribosomes in the nucleolus. Pol I activity is commonly deregulated in human cancers. Based on the discovery of lead molecule BMH-21, a series of pyridoquinazolinecarboxamides were synthesized as inhibitors of Pol I and activators of the destruction of RPA194, the Pol I large catalytic subunit protein. The present invention identifies a set of bioactive compounds, including purified stereoisomers, that potently cause RPA194 degradation that function in a tightly constrained chemical space. Pharmaceutical compositions comprising these compounds and their uses in cancer and other Pol I related diseases is also provided.
Type:
Grant
Filed:
March 20, 2015
Date of Patent:
May 11, 2021
Assignee:
The Johns Hopkins University and Lieber Institute, Inc.
Inventors:
Marikki Laiho, Laureen Colis, James C. Barrow, Glen Ernst, Sara Sanders
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
December 22, 2017
Date of Patent:
May 4, 2021
Assignees:
ARVINAS OPERATIONS, INC., YALE UNIVERSITY
Inventors:
Andrew P. Crew, Kurt Zimmermann, Jing Wang, Craig M. Crews, Saul Jaime-Figueroa, George Burslem
Abstract: The present invention provides compounds inhibiting General amino acid Control Non-derepressible 2 kinase (“GCN2”), compositions thereof, and methods of using the same for treating various disorders, such as cancer.
Inventors:
Andrew Bayly, Matthew Bleich, Jean-Damien Charrier, James Dodd, Steven Durrant, Meredith Suzanne Eno, Gorka Etxebarria I Jardi, Simon Everitt, Damien Fraysse, Shazia Kelly, Ronald Knegtel, Igor Mochalkin, Michael Mortimore, Kiri North, Filippos Porichis, Robert Pullin, Alistair Rutherford, Pierre-Henri Storck, Heather Clare Twin, Yufang Xiao
Abstract: The aim of the present invention is to provide a method capable of producing an optically active pyrimidinamide derivative on an industrial scale. Compound (I) or a salt thereof is subjected to an asymmetric reduction reaction, the obtained compound (II) or a salt thereof is subjected to a deprotection reaction, and the obtained compound (III) or a salt thereof is reacted with compound (VI) or a salt thereof to obtain compound (V) or a salt thereof. wherein each symbol is as defined in the specification.
Abstract: Provided herein are heterocyclic derivative compounds of Formula (I) and pharmaceutical compositions comprising said compounds. The compounds of Formula (I) are useful for inhibiting plasma kallikrein. Furthermore, the disclosed compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
Abstract: Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
Type:
Grant
Filed:
May 11, 2017
Date of Patent:
April 20, 2021
Assignees:
Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Medshine Discovery Inc.
Abstract: The aryl sulfonamide compounds of this invention have powerful and cell-type specific Bcl inhibitory activity. Selected compounds in this class promote apoptosis in senescent cells, and are being developed for treating senescent-related conditions. Selected compounds in this class promote apoptosis in cancer cells, and can be developed as chemotherapeutic agents.
Abstract: The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).
Type:
Grant
Filed:
March 2, 2018
Date of Patent:
April 20, 2021
Assignee:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Kevin N. Dalby, Ramakrishna Edupuganti, Juliana Taliaferro, Ju Hyeon Lee