Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds as antagonist of TLR7 and/or TLR8 and/or TLR9 in the treatment of autoimmune diseases as well as auto-inflammation diseases.
Type:
Grant
Filed:
September 6, 2018
Date of Patent:
January 10, 2023
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Zongxing Qiu, Hong Shen, Wei Zhu, Fabian Dey, Ge Zou, Hongtao Xu
Abstract: Ebola virus and Marburg virus are filoviruses and are responsible for outbreaks that cause up to 90% fatality, including the recent outbreak in West Africa that has resulted in over 11,000 deaths. The present disclosure generally relates to novel arylnaphthalene compounds as a vacuolar-ATPase inhibitor that are useful for the treatment of various viral infections, including those infections caused by filoviruses. Pharmaceutical composition matters and methods of use are within the scope of this invention.
Type:
Grant
Filed:
March 18, 2019
Date of Patent:
January 3, 2023
Assignee:
Purdue Research Foundation
Inventors:
Vincent Jo Davisson, Aaron Raymond Lindstrom
Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Abstract: The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
Type:
Grant
Filed:
January 8, 2021
Date of Patent:
January 3, 2023
Assignee:
Oyster Point Pharma, Inc.
Inventors:
Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Timothy J. Cuthbertson, Gary Maurice Dull, Craig Harrison Miller, Joseph Pike Mitchener, Jr., Julio A. Munoz, Pieter Albert Otten
Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.
Type:
Grant
Filed:
May 15, 2020
Date of Patent:
December 20, 2022
Assignee:
NURIX THERAPEUTICS, INC.
Inventors:
Arthur T. Sands, Neil F. Bence, Christoph W. Zapf, Frederick Cohen, Chenbo Wang, Thomas Cummins, Hiroko Tanaka, Hunter Shunatona, Mario Cardozo, Dahlia Weiss, Jennifa Gosling
Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or produg thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
Type:
Grant
Filed:
June 5, 2020
Date of Patent:
December 13, 2022
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
Abstract: The present disclosure provides certain fused tricyclic ring derivatives that are Src Homology-2 phosphatase (SHP2) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of SHP2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of CRBN, and the treatment of CRBN-mediated disorders.
Type:
Grant
Filed:
January 14, 2019
Date of Patent:
November 29, 2022
Assignee:
KYMERA THERAPEUTICS, INC.
Inventors:
Nello Mainolfi, Nan Ji, Arthur F. Kluge
Abstract: Described herein are compounds of the formula (I), as well as pharmaceutical compositions comprising such compounds, and methods for using such compounds/pharmaceutical compositions for treating neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, and multiple sclerosis (MS).
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
November 29, 2022
Assignee:
University of Massachusetts
Inventors:
Jeanne A. Hardy, Penchala Narasimharao Meka
Abstract: Disclosed are compounds, compositions and methods for treating diseases, disorders, or medical conditions that are affected by the modulation of DHODH. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, X, and Y are defined herein.
Type:
Grant
Filed:
April 16, 2020
Date of Patent:
November 22, 2022
Inventors:
Scott Kuduk, Zhuming Zhang, Lindsey DeRatt, Aihua Wang
Abstract: Provided herein, in some embodiments, are cytosine analogs, compositions comprising cytosine analogs, and methods of use for inhibiting a Ten-eleven translocation (TET) enzyme.
Type:
Grant
Filed:
March 20, 2020
Date of Patent:
November 22, 2022
Assignee:
President and Trustees of Bates College
Inventors:
Andrew Kennedy, Gabriella N. L. Chua, Kelly L. Wassarman, Haoyu Sun
Abstract: The present invention provides compounds and methods for treating, ameliorating, and/or preventing a MKP-5 modulated disease. In certain embodiments, the MKP-5 modulated disease is a fibrotic disease.
Type:
Grant
Filed:
December 18, 2018
Date of Patent:
November 22, 2022
Assignee:
YALE UNIVERSITY
Inventors:
Anton Bennett, Jonathan Ellman, Haya Jamali, Karen S. Anderson, Elias Lolis, Denton Hoyer
Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
Type:
Grant
Filed:
March 12, 2021
Date of Patent:
November 22, 2022
Assignee:
Novartis AG
Inventors:
Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
Abstract: Disclosed are compounds inhibiting ErbBs (e.g., EGFR or Her 2), especially mutant forms of ErbBs, and BTK, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition can effectively treat ErbBs (especially mutant forms of ErbBs) or BTK associated diseases, including cancer.
Abstract: Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound “G”): and precursors thereof.
Type:
Grant
Filed:
September 9, 2020
Date of Patent:
November 15, 2022
Assignee:
KEZAR LIFE SCIENCES
Inventors:
Henry Johnson, Sean Dalziel, Dustin McMinn
Abstract: Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
Abstract: Disclosed is method for treating cancer in a mammal, comprising administering to a mammal in need thereof a compound of the formula: wherein R1, R2, and R3 are as defined herein, wherein the cancer is an autophagy-dependent cancer, in an amount sufficient to induce autophagy in the cell and cause the death of cancer cells. Also disclosed is a method for selectively killing cancer cells in a patient afflicted with cancer, comprising administering to the mammal, wherein the cancer cells are autophagy-dependent cancer cells, in an amount sufficient to induce autophagy in the cells and cause the death of the cancer cells.
Type:
Grant
Filed:
May 26, 2020
Date of Patent:
October 18, 2022
Assignee:
The United States of Americans represented by the Secretary, Department of Health and Human Services
Inventors:
Melvin L. DePamphilis, Gaurav Sharma, Juan Jose Marugan, Marc Ferrer, Ajit Roy
Abstract: Compound of formula (I) and its addition salts with pharmaceutically acceptable acids, and methods in which an effective amount of the compound or any pharmaceutically acceptable salt thereof is administered (as a medicament) to an individual in need thereof.
Type:
Grant
Filed:
April 9, 2018
Date of Patent:
October 18, 2022
Assignees:
COMMISSARIAT À L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, PERHA PHARMACEUTICALS
Abstract: The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.
Type:
Grant
Filed:
September 13, 2017
Date of Patent:
October 11, 2022
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN