Abstract: The invention provides antifungal compounds, antifungal compositions, and intermediates for the preparation of antifungal compounds and antifungal compositions. The invention also provides methods of inhibiting fungi and methods of treating fungal infections, for example, with a compound or composition described herein. The antifungal compositions can include antifungal adjuvants such as essential oils or essential oil extracts, which adjuvants further improve the antifungal activity of the compositions.
Type:
Grant
Filed:
July 26, 2017
Date of Patent:
February 16, 2021
Assignees:
University of Southern California, CNRS, Universite Grenoble Alpes, INSERM
Inventors:
Charles E. McKenna, Carlo Petosa, Jerome Govin, Boris A. Kashemirov, Elena Ferri, Flore Mietton
Abstract: Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agent
Abstract: Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and methods of treatment or prevention thereof.
Type:
Grant
Filed:
May 10, 2017
Date of Patent:
February 2, 2021
Assignee:
GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
Inventors:
Richard K. Plemper, Eddy Lee, John Vernachio, Elyse Bourque
Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases. The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.
Type:
Grant
Filed:
November 22, 2017
Date of Patent:
January 26, 2021
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
James Bradner, Dennis Buckley, Mette Ishoey Rosenbaum, Georg Winter
Abstract: Disclosed herein are salts of (R)-2-fluoro-10a-methyl-7,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(5H)-one, and crystalline forms (polymorphs) thereof. Also disclosed herein are methods of preparing those crystalline forms, and methods of using at least one of those crystalline forms in treating a cancer responsive to inhibition of PARP, especially a cancer associated with BRCA1/2 mutant activities or other HR deficiencies, in a subject.
Abstract: The present invention relates to bicyclic pyridine, pyrazine, and pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K? inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Type:
Grant
Filed:
June 15, 2017
Date of Patent:
January 19, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Didier Jean-Claude Berthelot, Laurence Anne Mevellec, Patrick Rene Angibaud, Sophie Coupa, Christophe Gabriel Marcel Demestre, Lieven Meerpoel, Guillaume Jean Maurice Mercey, Christophe Meyer, Elisabeth Therese Jeanne Pasquter, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Olivier Alexis Georges Querolle
Abstract: The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.
Type:
Grant
Filed:
March 15, 2018
Date of Patent:
January 19, 2021
Assignee:
Celgene CAR LLC
Inventors:
Gregg Brian Feigelson, Maryll E. Geherty, Richard Martin Heid, Jr., Mohit Kothare, Hon-Wah Man, Alexander L. Ruchelman, John F. Traverse, Kelvin Hin-Yeong Yong, Chengmin Zhang
Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R1, R2, R3, R4, R4?, R5, R6, X, and n are described herein.
Type:
Grant
Filed:
February 13, 2017
Date of Patent:
January 12, 2021
Assignee:
VALO EARLY DISCOVERY, INC.
Inventors:
David Joseph Guerin, Kenneth W. Bair, Justin A. Caravella, Stephanos Ioannidis, Jr., David R. Lancia, Jr., Hongbin Li, Steven Mischke, Pui Yee Ng, David Richard, Shawn E. R. Schiller, Tatiana Shelekhin, Zhongguo Wang
Abstract: The invention relates to stable, isotopically labeled compounds for use in mass spectrometry analysis for quantifying methotrexate in a sample. Exemplary compounds include isotopically labeled variants of methotrexate.
Abstract: Disclosed are new small molecules having a pyrrolopyrimidine core structure and the uses thereof for modulating glucocerebrosidase activity. Also disclosed are pharmaceutical compositions comprising the small molecules which may be administered in methods of treating diseases or disorders associated with glucocerebrosidase activity, including neurological diseases and disorders such as Gaucher's disease and Parkinson's disease. The small molecules may be utilized to generate activated glucocerebrosidase. The activated glucocerebrosidase thusly generated can be administered in enzyme replacement therapy and/or utilized in screening assays for new small molecules that bind to the activated glucocerebrosidase and/or modulate the activity of the activated glucocerebrosidase.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
January 5, 2021
Assignee:
Northwestern University
Inventors:
Dimitri Krainc, Richard B. Silverman, Jianbin Zheng
Abstract: The disclosure provides compounds of the formula I and the pharmaceutically acceptable salts thereof. The variables, e.g. R1, R2, R3, R4, A, B, J, V, W, M, J and Ar are defined herein. The disclosure also provides pharmaceutical compositions comprising a compound or salt of formula I and a pharmaceutically acceptable carrier, methods of inhibiting dihydrofolate reductase (DHFR) in vitro or in vivo with a compound or salt of formula I, and methods of treating a bacterial infections, fungal infections, and protozoal infections with a compound or salt of formula I. A compound or salt of formula I can be the first and only active ingredient used in a pharmaceutical composition or method of this disclosure or may be combined with one or more additional active ingredients that are not compounds or salts of formula I.
Type:
Grant
Filed:
January 9, 2017
Date of Patent:
December 22, 2020
Assignee:
UNIVERSITY OF CONNECTICUT
Inventors:
Dennis Wright, Amy C. Anderson, Eric Scocchera, Narendran Gummudipundi Dayanandan, Santosh Keshipeddy, Stephanie Reeve, Michael N. Lombardo, Michael Henry Cynamon
Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
December 22, 2020
Assignee:
SHY Therapeutics LLC
Inventors:
Yaron R. Hadari, Luca Carta, Michael Schmertzler, Theresa M. Williams, Charles H. Reynolds
Abstract: The present invention provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula: wherein A3 is CR3A, CR3AR3B, N or NR3C; R3A, R3B, R4A and R4B are each independently a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted non-aromatic carbocyclyl; R3C is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted non-aromatic carbocyclyl; ring T1 is substituted or unsubstituted nitrogen-containing non-aromatic heterocycle; R1 is a hydrogen atom, halogen, cyano, or substituted or unsubstituted alkyl; R2 is each independently substituted or unsubstituted alkyl or the like: n is 1 or 2; R3 is substituted or unsubstituted aromatic carbocyclyl or the like; R4 is a hydrogen atom or a carboxy protecting group.
Abstract: The present disclosure provides compounds of Formula (I?), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.
Type:
Grant
Filed:
October 22, 2018
Date of Patent:
December 15, 2020
Assignee:
Massachusetts Institute of Technology
Inventors:
Angela N. Koehler, Eric Stefan, Francisco Caballero, Dylan Vijith Neel, Nicholas B. Struntz, Helen L. Evans, Andrew Chen
Abstract: The present application provides bifunctional compounds of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 4 (CDK4) and/or cyclin-dependent kinase 6 (CDK6). The present application also relates to methods for the targeted degradation of CDK4 and/or CDK6 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK4 and/or CDK6 which can be utilized in the treatment of disorders modulated by CDK4 and/or CDK6.
Type:
Grant
Filed:
April 21, 2017
Date of Patent:
December 15, 2020
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski, Baishan Jiang, Eric Wang
Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
January 10, 2020
Date of Patent:
December 15, 2020
Assignee:
ENANTA PHARMACEUTICALS, INC.
Inventors:
Brian C. Shook, In Jong Kim, Thomas P. Blaisdell, Jianming Yu, Joseph Panarese, Yat Sun Or
Abstract: The present application provides bifunctional compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which act as protein degradation inducing moieties for cyclin-dependent kinase 8 (CDK8). The present application also relates to methods for the targeted degradation of CDK8 through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to CDK8 which can be utilized in the treatment of disorders modulated by CDK8.
Type:
Grant
Filed:
April 21, 2017
Date of Patent:
December 15, 2020
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, Tinghu Zhang, Calla M. Olson, Yanke Liang, Nicholas Kwiatkowski