Abstract: Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.
Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.
Type:
Grant
Filed:
May 24, 2017
Date of Patent:
March 30, 2021
Assignee:
Sarepta Therapeutics, Inc.
Inventors:
Baozhong Cai, Mitchell Martini, Ross Shimabuku, Katie Thomas
Abstract: Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.
Type:
Grant
Filed:
June 30, 2017
Date of Patent:
March 16, 2021
Assignee:
SAREPTA THERAPEUTICS, INC.
Inventors:
Baozhong Cai, Mitchell Martini, Katie Thomas, Ross Shimabuku
Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
Type:
Grant
Filed:
April 29, 2019
Date of Patent:
March 16, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Mihir B. Mandal, David B. Olsen, Jing Su, Lihu Yang, Katherine Young, Takao Suzuki, Lanying You
Abstract: The invention relates to the use, as an extraction agent for extracting at least one rare earth from an aqueous phase including phosphoric acid, of at least one compound of the following general formula (I): where n is an integer equal to 0, 1 or 2, R1 and R2 are H or an aliphatic hydrocarbon group, one of R3 and R4 has the following formula (II): where R5 and R6 are a hydrocarbon, hydroxyl or alkoxyl group, and the other one of R3 and R4 has one of the following formulas (II?) and (III): where R5? and R6? are a hydrocarbon, hydroxyl or alkoxyl group, and R7 and R8 are H or an aliphatic hydrocarbon group. The invention also relates to a method for recovering at least one rare earth using said compound, as well as to specific compounds as such.
Type:
Grant
Filed:
September 4, 2019
Date of Patent:
March 2, 2021
Assignees:
COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE MONTPELLIER
Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R1, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
Type:
Grant
Filed:
August 26, 2020
Date of Patent:
February 9, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
Type:
Grant
Filed:
June 18, 2019
Date of Patent:
December 22, 2020
Assignees:
University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States Government as represented by the Department of Veterans Affairs
Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof.
Type:
Grant
Filed:
June 7, 2017
Date of Patent:
December 1, 2020
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Jeffrey Michael Axten, Mui Cheung, Anthony William Dean, Michael P. DeMartino, Hilary Schenck Eidam, Biswajit Kalita, Raghava Reddy Kethiri, Rajendra Kristam
Abstract: Compositions comprising small molecule mitofusin agonists are described. The mitofusin modulating agents are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin 1 (Mfn1) and/or mitofusin 2 (Mfn2), or mitochondrial dysfunction. Methods of treatment, pharmaceutical formulations, and screening methods for identifying compounds that regulate mitochondrial function are also described.
Abstract: Compounds of formula (I), wherein Ar is an aryl group optionally further substituted with one or more groups R3; A is a lipophilic, hydrophobic moiety; R1 is a phosphodiester, phosphotriester, thioether or amide group; X is an unsubstituted or substituted C6 to C24 alkylene or alkenylene group, which is optionally interrupted by one or more —NR9—, —O— or —S— linkages, R2 is —YC(R4)(R5)CO2R6; and pharmaceutically acceptable salts or solvates thereof are useful as endosomolytic agents particularly for the delivery of nucleic acids useful in gene therapy.
Type:
Grant
Filed:
September 27, 2017
Date of Patent:
November 24, 2020
Assignee:
UCB Biopharma SRL
Inventors:
Terence Seward Baker, Michael Anthony William Eaton, Timothy John Norman, James Petrie Turner
Abstract: Provided herein are processes, compounds and compositions for making (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid. Also provided herein a pharmaceutical compositions containing (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid.
Type:
Grant
Filed:
May 28, 2019
Date of Patent:
November 17, 2020
Assignee:
NORTHWESTERN UNIVERSITY
Inventors:
Richard B. Silverman, Matthew Moschitto
Abstract: The invention relates to the compounds of formula I, formula II and formula III or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II and formula III, and methods for treating or preventing Parkinson's disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment or management of Parkinson's disease such as Parkinson's disease, scleroderma, restless leg syndrome, hypertension and gestational hypertension.
Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating KIT mediated diseases.
Type:
Grant
Filed:
March 5, 2019
Date of Patent:
November 10, 2020
Assignee:
AstraZeneca AB
Inventors:
Jason Kettle, Stuart Pearson, Martin Packer, James Smith, Tudor Grecu
Abstract: Imidazole-based compounds as hepatitis C virus (HCV) inhibitors. The compounds have an imidazole core that is disubstituted via amide links. Also described are a pharmaceutical composition incorporating the imidazole-based compound, a method of preparing these compounds, and a method for using the pharmaceutical composition in the treatment of HCV infection.
Abstract: Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.
Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R2A, R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Type:
Grant
Filed:
January 17, 2019
Date of Patent:
October 13, 2020
Assignee:
Pfizer Inc.
Inventors:
Douglas Carl Behenna, Ping Chen, Kevin Daniel Freeman-Cook, Robert Louis Hoffman, Mehran Jalaie, Asako Nagata, Sajiv Krishnan Nair, Sacha Ninkovic, Martha Alicia Ornelas, Cynthia Louise Palmer, Eugene Yuanjin Rui
Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
Type:
Grant
Filed:
May 1, 2020
Date of Patent:
October 6, 2020
Assignee:
BRISTOL-MYERS SQUIBB COMPANY
Inventors:
Liqi He, Sanjeev Gangwar, Yam B. Poudel, Prasanna Sivaprakasam
Abstract: Disclosed is a composition and method for a therapeutic treatment that is able to combat certain conditions such as alcohol dependence, opioid abuse treatment, neurological disorders, neuropathic pain, and fibromyalgia. The novel gliotoxin analog compound acts by acting as an antagonist to one or more opioid receptors, which, when present leads to the inhibition of conditions, providing increased performance over known treatments. The disclosed compounds also shows the ability to cross the blood-brain-barrier in a highly efficient manner.
Type:
Grant
Filed:
October 30, 2018
Date of Patent:
September 29, 2020
Assignee:
TEXAS TECH UNIVERSITY SYSTEM
Inventors:
Nadezhda German, Mohammad Anwar Hossain
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R9, Y, W, m, n, p and q are as defined herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
April 10, 2019
Date of Patent:
September 29, 2020
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Patrick Di Giorgio, Jerome Hert, Daniel Hunziker, Patrizio Mattei, Markus Rudolph, Petra Schmitz
Abstract: The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
May 8, 2018
Date of Patent:
September 15, 2020
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Lars Wortmann, Ulrich Lücking, Julien Lefranc, Hans Briem, Marcus Koppitz, Knut Eis, Franz Von Nussbaum, Benjamin Bader, Antje Margret Wengner, Gerhard Siemeister, Wilhelm Bone, Philip Lienau, Joanna Grudzinska-Goebel, Dieter Moosmayer, Uwe Eberspächer, Hans Schick