Abstract: The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.
Type:
Grant
Filed:
June 11, 2019
Date of Patent:
June 20, 2023
Assignee:
The Regents of the University of Colorado, a body corporate
Abstract: The present invention relates to pyrazole derivatives of formula (X) wherein ring A is a pyrazole and substituents RB1, RB2, n, RQ1, RQ2, RQ3, and RQ4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.
Type:
Grant
Filed:
January 29, 2021
Date of Patent:
June 20, 2023
Assignee:
SYNGENTA CROP PROTECTION AG
Inventors:
Sally Elizabeth Russell, James Alan Morris
Abstract: The present disclosure provides tetrahydro-1H-pyrido[3,4-b]indole compounds or a pharmaceutically acceptable salt, solvate, hydrate, prodrug, stereoisomer, tautomer, rotamer, N-oxide and/or substituted derivative or, optionally in a pharmaceutical composition, for the modulation of disorders mediated by estrogen, or other disorders as more fully described herein.
Type:
Grant
Filed:
December 6, 2021
Date of Patent:
June 13, 2023
Assignee:
Olema Pharmaceuticals, Inc.
Inventors:
David C. Myles, Peter J. Kushner, Cyrus L. Harmon
Abstract: Disclosed are novel analogs of cytisine, a process for their preparation, pharmaceutical compositions containing them, and their use in the prevention of or treatment of CNS disorders including addictive disorders.
Type:
Grant
Filed:
August 17, 2017
Date of Patent:
June 6, 2023
Inventors:
Timothy Charles Gallagher, Hugo Rego Campello
Abstract: Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
Abstract: A tetracarboxylic dianhydride includes: at least one acid dianhydride (A) selected from the group consisting of compounds each having an endo/exo type three-dimensional structure represented by a particular general formula and their enantiomeric compounds each having an exo/endo type three-dimensional structure; and/or an acid dianhydride (B) having an endo/endo type three-dimensional structure represented by a particular general formula, wherein a content of the acid dianhydride (B) in a total amount of the acid dianhydrides (A) and (B) is 30 to 100% by mole in a mole ratio.
Abstract: Disclosed herein are methods of treating or suppressing a disorder selected from the group consisting of ?-synucleinopathies, tauopathies, ALS, traumatic brain injury, and ischemic-reperfusion related injuries.ury, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of the formula: or the hydroquinone form thereof; or a solvate or hydrate thereof.
Type:
Grant
Filed:
November 10, 2021
Date of Patent:
June 6, 2023
Assignee:
PTC THERAPEUTICS, INC.
Inventors:
Andrew W. Hinman, Charles R. Holst, Angela Minnella, Paul Mollard, Sean Pintchovski, Jeffrey K. Trimmer, Eric Torrey
Abstract: The present invention relates to IL-8 inhibitor compounds, preferably dual CXCR1/CXCR2 receptor inhibitors, useful in the treatment and/or prevention of some sarcomas, preferably in the treatment and/or prevention of osteosarcoma, Ewing sarcoma, rhabdomyosarcoma or lung metastasis associated thereof.
Type:
Grant
Filed:
October 23, 2018
Date of Patent:
May 30, 2023
Assignees:
Dompe' Farmaceutici S.P.A., Research Institute at Nationwide Children's Hospital
Abstract: The present disclosure describes the use of 2,4-disulfonyl phenyl tert-butyl nitron (2,4-ds-PBN) in the treatment of temozolomide drug resistant gliomas. The 2,4-ds-PBN may be used combined with other chemo- and radiotherapies and surgery, including temozolomide, to reduce glioma occurrence, recurrence, spread, growth, metastasis, and vascularization, and to inhibit development of temozolomide resistance.
Abstract: A process for synthesizing an azo compound by oxidation of a hydrogen compound in the presence of a catalyst and a compound of formula (I) is described in which R1, R2 and R3 (R1)(R2)C(PO3(R3)2)2??(I) are as defined. The use of a compound of formula (I) as complexing agent for a catalyst is also described.
Abstract: A method for preparing 18F-BPA and an intermediate, by which high-purity 18F-BPA is obtained. The method simplifies the synthesis steps after 18F labeling, and is easy to operate and efficient.
Type:
Grant
Filed:
February 9, 2021
Date of Patent:
May 23, 2023
Assignee:
NEUBORON MEDTECH LTD.
Inventors:
Shi-hong Li, Jing He, Heng Yan, Fei Cai
Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to oxadiazaspiro compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular against drug abuse and addiction.
Type:
Grant
Filed:
December 21, 2020
Date of Patent:
May 16, 2023
Assignee:
ESTEVE PHARMACEUTICALS, S.A.
Inventors:
Marina Virgili-Bernado, Carmen Almansa-Rosales, Carlos Alegret-Molina
Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating renal diseases are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
Type:
Grant
Filed:
August 11, 2021
Date of Patent:
May 16, 2023
Assignee:
VTV THERAPEUTICS LLC
Inventors:
Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
Abstract: The present invention relates to an organic electronic device, comprising a first electrode, a second electrode, and a substantially organic layer comprising a compound according to formula (I) between the first and the second electrode: wherein M is a metal ion, each of A1-A4 is independently selected from H, substituted or unsubstituted C6-C20 aryl and substituted or unsubstituted C2-C20 heteroaryl and n is valency of the metal ion.
Type:
Grant
Filed:
February 25, 2021
Date of Patent:
May 16, 2023
Assignee:
Novaled GmbH
Inventors:
Sascha Dorok, Mike Zoellner, Carsten Rothe, Omrane Fadhel
Abstract: High purity 2-naphthylacetonitrile with fewer impurities can be used as a starting material or intermediate for synthesizing various pharmaceutical products, agricultural chemicals, and chemical products, and a production method thereof. A high purity 2-naphthylacetonitrile having an HPLC purity of 2-naphthylacetonitrile of not less than 95 area %, and containing naphthalene compounds represented by the formulas (a)-(j) at a content of a predetermined area % or below. A method for producing high purity 2-naphthylacetonitrile, may include: subjecting 2?-acetonaphthone to a Willgerodt reaction in the presence of an additive where necessary, and hydrolyzing the obtained amide compound to give 2-naphthylacetic acid; and reacting the 2-naphthylacetic acid obtained in the subjecting, a halogenating agent and sulfamide in the presence of a catalyst as necessary in an organic solvent to give 2-naphthylacetonitrile.
Abstract: A method for producing a maleimide compound having a group represented by the formula (a1), the method including condensing a primary amino group in a raw material compound having the primary amino group and dicarboxylic anhydride represented by the formula (a2) to generate a group represented by the formula (a3); and heating a compound having the group represented by the formula (a3), and converting the group represented by the formula (a3) into the group represented by the formula (a1).
Abstract: The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases.
Abstract: The present invention relates to the use of efficient phosphorous substances, in particular based on diphenylamine and heterocyclic diphenylamine derivatives as stabilizers for organic materials, in particular for plastic materials, against oxidative, thermal and/or actinic degradation. The present invention additionally relates to an organic material that has been correspondingly stabilized as described above. The invention further relates to a method of stabilizing organic materials and to specific stabilizers.
Type:
Grant
Filed:
February 14, 2018
Date of Patent:
April 25, 2023
Assignee:
Fraunhofer-Gesellschaft zur förderung der angewandten Forschung e.V.
Inventors:
Michael Ciesielski, Max Briesenick, Rudolf Pfaendner
Abstract: Described herein are corrole-based frameworks and methods for making the same. The corrole-based frameworks have unique structural and physical properties, which lends them to be versatile in a number of different applications and uses such as in gas storage/separation, proton conduction, biomedicine, sensing, and catalysis. In one aspect, the corrole-based frameworks are organic frameworks. In other aspects, the corrole-based frameworks are metal-organic frameworks.