Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
February 3, 2021
Date of Patent:
March 7, 2023
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Yao-Ling Qiu, Xuri Gao, Jorden Kass, Hui Cao, Wei Li, Xiaowen Peng, Byung-Chul Suh, Yat Sun Or
Abstract: The disclosure relates to a pectin-adriamycin conjugate, and discloses a preparation method and use of the conjugate above. The pectin-adriamycin conjugate of the disclosure has a completely new chemical structure and can be accumulated in a malignant tumor tissue for a long time with a high concentration in a targeting manner so as to achieve the purposes of enhancing effects and reducing toxicity, and the indications are chemotherapies of various solid malignant tumors.
Type:
Grant
Filed:
June 18, 2019
Date of Patent:
March 7, 2023
Assignee:
SICHUAN YINGRUI PHARMACEUTICAL TECHNOLOGY COMPANY
Abstract: Provided herein are photochemical separations. The methods herein can include exposing a first metal complex and a second metal complex to light to facilitate an irreversible chemical reaction to form a modified first metal complex. The modified first metal complex then may be separated from the second metal complex. Compositions also are provided.
Type:
Grant
Filed:
July 20, 2018
Date of Patent:
February 28, 2023
Assignee:
The Florida State University Research Foundation, Inc.
Inventors:
Kenneth Hanson, Thomas Edward Schoenzart, Sahan Salpage
Abstract: Disclosed are methods and compositions for repolarizing a tumor associated macrophage (TAM) from M2 to M1 comprising administering to a subject in need thereof an effective dose of a compound comprising a dextran backbone and one or more CD206 targeting moieties conjugated thereto. In certain aspects, the compound further comprises a therapeutic agent selected from: paclitaxel, gemcitabine, lapatinib, and doxorubicin. In further aspect, the therapeutic agent comprises a chelator and at least one metal ion. In certain implementations, the at least one metal ion comprises at least one Cu(II) ions.
Abstract: A method of producing a halosiloxane, the method comprising: combining water, a halosilane, and a first solvent, where the first solvent has a water solubility of >1.5 grams in 100 ml of solvent, to form a reaction mixture having a temperature above the melting point temperature of the solvent, partially hydrolyzing and condensing the halosilane to form a reaction product mixture comprising the halosiloxane, the solvent, a hydrogen halide and unreacted halosilane, and, optionally, adding a second solvent with a boiling point?the boiling point of the halosiloxane to the reaction mixture or the reaction product mixture.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
February 21, 2023
Assignee:
DDP SPECIALTY ELECTRONIC MATERIALS US 9 LLC
Inventors:
Noel Mower Chang, Barry M. Ketola, Andrew R. Millward, Xiaobing Zhou
Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.
Type:
Grant
Filed:
March 16, 2021
Date of Patent:
February 21, 2023
Assignee:
Heptares Therapeutics Limited
Inventors:
John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
Abstract: In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The medicant moiety can be a toxin including an acylfulvene or a drug moiety. The affinity moiety can be an antibody, a binding protein, a steroid, a lipid, a growth factor, a protein, a peptide or non peptidic. The affinity moiety can be covalently bound to the medicant via a linker. Novel linkers that can be directed to cysteine, arginine or lysine residues based on solution pH allow greater flexibility in preserving and/or generating specific epitopes in the AMC.
Abstract: The present invention relates to a novel compound for preventing or treating neurodegenerative diseases and use thereof. Provided is a novel compound of Formula (I). The compound can effectively promotes the proliferation of neural progenitor cells in both in vitro and in vivo experiments, and can serves as a treatment approach to promote nerve regeneration to fight against cognition impairment associated with aging and neurodegenerative diseases.
Abstract: Nanoscale metal halide perovskites are provided. The nanoscale metal halide perovskites may have a 2D structure, a quasi-2D structure, or a 3D structure. Methods also are provided for making the nanoscale metal halide perovskites. The color emitted by the nanoscale metal halide perovskites may be tuned.
Type:
Grant
Filed:
December 29, 2020
Date of Patent:
February 14, 2023
Assignee:
Florida State University Research Foundation, Inc.
Abstract: The invention provides monoferrocenyl compounds of general formula I. The invention also provides substrates labelled with the compounds, functionalised derivatives of the compounds and methods of using the compounds, functionalised derivatives and labelled substrates in electrochemical assays.
Type:
Grant
Filed:
April 5, 2021
Date of Patent:
February 7, 2023
Assignee:
Binx Health Limited
Inventors:
Barrie J. Marsh, Christopher G. Frost, Jonathan Sharp
Abstract: Disclosed are methods for purifying polyols containing oxyalkylene units that is an alkali metal catalyzed alkoxylation reaction product of an alkylene oxide and an H-functional starter. The methods include neutralizing the alkali metal ions with an aqueous solution comprising water and sulfuric acid, in which: (i) the sulfuric acid is present in an amount of no more than 5% by weight, based on the total weight of the aqueous solution, and (ii) the sulfuric acid is used in an amount of 2% to 10% more than the theoretical amount necessary to neutralize all of the alkali metal ions present. The methods can produce polyols having a low content of 2-methyl-2-pentenal.
Abstract: The invention provides methods for treating a subject afflicted with a memory impairment or a cognitive dysfunction. Additional methods for improving memory and memory related functions in healthy subjects are also provided. The Methods include administration of an inhibitor of Na/K-ATPase.
Type:
Grant
Filed:
February 24, 2019
Date of Patent:
February 7, 2023
Assignee:
CARMEL HAIFA UNIVERSITY ECONOMIC CORPORATION LTD.
Abstract: This disclosure features compounds and compositions that are useful in methods of treating coronavirus infections (e.g., useful in methods of treating COVID-19) in a subject in need thereof. The methods include administering to the subject niclosamide compounds (or pharmaceutically acceptable salts and/or co-crystals thereof, e.g., niclosamide). In some embodiments, the niclosamide compounds have one or more properties that include, but are not limited to: a particular purity or a particular particle size. In an aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for respiratory administration (e.g., via inhalation and/or intranasally). In another aspect, the niclosamide compounds described herein (e.g., niclosamide) can form part of compositions, dosage forms (e.g., unit dosage forms), and the like, which are suitable for administration to the GI tract (e.g.
Abstract: Provided is a production method for a gel composition including steps (1) to (3) mentioned below: step (1) of mixing at room temperature a partial degradation product of the galactose moiety of galactoxyloglucan and an aqueous solvent to obtain a mixture; step (2) of cooling or freezing the mixture obtained in step (1); and step (3) of gelling the mixture cooled or frozen in step (2) by heating to obtain a gel composition that includes the galactose-partial degradation product.
Type:
Grant
Filed:
April 14, 2021
Date of Patent:
January 31, 2023
Assignee:
Sumitomo Pharma Food & Chemical Co., Ltd.
Abstract: Various methods and compositions for treating age-associated conditions and other medical conditions, such as muscle diseases, type 2 diabetes, and/or obesity are described. Methods of enhancing cellular uptake of NMN and stimulating NAD+ production are further described. Various mammalian cells and mammalian cell lines are described including those comprising a cDNA encoding a Slc12a8 protein. Gene therapy vectors comprising a nucleic acid encoding Slc12a8 and non-human animals comprising an inactivating mutation in a Slc12a8 gene are also disclosed. Also described are methods for screening a candidate compound to identify compounds that promote NMN transport.
Abstract: This invention relates to compounds that are useful as cancer therapies. The compounds comprise azithromycin derivatives having a phosphonium cation tethered to the azithromycin macrocycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.
Type:
Grant
Filed:
April 20, 2018
Date of Patent:
January 24, 2023
Inventors:
Tim Sparey, Andrew Ratcliffe, David Hallett, Brett Stevenson, Edward Cochrane, Alexandre Froidbise
Abstract: Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds.
Type:
Grant
Filed:
December 31, 2020
Date of Patent:
January 17, 2023
Assignee:
THE USA, AS REPRESENTED BY THE SECRETARY, DHHS
Inventors:
Amy Hauck Newman, Oluyomi M. Okunola-Bakare, Jianjing Cao
Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
Type:
Grant
Filed:
November 20, 2020
Date of Patent:
January 17, 2023
Assignee:
Agency for Science, Technology and Research
Abstract: New host-protective molecules containing conjugated triene and diene double bonds with each carrying a 13-carbon position alcohol and were derived from n-3 docosapentaenoic acid (DPA, C22:5) were produced in neutrophil-endothelial co-cultures, and they are present in human and mouse tissues after sterile inflammation or infection. These compounds, termed 13-series resolvins (RvT), demonstrated potent protective actions increasing mice survival during Escherichia coli infections. Their biosynthesis during neutrophil-endothelial cell interactions was initiated by endothelial cyclooxygenase-2 (COX-2) and increased by atorvastatin via S-nitrosylation of COX-2. Atorvastatin and RvT were additive in E. coli infections in mice where they accelerated resolution of inflammation and increased survival >60%. Results documented novel host protective molecules in bacterial infections, namely RvT, derived from n-3 DPA via transcellular biosynthesis and increased by atorvastatin.
Type:
Grant
Filed:
September 23, 2019
Date of Patent:
January 17, 2023
Assignee:
The Brigham and Women's Hospital, Inc.
Inventors:
Jesmond Dalli, Nan Chiang, Charles N. Serhan