Abstract: A method for producing a homocyclic or heterocyclic compound includes reacting a compound of formula (I) with a compound of formula (II) in presence of a base: R1—B-G??(I) In formula (I), B is an unsaturated moiety selected from substituted or unsubstituted vinylene, ethynylene, aryleneethynylene, substituted or unsubstituted arylenevinylene, and a combination thereof, the vinylene or arylenevinylene has n (=0, 1 or 2) substituent(s) R2, G is an electron-withdrawing group, R1 is hydrogen or a substituent, and two of R1, R2 and G may joint together to form a ring. In formula (II), R3 and R4 are independently hydrogen or a substituent, R5 is an electron-withdrawing group, and two of R3, R4 and R5 may joint together to form a ring. The conjugate acid of the base has a pKa in the range of 1 to 15.
Abstract: This invention relates to pharmaceutically acceptable ergoline analogues and salts thereof. In particular, though not exclusively, the invention relates to formulations and uses of the same as a medicament.
Type:
Grant
Filed:
September 9, 2022
Date of Patent:
July 11, 2023
Assignee:
BECKLEY PSYTECH LIMITED
Inventors:
Massimo Muratore, Amir Lotfi Moghaddam, Christopher Wong
Abstract: Disclosed are a crystal form of a thieno[2,3-c]pyridazine-4(1H)-one compound, a preparation method therefor and the use thereof in the preparation of a drug as an inhibitor of ACC1 and ACC2.
Abstract: Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
Abstract: The present invention relates generally to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to methods for the use of calmodulin inhibitors and calcium channel blockers for treatment of ribosomal disorders and ribosomopathy, e.g. Diamond Blackfan anemia (DBA).
Abstract: Disclosed is a process to produce a purified vapor comprising dialkyl-furan-2,5-dicarboxylate (DAFD). Furan-2,5-dicarboxylic acid (FDCA) and an alcohol in an esterification zone to generate a crude diester stream containing dialkyl furan dicarboxylate (DAFD), unreacted alcohol, 5-(alkoxycarbonyl)furan-2-carboxylic acid (ACFC), and alkyl furan-2-carboxylate (AFC). The esterification zone comprises at least one reactor that has been previously used in an DMT process.
Type:
Grant
Filed:
March 22, 2021
Date of Patent:
May 23, 2023
Assignee:
Eastman Chemical Company
Inventors:
Kevin John Fontenot, Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh
Abstract: Heterocyclic compounds are provided as arginase inhibitors, in particular to a compound represented by Formula (I), or a pharmaceutically acceptable salt, stereoisomer or tautomer, or prodrug thereof and a pharmaceutical composition including the compound.
Abstract: A composition comprising a therapeutically effective amount of a cannabinoid and protocatechuic acid is provided. The disclosure further provides a method of treating inflammation comprising administering a composition comprising a therapeutically effective amount of a cannabinoid and protocatechuic acid to a patient in need thereof. The disclosure further provides a method of treating inflammation including administering a composition including protocatechuic acid and a composition including a cannabinoid to a patient in need thereof. In embodiments, the composition including protocatechuic acid and the composition including a cannabinoid may be administered simultaneously within about 60 minutes of each other. In embodiments, the cannabinoid includes Cannabidiol (CBD).
Abstract: A process for preparing a nitrated compound, including the step of reacting a compound (A) including at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein the heteroaromatic ring includes at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I) wherein Y is selected from the group consisting of hydrogen and nitro.
Abstract: The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds useful as activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.
Type:
Grant
Filed:
April 23, 2021
Date of Patent:
May 16, 2023
Assignee:
FORMA THERAPEUTICS, INC.
Inventors:
Anna Ericsson, Neal Green, Gary Gustafson, Bingsong Han, David R. Lancia, Jr., Lorna Mitchell, David Richard, Tatiana Shelekhin, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
Abstract: Compounds of Formula (I) and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents, e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression). Methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding ?-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.
Abstract: The present subject matter provides a crystalline form of the compound having the following structure: wherein the crystalline form is a polymorph, hydrate or solvate.
Type:
Grant
Filed:
July 16, 2018
Date of Patent:
April 25, 2023
Assignee:
ADAMA MAKHTESHIM LTD.
Inventors:
Michael Grabarnick, Gal Suez, Zoltán Német, Samaa Alasibi
Abstract: Catalysts comprising MoP and MoP2 are disclosed, wherein the catalyst is a composite. The catalyst may have a molar ratio of MoP:MoP2 within a range of 5:95 to 95:5. The catalyst may be used as a cathode active material for hydrogen generation from neutral pH solutions, such as wastewater or seawater. Methods of making the catalyst also are disclosed.
Abstract: Provided herein are novel lipase inhibitors and methods for using the same to treat inflammation, multisystem organ failure, necrotic pancreatic acinar cell death, acute pancreatitis, sepsis (e.g., culture negative sepsis), burns, and acne. For example, provided herein are two novel lipase inhibitors useful in the methods described herein: or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 20, 2022
Date of Patent:
April 11, 2023
Assignee:
Mayo Foundation for Medical Education and Research
Inventors:
Vijay P. Singh, Sampath-Kumar Anandan, Kevin Greenman, Zeeshan Kamal
Abstract: A composition comprising a therapeutically effective amount of a cannabinoid and protocatechuic acid is provided. The disclosure further provides a method of treating inflammation comprising administering a composition comprising a therapeutically effective amount of a cannabinoid and protocatechuic acid to a patient in need thereof. The disclosure further provides a method of treating inflammation including administering a composition including protocatechuic acid and a composition including a cannabinoid to a patient in need thereof. In embodiments, the composition including protocatechuic acid and the composition including a cannabinoid may be administered simultaneously within about 60 minutes of each other. In embodiments, the cannabinoid includes Cannabidiol (CBD).
Abstract: There is provided a method of producing ethylene oxide and ethylene glycol capable of reducing a concentration in discharged water of 1,4-dioxane contained generated in a step of producing ethylene oxide and ethylene glycol. A method of producing ethylene oxide and ethylene glycol includes a predetermined step of producing ethylene oxide, and a step of extracting a part of a column bottom liquid of an ethylene oxide stripping column in the step of producing ethylene oxide and supplying the extracted column bottom liquid to a by-produced ethylene glycol concentration column, concentrating ethylene glycol produced as a by-product in the step of producing ethylene oxide, and distilling and separating 1,4-dioxane produced as a by-product in the step of producing ethylene oxide, wherein the by-produced ethylene glycol concentration column is a divided wall distillation column.
Abstract: The invention provides a polycondensation catalyst for producing polyester by an esterification reaction or a transesterification reaction of a dicarboxylic acid or an ester-forming derivative thereof and a glycol, wherein the polycondensation catalyst comprises particles of a water-insoluble or hardly water-soluble phosphate having on the surfaces a coating layer of titanic acid in an amount, of 0.1 to 100 parts by weight in terms of TiO2 per 100 parts by weight of the phosphate.
Abstract: A process for preparing a silver-containing catalyst for the oxidation of ethylene to ethylene oxide (EO) including the steps of: providing a support having pores; providing a silver-containing impregnation solution; adding an amount of surfactant to the impregnation solution; contacting the support with the surfactant-containing impregnation solution; and removing at least a portion of the impregnation solution prior to fixing the silver upon the carrier in a manner which preferentially removes impregnation solution not contained in the pores. The use of the surfactant results in improved drainage of the silver impregnation solution from the carrier exteriors during the catalyst synthesis. As a result, the amount of silver-containing impregnation solution necessary for the synthesis of the EO catalyst was reduced by up to 15% without reducing the catalyst performance.
Type:
Grant
Filed:
November 30, 2018
Date of Patent:
March 28, 2023
Assignee:
Dow Technology Investments LLC
Inventors:
Daniel Grohol, Thomas Z. Srnak, Cathy L. Tway, George L. Athens, Kyle R. Essenmacher, Gary M. Seabolt, Tim D. Munro
Abstract: 3-Carbonylamino-8-aminoisoquinoline compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the 3-carbonylamino-8-aminoisoquinoline compounds.
Type:
Grant
Filed:
October 3, 2019
Date of Patent:
March 28, 2023
Assignee:
Genentech, Inc.
Inventors:
Jun Liang, Rohan V. Mendonca, Michael Siu, John Tellis, Weiru Wang, BinQing Wei, Bryan Chan, Edna F. Choo, Joy Drobnick, Lewis J. Gazzard, Timothy Heffron
Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a triazole-methyl-piperidinyl-pyrolyl-propenone structure which function as modulators of shared epitope (SE)—calreticulin (CRT) binding and/or interaction, and their use as therapeutics for the treatment of immunoregulatory abnormalities (e.g., autoimmune diseases, inflammatory diseases (e.g., chronic inflammatory disease), and bone erosive diseases) by selectively inhibiting SE-CRT interactions and/or signal transduction pathways commonly overactive or dysregulated in arthritic and/or other diseases or conditions.
Type:
Grant
Filed:
October 14, 2021
Date of Patent:
March 28, 2023
Assignee:
The Regents of the University of Michigan