Abstract: A comonomer comprising: wherein W is selected from the group consisting of: S, Se, O, and N-Q; and Q is selected from the group consisting of: a straight-chain or branched carbyl, silyl, or hydrocarbyl, a branched or cyclic alkyl with 1 to 30 atoms, a fused substituted aromatic ring, and a fused unsubstituted aromatic ring. In this comonomer, A and B are independently selected from the group consisting of: H, Br, an aryl group, and a heteroaryl group.
Type:
Grant
Filed:
August 26, 2020
Date of Patent:
July 18, 2023
Assignee:
Phillips 66 Company
Inventors:
Hualong Pan, Kathy Woody, Brian J. Worfolk
Abstract: Disclosed are compounds that activate excitatory amino acid transporter 2 (EAAT2), as well as methods of using these compounds to treat or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.
Type:
Grant
Filed:
June 4, 2019
Date of Patent:
July 18, 2023
Assignees:
OHIO STATE INNOVATION FOUNDATION, THE BRIGHAM AND WOMAN'S HOSPITAL, INC.
Abstract: The present invention provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
Type:
Grant
Filed:
December 17, 2020
Date of Patent:
July 18, 2023
Assignee:
NOVARTIS AG
Inventors:
Simona Cotesta, Marc Gerspacher, Catherine Leblanc, Edwige Liliane Jeanne Lorthiois, Bo Liu, Rainer Machauer, Robert Mah, Christophe Mura, Pascal Rigollier, Nadine Schneider, Stefan Stutz, Andrea Vaupel, Nicolas Warin, Rainer Wilcken
Abstract: The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
Abstract: The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, pain, behavioral and psychological symptoms of dementia and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.
Abstract: The present disclosure relates to the technical field of drug synthesis, in particular to a method for preparing lornoxicam. The method includes the following steps: using 6-chloro-4-hydroxy-2-methyl-2-H-thieno[2,3-e]-1,2-thiazine methyl carboxylate-1,1-dioxide and 2-aminopyridine as raw materials, and xylene as a solvent; mixing the raw material and solvent, and adding a stabilizer, to obtain a mixture; subjecting the mixture to an ammonolysis; cooling the resulting reactant; conducting a vacuum concentration to remove the solvent; adding an organic solvent and slurrying, and filtering, to obtain a crude lornoxicam; and refining the crude lornoxicam to obtain the lornoxicam. In the present disclosure, p-toluenesulfonic acid is used as a stabilizer to reduce the reaction temperature and promote the reaction to proceed forward, thereby improving the quality and yield of the product.
Abstract: Disclosed herein are compounds of formula I: or a pharmaceutically acceptable salt thereof, where the variables are as defined herein. These compounds are useful in treating RET associated cancers. Formulations containing the compounds of formula I and methods of making the compounds of formula I are also disclosed.
Type:
Grant
Filed:
November 5, 2021
Date of Patent:
July 11, 2023
Assignee:
Eli Lilly and Company
Inventors:
Gabrielle R. Kolakowski, Erin D. Anderson, Steven W. Andrews, Christopher Pierre Albert Jean Boldron, Kevin R. Condroski, Thomas C. Irvin, Manoj Kumar, Elizabeth A. McFaddin, Megan L. McKenney, Johnathan Alexander McLean, Tiphaine Mouret, Michael J. Munchhof, Thomas Pierre Dino Pancaldi, Michael Alexander Pilkington-Miksa, Marta Pinto
Abstract: The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Type:
Grant
Filed:
May 5, 2021
Date of Patent:
July 4, 2023
Assignee:
Ajax Therapeutics, Inc.
Inventors:
Craig E. Masse, Jeremy R. Greenwood, Sayan Mondal, Jiayi Xu, Phani Ghanakota, Fiona Michelle McRobb, Nicholas Boyles
Abstract: Disclosed is a method for preparing a pyrrolidinyl urea derivative, which acts as a TrkA inhibitor, and further disclosed are an intermediate compound of a compound of formula (I) and a preparation method therefor.
Abstract: Disclosed are compounds of following formula (I): in which all symbols have the same meanings as the definitions described in the specification; or a salt thereof. The compounds or a salt thereof are useful as a prophylactic and/or therapeutic agent for cancer, Huntington's disease, Alzheimer's disease and the like.
Abstract: Described herein are MK2 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of autoimmune disorders, chronic inflammatory disorders, acute inflammatory disorders, auto-inflammatory disorders, fibrotic disorders, metabolic disorders, neoplastic disorders, and cardiovascular or cerebrovascular disorders.
Type:
Grant
Filed:
July 7, 2022
Date of Patent:
June 27, 2023
Assignee:
XINTHERA, INC.
Inventors:
Robert L. Hoffman, Lynnie Trzoss, Qing Dong, Stephen W. Kaldor
Abstract: The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
Type:
Grant
Filed:
October 30, 2020
Date of Patent:
June 27, 2023
Assignee:
REVOLUTION MEDICINES, INC.
Inventors:
Christopher Michael Semko, Gang Wang, G. Leslie Burnett, James Bradley Aggen, Gert Kiss, James Joseph Cregg, Micah James Evans Gliedt, Jennifer Pitzen, Julie Chu-Li Lee, Walter Won, Arun P. Thottumkara, Adrian Liam Gill
Abstract: The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), Formula (II), Formula (III), or Formula (IV), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
Type:
Grant
Filed:
June 25, 2019
Date of Patent:
June 27, 2023
Assignee:
PTC Therapeutics, Inc.
Inventors:
Guangming Chen, Anuradha Bhattacharyya, Yao Jiang, Gary Mitchell Karp, Jana Narasimhan, Anthony Turpoff, Nanjing Zhang
Abstract: The present invention relates to: a process for preparing 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide or chloride; a method of converting 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide to 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride; and the purification of 7-bis-(dimethylamino)-phenothiazin-5-ium chloride by crystallization from aqueous solution of hydrochloric acid, leading to a pharmaceutically acceptable 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride (methylthioninium chloride, methylene blue, MTC) of formula I below reported.
Type:
Grant
Filed:
June 9, 2021
Date of Patent:
June 20, 2023
Assignee:
MIKROCHEM SPOL. S R.O.
Inventors:
Daniela Benadiková, Juraj Cech, Erik Juhás, Vladimír Oremus, Vendel {hacek over (S)}mahovský
Abstract: A novel compound represented by the following general formula (1), or a salt thereof, which has a superior EP4 receptor agonist activity, and a medicament containing the compound or a salt thereof as an active ingredient, which can be used for promotion of osteogenesis, therapeutic treatment and/or promotion of healing of fracture and the like.
Abstract: The present invention discloses salts of a Compound 1: useful in the prophylaxis and/or treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving degradation and/or disruption of cartilage homeostasis, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
Abstract: Provided is a tartrate salt of 3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine and crystalline forms thereof. Also provided are pharmaceutical compositions comprising a tartrate salt disclosed herein and crystalline forms thereof and a pharmaceutically acceptable excipient, and a method of treating a disease or disorder, such as disease or disorder associated with neuroinflammation, comprising administering to a subject in need thereof, a therapeutically effective amount of an acid addition salt disclosed herein or the pharmaceutical composition of the acid addition salt.
Type:
Grant
Filed:
September 13, 2022
Date of Patent:
May 30, 2023
Assignee:
Pioneura Corporation
Inventors:
Harris A. Gelbard, John M. McCall, Jesse Damsker, Arthur Romero
Abstract: A method for producing an aromatic dianhydride includes reacting an aromatic diimide with a substituted or unsubstituted phthalic anhydride in an aqueous medium in the presence of an amine exchange catalyst to provide an aqueous reaction mixture including an N-substituted phthalimide, an aromatic tetraacid salt, and at least one of an aromatic triacid salt and an aromatic imide diacid salt. The method further includes removing the phthalimide from the aqueous reaction mixture by extracting the aqueous reaction mixture with an organic solvent in a first extractor for a first time period, at a first extraction temperature and subsequent to the first time period, extracting the aqueous reaction mixture with an organic solvent in a second extractor for a second time period, at a second extraction temperature. The aromatic tetraacid salt is converted to the corresponding aromatic dianhydride. Aromatic dianhydrides prepared according to the method are also described.
Type:
Grant
Filed:
May 13, 2019
Date of Patent:
May 30, 2023
Assignee:
SHPP GLOBAL TECHNOLOGIES B.V.
Inventors:
Aaron Matthew Royer, Sivakumar Periyasamy, Ravi Gautam, Jorge Jimenez Umana, Gregory L. Hemmer, Robert Werling, Hareesh Shamrao Deshpande
Abstract: Disclosed are a compound containing a fused ring, a use thereof and a pharmaceutical composition containing same. Provided are a compound as shown in formula I-A, a pharmaceutically acceptable salt thereof, a solvate thereof, a solvate of the pharmaceutically acceptable salt thereof or a crystal form thereof. The compound can significantly reduce the levels of HBsAg, HBeAg and HBV DNA, and can be used for preparing a drug for treating hepatitis B, and has good market prospects.
Type:
Grant
Filed:
April 22, 2020
Date of Patent:
May 30, 2023
Assignee:
NANJING HEPO PHARMACEUTICAL CO., LTD
Inventors:
Pengfei Qian, Fengbo Li, Xuejun Liu, Xiaodong Chen, Lijun Guo, Kai Sun