Abstract: A process for producing THC-O-acetate using a succession of distillation, salting-out assisted liquid-liquid extractions (SALLEs), and solvent recovery techniques. Tetrahydrocannabinol (THC) in cannabis oil reacts with acetic anhydride under reflux to produce THC-O-acetate and acetic acid. The resulting crude product is distilled and subjected to a SALLE with hexane followed by a SALLE with petroleum ether, before being distilled again in order to obtain a refined, THC-O-acetate product.
Type:
Grant
Filed:
September 4, 2020
Date of Patent:
August 24, 2021
Assignee:
Nextleaf Solutions Ltd.
Inventors:
Krupal Devendra Pal, Ryan Delmoral Ko, Brock Aston Hughes, Ivan Jason Casselman
Abstract: The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.
Type:
Grant
Filed:
May 4, 2020
Date of Patent:
August 17, 2021
Assignee:
AbbVie Inc.
Inventors:
Brian P. Enright, Ye Huang, Philip R. Kym, Yanbin Lao, Xiaochun Lou, Sean E. Mackey, Peter T. Mayer, Christopher P. Miller, Valentino J. Stella, Eric A. Voight
Abstract: The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by ROR?.
Abstract: Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Type:
Grant
Filed:
September 17, 2019
Date of Patent:
August 10, 2021
Assignee:
METACRINE, INC.
Inventors:
Nicholas D. Smith, Steven P. Govek, Karensa L. Douglas, Andiliy G. Lai
Abstract: Provided is the use of an aromatic ring drug in inhibiting a key transcription factor of malignant melanoma. In particular, provided is the use of a compound as represented by formula A, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition or preparation. The pharmaceutical composition or preparation is used for: (a) inhibiting a key transcriptional regulatory factor of malignant melanoma, namely MITF (Microphthalmia-associated Transcription Factor); (b) treating MITF-related diseases such as melanoma, pancreatic cancer, skin hypersensitivity and asthma; and (c) regulating physiological activities in which MITF is involved, such as skin whitening. In the formula, each group is as defined in the description.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
August 3, 2021
Assignee:
SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
Inventors:
Jing Wang, Min Guo, Pengfei Fang, Biao Yu
Abstract: The invention relates to Mycobacterium tuberculosis-thioredoxin reductase inhibitors, processes for the preparation thereof, drugs containing said compounds, and the use of said compounds for manufacturing drugs.
Abstract: According to the present invention, a cured product obtained by curing a curable composition including a compound represented by General Formula 1, in which a birefringence ?n (587 nm) is 0.00??n (587 nm)?0.01, is provided, and this cured product is suitable for manufacturing an optical member. Pol1-Sp1-L1-Ar-L2-Sp2-Pol2??(General Formula 1) In formula, Ar is an aromatic ring group represented by General Formula 2-2 and the like. In formula, Z1 and Z2 each represent a hydrogen atom, a methyl group, and the like; A1 and A2 each represent —S— and the like; X represents C(Rz)2 and the like (where Rz is a substituent, and two Rz's may form a ring); L1 and L2 each represent a single bond, —O—, —OC(?O)—, —OC(?O)O—, —OC(?O)NH—, and the like; Sp1 and Sp2 each represent a single bond or a divalent linking group; Pol1 and Pol2 each represent a hydrogen atom or a polymerizable group; and a compound represented by General Formula 1 has at least one polymerizable group.
Abstract: Disclosed are methods and pharmaceutical compositions for treating a cancer in a subject in need thereof, the cancer characterized by proteolytic cleavage by taspase1 of the mixed-lineage leukemia 1 gene product (MLL1), the method comprising administering to the subject a therapeutic agent that inhibits cleavage by taspase1 of MLL1. Suitable therapeutic agents may include agents that inhibit the kinase activity of casein kinase II (CKII). Cancer treated by the disclosed methods and pharmaceutical compositions may include leukemia such as Acute Lymphoblastic Leukemia (ALL) and/or Acute Myeloid Leukemia (AML) and in particular, leukemia characterized by rearrangements in MLL1.
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:
December 18, 2019
Date of Patent:
July 20, 2021
Assignee:
Eastman Chemical Company
Inventors:
Kevin John Fontenot, Mesfin Ejerssa Janka, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh
Abstract: The present disclosure provides a substituted pyridine derivative, which can be used as a bioactive compound for inhibiting stomach cell lines and/or inducing regeneration of damaged stomach lining.
Type:
Grant
Filed:
December 29, 2016
Date of Patent:
July 20, 2021
Assignee:
UNITED ARAB EMIRATES UNIVERSITY
Inventors:
Hany Abdel Aziz Eldeab, Yaser E. Greish, Sneha Thomas, Sherif M. Karam
Abstract: The present disclosure provides macrocyclic compounds inspired by the immunophilin ligand family of natural products FK506 and rapamycin. The generation of a Rapafucin library of macrocyles that contain FK506 and rapamycin binding domains should have great potential as new leads for developing drugs to be used for treating diseases.
Type:
Grant
Filed:
October 1, 2019
Date of Patent:
July 20, 2021
Assignees:
The Johns Hopkins University, Rapafusyn Pharmaceuticals, Inc.
Inventors:
Jun Liu, Sam Hong, Brett R. Ullman, Joseph E. Semple, Kana Yamamoto, Puneet Kumar, Magesh Sadagopan, Jennifer C. Schmitt
Abstract: The present invention relates to a compound having the structure of formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof, where X, Y, Z, R, R1, R2, R3, R4, R5, and R6 are as described herein. The present invention also relates to compositions containing the compound having the structure of formula (I), and a method of treating cancer in a subject.
Type:
Grant
Filed:
November 14, 2019
Date of Patent:
July 20, 2021
Assignee:
ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
Inventors:
Arvin C. Dar, Ross L. Cagan, Alex P. Scopton, Masahiro Sonoshita
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, R6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
July 8, 2019
Date of Patent:
July 13, 2021
Assignee:
ChemoCentryx, Inc.
Inventors:
Viengkham Malathong, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Penglie Zhang
Abstract: An object of the invention is to provide compounds of formula (1) or salts thereof which are effective as agricultural and horticultural fungicides. In the formula, R1 represents, for example, a hydroxy group or a cyano group, R2, R3 and R4 are independent of one another and each represent, for example, a hydrogen atom or a halogen atom, R5 represents, for example, a hydrogen atom or a halogen atom, X represents an oxygen atom or a sulfur atom, Y represents, for example, a phenyl group or a pyridyl group, and the bond including the broken line represents a double bond or a single bond.
Abstract: Process to continuously prepare a cyclic carbonate product by reacting an epoxide compound with carbon dioxide in the presence of a supported dimeric aluminium salen complex which complex is activated by a halide compound comprising the following steps, (a) contacting carbon dioxide with the epoxide compound in a suspension of liquid cyclic carbonate and the supported dimeric aluminium salen complex which complex is activated by a halide compound, (b) separating part of the cyclic carbonate product from the supported dimeric aluminium salen complex, (c) separating the halide compound from the cyclic carbonate product to obtain purified cyclic carbonate product, (d) use all or part of the halide compound as obtained in step (c) to activate deactivated supported dimeric salen complex.
Abstract: Compounds represented by general Formulae I to IV as described herein are disclosed. Further disclosed are composition utilizing the herein disclosed compounds and using the same for the treatment of glycogen storage disorders.
Type:
Grant
Filed:
February 22, 2018
Date of Patent:
July 6, 2021
Assignees:
Hadasit Medical Research Services and Development Ltd., Ramot at Tel-Aviv University Ltd.
Inventors:
Or Kakhlon, Miguel Enrique Weil, Leonardo Javier Solmesky
Abstract: Provided are a compound for treating metabolic diseases having the structure as shown in formula (I) or formula (II), or a racemate, stereoisomer, geometric isomer, tautomer, solvate, hydrate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound is an activator of FXR and/or a TGR5 receptor, and thus has the activity of activating FXR and/or a TGR5 receptor, and can be used in the preparation of drugs for treating chronic liver diseases, metabolic diseases or portal hypertension.
Type:
Grant
Filed:
August 15, 2018
Date of Patent:
June 8, 2021
Assignee:
XI' AN BIOCARE PHARMA LTD.
Inventors:
Guoqin Fu, Wei Ding, Bo Yin, Chao Yang, Cuiqin Wang, Yong Dou, Ruiling Wang
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
June 8, 2021
Assignee:
SRX CARDIO, LLC
Inventors:
Thomas E Barta, Jonathan W Bourne, Kyle D Monroe, Michael M Muehlemann
Abstract: Methods of treating patients diagnosed with AML or MDS harboring mutant IDH-1 include detecting an IDH1 mutation and the therapeutic administration of an inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA) or cytarabine.
Type:
Grant
Filed:
July 30, 2019
Date of Patent:
May 25, 2021
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu