Abstract: Chiral acetyl-protected aminoethyl quinoline (APAQ), pyridine and imazoline ligands are disclosed that enable Pd (II)-catalyzed enantioselective arylation or heteroarylation of ubiquitous prochiral ?-methylene C—H bonds of aliphatic amides offers an alternative disconnection for constructing ?-chiral centers. Systematic tuning of the ligand structure reveals that a six-membered instead of a five-membered chelation of these types of ligands with the Pd(II) is important for accelerating the C(sp3)-H activation thereby achieving enantioselectivity for quinoline and pyridine ligands.
Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating diseases or disorders in a subject where the subject is in need of an inhibitor of MEK where the Compound is according to Formula (I), where X1, R1, R2, R2a, R3, R3a, and R3b are as described herein.
Abstract: The present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.
Inventors:
Hartmut Beck, Raimund Kast, Mark Meininghaus, Chantal Fuerstner, Timo Stellfeld, Clemens-Jeremias Von Buehler, Lisa Dietz, Michaela Bairlein, Johanna Anlahr, Hannah Joerissen, Peter Hauff, Joerg Mueller, Karoline Droebner, Jens Nagel
Abstract: The present application relates to novel substituted N-arylethyl-2-arylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.
Abstract: This disclosure relates to compounds that are CBP inhibitor and methods of using such compounds in the treatment and diagnosis of diseases and disorders.
Type:
Grant
Filed:
July 13, 2018
Date of Patent:
August 24, 2021
Assignee:
University of Massachusetts
Inventors:
Wei Zhang, Alex Mugwiria Muthengi, Hailemichael O. Yosief
Abstract: A compound, or a pharmaceutically acceptable salt or isomer thereof, of Formula I: wherein R is hydrogen, alkyl, substituted alkyl, alkenyl, or substituted alkenyl; R1 is hydrogen, alkoxy, or substituted alkoxy; R2 is hydrogen, alkyl, or substituted alkyl; and R3 is hydrogen, alkyl, or substituted alkyl.
Type:
Grant
Filed:
February 19, 2018
Date of Patent:
August 3, 2021
Assignees:
University of Pittsburgh—Of the Commonwealth System of Higher Education, Universite Le Havre Normandie
Inventors:
Abdelhadi Rebbaa, Sebastien Comesse, Adam Daich, Martin Lawson, Catalin Pintiala
Abstract: Disclosed is a process for purifying one or more chemical constituents from plant matter using extraction with a fluid that is not a solvent, for example, with a vegetable oil. The extracted chemical constituents may then optionally be further processed by heating in order to induce desired chemical transformations. The extracted chemical constituents are also processed by concentrating at reduced pressure, for example, by distillation.
Abstract: The present disclosure relates to a process for the production of aromatic primary amines, by reacting an aromatic dialdehyde with hydrogen and ammonia or an ammonia-liberating compound, in the presence of a hydrogenation catalyst and an amine, wherein the molar ratio of the amine to the aromatic dialdehyde is no less than 1:4 at the start of the reaction.
Abstract: Described herein is an hydrofluorocarboximidate of formula (I) where: RH is a linear or branched alkyl group comprising 1 or 2 carbon atoms and (a) Rf1 and Rf2 are independent-selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from oxygen, nitrogen, or combinations thereof; or (b) Rf1 and Rf2 are connected to form a ring structure comprising a total of 4-8 carbon atoms and in addition to the nitrogen atom from the carboximidate the ring structure may optionally comprises at least one catenated atom selected from oxygen, nitrogen, or combinations thereof. A method of making the hydrofluorocarboximidate with improved yield is described as well as various uses for the hydrofluorocarboximidate of Formula (I).
Abstract: Methods for extracting and concentrating cannabinoids using ultrasound-enhanced solvent extraction. Freshly harvested cannabis plant materials, which may be selectively chosen plant parts or the entire plant itself, are shredded to a particular particle size. The plant material is then mixed with a solvent to form a slurry, and thereafter subjected to ultrasound to release intracellular contents into the solvent. Filtering steps are then applied to remove biomass, waxes and chlorophyll. Water removal and solvent recovery steps are further applied to ultimately derive an extract having high concentrations of target cannabinoids, and in particular cannabidiol (CBD). The methods may be deployed on-site in batch or continuous flow processes, and may further be utilized to derive other types of materials from plants, such as essential oils.
Abstract: A novel polycyclic amide compound, preparation process and use thereof are provided. The compound has cytotoxic biological activity, particularly for the treatment and/or prevention of cell proliferative diseases such as cancer. This compound is a compound represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, enantiomer or racemic mixture, prodrug and N-oxide thereof, wherein, R, R1-R3 are independently selected from hydrogen, C1-5 alkyl, or C1-5 having a hydroxyl group or a halogen, and may be bonded to each other to form a ring, Z is an arbitrary substituent group, X1 and X2 may be carbon or nitrogen respectively, Q is oxygen or sulfur. Compared to the existing known polycyclic amide compounds, the novel polycyclic amide compound has more potent cytotoxicity and can be used for the treatment of diseases such as tumors, cancers, Alzheimer's disease, autoimmune diseases, cataracts, psychological disorders, depression and/or anxiety.
Abstract: The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R1a, R1b, R1c, R1d, R2, R3, R8a, R8b, R10, X, Z2, m, and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer.
Type:
Grant
Filed:
March 30, 2018
Date of Patent:
June 29, 2021
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various pp diseases, including cancer and infectious diseases.
Type:
Grant
Filed:
March 26, 2018
Date of Patent:
June 29, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, Denis R. St. Laurent, Jeffrey Lee Romine, Paul Michael Scola
Abstract: Provided is a hair restoration/growth stimulating agent containing at least one type of flavonoid represented by formula (I) as an active ingredient. Further provided is a hair restoration/growth stimulating agent containing at least one type of phenylpropanoid represented by formula (II) as an active ingredient.
Abstract: Disclosed herein are borazine, borate, and azaborinine compounds and compositions, methods of making said compounds and compositions, and methods of forming aromatic difluorocarbon compounds and difluorocarbon compounds.
Type:
Grant
Filed:
June 28, 2019
Date of Patent:
June 8, 2021
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Abstract: The present invention provides an isoindolone-imide ring-1,3-dione-2-ene compound, and a preparation method, a pharmaceutical composition and use thereof. Specifically, the present invention provides a compound of Formula (I) below or a pharmaceutically acceptable salt thereof, wherein Ar is an isoindolinone-imide group represented by Formula (II), L is absent or is a divalent, trivalent or tetravalent linking group, and X is a group represented by Formula (III). Definitions of the other groups are as described in the specification. The compound of Formula (I) is an autophagy modulators, particularly a mammalian ATG8 homolog modulator.
Abstract: The invention relates to novel compounds of the formula (I) in which Aa, Ab, Ac, Ad, Q, R1 and n have the definitions given above, to their use as acaricides and/or insecticides for controlling animal pests and to processes and intermediates for their preparation.
Type:
Grant
Filed:
February 14, 2019
Date of Patent:
June 1, 2021
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ruediger Fischer, Dominik Hager, Laura Hoffmeister, Matthieu Willot, Kerstin Ilg, Ulrich Goergens, Andreas Turberg
Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
May 18, 2021
Assignee:
The Regents of the University of California
Inventors:
Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
Abstract: A composition for preventing or treating an aging-related disease includes a novel decursin derivative as an active ingredient, wherein the novel decursin derivative has exhibited an excellent effect of inhibiting progerin expression and excellent effect of inhibiting binding between progerin and lamin A, and it has been confirmed that the novel decursin derivative prolongs the survival period of animal models in which progerin was induced.
Type:
Grant
Filed:
April 25, 2018
Date of Patent:
May 18, 2021
Assignee:
PRG S&TECH INC
Inventors:
Bum Joon Park, Gyu Yong Song, Yu Seok O, Jee Hyun Lee, Eun Ju Yun