Abstract: The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are ?v?6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
Type:
Grant
Filed:
June 26, 2020
Date of Patent:
January 24, 2023
Assignee:
Pliant Therapeutics, Inc.
Inventors:
Jacob Cha, Chengguo Dong, Timothy Hom, Lan Jiang, Katerina Leftheris, Hui Li, David John Morgans, Jr., Manuel Munoz, Maureen Reilly, Yajun Zheng, Christopher Bailey, Darren Finklestein
Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof.
Type:
Grant
Filed:
June 11, 2020
Date of Patent:
January 10, 2023
Assignee:
GlaxoSmithKline Intellectual Property Development Limited
Inventors:
Jeffrey Michael Axten, Mui Cheung, Michael P. Demartino, Hilary Schenck Eidam, Raghava Reddy Kethiri, Biswajit Kalita
Abstract: Described herein are Dendrilla membranosa compounds and derivatives thereof. Also described herein are formulations that can contain an amount of one or more Dendrilla membranosa compounds or derivatives thereof and a carrier. Also described herein are methods of administering one or more Dendrilla membranosa compound and/or derivative thereof or a formulation thereof to a subject in need thereof.
Type:
Grant
Filed:
December 16, 2019
Date of Patent:
January 10, 2023
Assignees:
UNIVERSITY OF SOUTH FLORIDA, THE UAB RESEARCH FOUNDATION
Inventors:
Bill J. Baker, Lindsey N. Shaw, Andrew Jason Shilling, Alexandre Jean Bory, Jessie Allen (Adams), Charles Dunkle Amsler, Jr., James Bruce McClintock
Abstract: According to this method, a fatty acid of CnH2nO2 (n=5 to 14) is mixed with a plurality of metal sources selected from Zn, In, Sn, Sb, and Al, thereby fatty acid metal salts are obtained, subsequently the fatty acid metal salts are heated at 130° C. to 250° C., and a metal soap that is a precursor is obtained. This precursor is heated at 200° C. to 350° C., and metal oxide primary particles are dispersed in the precursor melt. To this dispersion liquid, a washing solvent having a ?P value higher by 5 to 12 than the ?P value of the Hansen solubility parameter of the final dispersing solvent is added, thereby the metal oxide primary particles are washed and agglomerated, metal oxide secondary particles are obtained, and then washing is repeated.
Abstract: The invention discloses a method for the preparation of fluoro alkylated compounds by homogeneous Ni catalyzed fluoro alkylation with fluoro alkyl halides in the presence of a base.
Type:
Grant
Filed:
February 20, 2020
Date of Patent:
December 20, 2022
Assignee:
ARXADA AG
Inventors:
Christoph Taeschler, Stefan Ellinger, Florencio Zaragoza Doerwald, Matthias Beller, Helfried Neumann, Florian Fischer, Shaoke Zhang, Nicolas Rotta-Loria
Abstract: A composition having gel-like consistency contains metronidazole, terconazole, a physiologically acceptable thickener and water. The composition is useful for treating bacterial vaginosis as well as vulvovaginal candidiasis.
Abstract: The present disclosure provides pharmaceutical combinations comprising at least one spliceosome modulator and at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors. Also provided are methods of treating cancer comprising administering a therapeutically effective amount of at least one spliceosome modulator and a therapeutically effective amount of at least one inhibitor chosen from BCL2, BCL2/BCLxL, and BCLxL inhibitors.
Type:
Grant
Filed:
October 30, 2018
Date of Patent:
December 13, 2022
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Daniel Aird, Laura Corson, Ping Zhu, Markus Warmuth, Silvia Buonamici, Peter Gerard Smith, Peter Fekkes
Abstract: Techniques regarding post polymerization modifications to polycarbonate polymers via a flow reactor are provided. For example, one or more embodiments described herein can comprise a cyclic carbonate monomer that can be employed to facilitate polymerization of one or more polycarbonate platforms susceptible to post polymerization modification. For instance, one or more embodiments can regard a cyclic carbonate molecular backbone covalently bonded to an aryl halide functional group via in accordance with a chemical structure selected from the group consisting of: In the chemical structures, “R1” can be selected from the group consisting of a hydrogen atom and a functional group comprising a first alkyl group; “L” can represent a linkage group, comprising: a second alkyl group and an end group having at least one member selected from the group consisting of an oxygen atom and a nitrogen atom; and “A” can represent the aryl halide functional group.
Type:
Grant
Filed:
May 22, 2020
Date of Patent:
December 6, 2022
Assignees:
INTERNATIONAL BUSINESS MACHINES CORPORATION, AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventors:
Nathaniel H. Park, Victoria A Piunova, Dmitry Zubarev, James L. Hedrick, Yi Yan Yang, Eddy Wei Ping Tan
Abstract: The present disclosure describes pharmaceutical formulations of bromocriptine and methods of manufacturing and using such formulations. The formulations are useful for treating physiological disorders including improving glycemic control in the treatment of type 2 diabetes. Also disclosed is synthesis of bromocriptine citrate, and compositions and dosage forms containing bromocriptine citrate.
Abstract: An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): wherein ring A, ring B, R1 to R6, l, m, and n are as defined in the specification.
Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.
Type:
Grant
Filed:
April 14, 2020
Date of Patent:
November 29, 2022
Assignee:
Novartis AG
Inventors:
Ha-Soon Choi, James Paul Lajiness, Srinivasa Reddy Natala, Bao Nguyen, Hank Michael James Petrassi, Zhicheng Wang
Abstract: Described herein are synthetic progestogens, such as 6?,7?:15?,16?-Dimethylene-3-oxo-17?-pregn-4-ene-21,17-carbolactone, as well as pharmaceutical compositions comprising the same. Also described are methods of use.
Type:
Grant
Filed:
July 1, 2022
Date of Patent:
November 22, 2022
Assignee:
LABORATORIOS LEON FARMA SA
Inventors:
Philippe Perrin, Jose Luis Velada, Dominique Drouin
Abstract: It discloses a proteolysis targeting chimeric molecule, a preparation method and an application thereof. The proteolysis targeting chimeric molecule provided by the disclosure can inhibit the expression of BCR-ABL and/or CRBN protein in BCR-ABL and/or CRBN positive leukemia K562 cells to varying degrees, and thus can be used to prepare drugs for treating BCR-ABL and/or CRBN positive leukemia, wherein the proteolysis targeting chimeric molecule with n=3 has excellent photo-isomerization activity, and can be used in preparation of the reagents or drugs for light-regulated degradation of BCR-ABL and/or CRBN protein. The disclosure also provides a method for synthesizing the series of proteolysis targeting chimeric molecules.
Abstract: The present invention relates to a new process for preparing quinoline compounds of the general formula (II): in which Q, A, R4, R3 and R3?, are as defined herein, as well as to the intermediate compounds of said new process.
Type:
Grant
Filed:
December 14, 2018
Date of Patent:
November 22, 2022
Assignee:
Bayer Animal Health GMBH
Inventors:
Florian Erver, Frank Memmel, Thomas Himmler, Andreas Karl Steib, Marc Nowakowski
Abstract: Described herein are catalytic hydrogenation and the use of ruthenium complexes having a bidentate diphosphine ligand or two monodentate phosphine ligands, two carboxylate ligands, and optionally a diamine ligand in hydrogenation processes for the reduction of imines into the corresponding amines.
Abstract: A method of producing a cannabinoid nanoparticle carrier composition for administration to a human, including the steps of incorporating non-ionic surfactants with cannabinoid oils and lipids; inducing sonication for a predetermined period of time at a predetermined amplification with a ultrasonic liquid processor until completely integrated; dissolving ascorbic acid into a carrier fluid; combining in sequence the non-ionic surfactants, lipids, and cannabinoids with a carrier fluid consisting of distilled water and ascorbic acid; sonicating using an ultrasonic liquid processor at predetermined amplitude for a predetermined period of time at a controlled temperature.
Abstract: The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard.
Abstract: A method for producing a nitroso compound of the following formula (3), comprising reacting a compound of the following formula (1) with a compound of the following formula (2) by using a tertiary alcohol and a base. wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently a hydrogen atom, a halogen atom, a (C1-C4) alkyl, or a (C1-C4) alkoxy.