Abstract: A method for producing monovalent unsaturated free fatty acids having 20 and/or 22 carbons or low-grade alcohol esters thereof, said method involving the following: obtaining free fatty acids or low-grade alcohol esters through the hydrolysis or alcoholysis of oils and fats derived from marine products; carrying out distillation on the free fatty acids or low-grade alcohol esters, and reducing the concentration of fatty acids with 18 or less carbons in the low-grade alcohol esters or free fatty acids; and collecting fractions of monovalent unsaturated free fatty acids having 20 and/or 22 carbons or low-grade alcohol esters thereof by column chromatography based on reversed-phase distribution.
Abstract: The present disclosure relates to the preparation of polymorphic mixtures of Cepharanthine.2HCl. Mixtures of at least two polymorphic forms can be formed into a mobile liquid phase in organic/aqueous solvent mixtures along with enteric polymer that can be spray dried to produce solid particulate enteric formulations for medicinal drug-treatment applications.
Type:
Grant
Filed:
March 19, 2018
Date of Patent:
March 3, 2020
Assignee:
Southwest Research Institute
Inventors:
William E. Bauta, Joseph A. McDonough, Hong Dixon, Stephen T. Wellinghoff, Kevin Fitzpatrick
Abstract: Provided are a reducible degradable hyperbranched-polymer nanomicelle and a method for preparation thereof and an application thereof. Cystamine and polyethylene glycol diglycidyl ether are polymerized by means of a nucleophilic addition mechanism; in one step, a hyperbranched polymer alternatingly arising from cystamine and polyethylene glycol structural units is synthesized and obtained; then, a hyperbranched nanomicelle is formed by means of self-assembly during the process of dialysis. The hyperbranched-polymer chain segments contain both tertiary aminos and disulfide bond structural units and have pH- and reduction responsiveness, and the hyperbranched three-dimensional cavity structure imparts a drug-carrying ability to the nanomicelle.
Type:
Grant
Filed:
July 29, 2016
Date of Patent:
March 3, 2020
Assignee:
JIANGNAN UNIVERSITY
Inventors:
Caihua Ni, Yamin Zhou, Liping Zhang, Gang Shi
Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.
Abstract: The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21).
Abstract: Plant phenols, in particular, plant phenolic acids, like rosmarinic acid, ellagic acid, and chlorogenic acid, are used in the treatment or prevention of eosinophilic esophagitis.
Abstract: The present invention provides compositions or formulations comprising the combination of a compound of 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione or a salt thereof or hydrate of the foregoing, and a cyclodextrin; or in further combination with an excipient comprising L-Arginine or other additives, wherein the compositions or formulations increases water solubility and oral bioavailability of 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and its related compounds. The method of making or using the compositions or formulations is also disclosed. Such compositions or formulations may be used in treatment of certain diseases including asthma through inhibition of matrix metalloproteinase-12.
Abstract: Extracts or beverages whose ratio between the content of 2,5-piperazinedione,3,6-bis(phenylmethyl)-,(3S,6S)-(unit: ?g/100 g) and Brix (Bx) is 6 (?g/100 g)/Bx or more are good in flavor and feeling on the tongue and further have a good appearance.
Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
Type:
Grant
Filed:
June 17, 2016
Date of Patent:
January 7, 2020
Assignee:
Hadasit Medical Research Services and Development Ltd.
Inventors:
Itzhak E. Lerner, Moshe Flashner-Barak, Erwin v Achthoven, Hans Keegstra, Ruud Smit
Abstract: Embodiments disclosed herein generally relate to methods of treating posttraumatic stress disorder (PTSD) using acamprosate formulations and/or acamprosate formulations in combination with at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
Type:
Grant
Filed:
July 15, 2016
Date of Patent:
December 24, 2019
Assignee:
Synchroneuron, Inc.
Inventors:
Barry S. Fogel, William D. Kerns, Kei-Lai Fong
Abstract: The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
Abstract: Plant phenols, in particular, plant phenolic acids, like rosmarinic acid, ellagic acid, and chlorogenic acid, are used in preventing or reducing transepidermal water loss (TEWL) and associated disorders and diseases.
Abstract: What is disclosed is a semi-solid controlled release pharmaceutical composition containing biocompatible and bioerodible semi-solid lipid matrix incorporating local anesthetics agents to form a semi-solid solution, a method of using the pharmaceutical composition to treat, and a method of making the pharmaceutical composition.
Abstract: An agrochemical composition contains a component (A): a compound represented by formula (I) (wherein, R1, R2, R3a, R3b, R4a, R4b, and R5 each independently represents an unsubstituted or substituted C1-6 alkyl group or the like, n represents an integer of 0 to 4, o and p each independently represents an integer of 2 to 4, and X represents a carbon atom or a nitrogen atom) or a salt thereof, and a component (B): a hydrolysis inhibitor.
Abstract: The present invention relates to novel 4-pregenen-11?-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.
Type:
Grant
Filed:
August 4, 2016
Date of Patent:
December 3, 2019
Assignee:
ALLERGAN, INC.
Inventors:
Jeffrey L. Edelman, Alissar Nehme, Thomas C. Malone
Abstract: A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising a pharmacologically active ingredient (A), a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.
Type:
Grant
Filed:
February 21, 2018
Date of Patent:
December 3, 2019
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Sebastian Schwier, Ulrike Bertram, Anja Geissler, Kornelia Griessmann, Johannes Bartholomäus
Abstract: Compositions involving a modified egg yolk extract for use as an effective anti-cancer agent are described. The modified egg yolk extract involves specific fractions of phosphatidylcholines and sphingomyelins modified and produced from a chemical synthesis applied to the extract that produce a beneficial effect on the inhibition of cancerous cell growth. Methods of administering these compositions are also described.
Type:
Grant
Filed:
June 29, 2017
Date of Patent:
December 3, 2019
Assignee:
MACHAVERT PHARMACEUTICALS LLC
Inventors:
Jakub Staszak-Jirkovsky, Lukas Kobr, Gregory F. Miknis, Colleen Hudson, Luca Monfregola, Pavel Jirkovsky, Zbon{hacek over (c)}áková Milada, Jason Duex, Pitchaimani Kandasamy
Abstract: Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
Type:
Grant
Filed:
September 6, 2018
Date of Patent:
December 3, 2019
Assignee:
AMGEN INC.
Inventors:
Sean P. Brown, Mike Elias Lizarzaburu, Nick A. Paras, Joshua Taygerly, Marc Vimolratana, Xianghong Wang
Abstract: The present invention provides a pharmaceutical composition for preventing or treating macular degeneration, which comprises benzopyran derivatives substituted with secondary amines including imidazole or pharmaceutically acceptable salts thereof as an active ingredient. The pharmaceutical composition of the present invention may be used in the form of eye drops.
Type:
Grant
Filed:
March 30, 2018
Date of Patent:
November 26, 2019
Assignee:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Kyu-Yang Yi, Sung-Eun Yoo, Nack-Jeong Kim, Jee-Hee Suh, Choun-Ki Joo, Jun-Sub Choi, Jae-Sik Yang, Geun-Hyeog Lee, Yun-Seok Cho, Jin-Ha Park, Hye-Sung Lee
Abstract: It was found that finafloxacin eradicates pathogens from patients suffering from bacterial infections like urinary tract infections and pyelonephritis more quickly than other fluoroquinolones regularly used for the treatment of these patients. Due to the efficacy of finafloxacin reduced treatment durations without increasing the daily dosage of finafloxacin and at the same time no or shorter stays in hospital are realizable, thus improving patient convenience and significantly lowering the costs of hospitalization and treatment. Reduced hospitalization periods do also clearly reduce the risk of nosocomial infections and of generating drug-resistant strains through extended therapy. The inventive treatment regimens comprise an oral finafloxacin administration for 1-5 days or a parenteral finafloxacin administration for 1-5 days for use in the treatment of a complicated urinary tract infection or pyelonephritis. However, a prior short parenteral administration of finafloxacin (e.g.
Type:
Grant
Filed:
November 10, 2015
Date of Patent:
November 26, 2019
Assignee:
MerLion Pharmaceuticals Pte. Ltd.
Inventors:
Christine Bentley, Carsten Fischer, Mark Lückermann, Andreas Vente, Sven-Eric Wohlert