Abstract: Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
Abstract: The invention relates to a morphinan-derivative that targets NMDA receptors on pancreatic islets and has the general formula (I) wherein R1 is selected from —OH, —CO2H, —R0, —OR0, —OC(?O)R0, —OC(?O)OR0 or —OC(?O)NHR0; and R2 is selected from —H, —R0, —C(?O)R0, —C(?O)OR0, —C(?O)NHR0 or —C(?NH)—NH—C(?NH)—NH2; wherein R0 is in each case independently selected from —C1-C6-alkyl, -aryl, -heteroaryl, —C1-C6-alkyl-aryl or —C1-C6-alkyl-heteroaryl, in each case independently unsubstituted or substituted; or its physiologically acceptable salt and/or stereoisomer, including mixtures thereof in all ratios, for use in the treatment of a disease or condition, where the disease or condition is insulin-dependent diabetes mellitus, non-insulin-dependent diabetes mellitus, obesity, and/or diabetic nephropathy.
Type:
Grant
Filed:
August 22, 2012
Date of Patent:
June 21, 2016
Inventors:
Eckhard Lammert, Jan Marquard, Thomas Meissner
Abstract: A method of making an anti-Markovnikov addition product is carried out by reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product; the dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst. Compositions useful for carrying out such methods are also described.
Type:
Grant
Filed:
May 6, 2013
Date of Patent:
June 14, 2016
Assignee:
The University of North Carolina at Chapel Hill
Inventors:
David A. Nicewicz, David S. Hamilton, Andrew J. Perkowski
Abstract: A method for producing glycolide provided with: step (1) wherein a GAO composition, which preferably contains a high-boiling-point organic solvent or a solubilizing agent, is supplied into a reactor and heated to a temperature at which a depolymerization reaction of the GAO occurs; step (2) wherein the heating is continued to subject the GAO to the depolymerization reaction, thereby producing glycolide; step (3) wherein glycolide is distilled out of the reactor; step (4) wherein the distillate is introduced into a rectifier and is rectified by means of gas-liquid countercurrent contact; and step (5) wherein glycolide is recovered.
Abstract: A novel coumarin derivative or a pharmaceutically acceptable salt thereof and also to provide a pharmaceutical agent containing such a compound as an active ingredient is provided. The coumarin derivative or a pharmaceutically acceptable salt thereof exhibits an excellent suppressive action to the destruction of cartilage and suppressive action to the proliferation of synovial cells in a pharmacological test where the release of sulfated glycosaminoglycans (sGAG) and the proliferation of synovial cells are used as indicators whereby it is very useful as an active ingredient of a pharmaceutical composition such as a preventive or therapeutic agent for arthropathy such as osteoarthritis or chronic rheumatoid arthritis.
Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
Type:
Grant
Filed:
July 13, 2015
Date of Patent:
June 14, 2016
Assignee:
Life Technologies Corporation
Inventors:
Jolene Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick Pinson, Stephen Yue
Abstract: The present invention relates to arylated camphenes, processes for their preparation and uses thereof for the manufacture of medicaments for the treatment of diseases, disorders or conditions associated with, or benefiting from stimulation of CB2 receptors.
Type:
Grant
Filed:
March 31, 2014
Date of Patent:
June 14, 2016
Assignee:
YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
Inventors:
Raphael Mechoulam, Lital Magid, Esther Shohami, Itai Bab
Abstract: The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a Monascus fermented product with acetone for three times; elevating the concentration of the Monascus fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the Monascus fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially.
Abstract: Provided herein is technology relating to deuterated amiexanox and particularly, but not exclusively, to compositions comprising deuterated amiexanox, methods of producing deuterated amiexanox, and uses of deuterated amiexanox. Provided herein are deuteratecl amiexanox compounds for the treatment of obesity, insulin resistance, diabetes, and steatosis. In addition, the deuterated compounds are anti-inflammatory antiallergic immunomodulators. e.g., for the treatment of diseases associated with inflammation. The deuterium kinetic isotope effect associated with placing deuterium at the site of metabolic derivatization slows metabolic derivatization and thus increases the lifetime of the active drug in vivo.
Type:
Grant
Filed:
May 2, 2014
Date of Patent:
June 14, 2016
Assignee:
THE REGENTS OF THE UNIVERSITY OF MICHIGAN
Inventors:
Alan R. Saltiel, Hollis D. Showalter, Scott Larsen
Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
Type:
Grant
Filed:
October 20, 2014
Date of Patent:
June 7, 2016
Assignee:
Ligand Pharmaceuticals Incorporated
Inventors:
Lin Zhi, Robert I. Higuchi, Cornelis Arjan Van Oeveren, Thomas Lot Stevens Lau
Abstract: The present invention discloses a composition for lowering blood lipid and elevating high-density lipoprotein and a method for manufacturing the same; the composition comprises monascin or ankaflavin, or a combination thereof; the manufacturing method comprises the steps of: treating a Monascus fermented product with acetone for three times; elevating the concentration of the Monascus fermented product by a process of decompress concentration; and extracting the monascin and the ankaflavin from the Monascus fermented product with a silica gel column chromatography, a Sephadex LH-20 column chromatography, the silica gel column chromatography, and a preparative high performance liquid chromatography sequentially.
Abstract: The present disclosure is directed to generally methods for treating mammographic breast density and/or breast stiffness in a patient in need thereof, such as a premenopausal or perimenopausal patient, comprising the administration of an effective amount of androgenic agent and an effective amount of an aromatase inhibitor. These methods may also be useful in post-menopausal woman.
Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
Type:
Grant
Filed:
July 24, 2015
Date of Patent:
May 31, 2016
Assignee:
Galapagos NV
Inventors:
Steven Emiel Van Der Plas, Hans Kelgtermans, Sébastien Jean Jacques Cédric Dropsit Montovert, Sébastien Laurent Xavier Martina, Martin James Inglis Andrews
Abstract: The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.
Type:
Grant
Filed:
September 6, 2013
Date of Patent:
May 31, 2016
Assignee:
Council of Scientific and Industrial Research
Abstract: The present invention relates to a novel coumarin derivative, to a method for preparing the same, and a multi-fluorescent substance that includes a plurality of the coumarin derivatives and is able to emit light using an LED light source. A novel coumarin derivative multi-fluorescent substance according to the present invention has an optimal emission wavelength band of 512 nm to 590 nm and thereby is effective in improving a signal intensity and stability since light emission using an LED light source is possible. In addition, higher fluorescence reactivity is exhibited compared to coumarin fluorescent substances known in the related arts since one molecule has a plurality of fluorescent substances, and the problem of the coumarin fluorescent substance possibly binding to a binding site of the antigen of the antibody is solved since fluorescence detection is possible even when a minimum number of fluorescent substance molecules bind to an antibody.
Type:
Grant
Filed:
March 5, 2012
Date of Patent:
May 31, 2016
Assignee:
GENBODY INC.
Inventors:
Hyun Park, Hak Sung Kim, Hyun Ok Song, Chom Kyu Chong, Sung Yeon Kim
Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.
Abstract: The art relates to provision of a method for manufacturing an (meth)acrylic polymerizable monomer that can be used in various applications, such as an optical material, a resist material, a coating material and a laminate material, and provision of a new ?-(meth)acryloyloxy-?-butyrolactone compound by applying the manufacturing method. The method for manufacturing the ?-(meth)acryloyloxy-?-butyrolactone compound is described, in which a (meth)acrylate compound having a carbonyl group and a ketene compound are condensed and isomerized. Further, the manufacturing method is applied to the new ?-(meth)acryloyloxy-?-butyrolactone compound.
Abstract: Non-domesticated mammalian animals are sedated and immobilized by injecting an effective amount of pharmaceutically effective combination of nalbuphine hydrochloride and medetomidine hydrochloride into the animal from a dart. Azaperone tartrate may also be included, if desired.
Type:
Grant
Filed:
March 11, 2015
Date of Patent:
May 17, 2016
Assignee:
Wildlife Laboratories, Inc.
Inventors:
Lisa L. Wolfe, Michael W. Miller, William R. Lance, David K. Smith
Abstract: The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
Abstract: This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma.