Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.
Abstract: The disclosure relates to methods of managing blood sugar levels and compositions related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diabetes, insulin resistance, or hyperglycemia comprising administering to a subject diagnosed with, at risk of or exhibiting symptoms of diabetes, insulin resistance, or hyperglycemia a pharmaceutical composition comprising a compound comprising formula I.
Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion in human blood plasma to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt, Cu(II) ion in the presence of a reducing agent, or copper metal.
Type:
Grant
Filed:
October 7, 2014
Date of Patent:
May 26, 2015
Assignee:
The Scripps Research Institute
Inventors:
K. Barry Sharpless, Valery Fokin, Vsevold A. Rostovtsev, Luke Green, Fahmi Himo
Abstract: The present invention relates to a covalently organo-modified LDH (LDH/APTES) was found to be an efficient and reusable heterogeneous catalyst for C—C bond forming reactions (i.e. Aldol condensation, Knoevenagel condensation, Henry reaction, Michael addition). More particularly, this catalyst shows consistent activity for several cycles in C—C bond forming reaction. These catalysts were successfully characterized by XRD, FT-IR, 29Si CP MAS NMR.
Type:
Grant
Filed:
February 14, 2012
Date of Patent:
May 19, 2015
Assignee:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
Type:
Grant
Filed:
March 13, 2014
Date of Patent:
May 12, 2015
Assignee:
Dow AgroSciences LLC
Inventors:
Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew L. Ward, Thomas C. Sparks
Abstract: Provided is an amide ester that is useful as an intermediate manufacturing product for an aroma compound such as spilanthol or the like. Also provided is a spilanthol manufacturing method using said amide ester. High-purity spilanthol can be manufactured by reacting an amide ester represented by general formula (1) with a basic compound. (In the formula, R1 represents a C1-6 alkyl group or a phenyl group that may be substituted with a C1-4 alkyl group, a C1-4 alkoxy group, or a halogen atom; R2 represents a C1-8 hydrocarbon group; and the wavy lines represent cis configurations, trans configurations, or a mixture of the two configurations.
Type:
Grant
Filed:
July 14, 2010
Date of Patent:
May 12, 2015
Assignee:
Takasago International Corporation
Inventors:
Shigeru Tanaka, Kenya Ishida, Kenji Yagi, Hideo Ujihara
Abstract: A method for cultivating Monarda fistulosaincludes planting seeds at rates between about 2.5 and about 5 pounds per acre, preferably about 4 pounds per acre. Fuel costs are reduced because seeding, mowing the first season, and harvesting in seasons thereafter are all that is required. Reduction in herbicide use results from the heavy rate of planting, improved germination attributed to rolling, and the plant's natural herbicides which are more highly effective when seeded at the higher rate. The method includes seeding, mowing during a first growing season, and harvesting each season thereafter. This method results in oil without weed contamination and carvacrol levels are high.
Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
Type:
Grant
Filed:
November 11, 2010
Date of Patent:
May 5, 2015
Assignee:
Merial, Inc.
Inventors:
Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
Abstract: The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus BANI can be used to produce radiotracers retained in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.
Type:
Grant
Filed:
July 22, 2013
Date of Patent:
May 5, 2015
Assignee:
Atomic Energy Council—Institute of Nuclear Energy Research
Abstract: Use of transition metal complexes of the formula (I) in organic light-emitting diodes where: M1 is a metal atom; carbene is a carbene ligand; L is a monoanionic or dianionic ligand; K is an uncharged monodentate or bidentate ligand selected from the group consisting of phosphines; CO; pyridines; nitriles and conjugated dienes which form a ? complex with M1; n is the number of carbene ligands and is at least 1; m is the number of ligands L, where m can be 0 or ?1; o is the number of ligands K, where o can be 0 or ?1; where the sum n+m+o is dependent on the oxidation state and coordination number of the metal atom and on the denticity of the ligands carbene, L and K and also on the charge on the ligands carbene and L, with the proviso that n is at least 1, and also an OLED comprising these transition metal complexes, a light-emitting layer comprising these transition metal complexes, OLEDs comprising this light-emitting layer, devices comprising an OLED according to the present invention, and specific t
Type:
Grant
Filed:
November 13, 2014
Date of Patent:
May 5, 2015
Assignee:
BASF SE
Inventors:
Markus Bold, Christian Lennartz, Martina Egen, Hans-Werner Schmidt, Mukundan Thelakkat, Markus Baete, Christian Neuber, Wolfgang Kowalsky, Christian Schildknecht, Hans-Hermann Johannes
Abstract: This invention relates to a metathesis catalyst compound comprising an asymmetrically substituted N-heterocyclic carbene (NHC) metathesis catalyst and a process to make linear alpha-olefins comprising contacting a feed material and an optional alkene (such as ethylene) with said catalyst, where the feed material is a triacylglyceride, fatty acid, fatty acid alkyl ester, and/or fatty acid ester, typically derived from biodiesel.
Type:
Grant
Filed:
November 3, 2010
Date of Patent:
May 5, 2015
Assignee:
ExxonMobil Chemical Patents Inc.
Inventors:
Matthew W. Holtcamp, Matthew S. Bedoya, Catherine A. Faler, Caol P. Huff, John R. Hagadorn, Ravindra Ganesh
Abstract: [Problem]To provide a novel polymer derivative of a cytidine metabolic antagonist which allows release of a medicament irrespective of enzymes of the living body and is expected to have high therapeutic effects.
Type:
Grant
Filed:
November 16, 2011
Date of Patent:
April 28, 2015
Assignee:
Nippon Kayaku Kabushiki Kaisha
Inventors:
Keiichirou Yamamoto, Manami Okazaki, Dai Kawamura
Abstract: The present application relates to novel substituted 1-benzylcycloalkylcarboxylic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
Type:
Grant
Filed:
December 6, 2011
Date of Patent:
April 28, 2015
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Thomas Lampe, Michael G. Hahn, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Sherif El Sheikh, Volkhart Min-Jian Li, Eva-Maria Becker, Friederike Stoll, Andŕeas Knorr, Peter Kolkhof, Elisabeth Woltering
Abstract: Metal imidazolate complexes are described where imidazoles ligands functionalized with bulky groups and their anionic counterpart, i.e., imidazolates are described. Compounds comprising one or more such polyalkylated imidazolate anions coordinated to a metal or more than one metal, selected from the group consisting of alkali metals, transition metals, lanthanide metals, actinide metals, main group metals, including the chalcogenides, are contemplated. Alternatively, multiple different imidazole anions, in addition to other different anions, can be coordinated to metals to make new complexes. The synthesis of novel compounds and their use to form thin metal containing films is also contemplated.
Type:
Grant
Filed:
June 3, 2011
Date of Patent:
April 28, 2015
Assignee:
Air Products and Chemicals, Inc.
Inventors:
John Anthony Thomas Norman, Melanie K. Perez, Xinjian Lei, Daniel P. Spence, Sergei Vladimirovich Ivanov, Wade Hampton Bailey, III
Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
Type:
Grant
Filed:
February 2, 2012
Date of Patent:
April 28, 2015
Assignee:
National University Corporation Nagoya University
Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
Type:
Grant
Filed:
May 23, 2011
Date of Patent:
April 28, 2015
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Stefan Scheuerer
Abstract: A compound having formula (I): wherein: R, A, R1 and R2, are as defined in the specification, and pharmaceutical formulas thereof, and methods of use thereof, as Kinase inhibitors.
Type:
Grant
Filed:
March 2, 2007
Date of Patent:
April 21, 2015
Assignee:
Nerviano Medical Sciences S.r.l.
Inventors:
Tiziano Bandiera, Jay Aaron Bertrand, Paolo Pevarello, Ettore Perrone, Andrea Lombardi Borgia, Sten Christian Orrenius, Mauro Angiolini, Daniele Fancelli
Abstract: A process for preparing an ester of formula (I): R3CH2—(CR1R2)n—CH2—O—CO—(CR1R2)n—CH2R3??(I) wherein n is 1-3 and R1 and R2 are each, independently, a hydrogen atom or a carbon-linked organic group and R3 is a carbon-linked organic group, is provided by hydrogenation of a certain lactone, carboxylic acid or its ester reactant.
Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Type:
Grant
Filed:
December 16, 2010
Date of Patent:
April 14, 2015
Assignee:
AbbVie Inc.
Inventors:
Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
Abstract: Provided is a two-photon fluorescent probe, and more particularly, a two-photon fluorescent probe which is one or more selected from compounds represented by Formulae 1 and 2, a method for manufacturing the same, and an imaging method of zinc ions within the mitochondrion using the same. Since two probes are introduced into one molecule, the two-photon fluorescent probe of the present invention can selectively dye the mitochondria, simultaneously with reacting with zinc ions, thereby generating intense fluorescence. Thus, the two-photon fluorescent probe of the present invention can be used for the imaging of zinc ion distribution and activation within the mitochondrion in living cells or intact biological tissues.
Type:
Grant
Filed:
October 18, 2011
Date of Patent:
April 14, 2015
Assignee:
AJOU University Industry-Academic Cooperation Foundation