Abstract: The present invention relates to a two-photon fluorescent probe, more particularly a two-photon fluorescent probe represented by Formula 1, a method for preparing same and a method for imaging thiols in mitochondria using same. The two-photon fluorescent probe according to the present invention, having two probes introduced in one molecule, can selectively dye mitochondria and emit intense fluorescence by reacting with thiols. Accordingly, it can be used to image the distribution and activation of thiols in a living cell or an intact living tissue.
Type:
Grant
Filed:
October 17, 2011
Date of Patent:
April 14, 2015
Assignee:
Ajou University Industry-Academic Cooperation Foundation
Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
Type:
Grant
Filed:
September 23, 2011
Date of Patent:
April 14, 2015
Assignee:
AbbVie Deutschland GmbH & Co. KG
Inventors:
Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
Abstract: The present invention provides a convenient and industrially viable process for preparation of Zolmitriptan (I) having desired purity. The invention specifically relates to a method for isolating (S)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one hydrochloride (IIIa) of desired purity by separating the undesired inorganic side products such as stannous hydroxide by manipulation of pH at different stages and finally treating with N,N-dimethylamino butyraldehyde diethyl acetal in an acidic medium to provide Zolmitriptan (I) conforming to regulatory specifications.
Abstract: Provided herein are compounds, preparations and formulations comprising pyrazine derivatives having multiple poly(ethylene glycol) containing substituents. Many of the compounds disclosed herein are excretable by the renal system of a subject or patient and are useful for visualizing the renal system of a subject or patient. Upon excitation by electromagnetic radiation, a number of the compounds disclosed herein exhibit luminescence and are externally detectable when present in the body fluid of a patient or subject. Also provided herein are methods for visualizing the renal system of a subject or patient.
Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
November 4, 2013
Date of Patent:
April 7, 2015
Assignee:
Allergan, Inc.
Inventors:
Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
Type:
Grant
Filed:
July 2, 2014
Date of Patent:
March 31, 2015
Assignee:
Incyte Corporation
Inventors:
Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
Abstract: The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. The invention also relates to cosmetic or dermocosmetic compositions intended to fight skin disorders associated with said glycosylation by-products.
Abstract: The present invention relates to a process for the separation of vinyl acetate from a gas mixture formed by the reaction of ethylene with acetic acid and oxygen in the gas phase over catalysts comprising palladium or palladium compounds.
Type:
Grant
Filed:
November 28, 2009
Date of Patent:
March 31, 2015
Assignee:
Celanese International Corporation
Inventors:
Bernd Rinne, Stefan Hess, Ali Hotaman, Michael J. Bayer, Berthold Nuber
Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
Type:
Grant
Filed:
December 10, 2013
Date of Patent:
March 31, 2015
Assignee:
Allergan, Inc.
Inventors:
Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
Abstract: The present invention refers to the synthesis of precatalysts and the use of such precatalysts in ethylene oligomerization reactions for the selective production of alpha-olefins. More specifically, it refers to the preparation and use of coordination compounds containing polydentate ligands comprising Group 6 and 10 transition metal compounds, in particular chromium (III) and nickel (II). Such catalytic precursors present high catalytic activity and selectivity for the production of alpha-olefins.
Type:
Grant
Filed:
September 30, 2011
Date of Patent:
March 31, 2015
Assignees:
Petroleo Brasileiro S.A.—Petrobras, Universidade Federal do Rio Grande do Sul-UFRGS
Inventors:
Osvaldo de Lazaro Casagrande Junior, Carlos Rene Klotz Rabello, Lucilene Losch de Oliveira, Ana Helena Dias Pereira dos Santos, Roberta Campedelli, Adao Lauro Bergamo
Abstract: A process for preparing cycloaliphatic amines by hydrogenating the corresponding aromatic compounds with hydrogen-comprising gas at a temperature of from 30 to 280° C. and a pressure of 50-350 bar, in the presence of ruthenium catalysts. The hydrogenation is performed in the presence of from 1% by weight to 500% by weight, based on the catalyst calculated as elemental ruthenium (Ru), of suspended inorganic additives, and to the use of the cycloaliphatic amines as a synthesis unit.
Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
Type:
Grant
Filed:
September 29, 2009
Date of Patent:
March 24, 2015
Inventors:
Christopher Oalmann, Robert B. Perni, Chi B. Vu
Abstract: The invention provides a silicon-containing bianthracene derivative, a production process and use thereof, and an organic electroluminescent device. The invention belongs to the technical field of organic electroluminescence, and can give a blue light-emitting material being able to form a dense film. The silicon-containing bianthracene derivative has a molecular structure of the following general formula, wherein R group represents an aryl group having a carbon atom number of 6-14, an aromatic heterocyclic group having a carbon atom number of 8-18, a fused-ring aromatic group having a carbon atom number of 9-15, a fluorenyl group, or a triarylamino group. The silicon-containing bianthracene derivative mentioned in the invention can be used in an organic electroluminescent device.
Type:
Grant
Filed:
January 27, 2014
Date of Patent:
March 24, 2015
Assignees:
BOE Technology Group Co., Ltd., JiLin OLED Material Tech. Co., Ltd.
Inventors:
Yinan Liang, Xiaoyu Ma, Hui Wang, Wenyu Ma
Abstract: A radioisotope labeled reagent includes a compound having the general formula (I), L-(aCbH2)naCbH3??(I) where a in each occurrence independently is a carbon mass number between 11 and 14 inclusive, b in each occurrence independently is a hydrogen mass number between 1 and 3 inclusive, such that a in each occurrence is not 12 simultaneously with b in each occurrence being 1; L is a leaving group R1SO2—O—, R1—S—, 12C1H3(12C3H2)n—S—R1C(O)O—, NC—, (R1)3P—, XMg- and Li—, where n is an integer between 0 and 3 inclusive, where X is chloro, bromo or iodine, where R1 is H, aryl, a substituent containing aryl, C1-C20 alkyl, a substituent containing C1-C20 alkyl, C2-C20 alkenyl, a substitute containing C2-C20 alkenyl, C2-C20 alkynyl, and a substitute containing C2-C20 alkynyl with the proviso that when n is 0, a is 13 and b is 2 and R1 in R1—S is not aryl.
Abstract: The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).
Abstract: A process for the manufacture of a cyclic compound of formula (I) which comprises (a) adding an acid halide of formula R1—C (O)—X, to a vinyl ether of formula (II): CH2?CH—OR2, to produce an addition product, and (b) reacting the addition product with a compound of formula (III): Y-A-Z; wherein R1 is a halogenated alkyl group; wherein X is fluorine, chlorine, or bromine; wherein R2 is an alkyl group, an aralkyl group, or an aryl group; wherein Z and Y designate independently carbon or a heteroatom; and wherein A is a linking group between Z and Y comprising 0, 1, 2 or 3 atoms in the cycle.
Abstract: The present invention provides a novel ligand represented by the following formula and a novel transition metal complex having the ligand, which shows superior enantioselectivity and catalytic efficiency, particularly high catalyst activity, in various asymmetric synthesis reactions. A transition metal complex having, as a ligand, a compound represented by the formula wherein R4 is a hydrogen atom or a C1-6 alkyl group optionally having substituent(s), and R5 and R6 are each a C1-6 alkyl group optionally having substituent(s), or the formula is a group represented by the formula wherein ring B is a 3- to 8-membered ring optionally having substituent(s).
Abstract: The invention relates to the platinum N-heterocycle derivatives of general formula (I) in which—R1 and/or R2 are, independently of one another, an aryl or aralkyl group, each optionally substituted, a linear or branched C1-C6 alkyl group, a monocyclic C3-C7 cycloalkyl group or a linear or branched C2-C6 alkenyl group, or else R? is a hydrogen atom and R is a group selected from the following groups: cycloalkyl or heterocycloalkyl, which is monocyclic or bicyclic and has from 3 to 8 carbon atoms, or benzyl, which is optionally substituted, or else R and R? form, together with NH, a C3-C8 monocyclic or bicyclic heterocycloalkyl, V is a nitrogen atom or a C—R4 radical, R3 and/or R4 are hydrogen or a phenyl group or R3 and R4 may also together form a C3-C6 alkylene radical or a C3-C6 heteroalkylene radical with one or more nitrogenous heteroatoms, it being possible for the carbon atoms of the heteroalkylene radical to be modified in the form of a carbonyl radical, and X is iodine, bromine, chlorine or a nitra
Type:
Grant
Filed:
June 21, 2013
Date of Patent:
March 17, 2015
Assignee:
Centre National de la Recherche Scientifique
Inventors:
Patrick Mailliet, Angela Marinetti, Myriem Skander
Abstract: This invention relates to a method of preparing a radioisotope nanostructure having a ligand-metal framework, and a radioisotope nanostructure prepared thereby. The method of preparing the radioisotope nanostructure of the invention has a simple preparation process and can thus be applied to mass production of a radioisotope nanostructure. Also, because this radioisotope nanostructure is nano-sized spherical particles and has no reactive group, it can be easily dispersed in a fluid, and this nanostructure is physically and chemically stable and thus can be utilized as a radioisotope tracer in the fields of refineries, chemistry, cement, agriculture, water resources, marine, etc. Furthermore, this nanostructure can be used for diagnosis and/or treatment in medical fields, and can be applied to checking whether a nanomaterial is harmful. In addition, this nanostructure is expected to be applicable in a variety of fields using radioisotopes.
Type:
Grant
Filed:
December 13, 2012
Date of Patent:
March 10, 2015
Assignee:
Korea Atomic Energy Research Institute
Inventors:
Sung Hee Jung, Seong-Ho Choi, Jong Bum Kim, Jin Ho Moon, Min Seok Oh