Abstract: The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
Abstract: The present disclosure provides conjugate structures and hydrazinyl-pyrrolo compound structures used to produce these conjugates. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
Type:
Grant
Filed:
November 26, 2014
Date of Patent:
November 15, 2016
Assignee:
Redwood Bioscience, Inc.
Inventors:
David Rabuka, Aaron Edward Albers, Romas Alvydas Kudirka, Albert W. Garofalo
Abstract: Compounds of formula (I) are useful for inhibiting a proteasome in a cell. Compounds, pharmaceutical compositions and methods of use are provided herein.
Type:
Grant
Filed:
April 7, 2015
Date of Patent:
November 15, 2016
Assignee:
University of Kentucky Research Foundation
Inventors:
Kyung-Bo Kim, Vinod Kasam, Wooin Lee, Dong-Eun Kim, Zach Miller, Chang-Guo Zhan, Do-Min Lee
Abstract: The invention provides compounds having the general formula (I): and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
November 15, 2016
Assignees:
GENENTECH, INC., XENON PHARMACEUTICALS INC.
Inventors:
Chien-An Chen, Sultan Chowdhury, Christoph Martin Dehnhardt, Shaoyi Sun
Abstract: The present invention relate to compounds of general formula A. The invention also provides the synthesis of 3,4,5-trimethoxystyrylarylaminopropenones useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof. wherein: R=H, OMe, Cl, F, OH, Me X=aryl, heteroaryl.
Type:
Grant
Filed:
April 17, 2015
Date of Patent:
November 8, 2016
Assignee:
Council of Scientific and Industrial Research
Abstract: The invention relates inter alia to halogen-substituted compounds of the general formula (I) in which the radicals A1-A4, T, n, W, Q, R1 and Z1-Z3 have the meanings given in the description. Also described are processes for preparing the compounds of the formula (I) and possible intermediates for the preparation of these compounds. The compounds according to the invention are particularly suitable for controlling insects, arachnids and nematodes in agriculture and ectoparasites in veterinary medicine.
Type:
Grant
Filed:
February 3, 2014
Date of Patent:
November 8, 2016
Assignee:
BAYER CROPSCIENCE AKTIENGESELLSCHAFT
Inventors:
Michael Maue, Kerstin Ilg, Anne Decor, Thomas Bretschneider, Julia Johanna Hahn, Werner Hallenbach, Reiner Fischer, Hans-Georg Schwarz, Ulrich Goergens, Klaus Raming, Johannes Koebberling, Walter Huebsch, Andreas Turberg, Niels Lindner
Abstract: The invention is directed to a compound of formula I, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula I, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria.
Type:
Grant
Filed:
October 21, 2015
Date of Patent:
October 25, 2016
Assignee:
MediSynergics, LLC
Inventors:
Dennis Michael Godek, Harry Ralph Howard
Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
Type:
Grant
Filed:
October 22, 2012
Date of Patent:
October 18, 2016
Assignee:
Oryzon Genomics S.A.
Inventors:
Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, María de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
February 13, 2013
Date of Patent:
October 11, 2016
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
Abstract: A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: the process comprising the reaction of a carbamate of Formula (II?): Formula (I?): with a primary or secondary amine of the formula R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
Type:
Grant
Filed:
July 28, 2011
Date of Patent:
October 4, 2016
Assignee:
BIAL—PORTELA & CA, S.A.
Inventors:
David Alexander Learmonth, Brian Broadbelt, Jorge Bruno Reis Wahnon
Abstract: The invention relates to the field of chemical and pharmaceutical industry and medicine and concerns compounds which can be used to produce agents for the treatment of cardiovascular diseases. The use of 2-[2-cyano-2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]ethylidene]indolin-3-one of formula I is proposed as a biologically active compound exhibiting the properties of exogenous nitric oxide donor, a platelet aggregation inhibitor, also exhibiting antihypertensive activity and activating activity towards the soluble guanylate cyclase enzyme. Variants of methods for synthesizing the above compound are also proposed.
Abstract: A method of preparing acrolein from glycerol or glycerine is disclosed. The method includes dehydrating glycerol or glycerine in the presence of a catalyst consisting of at least (a) a mixed oxide of zirconium and at least one metal, said metal being selected from niobium, tantalum and vanadium, or (b) a zirconium oxide and at least one metal oxide, the metal being selected from niobium, tantalum and vanadium, or (c) a silicon oxide and a mixed oxide of zirconium and at least one metal, the metal being selected from tungsten, cerium, manganese, niobium, tantalum, titanium, vanadium and silicon, or (d) a titanium oxide and a mixed oxide of zirconium and at least one metal, said metal being selected from tungsten, cerium, manganese, niobium, tantalum, titanium, vanadium and silicon.
Type:
Grant
Filed:
August 27, 2013
Date of Patent:
September 20, 2016
Assignees:
ADISSEO FRANCE S.A.S., CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
Abstract: Novel compounds below are useful for preventing or treating diseases caused by protozoans. At least one of a compound represented by Formula (I) (wherein, X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents —CHO, —C(?O)R5, —COOR5 (wherein R5 represents a C1-7 alkyl group), —CH2OH or —COOH; and R4 represents a C1-16 alkyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), a C2-16 alkenyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s), or a C2-16 alkynyl group having one or more substituents on a terminal carbon atom and/or non-terminal carbon atom(s)), an optical isomer thereof, and a pharmaceutically acceptable salt is used.
Abstract: A method of manufacture of the primary explosive material copper(I) 5-nitrotetazolate (DBX-1) by a synthesis starting with 5-aminotetrazolate (5-AT); wherein, the synthesis provides intermediates acid copper salt of 5-NT and sodium 5-nitrotetrazolate (NaNT) sodium 5-nitrotetrazolate (NaNT)—that are both, free of any 5-aminotetrazolate (5-AT) starting material—such that the subsequent production of the DBX-1 is not inhibited. Further, this method utilizes an internal filter within the reactor—to minimize handling of explosively dangerous intermediates.
Type:
Grant
Filed:
February 23, 2015
Date of Patent:
September 13, 2016
Assignee:
The United States of America as Represented by the Secretary of the Army
Inventors:
Neha Mehta, Karl Oyler, Gartung Cheng, Jerry Salan, Shannon Lenahan
Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
Type:
Grant
Filed:
December 19, 2014
Date of Patent:
September 6, 2016
Assignee:
Supernus Pharmaceuticals, Inc.
Inventors:
Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
Abstract: A platinum/carbon nanotube catalyst applicable to heterogeneous asymmetric hydrogenation, which is fabricated by supporting platinum on carbon nanotube carriers, and prepared by the steps of: heating purified carbon nanotubes in nitric acid, filtering and washing the same with water until pH value of the filtrate becomes neutral, drying the carbon nanotubes; immersing the carbon nanotube carriers obtained in an aqueous chloroplatinic acid solution and carrying out ultrasonic treatment at room temperature; immersing the mixture of the carbon nanotubes and the aqueous chloroplatinic acid solution under stirring; drying the material by heating to 110° C. from room temperature and maintaining this temperature; grinding the product to fine powders, reducing the fine powders with an aqueous sodium formate solution under a heating condition, filtering and washing the product with deionized water, and drying the product.
Type:
Grant
Filed:
March 30, 2015
Date of Patent:
September 6, 2016
Assignee:
DALIAN INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES
Abstract: Provided is a multi-arm polyethylene glycol derivative having a narrow molecular weight distribution. A multi-arm polyethylene glycol derivative represented by the formula (1): m[Z—YnCH2CH2OX—O-L-O—XOCH2CH2nY—Z]m??(1) wherein, L represents a group selected from a linear or branched alkylene, arylene, or cycloalkylene group having two or more carbon atoms and combinations thereof, which may have an ether bond in a chain; X represents a dehydroxylation residue of a linear sugar alcohol having 5 or 7 carbon atoms; m is the number of polyethylene glycol chains bonded to X and represents 4 or 6; n is the average addition molar number of oxyethylene groups and n represents an integer of 3 to 600; Y represents a single bond or an alkylene group which may have an ester bond, a urethane bond, an amide bond, an ether bond, a carbonate bond, a secondary amino group, a urea bond, a thioether bond or a thioester bond in a chain or at an end; and Z represents a chemically reactive functional group.
Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption.
Abstract: A novel compound which has excellent ultraviolet-absorbing function (especially UVA absorbing function) and excellent hydrophilicity. A benzylidene azolidine derivative represented by structural formula (I) or a salt thereof. In structural formula (I), n represents an integer of 1-5; A1 represents O, S or N-A4; and each of A2, A3 and A4 independently represents a hydrogen atom, an alkyl group which may be substituted by a hydroxyl group and has 1-8 carbon atoms, or the like (provided that at least one of A2, A3 and A4 contains one or more hydroxyl groups). In this connection, when n is an integer of 2-5, the plurality of A3O— moieties may be the same as or different.
Abstract: This invention provides a platinum/carbon nanotube catalyst applicable to heterogeneous asymmetric hydrogenation, which is fabricated by supporting platinum on carbon nanotube carriers. The catalyst is prepared by the steps of: heating purified carbon nanotubes in nitric acid, filtering and washing the same with water until pH value of the filtrate becomes neutral, drying the carbon nanotubes; immersing the carbon nanotube carriers obtained in an aqueous chloroplatinic acid solution and carrying out ultrasonic treatment at room temperature; immersing the mixture of the carbon nanotubes and the aqueous chloroplatinic acid solution under stirring; drying the material by heating to 110° C. from room temperature and maintaining this temperature; grinding the product to fine powders, reducing the fine powders with an aqueous sodium formate solution under a heating condition, filtering and washing the product with deionized water, and drying the product.
Type:
Grant
Filed:
May 11, 2010
Date of Patent:
August 23, 2016
Assignee:
DALIAN INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES