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 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 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: 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 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: Compositions of P4HB with high purity have been developed. The compositions are prepared by washing P4HB biomass prior to solvent extraction, and precipitating P4HB from solution. The same solvent is preferably used to wash the P4HB biomass, and as a non-solvent to precipitate the polymer from a P4HB solvent solution. The highly pure P4HB compositions are suitable for preparing implants. The implants may be used for the repair of soft and hard tissues.
Abstract: A family of amine mining collectors that uses alkoxylates allows for the easy adjustment of solubility and molecular weight useful because anionic and cationic mineral collectors require such varying degrees of solubility and molecular weight. The family of the present invention allows for the optimization of both parameters and an increase in collector efficiency.
Abstract: This invention relates to novel isonitriles, including arylthio isonitriles, and methods for their preparation. The isonitriles include a conjugated ring system. The structure is designed with the flexibility to have multiple substitution patterns. The isonitriles may be used in applications including, but not limited to, pharmaceutical compositions.
Type:
Grant
Filed:
February 20, 2015
Date of Patent:
November 1, 2016
Assignee:
Duquesne University of the Holy Ghost
Inventors:
Fraser Fergusson Fleming, Jesus Armando Lujan-Montelongo
Abstract: A method for producing a nanoparticle to separate a diketopyrrolopyrrole pigment includes separating an ?-type diketopyrrolopyrrole pigment nanoparticle having high crystallinity by carrying out separation of the diketopyrrolopyrrole pigment and crystal type transformation to the ?-type with substantially a single step. The ?-type diketopyrrolopyrrole pigment nanoparticle is separated by mixing a diketopyrrolopyrrole pigment solution having the diketopyrrolopyrrole pigment dissolved in a solvent and an alcohol solvent containing an alcohol compound solvent in a thin film fluid formed between at least two processing surfaces 1 and 2 arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other. An acidic substance is contained in at least any one of the diketopyrrolopyrrole pigment solution and the alcohol solvent at this moment.
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 relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.
Type:
Grant
Filed:
July 27, 2015
Date of Patent:
October 18, 2016
Assignee:
GE Healthcare Limited
Inventors:
Anthony Eamon Storey, Clare Louise Jones, Denis Raymond Christophe Bouvet, Nicolas Lasbistes, Steven Michael Fairway, Lorenzo Williams, Alexander Mark Gibson, Robert James Nairne, Farhad Karimi, Bengt Langstrom
Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
August 20, 2014
Date of Patent:
October 11, 2016
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
William Buffham, Hannah Canning, Richard Davenport, William Farnaby, Stephen Mack, Alka Parmar, Susanne Wright
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: Compounds of formula (I), wherein R1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.
Type:
Grant
Filed:
May 23, 2013
Date of Patent:
October 4, 2016
Assignee:
ORION CORPORATION
Inventors:
Marko Ahlmark, David Din Belle, Mika Kauppala, Anne Luiro, Taina Pajunen, Jarmo Pystynen, Eija Tiainen, Matti Vaismaa, Josef Messinger
Abstract: The invention provides a method for producing an aromatic amide carboxylic acid derivative represented by the following Formula (2), including a step of reacting an aromatic amide halide derivative represented by the following Formula (1) with carbon monoxide. In the following Formulae (1) and (2), R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; X1 represents a fluorine atom or a cyano group; X2 represents a halogen atom; and n represents an integer of from 0 to 3.
Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
Type:
Grant
Filed:
October 6, 2014
Date of Patent:
October 4, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.
Type:
Grant
Filed:
September 5, 2014
Date of Patent:
October 4, 2016
Assignee:
NOVARTIS AG
Inventors:
Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Clive McCarthy, Heinrich Rueeger, Frank Hans Seiler, Frédéric Stauffer
Abstract: The present invention is directed to a process for the manufacture of methyl limonitrile comprising a mixture of 3,7-dimethyl-2,6-nonadiene nitrile, 3,7-dimethyl-3,6-nonadiene nitrile and 7-methyl-3-methylene-6-nonene nitrile comprising the following steps: a) reacting 6-methyl-5-octen-2-one with cyano acetic acid and removing carbon dioxide and water, wherein the reaction and the removal of carbon dioxide and water are performed in the presence of a base and a co-base 1 in an organic solvent, and wherein the organic solvent is a solvent which forms a heteroazeotrop with water; b) removing the solvent and the base of the reaction mixture obtained after having performed step a) or step c) by distillation to obtain a reaction mixture, whereby this step may optionally be performed in the presence of a co-base 2; c) isomerizing the reaction mixture obtained after having performed step a) or step b) to obtain an isomerized reaction mixture in the presence of a co-base 2; whereby step b) can be performed before or
Type:
Grant
Filed:
February 11, 2013
Date of Patent:
October 4, 2016
Assignee:
DSM IP ASSETS B.V.
Inventors:
Angela Wildermann, Werner Bonrath, Raphael Beumer, Silke Dorn
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 is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
Type:
Grant
Filed:
October 30, 2015
Date of Patent:
September 27, 2016
Assignee:
Janssen Pharmaceutica NV
Inventors:
Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson