Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.
Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
Type:
Grant
Filed:
July 21, 2014
Date of Patent:
October 25, 2016
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Susanne Röhrig, Alexander Hillisch, Julia Straβburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Anja Buchmüller, Christoph Gerdes, Henrik Teller, Martina Schäfer, Adrian Tersteegen
Abstract: The invention provides a method of activating PPAR ? and a method of treating or preventing a disease associated with PPAR ? by administering a tricyclic compound having a PPAR ? agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
Abstract: Processes for producing acetic acid herein generally include contacting methanol and carbon monoxide in the presence of a reaction medium under carbonylation conditions sufficient to form acetic acid, the reaction medium including a carbonylation catalyst selected from rhodium catalysts, iridium catalysts and palladium catalysts; from 1 wt. % to 14 wt. % water; and a plurality of additives, in-situ generated derivatives of the plurality of additives or combinations thereof; the plurality of additives including a first additive including one or more phosphine oxides and a second additive selected from heteropolyacids, metal salts and combinations thereof, the heteropolyacids represented by the formula HnM12XO40, wherein H is hydrogen, M is selected from tungsten and molybdenum, X is selected from phosphorous and silicon and O is oxygen and n is 3 or 4, the metal salts are selected from transition metal salts, lanthanide metal salts and combinations thereof; and recovering acetic acid from the process.
Type:
Grant
Filed:
September 22, 2014
Date of Patent:
October 25, 2016
Assignee:
LyondellBasell Acetyls, LLC
Inventors:
Noel C. Hallinan, Brian A. Salisbury, Daniel F. White, David L. Ramage, Jared T. Fern
Abstract: Diesters are prepared by first hydrolyzing dinitrile compounds into imide compounds and then reacting such imide compounds with at least one alcohol.
Abstract: Methods of treating or suppressing oxidative stress disorders affecting normal electron flow in the cells, including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases, diseases of aging and diseases caused by reactive oxygen species are disclosed, as well as compounds useful in the methods of the invention, such as such as catechol or ortho-quinone derivatives of Formula (I).
Abstract: The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11?-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11?-HSD1 (11?-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11?-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
Type:
Grant
Filed:
June 4, 2013
Date of Patent:
October 11, 2016
Assignees:
AHN-GOOK PHARMACEUTICAL CO., LTD., BAMICHEM CO., LTD, INCHEON UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION
Inventors:
Soon Kil Ahn, Jin Auh, Nam Song Choi, Chang Kyun Han, Tae-Jeong Kim, Kamsa Pae, Young June Shin, Dong-Oh Han, Cheol Kyu Han
Abstract: The invention refers to compounds of general formula (I) wherein the variables take various meanings, pharmaceutical compositions containing them and their use in medicine, particularly in pain therapy.
Type:
Grant
Filed:
July 29, 2014
Date of Patent:
October 11, 2016
Assignee:
LABORATORIOS DEL DR. ESTEVE S.A.
Inventors:
Antoni Torrens-Jover, Rosa Ortuño-Mingarro, Àlex Pericas-Cano, Èric Ferrer-Mallofrè
Abstract: The present invention relates to a process for the preparation of catalytic support and the supported bimetallic catalysts, used in the production of ethylene homopolymers and ethylene copolymers with ?-olefins, of high and ultra high molecular weight with broad molecular weight distribution, in gas or liquid phase polymerization processes, the latter being in slurry, bulk or suspension, and the products obtained from these processes.
Type:
Grant
Filed:
March 4, 2011
Date of Patent:
October 4, 2016
Assignee:
Braskem America, Inc.
Inventors:
Marcia Silva Lacerda Miranda, Fernanda Oliveira Vieira da Cunha
Abstract: The present disclosure relates to compounds of the formula wherein R2 and A are certain substituents, Y is an ester group, a nitrile group or an amido group and Z is O, S or N+R2, and which compounds are, for example, useful as intermediates for pyrazole fungicides. The compounds of the present disclosure can be prepared by the reaction of a compound of formula R2—C(O)—CH2Y, with an orthoformate HC—(OR3)3 in the presence of a base, especially in the presence of an amine, e.g. triethylamine.
Abstract: This invention relates to a method for combating adverse effects arising from antipsychotic treatment. The invention furthermore relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a compound of formula I and an antipsychotic drug.
Type:
Grant
Filed:
September 2, 2009
Date of Patent:
October 4, 2016
Assignee:
Saniona A/S
Inventors:
Jørgen Scheel-Krüger, Henrik Björk Hansen
Abstract: Prepolymerized catalyst component for the polymerization of olefins CH2?CHR in which R is hydrogen or a hydrocarbyl radical with 1-12 carbon atoms, having average particle size equal to or lower than 30 ?m comprising a solid catalyst component comprising magnesium halide, a titanium compound having at least a Ti-halogen bond and at least two electron donor compounds one of which being selected from 1,3-diethers and the other one being selected from esters of aromatic mono or dicarboxylic acids, said solid catalyst component being prepolymerized with an olefin, having from 2 to 10 carbon atoms, to such an extent that the amount of the olefin prepolymer is equal to or lower than 50 g per g of solid catalyst component.
Abstract: The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitizers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes, syndrome X, hyperglycaemia, vascular disease and kidney disease. The present invention further relates to compounds and agents and compositions thereof for use in the treatment methods.
Type:
Grant
Filed:
May 31, 2013
Date of Patent:
September 27, 2016
Assignee:
Verva Pharmaceuticals Ltd
Inventors:
Gregory Royce Collier, Kenneth Russell Walder, James Alexander Campbell, Juan-Carlos Molero-Navajas, Nicky Konstantopoulos, Guy Yeoman Krippner
Abstract: The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
Type:
Grant
Filed:
January 22, 2013
Date of Patent:
September 27, 2016
Assignee:
BASF SE
Inventors:
Heidi Emilia Saxell, Peter Erk, Claude Taranta, Thomas Kroehl, Gerhard Cox, Martin Sukopp, Stefan Scherer, Antti Ojala, Gautam R. Desiraju, Rahul Banerjee, Prashant M. Bhatt
Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
Type:
Grant
Filed:
December 10, 2014
Date of Patent:
September 27, 2016
Assignee:
Concert Pharmaceuticals, Inc.
Inventors:
Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
Abstract: The catalyst disclosed is a catalyst including palladium-ruthenium alloy fine particles in which palladium and ruthenium form a solid solution. The palladium-ruthenium alloy fine particles used in this catalyst can be produced by a production method including the step of maintaining a solution containing a protective agent, a reducing agent, a palladium compound or palladium ions, and a ruthenium compound or ruthenium ions at a temperature equal to or higher than a predetermined temperature.
Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
Type:
Grant
Filed:
June 6, 2014
Date of Patent:
September 27, 2016
Assignee:
XenoPort, Inc.
Inventors:
Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
Abstract: Provided are chemical entities selected from compounds of formula (I), wherein R1, R2 and m have meanings given in the description, and pharmaceutically acceptable salts, solvates and stereoisomers thereof, which are inhibitors of ATR and are potentially useful in the treatment of cancer. Further provided are pharmaceutical compositions of the chemical entities, combination products containing the chemical entities, the use of the compositions as therapeutic agents, and methods of treatment using these compositions.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
September 27, 2016
Assignee:
Fundación Centro Nacional de Investigaciones Oncológicas Carlos III
Inventors:
Joaquín Pastor Fernández, Oscar Fernández-Capetillo Ruiz, Sonia Martínez González, Carmen Blanco Aparicio, María del Rosario Rico Ferreira, Luis Ignacio Toledo Lázaro, Sonsoles Rodríguez Arísteguí, Matilde Murga Costa, Carmen Varela Busto, Andrés Joaquín Lopez Contreras, Oliver Renner, María Nieto Soler, David Alvaro Cebrián Muñoz
Abstract: The instant invention describes tetrazole compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Type:
Grant
Filed:
May 28, 2014
Date of Patent:
September 20, 2016
Assignee:
Viamet Pharmaceuticals, Inc.
Inventors:
William J. Hoekstra, Michael R. Loso, Gary D. Gustafson, Daniel Knueppel, Zachary A. Buchan, Michael T. Sullenberger
Abstract: Process for preparing a vinylidenecarboxylic acid or ester thereof, wherein a reaction gas comprising gaseous formaldehyde, molecular oxygen and an alkycarboxylic acid or ester thereof is brought into contact with a solid catalyst whose active composition comprises a vanadium-phosphorus oxide having an average oxidation state of vanadium of from +4.40 to +5.0 to give a product gas comprising the vinylidenecarboxylic acid or ester thereof.
Type:
Grant
Filed:
May 14, 2014
Date of Patent:
September 6, 2016
Assignee:
BASF SE
Inventors:
Philipp Gruene, Cornelia Katharina Dobner, Marco Hartmann