Abstract: Molecule for attaching a radioactive parent nuclide to a support, comprising at least one functional group for attaching the radioactive parent nuclide; and a molecular moiety suitable for establishing a nonpolar bond to the support.
Abstract: Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an ?-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.
Abstract: The invention concerns a method of treating Angelman Syndrome (AS) in a subject, comprising inducing ketosis in the subject by administering a therapeutically effective amount of a ketone ester, such as an R,S-1,3-butanediol acetoacetate ester, wherein administration of the ketone ester elevates the blood ketone level in the subject. Other aspects of the invention include a method of increasing cognitive function and/or motor function in a subject with AS; and a method of decreasing seizures and increasing the latency to seize in a subject with AS.
Type:
Grant
Filed:
May 24, 2016
Date of Patent:
October 24, 2017
Assignee:
UNIVERSITY OF SOUTH FLORIDA
Inventors:
Edwin John Weeber, Stephanie Lynn Ciarlone, Dominic Paul D'Agostino
Abstract: The present invention is directed to pharmaceutical combination products comprising a muscarinic acetylcholine receptor antagonist, fluticasone propionate and salmeterol xinafoate, and to their use in the treatment of inflammatory or respiratory tract diseases.
Abstract: Provided herein are methods and compositions for selective and targeted cancer therapy, in particular certain benzothiophenes, benzothiazoles, oxalamides, N-acyl ureas and chromones, and their use in selectively treating certain adenocarcinomas. In some embodiments, the selective toxicity of the compounds may be mediated through SCD1 and/or CYP450 such as CYP4F11.
Type:
Grant
Filed:
September 4, 2014
Date of Patent:
October 17, 2017
Assignee:
Board of Regents of the University of Texas System
Inventors:
Joseph M. Ready, Deepak Nijhawan, Stephen S. Gonzales, Pano Theodoropoulos
Abstract: The present invention relates to a method for preparing methylated amines using carbon dioxide and to the use of the method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres and synthetic leathers, pesticides and fertilisers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres, synthetic leathers, pesticides and fertilisers, including a step of preparing methylated amines by the method according to the invention. The present invention also relates to a method for preparing marked methylated amines and to the uses thereof.
Type:
Grant
Filed:
June 4, 2013
Date of Patent:
October 10, 2017
Assignee:
Commissariat A L'Energie Atomique Et Aux Energies Alternatives
Abstract: A method for preparing N,N?-bis(2-cyanoethyl-1,2-ethylenediamine involves using glycol ether as a catalyst for synthesis reaction in which ethylenediamine and acrylonitrile at a molar ratio of 1:1.9-2.1 are reactant that react at 20-70°C to prepare N,N?-bis(2-cyanoethyl)-1,2-ethylenediamine; the method improves the yield to 98.15-98.98%; and the used glycol ether may be filtered and recycled, thereby saving costs and reducing environmental pollution.
Abstract: The present disclosure relates to management of Hepatitis C Virus (HCV) and associated condition. The present disclosure also relates to management of Hepatic Fibrosis. The present disclosure relates to administration of composition comprising pentameric type A procyanidin, trimeric procyanidin and tetrameric procyanidin, optionally along with pharmaceutically acceptable excipient, for management of Hepatic Fibrosis, Hepatitis C virus and associated conditions. The composition acts as an inhibitor at the entry stage of Hepatitis C virus into a cell. The composition inhibits different genotypes of Hepatitis C Virus.
Abstract: The present invention in one embodiment provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula I are as defined in the specification.
Abstract: The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity.
Type:
Grant
Filed:
October 11, 2013
Date of Patent:
October 3, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Petra Bloms-Funke, Gregor Bahrenberg, Wolfgang Schröder, Sven Kühnert, Simon Lucas
Abstract: A method for preparing N,N?-bis(2-cyanoethyl)-1,2-ethylenediamine involves using strongly acidic cation exchange resin as a catalyst for synthesis, and is advantageous for not only eliminating the need of distillation for purification and thereby reducing reaction time, but also improving the yield of N,N?-bis(2-cyanoethyl)-1,2-ethylenediamine to 97.70-98.08%; and the method benefits simplified process and reduced costs and helps to save water significantly, thereby minimizing environmental pollution.
Abstract: Described are ROR? modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.
Type:
Grant
Filed:
January 5, 2015
Date of Patent:
September 26, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jingwu Duan, T. G. Murali Dhar, Bin Jiang, Zhonghui Lu, Ananta Karmakar, Arun Kumar Gupta, Carolyn A. Weigelt
Abstract: The present invention describes the preparation of highly-performing “Acrylamide Free” polyelectrolytic polymers by using not toxic monomers and the way such new monomers can be advantageously used in the field of several civil and/or industrial applications. The new polyelectrolytic polymers developed herein can be then used both as replacement of the common acrylamide-based polymers and in the applications wherein the absence of residual toxic polymerization monomers is requested.
Type:
Grant
Filed:
March 10, 2015
Date of Patent:
September 26, 2017
Assignee:
ITALMATCH CHEMICALS S.P.A.
Inventors:
Antonio Alberto Lucio Barbieri, Manuela Crisci
Abstract: The present invention provides new therapeutic compounds for treatment of diseases caused or influenced by microtubule stability, such as proliferative diseases. The compounds are phenyl-analogs of the naturally occurring peloruside. The analogs are easier to synthesize, and hence open up the possibility to produce said compounds in large quantities for therapeutic use.
Type:
Grant
Filed:
November 28, 2014
Date of Patent:
September 26, 2017
Assignee:
UNIVERSITEIT GENT
Inventors:
Johan Van Der Eycken, Gert Smans, Jelle Cornelus, Dries Van Den Bossche, Nick Jacobs
Abstract: Methods and compositions for the treatment of acute or chronic cerebral ischemia by delivery of linear, blood soluble, non-toxic macromolecules.
Type:
Grant
Filed:
July 1, 2015
Date of Patent:
September 19, 2017
Assignee:
STC.UNM
Inventors:
Denis Bragin, Edwin Nemoto, Marina V. Kameneva
Abstract: A method for synthesizing dimethyl carbonate from methanol and urea, in which a saline ureic medium is used that includes at least one inorganic salt selected from the group made up of zinc (Zn) (II) chloride, tin (Sn) chlorides and iron (Fe) (III) chloride, characterized in that: methanol, in the presence of a catalytic composition, is placed in contact with the saline ureic medium that is at least partially liquid at a temperature referred to as synthesis temperature, which is higher than 140° C., such that reaction vapors are produced; the reaction vapors are condensed, and a condensate of the reaction vapors is collected, including dimethyl carbonate; the method is carried out at atmospheric pressure. A method for enriching and purifying dimethyl carbonate is also described.
Type:
Grant
Filed:
January 19, 2015
Date of Patent:
September 19, 2017
Assignees:
CHARABOT SA, INSITUT NATIONAL POLYTECHNIQUE DE TOULOUSE, INSTITUT NATIONAL DE LA RECHERCHE AGRONOMIQUE
Inventors:
Zephirin Mouloungui, Christophe Maruejouls, Sophie Lavoine-Hanneguelle
Abstract: The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R1-R4 of formula (I) and R1-R3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Type:
Grant
Filed:
November 25, 2015
Date of Patent:
September 19, 2017
Assignees:
GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
Inventors:
Marc Adler, Brian K. Albrecht, Sarah Bronner, Kevin X. Chen, Alexandre Côté, Terry Crawford, Patrick Cyr, Jackson Egen, Steven Kauder, Kwong Wah Lai, Jiangpeng Liao, Steven Magnuson, Jeremy Murray, Richard Pastor, F. Anthony Romero, Alexander M. Taylor, Vickie Hsiao-Wei Tsui, Fei Wang, Bing-Yan Zhu
Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
July 2, 2015
Date of Patent:
September 19, 2017
Assignee:
Novartis AG
Inventors:
Christopher M. Adams, David B. Belanger, Doug Bevan, Takeru Ehara, Luciana Ferrara, Nan Ji, Donglei Liu, Erik Meredith, Muneto Mogi, James Powers, Ganesh Prasanna, Mitsunori Kato
Abstract: The present invention provides novel crystalline forms of apremilast hemitoluene solvate, apremilast hydrate, and apremilast anhydrate and an amorphous form of apremilast, and processes for the preparation of these forms.