Abstract: Provided is a 1-(2-acyloxyethyl)cyclopropyl sulfonate compound of General Formula (2): wherein R1 is a monovalent hydrocarbon group having 1 to 10 carbon atoms and optionally containing one or more unsaturated bonds and Z is a monovalent hydrocarbon group having 1 to 10 carbon atoms and optionally containing one or more unsaturated bonds.
Abstract: The present disclosure provides a photoreactive synthetic regulator of protein function. The present disclosure further provides a light-regulated polypeptide that includes a subject synthetic regulator. Also provided are cells and membranes comprising a subject light-regulated polypeptide. The present disclosure further provides methods of modulating protein function, involving use of light.
Type:
Grant
Filed:
April 19, 2016
Date of Patent:
June 27, 2017
Assignee:
The Regents of the University of California
Inventors:
Dirk Trauner, Ehud Y. Isacoff, Richard H. Kramer, Matthew R. Banghart, Doris L. Fortin, Alexandre Mourot
Abstract: The present invention refers to an amorphous form of a thiocolchicine derivative, IDN 5404, to a process for producing it and to pharmaceutical compositions thereof. The amorphous form is characterized by the XRPD pattern, DSC profile and/or TG/DTA profile.
Type:
Grant
Filed:
March 26, 2015
Date of Patent:
June 27, 2017
Assignee:
INDENA S.P.A.
Inventors:
Walter Cabri, Federico Peterlongo, Daniele Ciceri, Andrea Gambini
Abstract: The present application relates to novel 3-(pyrimidin-2-yl)imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
February 17, 2015
Date of Patent:
June 27, 2017
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Alexandros Vakalopoulos, Alexey Gromov, Markus Follmann, Damian Brockschnieder, Johannes-Peter Stasch, Tobias Marquardt, Adrian Tersteegen, Frank Wunder, Gorden Redlich, Dieter Lang, Volkhart Min-Jian Li
Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
Type:
Grant
Filed:
June 26, 2015
Date of Patent:
June 27, 2017
Assignee:
ASTRAZENECA AB
Inventors:
David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
Abstract: Methods for treating a subject having a prostate cancer bone metastasis are disclosed. Methods for prophylactically treating a subject at risk of developing a prostate cancer bone metastasis are also disclosed. The methods for treating a subject having, or at risk of developing, a prostate cancer bone metastasis may include administering a prostatic acid phosphatase inhibiting agent to the subject. The methods for treating a subject having, or at risk of developing, a prostate cancer bone metastasis may also include administering a phosphonic acid to the subject. Further, the phosphonic acid may include a benzylaminophosphonic acid, such as [phenyl[(phenylmethyl)amino]methyl]-phosphonic acid).
Abstract: Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein GAr, L1, Z1 and Z2 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by voltage-gated sodium channels, e.g., Nav1.7 and/or Nav1.8. Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
Type:
Grant
Filed:
March 14, 2016
Date of Patent:
June 20, 2017
Assignee:
AbbVie Inc.
Inventors:
Jerome Daanen, David DeGoey, Jennifer M. Frost, Tammie Jinkerson, Steve Latshaw, Lei Shi
Abstract: An agrochemical formulation comprising a penetrant and an agrochemical active. The penetrant is an esterified and/or etherified polyol alkoxylate obtainable by directly esterifying and/or etherifying a polyol alkoxylate. There is also provided a method of making the penetrant comprising alkoxylation of a polyol, and esterification or etherification of the formed poyol alkoxylate. The penetrant is suitable for use in agrochemical formulations to enhance penetration of the active across a leaf cuticle.
Type:
Grant
Filed:
November 19, 2013
Date of Patent:
June 20, 2017
Assignee:
Croda International PLC
Inventors:
Trevor Graham Blease, Kathryn Marie Knight
Abstract: Production of methacrylic acid ester comprising a step of having acetone undergo a dehydration reaction in the presence of a dehydration reaction catalyst to obtain a reaction mixture; a step of separating a mixture containing propyne and propadiene as main components from the obtained reaction mixture; a step of separating the separated mixture containing propyne and propadiene as main components into a liquid, gas, or gas-liquid mixture containing propyne as a main component, and a liquid, gas, or gas-liquid mixture containing propadiene as a main component; and a step of bringing the obtained liquid, gas, or gas-liquid mixture containing propyne as a main component into contact with carbon monoxide and an alcohol having 1 to 3 carbon atoms in the presence of a catalyst containing at least one selected from the group consisting of Group 8 metal elements, Group 9 metal elements, and Group 10 metal elements.
Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitors of the complement alternative pathway, in particular of Factor B. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Type:
Grant
Filed:
July 14, 2014
Date of Patent:
June 20, 2017
Assignee:
Novartis AG
Inventors:
Christopher Michael Adams, Michael Paul Capparelli, Takeru Ehara, Rajeshri Ganesh Karki, Nello Mainolfi, Chun Zhang
Abstract: Disclosed herein is an antibacterial cleansing composition. The cleansing composition is free of triclosan and comprises lactic acid/lactate, at least one C2 to C3 alcohol, and glutamate diacetate. Lactic acid/lactate is present in the composition in an amount of about 5 weight percent (wt %) to about 15 wt %, based on the total weight of the composition. The C2 to C3 alcohol is present in an amount of about 1 wt % to about 20 wt %, based on the total weight of the composition. Glutamate diacetate is present in an amount of about 0.05 wt % to about 5 wt %. The pH of the composition is about 4 to about 5. The triclosan-free cleansing composition according to the invention has superior antibacterial activity that surpasses comparable triclosan-free formulations that do not contain glutamate diacetate.
Type:
Grant
Filed:
September 22, 2014
Date of Patent:
June 13, 2017
Assignee:
RUBBERMAID COMMERCIAL PRODUCTS/US
Inventors:
Yvan Vermeulen, Nirali Patel, John Van Cassel
Abstract: Imidazolidine-2,4-dione derivatives of formula (I): The compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation such as cancer.
Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
Type:
Grant
Filed:
August 26, 2016
Date of Patent:
June 13, 2017
Assignee:
SK BIOPHARMACEUTICALS CO., LTD.
Inventors:
Coo-Min Chung, Hyung-Jin Jun, Jin-Sung Kim, Hiu-Ho Kim, Hye-Kyung Min, Yong-Gil Kim, Jong-Gil Choi, Hongwook Kim
Abstract: The present invention is directed to methods for preparing a fluorosulfonate ester or a salt thereof, through a reaction of a dissolved sulfonyl fluoride (RFSO2F) with alkoxide anion (RO?) optionally in the presence of an aprotic base (B), where RF is fluorine or a C1-C8 perfluoroalkyl group, and R is a primary alkyl or alkoxyalkyl. Alkoxide anion (RO?) can be generated from a precursor such as an alcohol or silyl ester.
Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Type:
Grant
Filed:
February 6, 2015
Date of Patent:
June 13, 2017
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Remond Moningka, Nancy Jo Kevin
Abstract: A process utilizing nitric acid and oxygen as co-oxidants to oxidize aldehydes, alcohols, polyols, preferably carbohydrates, specifically reducing sugars to produce the corresponding carboxylic acids.
Abstract: The present invention produces ethanol in a stacked bed reactor that comprises a first catalyst and a second catalyst, wherein the first and second catalysts comprise at least one group VIII metal, and wherein the second catalyst is substantially free of copper. The crude ethanol product may be separated and ethanol recovered.
Type:
Grant
Filed:
January 11, 2012
Date of Patent:
June 6, 2017
Assignee:
CELANESE INTERNATIONAL CORPORATION
Inventors:
Heiko Weiner, Zhenhua Zhou, Radmila Jevtic, Victor J. Johnston
Abstract: The present invention aims to provide a compound superior in broad utility and stability, which is useful as a protecting reagent (anchor) of amino acid and/or peptide in liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide (—CONHR)-type, an organic synthesis reaction method (particularly peptide liquid phase synthesis method) using the compound, and a kit for peptide liquid phase synthesis containing the compound, and has found that the object can be achieved by a particular compound having a diphenylmethane skeleton.
Abstract: The disclosure relates to methods of controlling the state of a virus (lytic or lysogenic) in an individual, such as a method of reactivating a latent virus in an individual, comprising administering one or more agents that modulates the activity of signal transducer and activator of transcription 3 (STAT3) or any of p300, CBP or p300/CBP. Also contemplated are methods further comprising administering an HDAC modulating agent, such as an HDAC inhibiting agent or an HDAC activating agent.
Abstract: Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
Type:
Grant
Filed:
June 29, 2016
Date of Patent:
June 6, 2017
Assignees:
Array BioPharma Inc., Genentech, Inc.
Inventors:
James F. Blake, Adam Cook, John Gaudino, Indrani W. Gunawardana, Erik James Hicken, Kevin W. Hunt, Michael Lyon, Andrew T. Metcalf, Peter J. Mohr, David A. Moreno, Brad Newhouse, Li Ren, Jacob Schwarz, Huifen Chen, Lewis Gazzard, Jane Schmidt, Steve Do