Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.
Inventors:
Markus Berger, Hartmut Rehwinkel, Jan Dahmen, Anders Eriksson, Thomas Hansson, Nafizal Hossain, Per Tomas Klingstedt, Matti Lepisto, Stinabritt Nilsson, Martin Hemmerling, Karl Edman
Abstract: The present invention relates to water-soluble alkoxylated polyalkyleneimines having an inner block of polyethylene oxide comprising 5 to 18 polyethylene oxide units, a middle block of polyalkylene oxide comprising 1 to 5 polyalkylene oxide units and an outer block of polyethylene oxide comprising 2 to 14 polyethylene oxide units. The middle block is formed from polypropylene oxide units, polybutylene oxide units and/or polypentene oxide units. In addition, the present invention relates to water-soluble alkoxylated polyamines.
Type:
Grant
Filed:
July 11, 2014
Date of Patent:
August 22, 2017
Assignee:
BASF SE
Inventors:
Sophia Ebert, Björn Ludolph, Frank Huelskoetter, Kevin Christmas, Stefano Scialla, Brian J. Loughnane, Amy Eichstadt Waun, Darren Rees
Abstract: The use of one or more compounds of the formula (I) in which R is a straight-chain or branched saturated alkyl group having 5 to 11 carbon atoms or a straight-chain or branched mono- or polyunsaturated alkenyl group having 5 to 11 carbon atoms as antimicrobially active compound is described. The use is preferably in cosmetic, dermatological or pharmaceutical compositions, in crop protection formulations, in washing or cleaning compositions or in paints or coatings.
Type:
Grant
Filed:
July 31, 2012
Date of Patent:
August 15, 2017
Assignee:
CLARIANT INTERNATIONAL LTD.
Inventors:
Maurice Frederic Pilz, Peter Klug, Franz-Xaver Scherl, Joerg Grohmann
Abstract: The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
Type:
Grant
Filed:
February 5, 2016
Date of Patent:
August 8, 2017
Assignee:
Celgene Corporation
Inventors:
George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
Abstract: Inhibitors of EYA tyrosine phosphatase having the structure of Formula I are provided herein. The compounds are useful for the treatment of certain proliferative diseases and cancer.
Abstract: One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
Abstract: The present invention refers to novel substituted thiazole and oxazole compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties. The compounds are useful in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.
Type:
Grant
Filed:
February 4, 2015
Date of Patent:
August 1, 2017
Assignee:
Axxam S.P.A.
Inventors:
Paolo Pevarello, Stefan Lohmer, Chiara Llberati, Pierfausto Seneci, Cristina Pesenti, Adolfo Prandi
Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Type:
Grant
Filed:
January 9, 2017
Date of Patent:
August 1, 2017
Assignee:
Array BioPharma, Inc.
Inventors:
Steven W. Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, Hong-Woon Yang, Qian Zhao
Abstract: Compounds that are derivatives of oxindole conform to the general structure of Formula (I) These compounds are believed to exhibit antioxidant properties. A composition comprises an organic material and a compound conforming to the structure of Formula (I).
Type:
Grant
Filed:
February 4, 2015
Date of Patent:
August 1, 2017
Assignee:
Milliken & Company
Inventors:
Sanjeev K. Dey, Eduardo Torres, Suchitra Datta, Mary E. Mason, Philip G. Harris
Abstract: The invention relates to a process for the synthesis of Cariprazine, an antipsychotic compound useful in the treatment of positive and negative symptoms associated to schizophrenia, with the following structural formula: (A) The invention further relates to the synthesis of intermediates useful in the preparation of Cariprazine.
Type:
Grant
Filed:
October 14, 2014
Date of Patent:
August 1, 2017
Assignee:
CHEMO RESEARCH, S.L.
Inventors:
Maurizio Taddei, Elena Cini, Marcello Rasparini
Abstract: Polymorphs of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. Solvent forms of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are also disclosed.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
July 18, 2017
Assignee:
GILEAD CALISTOGA LLC
Inventors:
Suzanne Buttar, Ernest Carra, Tracy Ehiwe, Duong Tran, Fang Wang, Christopher Worrall, Jerry Evarts
Abstract: The present invention relates to a process for preparation of Echothiophate Iodide (I). Echothiophate Iodide (I) obtained by the process of the present invention is obtained as new crystalline form designated as Form-SET. The process for preparation of Echothiophate Iodide (I) according to present invention is an ecofriendly process that avoids the use of hazardous solvent systems and provides Echothiophate Iodide (I) of high purity. Pharmaceutical composition of the said crystalline Form-SET of Echothiophate Iodide (I) of high purity is useful in the treatment of ocular disorders like Glaucoma.
Abstract: The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof, characterized in that a compound of formula (II)—where L is leaving group—is reacted with compound of formula (III) and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.
Abstract: The invention relates to a novel process for preparation of dronedarone of formula (I) and pharmaceutically acceptable salts thereof the hydroxyl group is removed, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof.
Abstract: Cycloalkylalkylphosphonic acids are presented that are useful for forming a self-assembled monolayer (SAM) on a surface of a metal oxide layer. The combined SAM and metal oxide layer form the dielectric layer of an organic thin film transistor (OTFT). The OTFT can be formed with p-type and n-type organic semiconductor layers on the SAM. The OTFT display superior field effect mobilities and air stabilities to other SAMs and the SAMS of cycloalkylalkylphosphonic acids allow deposition of the organic semiconductors by either vapor deposition or solution processing techniques.
Abstract: The present invention provides a method for synthesizing cationic bleach activators via a single-bath reaction, comprising steps of: separately dissolving 4-chloromethylbenoyl chloride and lactam in its respective solvent, adding an acid-binding agent to the lactam solution, next adding dropwisely 4-chloromethylbenoyl chloride solution into the lactam/acid binding-agent solution, and finally adding tertiary amine to the solution above to make a reaction solution, which is further treated with mixing and refluxing. The washed and dried final product is TBLC cationic bleach activator. The method of the present invention greatly simplifies the synthesizing process and lowers the stringency of reaction conditions for preparing cationic bleach activators (TBLC). At the same time, the present method produces TBLC cationic bleach activators with high yields, making it a suitable option for industrial production of these bleach activators.
Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronic acid ester derivatives and their use as therapeutic agents.
Type:
Grant
Filed:
February 3, 2016
Date of Patent:
July 4, 2017
Assignee:
Rempex Pharmaceuticals, Inc.
Inventors:
Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer