Chalcogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/248)
  • Publication number: 20150141652
    Abstract: The present invention relates to an improved process for preparing 2-[(2E)-2-fluoro-2-(3-piperidinylidene)ethyl]-1H-isoindole-1,3(2H)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3E)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo 3-quinolinecarboxylic acid.
    Type: Application
    Filed: September 28, 2012
    Publication date: May 21, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Yolande Lydia Lang, Dominique Paul, Michel Depre
  • Publication number: 20150133668
    Abstract: The present invention is directed to an improved process for the preparation of methylphenidate, stereoisomer, mixture of stereoisomers and pharmaceutically acceptable salts thereof, more particularly, the sulfate and hydrochloride salts of methylphenidate, di-threo-methylphenidate and dex-methylphenidate. Methods of removing or reducing the amount of impurities from the above described process are also disclosed.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 14, 2015
    Inventors: Brian J. Smith, Stephen M. Stefanick, Charla Barr, Mark C. Dobish
  • Publication number: 20150118548
    Abstract: Provided is a lithium secondary cell which has high capacity, suppresses deterioration in capacity and improves cycle characteristics particularly when used in high-temperature environments and has long lifespan. Provided is a lithium secondary cell including a positive electrode active material layer containing a positive electrode active material, a negative electrode active material layer containing a negative electrode active material and an electrolytic solution for immersing the positive and negative electrode active material layers, wherein the electrolytic solution contains at least one certain ester compound.
    Type: Application
    Filed: May 28, 2013
    Publication date: April 30, 2015
    Applicant: NEC Corporation
    Inventors: Masahiro Suguro, Midori Shimura
  • Patent number: 9006227
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: April 14, 2015
    Assignee: Integrative Research Laboratories Sweden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Publication number: 20140309114
    Abstract: Amine salts of certain herbicides that in free acid form include at least one carboxylic acid moiety are described. Herbicide salts comprising the cation of various imidazole, piperazine, piperidine, and morpholine compounds are provided. The herbicide amine salts described are suitable for formulation into herbicidal application mixtures and/or stable concentration compositions that exhibit acceptable volatility characteristics upon application.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Applicant: MONSANTO TECHNOLOGY LLC
    Inventors: Junhua Zhang, Daniel R. Wright, William Abraham
  • Patent number: 8853392
    Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: October 7, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
  • Publication number: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140243278
    Abstract: Disclosed is an acid addition salt of donepezil, wherein acid counterion is selected from the group consisting of pamoic acid, cypionic acid, camphor sulfonic acid, enanthic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, valeric acid, Dibenzoyl-D-Tartaric acid and terephthalic acid. Disclosed is a process for the preparation and pharmaceutical composition comprising the same. More specifically, disclosed is concerned with the pamoate acid addition salts of donepezil. Disclosed also is long acting formulation comprising the acid addition salt of donepezil and process for the preparation thereof.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 28, 2014
    Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Jaya Abraham, Manish Parikh, Mahesh Suthar, Bipin Manavadariya, Vivek Mishra
  • Publication number: 20140171607
    Abstract: The present invention provides new ruthenium complexes of Formula (1), which contain a chelate ring created by a halogen atom X. The invention concerns also a method for the preparation of the new ruthenium complexes and their application in metathesis reactions.
    Type: Application
    Filed: June 4, 2012
    Publication date: June 19, 2014
    Applicant: UMICORE AG & CO. KG
    Inventors: Karol Grela, Michal Barbasiewicz, Michal Michalak
  • Publication number: 20140142313
    Abstract: The present invention provides a compound of new crystalline form I and form II of 1-[2-[(4-chlorophenyl)phenylmethoxy]ethyl]piperidinium monohydrochloride. The compound of form I has an X-ray diffraction pattern expressed in terms of 2-theta angles that comprises the following peaks: 15.5, 15.9, 17.6, 18.3, 18.8, 19.8, 20.2, 20.8, 21.2, 21.9, 22.9, 24.8, 25.7, 27.7, 28.0, and 30.6 degrees. In addition, the compound of form II has an X-ray diffraction pattern expressed in terms of 2-theta angles that comprises the following peaks: 14.8, 16.7, 17.3, 18.0, 18.2, 19.8, 20.5, 21.1, 22.8, 23.7, 25.0, 25.2, 25.4, 26.4, 27.8, 28.3, 29.0, 29.9, and 31.6 degrees.
    Type: Application
    Filed: November 16, 2012
    Publication date: May 22, 2014
    Applicant: SYN-TECH CHEM. & PHARM. CO., LTD.
    Inventors: Chin-Tsai FAN, Chen-Ming Hsiao, Rong-Bin HSIEH
  • Publication number: 20140128360
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: April 17, 2012
    Publication date: May 8, 2014
    Applicant: Integrative Research Laboratories Swenden AB
    Inventors: Clas Sonesson, Jonas Karlsson, Peder Svensson
  • Patent number: 8691994
    Abstract: The invention provides a composition and a method of using the composition for inhibiting the unwanted polymerization of ethylenically unsaturated monomers. The composition is prepared by reducing a nitroxide stable free radical to its corresponding hydroxylamine through reaction with a dialkyl/aryl hydroxylamine and subsequent addition of a polymerization prevention component selected from phenolic antioxidants, phenylenediamine and phenylenediamine derivatives, or phenothiazine and phenothiazine derivatives targeted towards ethylenically unsaturated monomers. The conversion of the nitroxide by the dialkyl/aryl hydroxylamine is to prevent it or the polymerization prevention component from being “spent”by reaction with each other, impurities or any other incompatible components. This allows previously incompatible combinations to now work effectively. In fact, the combination is more efficacious as the combination exerts a synergy due to the presence of various polymerization prevention reagents.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: April 8, 2014
    Assignee: Nalco Company
    Inventor: David Youdong Tong
  • Publication number: 20130316248
    Abstract: The invention relates to a method for producing perfluoroalkanesulfonic acid esters and for further transforming the same into the salts thereof. The invention also relates to the use of the produced compounds in electrolytes, batteries, capacitors, supercapacitors, and galvanic cells.
    Type: Application
    Filed: July 8, 2009
    Publication date: November 28, 2013
    Inventors: Nikolai Ignatyev, Michael Schmidt, Udo Heider, Peter Sartori, Andry Kucheryna
  • Patent number: 8592578
    Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: November 26, 2013
    Assignee: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Patent number: 8586750
    Abstract: The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: November 19, 2013
    Assignee: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Patent number: 8530137
    Abstract: The present invention provides a photoresist composition having a sulfonium salt comprising an anion represented by the formula (IA): wherein R1 and R2 independently represent a hydrogen atom, a C1-C12 aliphatic hydrocarbon group, a C3-C20 saturated cyclic hydrocarbon group, a C6-C20 aromatic hydrocarbon group or a C7-C21 aralkyl group, and the aliphatic hydrocarbon group, the saturated cyclic hydrocarbon group, the aromatic hydrocarbon group and the aralkyl group can have one or more substituents selected from the group consisting of a hydroxyl group, a cyano group, a fluorine atom, a trifluoromethyl group and a nitro group, and one or more —CH2— in the aliphatic hydrocarbon group can be replaced by —O— or —CO—, or R1 and R2 are bonded each other to form a C4-C20 nitrogen-containing ring together with the nitrogen atom to which they are bonded, an acrylic resin having an acid-labile group and being insoluble or poorly soluble in an aqueous alkali solution but becoming soluble in an aqueous alkali solutio
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: September 10, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tatsuro Masuyama, Satoshi Yamaguchi
  • Patent number: 8460851
    Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C(Q1)(Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: June 11, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Satoshi Yamaguchi, Koji Ichikawa
  • Publication number: 20130053572
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
    Type: Application
    Filed: January 19, 2011
    Publication date: February 28, 2013
    Inventors: Steven L. Colletti, Zhengwu James Deng, Matthew G. Stanton, Weimin Wang, Ivory Hills
  • Publication number: 20130041147
    Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3- oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Application
    Filed: October 17, 2012
    Publication date: February 14, 2013
    Applicant: BASF SE
    Inventor: BASF SE
  • Publication number: 20130030185
    Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Application
    Filed: October 1, 2012
    Publication date: January 31, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • Patent number: 8324246
    Abstract: Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: December 4, 2012
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Churlmin Seong, Chul Min Park, Soyoung Kim, Wookyu Park, Nosang Park
  • Patent number: 8314233
    Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: November 20, 2012
    Assignee: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Patent number: 8309720
    Abstract: The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: November 13, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Sergio Cesco-Cancian, Hongfeng Chen, Jeffrey S. Grimm, Neelakandha S. Mani, Christopher M. Mapes, David C. Palmer, Daniel J. Pippel, Kirk L. Sorgi, Tong Xiao
  • Patent number: 8299063
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: October 30, 2012
    Assignee: The University of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120232111
    Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.
    Type: Application
    Filed: April 28, 2006
    Publication date: September 13, 2012
    Applicant: Shiseido Company, Ltd.
    Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata
  • Publication number: 20120202723
    Abstract: Polyhydroxyl functional compounds that contain an all hydrocarbon backbone, wherein all of the hydroxyl groups are bonded to a primary carbon atom, are prepared through the reaction of an alpha, omega-terminal diol having a total of from about 6 to about 42 carbon atoms terminated with a mono-ol having a total of from about 4 to about 42 carbon atoms. The polyols can be used as additives in hydrocarbon oils, drilling fluids, industrial and automotive lubricating fluids, dispersants, engine lubricants, greases, coatings, adhesives, and also in magnetorheological fluids to improve various properties such as dispersion, wear protection, reduction of friction, high temperature stability, and improved aging.
    Type: Application
    Filed: February 3, 2012
    Publication date: August 9, 2012
    Inventors: Kirk J. Abbey, Daniel E. Barber
  • Patent number: 8236565
    Abstract: In various aspects, the present teachings provide labeling reagents and sets of labeling reagents for the relative quantitation, absolute quantitation, or both, of hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols. In various aspects, the present teachings also provide methods for the analysis hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols my MS/MS methods.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: August 7, 2012
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Sasi Pillai
  • Publication number: 20120157680
    Abstract: PROBLEM: Providing a novel ionic liquid, which is low-cost, environment-friendly, and has low viscosity and melting point. MEANS FOR SOLVING THE PROBLEM: The present invention is the invention of the ionic liquid represented by the general formula [1]: {wherein, R1 to R3 and n pieces of R4 each independently represent hydrogen atom or alkyl group having 1 to 4 carbon atoms, R5 to R7 each independently represent alkyl group, aralkyl group, or aryl group, R8 represents alkyl group, aralkyl group, aryl group, or the one represented by the general formula [2]: (wherein T represents alkylene chain having 1 to 8 carbon atoms, n represents 1 or 2, and R1 to R7 are the same as the above-described), X represents nitrogen atom or phosphorus atom, n represents 1 or 2. When n is 1, R3 and R4 are bound and may form cyclohexene ring together with the adjacent carbon atoms. In addition, when X is nitrogen atom, R5 to R7 or R5 to R6 may form hetero ring with nitrogen atom binding thereto}.
    Type: Application
    Filed: August 30, 2010
    Publication date: June 21, 2012
    Applicant: Wako Pure Chemical Industries, Ltd.
    Inventors: Tsutomu Watahiki, Kuniaki Okamoto, Motoshige Sumino
  • Patent number: 8202513
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: June 19, 2012
    Assignee: Bionomics Limited
    Inventors: Bernard Luke Flynn, Jonathan Bayldon Baell, Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Andrew John Harvey, Jorgen Alvar Mould, Dharam Paul
  • Patent number: 8193184
    Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.
    Type: Grant
    Filed: April 20, 2008
    Date of Patent: June 5, 2012
    Assignee: Unimed Pharma, SPOL, S.R.O.
    Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
  • Publication number: 20120107854
    Abstract: An N-alkylpiperidine methanethiol ester derivative represented by any one of the general formulae (1) to (4) or a salt thereof has been discovered. The N-alkylpiperidine methanethiol ester derivative or the salt thereof has specificity for acetylcholinesterase or butyrylcholinesterase and is useful as a reagent for measurement of cholinesterase activity by the Ellman method.
    Type: Application
    Filed: March 3, 2009
    Publication date: May 3, 2012
    Applicant: NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES
    Inventors: Tatsuya Kikuchi, Toshiaki Irie, Kiyoshi Fukushi, Toshimitsu Okamura
  • Patent number: 8153657
    Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: April 10, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jia Zhou
  • Publication number: 20120077977
    Abstract: The present invention relates to a process for preparing (meth)acrylic esters (F) of N,N-substituted amino alcohols, by transesterifying N,N-substituted amino alcohols (I) in which Y and Z are each independently C1-C20-alkyl, C3-C15-cycloalkyl, aryl, or Y and Z together with the nitrogen atom connecting them form a 5- to 9-membered saturated heterocyclic radical which optionally has oxygen, sulfur, nitrogen or C1-C4-alkyl-substituted nitrogen as a further heteroatom, and X is C2-C20-alkylene which may be interrupted by 1 to 10 nonadjacent oxy groups and/or unsubstituted or methoxy-substituted C1-C4-alkylimino groups, or a C3-C15-cycloalkylene, with at least one (meth)acrylic ester (D) in the presence of at least one heterogeneous catalyst (K), wherein the heterogeneous catalyst (K) is used without any further solvent and the content of polymerization inhibitors in the reaction mixture is <450 ppm, and to the use of the (meth)acrylic esters (F) of N,N-substituted amino alcohols.
    Type: Application
    Filed: September 20, 2011
    Publication date: March 29, 2012
    Applicant: BASF SE
    Inventors: Virginie Bette, Hermann Bergmann, Jochen Petzoldt, Frank Höfer
  • Publication number: 20120071457
    Abstract: A new metallo-?-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of ?-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-?-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of ?-lactam antibiotics against metallo-?-lactamase producing bacteria by combining the compound of the general formula (I) with ?-lactam antibiotics.
    Type: Application
    Filed: November 29, 2011
    Publication date: March 22, 2012
    Inventors: Ken Chikauchi, Mizuyo Ida, Takao Abe, Yukiko Hiraiwa, Akihiro Morinaka, Toshiaki Kudo
  • Patent number: 8129409
    Abstract: The present invention provides piperidine derivatives of formula (I): salts and optical isomers thereof and cosmetic compositions containing them.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: March 6, 2012
    Assignee: L'Oreal
    Inventors: Alexandre Cavezza, Michel Neuwels
  • Patent number: 8129406
    Abstract: Disclosed are selective inhibitors of matrix metalloproteinases represented by the following formula (I). wherein X is (CH2)nO, (CH2)nS, (CH2)nNR1, (CH2)n(CH2), or CH?CH, wherein n=0, 1, or 2; R and R1 are, independently, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heteroaryl group, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl; and Z is NH or CH2; or a pharmaceutically acceptable salt thereof. Also disclosed are methods of making such compounds and methods of using such compounds to inhibit tumor progression and to treat diseases such as arthritis.
    Type: Grant
    Filed: March 21, 2005
    Date of Patent: March 6, 2012
    Assignee: Southern Research Institute
    Inventor: Subramaniam Ananthan
  • Publication number: 20120050945
    Abstract: Disclosed is an ionic liquid: wherein: n is 1 or 2; R1 is selected from H and (C1-C6)alkyl; R2 is selected from —(CH2)wO[(CH2)xO(CH2)y]m(CH2)zCH3 and wherein w is 1 to 6, x is 1 to 6, y is 0 to 6, z is 0 to 6, m is 0 to 3 and [w+m(x+y)+z] is less than or equal to 12; and R3 is selected from H and methyl, wherein if n is 1 then R3 is methyl, and if n is 2 then R3 is H. Also disclosed are electrochemical devices and devices employing such electrochemical devices as energy sources.
    Type: Application
    Filed: February 8, 2011
    Publication date: March 1, 2012
    Applicant: INVISTA NORTH AMERICA S.A R.L.
    Inventors: Kenneth Richard Seddon, Tayeb Belhocine, Alberto V. Puga, Keith Whiston
  • Publication number: 20120015911
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: September 20, 2011
    Publication date: January 19, 2012
    Applicant: Bellus Health Inc.
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20110232870
    Abstract: Nitrogen-containing fluorochemical ketones are provided that can be useful in apparatuses that includes a device and a mechanism for transferring heat. The provided fluorochemical ketones are stable at temperatures above 170° C., are environmentally friendly, and are economical to produce. The provided apparatuses can be useful for vapor phase soldering of electronic devices.
    Type: Application
    Filed: March 26, 2010
    Publication date: September 29, 2011
    Inventors: Richard M. FLYNN, Michael G. COSTELLO, Michael J. BULINSKI, Daniel R. VITCAK, Phillip E. TUMA
  • Publication number: 20110171576
    Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C (Q1) (Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.
    Type: Application
    Filed: January 6, 2011
    Publication date: July 14, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Satoshi YAMAGUCHI, Koji ICHIKAWA
  • Patent number: 7943142
    Abstract: Disclosed herein is a purified toxin isolated from Euglena sanguinea. More specifically the toxin, termed euglenophycin, is an alkaloid having herbicidal and cytotoxicity against plant and mammalian cells.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 17, 2011
    Assignees: The United States of America as represented by the Secretary of Agriculture, Board of Trustees of Michigan State University
    Inventors: Paul V. Zimba, Kevin R. Beauchesne, Peter D. Moeller, Richard E. Triemer
  • Publication number: 20110105503
    Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.
    Type: Application
    Filed: June 20, 2008
    Publication date: May 5, 2011
    Applicants: NHWA PHARMA. CORPORATION, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
  • Patent number: 7919626
    Abstract: The invention provides a compound of formula I: wherein R1-R6, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of MAO-B enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: April 5, 2011
    Assignee: Helicon Therapeutics, Inc.
    Inventors: Xianbo Zhou, Roderick E. M. Scott, Rusiko Bourtchouladze, Alan P. Kaplan, Terence P. Keenan, Andrew McRiner
  • Patent number: 7910078
    Abstract: The present invention relates to a method for removing carbon dioxide (CO2) from a gas stream. Particularly, the present invention relates to a method for removing CO2 from a gas stream by a liquid absorbent having an amino alcohol derived from 4-amino-2-butanol. In comparison to conventional amines, the amino alcohols of the present invention have been found to provide a higher CO2 absorption capacity and a higher cyclic capacity for CO2 removal.
    Type: Grant
    Filed: August 23, 2007
    Date of Patent: March 22, 2011
    Assignee: University of Regina
    Inventors: Paitoon Tontiwachwuthikul, Andrew G. H. Wee, Raphael Idem, Kreangkrai Maneeintr, Gao-jun Fan, Amornvadee Veawab, Amr Henni, Adisorn Aroonwilas, Amit Chakma
  • Publication number: 20110046139
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.
    Type: Application
    Filed: April 27, 2009
    Publication date: February 24, 2011
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Publication number: 20110046371
    Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Application
    Filed: April 30, 2009
    Publication date: February 24, 2011
    Applicant: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Publication number: 20110040096
    Abstract: The present invention relates to a process for preparing 2-(aminomethylidene)-4,4-dihalo-3-oxobutyric esters of the formula (I), wherein R1, R2, R3 are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl, and/or R2 together with R3 and the nitrogen atom to which the two radicals are attached are a heterocyclic radical, in which a corresponding 3-aminoacrylic ester is reacted with a halogen-substituted acetyl fluoride in the presence of at least one alkali or alkaline earth metal fluoride; and the further conversion of halogen-substituted 2-(aminomethylidene)-3-oxobutyric esters of the formula (I) to halomethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.
    Type: Application
    Filed: April 30, 2009
    Publication date: February 17, 2011
    Applicant: BASF SE
    Inventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
  • Publication number: 20110009621
    Abstract: The invention relates, in particular, to supported transition metal complexes based on a polystyrene matrix comprising structural units of the formula (Ia): or supported transition metal complexes based on a silica gel matrix comprising structural units of the formula (II): where the radicals and indices have the meanings given in the description. The invention also relates to the use of the supported transition metal complexes in catalysis and corresponding processes for the transition metal-catalyzed conversion of starting material(s) into product(s). In particular, the invention relates to the field of olefin metathesis.
    Type: Application
    Filed: December 6, 2006
    Publication date: January 13, 2011
    Applicant: Raap Polymere GmbH
    Inventors: Willi Bannwarth, Florian Michalek, Jurgen Ruhe
  • Publication number: 20100324009
    Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.
    Type: Application
    Filed: August 24, 2010
    Publication date: December 23, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
  • Publication number: 20100317644
    Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.
    Type: Application
    Filed: August 24, 2010
    Publication date: December 16, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld