1,2-thiazoles (including Hydrogenated) Patents (Class 514/372)
Polycyclo ring system having the thiazole ring as one of the cyclos (Class 514/373)
  • Antimicrobial composition useful for preserving wood
    Patent number: 7951792
    Abstract: Antimicrobial compositions useful for preserving wood, and comprising a variety of antimicrobial compounds.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: May 31, 2011
    Assignee: Rohm and Haas Company
    Inventors: John W. Ashmore, Li Liang Chia, Beverly J. El A'mma
  • SULTAM DERIVATIVES
    Publication number: 20110124686
    Abstract: The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.
    Type: Application
    Filed: October 15, 2010
    Publication date: May 26, 2011
    Inventors: Kevin W. Anderson, Paul Gillespie, Nicholas J. S. Huby, Norman Kong, John L. Roberts, Pamela L. Rossman, Sung-Sau So
  • Isoxazole compounds as histamine Hmodulators
    Patent number: 7947718
    Abstract: Certain isoxazole compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: May 24, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
  • Trifluoromethylbenzamide derivatives and therapeutic uses thereof
    Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • PROTEASOME INHIBITORS AND THEIR USE IN TREATING PATHOGEN INFECTION AND CANCER
    Publication number: 20110118274
    Abstract: The present invention relates to proteasome inhibitors and their use in methods of treating a subject for a pathogen infection or cancer. The methods involve administering to the subject a compound of Formula (I). (I) where: Q is Formula or Formula, where the crossing dashed line illustrates the bond formed joining Q to the rest of the compound of Formula (I). The remainder of substituents of the compound of Formula (I) are defined in the present application.
    Type: Application
    Filed: August 25, 2008
    Publication date: May 19, 2011
    Applicant: CORNELL RESEARCH FOUNDATION, INC.
    Inventors: Carl Nathan, Gang Lin
  • Protein phosphatase inhibitors
    Patent number: 7939554
    Abstract: A method of inhibiting protein tyrosine phosphatase in a subject includes administering to the subject a therapeutically effective amount of at least one benzo-1,4-quinone, phenyl isothiazolone, or analog thereof to the subject.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: May 10, 2011
    Assignee: The Cleveland Clinic Foundation
    Inventor: Taolin Yi
  • COMPOSITION HAVING BIOCIDE ACTIVITY FOR AQUEOUS PREPARATIONS
    Publication number: 20110097311
    Abstract: The present invention refers to a process for bacterial stabilizing aqueous preparations like e.g. calcium carbonate slurries and a composition which can be used for the biocidal treatment of such aqueous preparations.
    Type: Application
    Filed: April 1, 2009
    Publication date: April 28, 2011
    Inventors: Nicola Di Maiuta, Patrick Schwarzentruber, Matthias Buri, Patrick Arthur Charles Gane
  • CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
    Publication number: 20110086879
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: November 5, 2010
    Publication date: April 14, 2011
    Applicants: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
    Publication number: 20110082116
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: December 14, 2010
    Publication date: April 7, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • Active Compound Combinations Comprising Arylamidines and N-Cycloalkylamides
    Publication number: 20110082036
    Abstract: The invention relates to active compound combinations comprising (A) an arylamidine compound of formula (I) and a N-cycloalkylamide compound (B) of formula (II). Moreover, the invention relates to a fungicidal composition comprising the compound combinations according to the present invention, to a method for curatively or preventively controlling phytopathogenic fungi, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed itselfs.
    Type: Application
    Filed: October 7, 2009
    Publication date: April 7, 2011
    Inventors: Philippe Desbordes, Jean-Pierre Vors, Benoit Hartmann, Christophe Dubost, Ralf Dunkel, Arounarith Tuch, Kerstin Ilg, Jörg Nico Greul, Stefan Hillebrand, Klaus Kunz, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Stephanie Gary
  • Indoles and Their Therapeutic Use
    Publication number: 20110071175
    Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: December 12, 2008
    Publication date: March 24, 2011
    Inventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara A. Vitabile-Woo, Mathias Domostoj
  • Imidazoles and triazoles, their preparation, and their use as pharmaceutical compositions
    Patent number: 7906539
    Abstract: The present invention relates to imidazoles and triazoles of general formula wherein R1 to R4 and X are defined as in claims 1 to 8, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: March 15, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Leo Thomas, Mohammad Tadayyon
  • METHOD FOR CONTROLLING MICROBIAL BIOFILM IN AQUEOUS SYSTEMS
    Publication number: 20110052656
    Abstract: A process has been found which increases the efficiency and effectiveness of introducing antimicrobial compounds into complex biofilm matrices through the use of liposome carriers, thereby removing the biofouling in industrial water bearing systems, including piping, heat exchanges, condensers, filtration systems and fluid storage tanks. According to one embodiment of the invention, antimicrobial compound containing liposomes are added to water systems prone to biofouling and biofilm formation. The liposomes, being similar in composition to microbial membranes or cells, are readily incorporated into the existing biofilm. Once the antimicrobial compound containing liposomes become entrained with the biofilm matrix, the decomposition or programmed disintegration of the liposome proceeds. Thereafter, the biocidal aqueous core is released to react directly with the biofilm encased microorganisms.
    Type: Application
    Filed: September 28, 2010
    Publication date: March 3, 2011
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Wilson Kurt Whitekettle, Gloria Jean Tafel, Qing Zhao, Linna Wang, Dorothy Reynolds, Paul Frail, Juan Jiang, David M. Polizzotti
  • Therapeutic compounds
    Patent number: 7897629
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: March 1, 2011
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old, Todd S. Gac
  • 5-aryl isoxazolines for controlling invertebrate pests
    Patent number: 7897630
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsufinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22; —S(O)pR25 or —S(O)(?NR28)R29; R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: March 1, 2011
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, Jr., Benjamin Kenneth Smith, Jeffrey Keith Long
  • Methods and compositions for increasing solubility of azole drug compounds that are poorly soluble in water
    Patent number: 7893097
    Abstract: The combination of any two of a polyol, a polyol ether, and a low carbon organic alcohol provides a synergistic effect on the solubility of azole compounds, such as metronidazole, in aqueous fluid.
    Type: Grant
    Filed: February 2, 2008
    Date of Patent: February 22, 2011
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Meidong Yang, Haigang Chen
  • ISOTHIOZOLES FOR TREATING CONDITIONS OF THE EYE
    Publication number: 20110039900
    Abstract: Disclosed herein are isothiozoles for treating conditions of the eye.
    Type: Application
    Filed: August 10, 2010
    Publication date: February 17, 2011
    Inventors: Veena Viswanath, John E. Donello
  • SUBSTITUTED PHENOXYBENZAMIDES
    Publication number: 20110039819
    Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: April 9, 2009
    Publication date: February 17, 2011
    Inventors: Marion Hitchcock, Ingo Hartung
  • Synergistic Microbicidal Compositions
    Publication number: 20110028525
    Abstract: This invention relates to synergistic combinations of selected isothiazolin-3-one microbicides in combination with a second microbicide or formulation ingredient or raw material. The combinations have greater efficacy than would be expected from combinations of the individual components. The combinations include mixtures of (a) Methyl-4-isothiazolin-3-one or (b) 1,2-Benzisothiazolin-3-one with one or more of a variety of other compounds.
    Type: Application
    Filed: July 23, 2010
    Publication date: February 3, 2011
    Inventors: Megan Anne Diehl, Dolores Ann Shaw
  • INDAZOLE DERIVATIVES
    Publication number: 20110028447
    Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.
    Type: Application
    Filed: February 26, 2009
    Publication date: February 3, 2011
    Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
  • Fungicidal agent combinations
    Patent number: 7875593
    Abstract: The invention relates to novel fungicidally active compound combinations of 2?-cyano-3,4-dichloroisothiazole-5-carboxanilide of the formula and active compounds listed in the disclosure.
    Type: Grant
    Filed: October 23, 2007
    Date of Patent: January 25, 2011
    Assignee: Bayer CropScience AG
    Inventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Rolf Pontzen, Wolfram Andersch, Lutz Aβmann
  • Substituted Sulfonic Acid Amide Compounds
    Publication number: 20110015065
    Abstract: The present invention relates to the use of substituted sulfonic acid amide compounds of formula I wherein Ra, n, Het, A, Y and D are as defined in the claims and the N-oxides and the salts thereof for combating phytopathogenic harmful fungi, and to compositions and seeds comprising at least one such compound. The invention also relates to novel substituted sulfonic acid amide compounds and processes for preparing these compounds.
    Type: Application
    Filed: February 10, 2009
    Publication date: January 20, 2011
    Applicant: BASF SE
    Inventors: Jochen Dietz, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Michael Puhl
  • Compounds as cannabinoid receptor ligands
    Patent number: 7872033
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: January 18, 2011
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • STABLE, SYNERGISTIC MIXTURES
    Publication number: 20110009462
    Abstract: The present invention relates to storage-stable, synergistically acting combinations comprising glutaraldehyde (GDA) and 2-methyl-2H-isothiazol-3-one (methylisothiazolinone, MIT) and, where appropriate, 2-bromo-2-nitropropane-1,3-diol (bronopol) and/or other active substances for protecting industrials materials.
    Type: Application
    Filed: October 28, 2008
    Publication date: January 13, 2011
    Applicant: LANXESS DEUTSCHLAND GMBH
    Inventors: Hermann Uhr, Peter Wachtler, Tanja Gerharz, Martin Kugler
  • MICROBICIDAL COMPOSITION
    Publication number: 20110003871
    Abstract: A solid microbicidal composition containing a mixture of 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one, magnesium sulfate, a metal nitrate, magnesium chloride, and water.
    Type: Application
    Filed: June 30, 2010
    Publication date: January 6, 2011
    Inventors: Beverly Jean El A'mma, Randall Wayne Stephens
  • SUBSTITUTED AMIDE BETA SECRETASE INHIBITORS
    Publication number: 20110003825
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Application
    Filed: August 23, 2010
    Publication date: January 6, 2011
    Applicant: Schering Corporation
    Inventors: Ying Huang, Guoqing Li, Andrew W. Stamford
  • Bicyclic derivatives as modulators of voltage gated ion channels
    Patent number: 7855220
    Abstract: Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
    Type: Grant
    Filed: September 8, 2006
    Date of Patent: December 21, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Timothy Neubert, Nicole Zimmermann, Esther Martinborough, Aarti Kawatkar, Andreas Termin
  • METHOD FOR INHIBITING BRASSININ OXIDASE
    Publication number: 20100317703
    Abstract: The present disclosure relates to a method for inhibiting brassinin oxidase comprising treating a pathogen that is producing BO with an effective amount of selected Paldoxin compounds.
    Type: Application
    Filed: June 15, 2010
    Publication date: December 16, 2010
    Applicant: UNIVERSITY OF SASKATCHEWAN
    Inventor: M. Soledade C. Pedras
  • Antimicrobial credit cards, identification cards, membership cards and identification badges and badge holders
    Patent number: 7851517
    Abstract: A system, method and apparatus provices an antimicrobial card, badge holder or token made from an antimicrobial polymereric material. The antimicrobial polymereric material includes one or more polymers and one or more antimicrobial agents that affect the growth of bacteria, fungi, virus or a combination thereof.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: December 14, 2010
    Inventor: Lisa Marie Holmes
  • Active Compound Combinations
    Publication number: 20100311580
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide, CAS No 224049-04-1) and another insecticide flubendiamide (CasNo 272451-65-7) and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Application
    Filed: November 27, 2008
    Publication date: December 9, 2010
    Applicant: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Malononitrile compound as pesticides
    Patent number: 7846956
    Abstract: The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: December 7, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiromasa Mitsudera, Ken Otaka, Jun Fujiwara
  • BIOCIDAL GRANULE, IN PARTICULAR FOR MAKING ASPHALT SHINGLE
    Publication number: 20100303875
    Abstract: The invention relates to biocidal granules composed of a mineral core coated with at least one porous inorganic layer including at least one organic compound capable of limiting or preventing the growth of microorganisms, in particular of algae. The invention also relates to a sol-gel process for the preparation of said biocidal granules and to the use of these biocidal granules in building materials, in particular shingles and siding coatings.
    Type: Application
    Filed: April 4, 2006
    Publication date: December 2, 2010
    Applicant: Saint-Gobain Materiaux De Construction S.A.S.
    Inventors: Sophie Vanpoulle, Christelle Pousse, Lethicia Gueneau, Philippe Barboux
  • Formulations of quaternary ammonium neuromuscular blocking agents
    Patent number: 7838515
    Abstract: Muscle relaxant formulations which include one or more quaternary ammonium neuromuscular blocking agents have a reduced tendency for hydrolytic degradation, and therefore a longer shelf life stability, when combined with one or more organic anions having at least six carbon atoms and having a pKa of less than 4.0 (preferably ranging from 0.5 to 3.5). Particularly good results are achieved when using acids of very low solubility in water, such as gentisic acid which is less than 1% soluble at room temperature.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: November 23, 2010
    Assignee: Lyotropic Therapeutics, Inc.
    Inventor: David M. Anderson
  • 3,5-SUBSTITUTED-1,3-OXAZOLIDIN-2-ONE DERIVATIVES
    Publication number: 20100292241
    Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: January 14, 2009
    Publication date: November 18, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
  • HALOALKYL HETEROARYL BENZAMIDE COMPOUNDS
    Publication number: 20100292274
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: May 11, 2010
    Publication date: November 18, 2010
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • METHODS FOR TREATING HEPATITIS C
    Publication number: 20100292187
    Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 18, 2010
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
  • ISOTHIAZOLIDINE 1,1-DIOXIDE AND TETRAHYDRO-2H-1,2-THIAZINE 1,1-DIOXIDE DERIVATIVES AS P2X7 MODULATORS
    Publication number: 20100292224
    Abstract: The present invention provides a compound of formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents optionally substituted C1-4 alkyl; X represents —(CR10R11)n— in which n represents 1 or 2; R2, R3 and R4 independently represent H, F or Me; and R5; R6; R7; R8 and R9 independently represent hydrogen, halogen, or cyano; or optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkyl, such that at least one of R5 and R9 represents a group other than hydrogen. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prevention of inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis.
    Type: Application
    Filed: December 5, 2008
    Publication date: November 18, 2010
    Applicant: GLAXO GROUP LIMITED
    Inventor: Daryl Simon Walter
  • LIQUID PRESERVATIVE COMPOSITIONS
    Publication number: 20100286218
    Abstract: A liquid preservative composition comprises (a) an alkanol fatty monoester; and (b) an aqueous isothiazolinone solution, an alkanol-substituted aromatic compound, or a combination thereof; and is free from formaldehyde, formaldehyde-releasing compounds, and paraben compounds. Preferred compositions comprise glyceryl caprylate, together with either phenethyl alcohol or an aqueous 2-methyl-4-isothiazolin-3-one solution.
    Type: Application
    Filed: January 23, 2009
    Publication date: November 11, 2010
    Inventors: Kenneth Berg, Teresa Germain
  • STABLE, LOW VOC, LOW VISCOUS BIOCIDAL FORMULATIONS AND METHOD OF MAKING SUCH FORMULATIONS
    Publication number: 20100286217
    Abstract: A stable, low VOC, low viscosity biocide formulation comprising an effective amount of at least one biocide, and a alkyl poly glycol liquid carrier of formula (I): R—O-(AO)n—H, wherein R is a C1-C3 alkyl; AO is an ethyleneoxide group, a propy-leneoxide group, a butyleneoxide group, or a block or random copolymer of two or more groups selected from an ethyleneoxide group, a propyleneoxide group, and a butyleneoxide group; and n is the average number of repeating AO units and is at least 4.
    Type: Application
    Filed: December 2, 2008
    Publication date: November 11, 2010
    Inventors: Ioana Annis, Sheila M. Tinetti, Emerentiana Sianawati, Paul Foley, Suzanne Debruhl, Pierre Marie Lenoir
  • Modulation of Pathogenicity
    Publication number: 20100280036
    Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them
    Patent number: 7825264
    Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: November 2, 2010
    Assignee: sanofi-aventis
    Inventors: Joachim Brendel, Heinrich Christian Englert, Stefan Peukert, Klaus Wirth, Michael Wagner, Jean-Marie Ruxer, Fabienne Pilorge
  • Organic compounds and their uses
    Patent number: 7825152
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: April 9, 2007
    Date of Patent: November 2, 2010
    Assignee: Novartis AG
    Inventors: Trixi Brandl, Jiping Fu, Francois Lenoir, David Thomas Parker, Michael Patane, Branko Radetich, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic, Aregahegn Yifru, Rui Zheng
  • Aminotetraline Derivatives, Pharmaceutical Composition, Containing Them, and Their Use in Therapy
    Publication number: 20100273739
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Substituted enaminones, their derivatives and uses thereof
    Patent number: 7820663
    Abstract: The present invention is related substituted enaminones represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Grant
    Filed: June 15, 2006
    Date of Patent: October 26, 2010
    Assignee: The Regents of the University of California
    Inventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
  • Methods For The Prophylaxis And/or Treatment Of Thromboembolic Disorders By Combination Therapy With Substituted Oxazolidinones
    Publication number: 20100267685
    Abstract: The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.
    Type: Application
    Filed: April 23, 2010
    Publication date: October 21, 2010
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Alexander Straub, Thomas Lampe, Josef Pernerstorfer, Elisabeth Perzborn, Jens Pohlmann, Susanne Röhrig, Karl-Heinz Schlemmer
  • MIF MODULATORS
    Publication number: 20100267714
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Application
    Filed: May 4, 2010
    Publication date: October 21, 2010
    Inventors: William L. Jorgensen, Richard J. Bucala
  • FUNGICIDAL COMPOSITION CONTAINING ACID AMIDE DERIVATIVE
    Publication number: 20100261675
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
  • FUNGICIDAL COMPOSITION CONTAINING ACID AMIDE DERIVATIVE
    Publication number: 20100261735
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
  • Use of Active Substance Combinations for Controlling Animal Pests
    Publication number: 20100248961
    Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.
    Type: Application
    Filed: November 27, 2008
    Publication date: September 30, 2010
    Applicant: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
  • ISOTHIAZOLIN BIODELIVERY SYSTEMS
    Publication number: 20100239650
    Abstract: A biodelivery system has been found which increases the efficiency and effectiveness of introducing antimicrobial compounds into complex biofilm matrices through the use of liposome carriers, thereby removing the biofouling in industrial water bearing systems, including piping, heat exchanges, condensers, filtration systems and fluid storage tanks. According to one embodiment of the invention, antimicrobial compound containing liposomes are added to water systems prone to biofouling and biofilm formation. The liposomes, being similar in composition to microbial membranes or cells, are readily incorporated into the existing biofilm. Once the antimicrobial compound containing liposomes become entrained with the biofilm matrix, the decomposition or disintegration of the liposome proceeds. Thereafter the biocidal core is released to react directly with the biofilm encased microorganisms.
    Type: Application
    Filed: March 20, 2009
    Publication date: September 23, 2010
    Inventors: Wilson Kurt Whitekettle, Gloria Jean Tafel