Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
  • Publication number: 20100261680
    Abstract: The invention relates to herbicidal compositions, their preparation, and their use for controlling unwanted vegetation. The compositions include an effective amount of an active compound combination that includes: (a) a substituted thien-3-yl-sulphonylaminocarbonyltriazolinone of formula (I-2) or salts thereof; and (b) at least one of the known herbicides listed in the disclosure and, (c) optionally a safener.
    Type: Application
    Filed: June 28, 2010
    Publication date: October 14, 2010
    Applicant: Bayer CropScience AG
    Inventors: Dieter FEUCHT, Peter Dahmen, Mark Wilhelm Drewes, Rolf Pontzen, Ernst Rudolf F. Gesing
  • Publication number: 20100261771
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: March 18, 2010
    Publication date: October 14, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiss, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Patent number: 7807690
    Abstract: A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.].
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: October 5, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
  • Publication number: 20100249185
    Abstract: The present invention relates to compounds that inhibit the activity of Hsp90 and inhibit topoisomerase II.
    Type: Application
    Filed: March 11, 2008
    Publication date: September 30, 2010
    Inventors: Zhenjian Du, Minghu Song, Weiwen Ying
  • Patent number: 7799815
    Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidin
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: September 21, 2010
    Assignee: Glaxo Group Limited
    Inventors: Giorgio Bonanomi, Romano Di Fabio, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
  • Publication number: 20100233116
    Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: August 13, 2007
    Publication date: September 16, 2010
    Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Shifeng Liu, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
  • Publication number: 20100222401
    Abstract: Compounds, compositions and methods for inhibiting vascular permeability and pathologic angiogenesis by modulating a signaling pathway delineated herein are described. Moreover, methods for producing and screening compounds and compositions capable of modulating the signaling pathway described herein, inhibiting vascular permeability, and inhibiting pathologic angiogenesis are also provided.
    Type: Application
    Filed: April 16, 2009
    Publication date: September 2, 2010
    Applicant: University of Utah Research Foundation
    Inventors: Dean Li, Christopher Jones, Nyall London
  • Patent number: 7772265
    Abstract: Novel compounds of the formula I in which R, X and n are as defined herein, are inhibitors of tyrosine kinase and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.
    Type: Grant
    Filed: April 1, 2008
    Date of Patent: August 10, 2010
    Assignee: Merck Patent GmbH
    Inventors: Teresa Mujica-Fernaud, Herwig Buchholz, Christophe Carola, Wilfried Rautenberg, Christian Sirrenberg
  • Publication number: 20100197696
    Abstract: The invention relates to compounds of formula wherein Het, A1, A2, A3, A4, D, W, T, Q, Y, X1, X2, R1, R2, R3, R4, k and m are as defined hereinabove, and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, to a process for the preparation of and to the use of those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, to pesticidal compositions in which the active ingredient has been selected from those compounds, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in agrochemically usable salt form, to a process for the preparation of and to the use of those compositions, to plant propagation material treated with those compositions, to a method of controlling pests, to intermediates and, where applicable, to possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form, for the preparation of those compounds, E/Z isomers, m
    Type: Application
    Filed: April 8, 2010
    Publication date: August 5, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Roger Graham Hall, Stephan Trah, Werner Zambach, Juraj Tuleja
  • Publication number: 20100190783
    Abstract: A Compound represented by the following general formula (1): wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc.; R2 represents optionally substituted phenyl, etc.; R3 represents optionally substituted C6-10 aryl, etc.; and Z1 and Z2 each independently represent hydrogen or salts thereof or hydrates of the foregoing.
    Type: Application
    Filed: March 29, 2010
    Publication date: July 29, 2010
    Inventors: Richard CLARK, Fumiyoshi MATSUURA, Kazunobu KIRA, Shinsuke HIROTA, Hiroshi AZUMA, Tadashi NAGAKURA, Tatsuo HORIZOE, Kimiyo TABATA, Kazutomi KUSANO, Takao OMAE, Atsushi INOUE
  • Patent number: 7745469
    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: July 20, 2004
    Date of Patent: June 29, 2010
    Assignee: Bayer CropScience AG
    Inventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Rolf Pontzen, Lutz Aβmann, Haruko Sawada
  • Publication number: 20100160399
    Abstract: The invention relates to a fungicidal mixture comprising prothioconazole or a salt or adduct thereof with an inorganic acid an organic acid or a metal ion; and at least one further fungicidal compound, selected from the group consisting of thiram, fenoxanil, benthivalicarb, metalaxyl, fludioxonil and prochloraz, in a synergistically effective amount and to methods for controlling harmful fungi, comprising applying the fungicidal mixture.
    Type: Application
    Filed: December 17, 2009
    Publication date: June 24, 2010
    Applicant: BASF AKTIENGESSELLSCHAFT
    Inventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Ulrich Schöfl, Siegfried Strathmann, Klaus Schelberger, Thomas Christen
  • Publication number: 20100144725
    Abstract: A method of controlling or preventing pathogenic damage and/or pest damage in a plant propagation material, a plant, part of a plant and/or plant organ that grow at a later point in time, which comprises applying on the plant, part of the plant, plant organ, plant propagation material or a surrounding area thereof a combination comprising (I) one or more of a defined strobilurin compound selected from azoxystrobin, trifloxystrobin and fluoxastrobin, (II) one or more of a defined DMI: triazole compound selected from difenoconazole, prothioconazole, tebuconazole and triticonazole, and (III) one or more further defined fungicide selected fludioxonil, thiabendazole and ipconazole, in any desired sequence or simultaneously, provided the combination does not consist essentially of azoxystrobin, tebuconazole and fludioxonil.
    Type: Application
    Filed: March 1, 2008
    Publication date: June 10, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Franz Brandl, Ronald Zeun, Michael Oostendorp
  • Patent number: 7732374
    Abstract: A fungicidal mixture comprising prothioconazole or its salts or adducts and at least one insecticide selected from the group consisting of fipronil, chlorpyrifos or thiamethoxam.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: June 8, 2010
    Assignee: BASF SE
    Inventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, V. James Spadafora, Thomas Christen
  • Patent number: 7713970
    Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: May 11, 2010
    Assignee: FMC Corporation
    Inventors: Edward J. Barron, Larry Y. Zhang, John W. Lyga, Matthew P. Whiteside
  • Publication number: 20100113447
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: August 10, 2009
    Publication date: May 6, 2010
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20100105559
    Abstract: An agrochemical composition includes a homogeneous single-phase liquid crystal in thermodynamic equilibrium. The agrochemical composition can be a surfactant composition or a pesticide composition. The surfactant composition is a blend of surfactants, whereas a pesticide composition has an active ingredient and one or more surfactant adjuvants. A pesticide composition, or a surfactant composition in combination with an active ingredient, may be used to control pests.
    Type: Application
    Filed: October 9, 2007
    Publication date: April 29, 2010
    Applicant: Huntsman Petrochemical Corporation
    Inventors: Curtis M. Elsik, Joe C. Arzola, Howard M. Stridde, Alan Stern
  • Publication number: 20100105669
    Abstract: The present invention relates to a composition containing (A) at least one specific carbamate fungicide, (B) at least one specific insecticide and optionally (C) at least one azole, the use of this composition for improving plant health and a method for improving plant health by treating a plant, its propagules or the locus where the plant is growing or is to grow with the above composition.
    Type: Application
    Filed: February 5, 2008
    Publication date: April 29, 2010
    Applicant: BASF SE
    Inventors: Dirk Voeste, Egon Haden, Marco-Antonio Tavares-Rodrigues, Edson Begliomini
  • Publication number: 20100099725
    Abstract: The present invention is directed to compounds of the structural Formula: wherein: R1 is H or —C1-C3 alkyl; R2 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, CH2—C?CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R1 and R2 are each H, then R3 is selected from the group consisting of —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, —CH2—C?CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: February 12, 2008
    Publication date: April 22, 2010
    Inventors: Lance Allen Pfeifer, Tianwei Ma, Nathan Bryan Mantlo, Laura Frey Michael, Fese Mambo Mokube, Chahrzad Montrose-Rafizadeh
  • Publication number: 20100093717
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of treating or inhibiting angiogenesis in a subject in need thereof and methods for blocking, occluding, or otherwise disrupting blood flow in neo vasculature, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 14, 2007
    Publication date: April 15, 2010
    Inventors: Weiwen Ying, Kevin Foley
  • Patent number: 7683087
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: March 23, 2010
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Martha de la Rosa, Zhi Hong, Stanley Lang
  • Patent number: 7683086
    Abstract: The invention relates to a fungicidal mixture that comprises (1) 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazolo-3-thion (prothioconazole) or the salts or adducts thereof and at least one further fungicidal composition, selected from (2) boscalid or (3) carboxine or (4) metrafenone or (5) a compound of formula (V) or (6) a compound of formula (VI) or (7) quinoxyfen or (8) dithianon or (9) thiram or (10) mepiquat chlorides or (11) cyazofamid or (12) fenoxanil or (13) a compound of formula (XIII) or (14) thiophanate methyl or (15) carbendazim or (16) metalaxyl or (17) fludioxonil or (18) thiabendazole or (19) quintozene or (20) prochloraz or (21) anthraquinone in a synergistically effective amount.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: March 23, 2010
    Assignee: BASF Aktiengesellschaft
    Inventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Ulrich Schöfl, Siegfried Strathmann, Klaus Schelberger, Thomas Christen
  • Publication number: 20100063039
    Abstract: Process for the protection of fish and invertebrates and all their stages of development against or for the treatment of mycoses caused by fungi of the genera Saprolegnia, Aphanomyces, Achlyaflagellata and other species important in aquacultures by use of 2-[[[[1-[3-(1-fluoro-2-phenylethyl)oxy]phenyl]ethylidene]amino]oxy]methyl]alpha-(methoxyimino)-N-methyl-alphaE-benzeneacetamide, amisulbrom, cyazofamid, enestrobin, famoxadone, fenamidone, fluoxastrobin, orysastrobin, picoxystrobin and pyribencarb. This use leads to an inhibition or destruction of pathogenic fungi. The composition, comprising at least one fungicide selected from the abovementioned group for use in fish farming and keeping is suitable for the prophylaxis and therapy of diseases of fish in aquaculture, in breeding ponds, breeding tanks, aquariums, natural stretches of game fish waters, ponds, and marine fish farms. Addition to the water and feed and direct application are the associated use forms.
    Type: Application
    Filed: April 8, 2008
    Publication date: March 11, 2010
    Inventors: Isolde Häuser-Hahn, Klaus Stenzel, Ulrike Wachendorff-Neumann
  • Publication number: 20100056464
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: September 3, 2009
    Publication date: March 4, 2010
    Applicant: Ardea Biosciences
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Publication number: 20100056465
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: September 4, 2009
    Publication date: March 4, 2010
    Applicant: Ardea Biosciences
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Publication number: 20100056526
    Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of circulatory diseases, metabolic diseases and/or central nervous system diseases.
    Type: Application
    Filed: November 21, 2007
    Publication date: March 4, 2010
    Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa
  • Publication number: 20100048594
    Abstract: The invention relates to compounds selected from among the group comprising general formulas (1), (2), (3), and/or (4) and/or the enantiomers, diastereomers, and derivatives thereof, and the pharmaceutically acceptable salts thereof for producing a medicament used for therapeutically and/or preventively treating disease and pathological conditions linked to regulation of the insulin and/or insulin-like growth factor (IGF) signalling pathway and/or for chemically inducing longevity.
    Type: Application
    Filed: November 14, 2007
    Publication date: February 25, 2010
    Applicant: RHEINISCHE FRIEDRICH-WILHELMS UNIVERSITAT
    Inventors: Michael Famulok, Markus Hafner, Anton Schmitz, Bernhard Fuss, Ingo Zinke, Michael Hoch
  • Patent number: 7666891
    Abstract: The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficiency virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficiency virus containing a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: February 23, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
  • Patent number: 7662813
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: February 16, 2010
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Elena Kostik, Junghyun Chae, Howard P Ng, Zhenjian Du, James Barsoum, Dinesh Chimmanamada, Chi-Wan Lee, Kevin Foley
  • Publication number: 20100022540
    Abstract: Novel triazole derivatives of the formula (I) in which R1—R6 and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Application
    Filed: April 20, 2007
    Publication date: January 28, 2010
    Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
  • Patent number: 7652051
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Publication number: 20100016392
    Abstract: In one aspect, this invention relates to a substantially water-insoluble pesticidal aggregate produced from a mixture comprising: (a) a polymer having at least three similarly charged electrostatic moieties; (b) an amphiphilic surfactant having at least one electrostatically charged moiety of opposite charge to the polymer; and (c) a pesticide. In other aspects, this invention relates pesticidal compositions comprising such a pesticidal aggregate and an agriculturally acceptable carrier, as well as to a method of controlling pests using such pesticidal compositions.
    Type: Application
    Filed: December 13, 2007
    Publication date: January 21, 2010
    Applicant: Innovaform Technologies, LLC
    Inventors: Alexander V. Kabanov, Michael Karas, Tatiana K. Bronitch, Robin Dexter
  • Publication number: 20090312381
    Abstract: The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.
    Type: Application
    Filed: May 21, 2007
    Publication date: December 17, 2009
    Applicant: BAYER HEALTHCARE AG
    Inventors: Heinrich Meier, Eckhard Bender, Ulf Brüggemeier, Ingo Flamme, Dagmar Karthaus, Peter Kolkhof, Daniel Meibom, Dirk Schneider, Verena Voehringer, Chantal Fürstner, Jörg Keldenich, Dieter Lang, Elisabeth Pook, Carsten Schmeck
  • Publication number: 20090291967
    Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.
    Type: Application
    Filed: March 5, 2009
    Publication date: November 26, 2009
    Applicant: ADHEREX TECHNOLOGIES, INC.
    Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
  • Patent number: 7618971
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 27, 2005
    Date of Patent: November 17, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, George D. Hartman, John Schreier
  • Publication number: 20090274632
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: August 19, 2008
    Publication date: November 5, 2009
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Publication number: 20090264474
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Application
    Filed: July 18, 2008
    Publication date: October 22, 2009
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Publication number: 20090239748
    Abstract: The present invention relates to fungicidal mixtures comprising, as active components, 1) at least one 2,5-disubstituted N-biphenylpyrazolecarboxamide of the formula I in which X=oxygen or sulfur; R1 and R2=cyano, nitro, halogen, C1-C6-alkyl, C1-C6-haloalkyl, methoxy, difluoromethoxy or trifluoromethoxy; R3=halogen, C1-C4-alkyl or C1-C4-haloalkyl; R4=hydrogen or halogen; and 2) at least one active compound II selected from groups A) to F): A) azoles; B) strobilurins; C) carboxamides; D) heterocyclic compounds; E) carbamates; F) other fungicides; in a synergistically effective amount, methods for controlling harmful fungi using mixtures of at least one compound I and at least one active compound II, the use of the compound(s) I with active compounds II for preparing such mixtures and also compositions and seed comprising these mixtures.
    Type: Application
    Filed: June 28, 2006
    Publication date: September 24, 2009
    Applicant: BASF Aktiengesellschaft
    Inventors: Jochen Dietz, Markus Gewehr, Siegfried Strathmann, Reinhard Stierl, Frank Werner, Maria Scherer
  • Publication number: 20090227640
    Abstract: The present application relates to novel heterocyclic compounds, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: October 9, 2006
    Publication date: September 10, 2009
    Applicant: BAYER HEALTHCARE AG
    Inventors: Stephan Bartel, Michael Hahn, Wahed Ahmed Moradi, Klaus Münter, Thomas Rölle, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder
  • Publication number: 20090215775
    Abstract: Compounds of formula (I) are disclosed for treatment of cancer.
    Type: Application
    Filed: May 16, 2006
    Publication date: August 27, 2009
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Publication number: 20090197825
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 26, 2008
    Publication date: August 6, 2009
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20090192205
    Abstract: A process for the release of a biologically active species comprising the steps of: providing a mesoporous oxide-based material having structural order and at least one level of porosity; fixing or immobilizing said biologically active species in said ordered mesoporous oxide; and providing said ordered mesoporous oxide with said fixed or immobilized biologically active species in vivo thereby realizing intraluminally induced substantially pH-independent supersaturation of said biologically active species resulting in enhanced transepithelial transport; wherein said biologically active species is a poorly soluble therapeutic drug classified as belonging to Class II or Class IV of the Biopharmaceutical Classification System and said ordered mesoporous oxide has a pore size in the range of 4 to 14 nm.
    Type: Application
    Filed: January 28, 2009
    Publication date: July 30, 2009
    Applicant: Katholieke Universiteit Leuven K.U. Leuven R&D
    Inventors: Patrick AUGUSTIJNS, Johan Adriaan Martens, Randy Mellaerts, Guy Van Den Mooter
  • Publication number: 20090156560
    Abstract: Disclosed herein are compounds that are tissue-nonspecific alkaline phosphatase inhibitors. The disclosed compounds are used to treat, prevent, or abate vascular calcification, arterial calcification and other cardiovascular diseases.
    Type: Application
    Filed: May 8, 2008
    Publication date: June 18, 2009
    Inventors: JOSE LUIS MILLAN, EDUARD SERGIENKO
  • Publication number: 20090143416
    Abstract: A method of inducing tolerance of plants against bacterioses which comprises treating the plants, the soil or seeds with an effective amount of a combination of a compound of the formula I in which X is halogen, alkyl or trifluoromethyl; m is 0 or 1; Q is C(?CH—CH3)—COOCH3, C(?CH—OCH3)—COOCH3, C(?N—OCH3)—CONHCH3, C(?N—OCH3)—COOCH3, N(—OCH3)—COOCH3, or a group Q1 ?wherein # denotes the bond to the phenyl ring; A is —O—B, —CH2O—B, —OCH2—B, —CH2S—B, —CH?CH—B, —C?C—B, —CH2O—N?C(R1)—B, —CH2S—N?C(R1)—B, —CH2O—N?C(R1)—CH?CH—B, or —CH2O—N?C(R1)—C(R2)?N—OR3, where B is phenyl, naphthyl, 5- or 6-membered hetaryl or 5- or 6-membered heterocyclyl, containing one to three N atoms and/or one O or S atom or one or two O and/or S atoms, the ring systems being unsubstituted or substituted as defined in the description; R1 is hydrogen, cyano, alkyl, haloalkyl, cycloalkyl, alkoxy, or alkylthio; R2 is phenyl, phenylcarbonyl, phenylsulfonyl, 5- or 6-membered hetaryl, 5- or 6-membered hetarylcarbonyl or 5- or 6-membere
    Type: Application
    Filed: March 6, 2007
    Publication date: June 4, 2009
    Inventors: Harald Kohle, Ted R. Bardinelli, Marco-Antonio Tavares-Rodrigues
  • Publication number: 20090131438
    Abstract: A compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof has an effect of inhibiting binding between S1P and its receptor Edg-1(S1P1), and is useful as a pharmaceutical product. [where A represents a sulfur atom, an oxygen atom, a formula —SO— or a formula —SO2—; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; R2 represents an alkyl group having 1 to 6 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms or the like; R3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a phenyl group or the like; R5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; and R6 represents an alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group].
    Type: Application
    Filed: August 4, 2005
    Publication date: May 21, 2009
    Applicant: Taisho Pharmaceutical Co., Ltd
    Inventors: Naoya Ono, Masakazu Sato, Fumiyasu Shiozawa, Makoto Yagi, Tetsuya Yabuuchi, Tetsuo Takayama, Hironori Katakai
  • Publication number: 20090131462
    Abstract: The invention relates to a fungicidally active agent containing at least one other defined fungicide in addition to the fungicide N-[2-(1,3-dimethylbutyl)-3-thienyl]-1-methyl-3-(trifluormethyl)-1H-pyrazol-4-carboxamide (penthiopyrad). The invention also relates to a method for controlling pathogenic fungi using one such agent, and to the use of said agent for controlling pathogenic fungi.
    Type: Application
    Filed: July 21, 2006
    Publication date: May 21, 2009
    Applicant: BASF AKTIENGESELLSCHAFT
    Inventors: Markus Gewehr, Reinhard Stierl, Horst Dieter Brix, Thomas Grote, Siegfried Strathmann, Maria Scherer, Frank Werner
  • Publication number: 20090124679
    Abstract: The present invention provides a fungicide composition having stable and high harmful bio-organism control effect on crop plants infected with plant diseases due to plant diseases. Specifically, the present invention provides a fungicide composition for agricultural or horticultural use, which comprises: (a) an indole compound represented by formula (I): wherein R1 and R2 each independently represents C1-4 alkyl, etc.; Y represents H, halogen, etc.; R3 and R4 each independently represents a hydrogen atom, alkyl, etc.; R5, R6, R7 and R8 each independently represents a hydrogen atom, alkyl, etc., and (b) at least other fungicide selected from the group consisting of Dimethomorph, Chlorothalonil, a copper compound, Iprovalicarb, Zoxamide, phosphorous acid or a salt thereof, Fluazinam, Cyazofamid, Flumorph, Benthiavalicarb-isopropyl, Ethaboxam, Methalaxyl-M and Benalaxyl-M.
    Type: Application
    Filed: October 21, 2005
    Publication date: May 14, 2009
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventor: Shigeru Mitani
  • Patent number: 7531566
    Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.
    Type: Grant
    Filed: January 20, 2006
    Date of Patent: May 12, 2009
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Peter A. Petillo
  • Publication number: 20090111857
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Application
    Filed: October 24, 2008
    Publication date: April 30, 2009
    Applicant: AstraZeneca AB
    Inventors: Peter DOVE, Kenneth Granberg, Methvin Isaac, Mats Nagard, Abdelmalik Slassi
  • Patent number: 7524863
    Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: April 28, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joanne M. Smallheer, Donald J. Pinto, Shuaige Wang, Jennifer X. Qiao, Wei Han, Zilun Hu