At 3-position Patents (Class 514/355)
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100160363Abstract: The present invention provides matrix-forming, sustained-release pharmaceutical formulations comprising four primary components: i) an effective amount of at least one drug substance; ii) at least one pharmaceutically acceptable, water-swellable, pH independent polymer; iii) at least one pharmaceutically-acceptable, anionic, pH dependent polymer; and (iv) a pharmaceutically-acceptable polymer selected from the group consisting of a) at least one pharmaceutically-acceptable cationic polymer; and b) at least one pharmaceutically acceptable hydrocolloid. The present formulations can be used with compounds having a wide range of solubilities as well as compounds characterized as having hydrophobic or hydrophilic characteristics.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Applicant: AAIPHARMA SERVICES CORP.Inventors: John R. Cardinal, Jack Lawrence James, Elsie Melsopp, David M. Oakley
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Patent number: 7732467Abstract: The present invention provides methods for reducing ?-amyloid deposition, ?-amyloid neurotoxicity and microgliosis in animals or humans afflicted with a cerebral amyloidogenic disease, such as Alzheimer's disease (AD), by administering therapeutically effective amounts of the dihydropyridine calcium channel antagonist, nilvadipine. The present invention also provides methods for diagnosing cerebral amyloidogenic diseases in animals or humans. Further provided are methods for reducing the risk of ?-amyloid deposition, ?-amyloid neurotoxicity and microgliosis in animals or humans suffering from traumatic brain injury by administering nilvadipine immediately after the traumatic brain injury and continuing treatment for a prescribed period of time thereafter.Type: GrantFiled: May 17, 2004Date of Patent: June 8, 2010Assignee: Alzheimer's Institute of America, Inc.Inventors: Michael J. Mullan, Daniel Paris
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Publication number: 20100137375Abstract: An emulsifiable concentrate (EC) formulation, comprising a) a phenylsemicarbazone compound of the formula (I), where R1 and R2 are, independently of one another, hydrogen, cyano, halogen, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy and R3 is C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, or an agriculturally acceptable salt thereof, b) a solvent system, comprising b1) ?-butyrolactone, b2) one or more aliphatic and/or aromatic ketones, and b3) optionally one or more aromatic hydrocarbons c) one or more emulsifiers, d) optionally, further formulation additives, has a high storage stability and excellent performance against insect pests.Type: ApplicationFiled: August 8, 2006Publication date: June 3, 2010Applicant: BASF SEInventor: Charles W. Finch
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Patent number: 7723371Abstract: The invention relates to a fungicidally active compound of the general Formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.Type: GrantFiled: November 13, 2006Date of Patent: May 25, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Harald Walter, Camilla Corsi, Josef Ehrenfreund, Hans Tobler
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Publication number: 20100120870Abstract: Soluble granule pesticidal compositions comprise Flonicamid, a dispersant, and a wetting agent are disclosed.Type: ApplicationFiled: April 13, 2005Publication date: May 13, 2010Inventor: Hong Liu
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Publication number: 20100119542Abstract: The present invention is directed to N-methylnicotinamide containing food extracts, and their use in treating lipoprotein abnormalities and skin diseases and disorders.Type: ApplicationFiled: December 8, 2009Publication date: May 13, 2010Inventor: Jerzy Gebicki
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Publication number: 20100120616Abstract: The invention relates to pesticidal mixtures comprising as active compounds 1) at least one cyanosulfoximine compound I of the formula (I) wherein R1, R2 and G are defined in the description; and 2) at least one active compound II selected from a group A comprising acteylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acetylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channel blockers, inhibitors of the lipid synthesis and other compounds as defined in the description, in synergistically gistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes in and on plants, and for protecting such plants being infested with pests and also for protecting seeds.Type: ApplicationFiled: March 18, 2008Publication date: May 13, 2010Inventors: Delphine Breuninger, Henricus Maria Martinus Bastiaans, Wolfgang Von Deyn, Juergen Langewald
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Publication number: 20100120871Abstract: Hair care compositions, methods, and articles of commerce that can increase the appearance of thicker and fuller hair. Such compositions can be applied to any areas where a thicker and fuller hair appearance is desired, such as the scalp or face. The present invention also relates to methods of marketing such compositions.Type: ApplicationFiled: November 9, 2009Publication date: May 13, 2010Inventors: Thomas Larry Dawson, JR., Robert Scott Youngquist
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Publication number: 20100113269Abstract: The present invention relates to a controlled release granule technology, methods of preparing such a granule and methods for using the granule in the control of pests.Type: ApplicationFiled: July 20, 2007Publication date: May 6, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andrew Pearson, Victor Chow, Johnny Reynolds, James Swanson
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Patent number: 7709506Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: August 7, 2006Date of Patent: May 4, 2010Assignee: GlaxoSmithkline LLCInventors: Nicola Mary Aston, Paul Bamborough, Ann Louise Walker
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Patent number: 7709478Abstract: The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.Type: GrantFiled: June 3, 2004Date of Patent: May 4, 2010Assignee: sanofi-aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart
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Publication number: 20100105742Abstract: A pearlescent liquid cosmetic composition and process for preparation is provided herein. The composition includes 14-25% of a C12-C22 fatty acid; 0.1-1.8% of an alkali metal C12-C22 fatty acid soap by weight of the composition; 0.1-10% niacinamide; and 20-85% water. The lustre effect is achieved by careful control of the level of alkali metal hydroxide used to neutralize the fatty acid.Type: ApplicationFiled: September 18, 2009Publication date: April 29, 2010Applicant: CONOPCO, INC., D/B/A UNILEVERInventors: Lei Huang, Bijan Harichian, Shanling Shi
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100087494Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: February 21, 2008Publication date: April 8, 2010Inventors: Pierre-Yves Coqueron, Rudiger Fischer, Oliver Gaertzen, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Klaus Kunz, Darren Mansfield, Amos Mattes, Oswald Ort, Philippe Desbordes
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Publication number: 20100080847Abstract: This invention relates to a medicinal composition, which rapidly disintegrates when taken in the oral cavity and shows sufficient hardness upon production, distribution and use in usual manner, can be obtained by adding, to a sugar alcohol and/or saccharide, a sugar alcohol and/or saccharide having a lower melting point than the first-mentioned sugar alcohol and/or saccharide and then subjecting the resulting powder to combined processing of compression and heating. This invention can provide medicinal compositions, which rapidly disintegrate when taken in the oral cavity without water and are excellent in handling ease owing to exhibition of sufficient hardness upon their production, transportation and use in usual manner, and can also provide a process for the production of the medicinal compositions, which is simpler and can avoid contact between an active ingredient and water as needed.Type: ApplicationFiled: December 4, 2009Publication date: April 1, 2010Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Hiroaki Nakagami, Yoshio Kuno
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Publication number: 20100075942Abstract: The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).Type: ApplicationFiled: January 12, 2006Publication date: March 25, 2010Applicant: ASTRAZENECA ABInventors: Keith Hopkinson Gibson, Elaine Sophie, Elizabeth Stokes, Michael James Waring, David Michael Andrews, Zbigniew Stanley Matusiak, Mark Maybury, Craig Anthony Roberts
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Patent number: 7683086Abstract: 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: GrantFiled: March 19, 2003Date of Patent: March 23, 2010Assignee: BASF AktiengesellschaftInventors: Eberhard Ammermann, Reinhard Stierl, Gisela Lorenz, Ulrich Schöfl, Siegfried Strathmann, Klaus Schelberger, Thomas Christen
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Publication number: 20100063105Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.Type: ApplicationFiled: October 18, 2006Publication date: March 11, 2010Applicant: UCB SAInventors: Neil S. Cutshall, Kraig M. Yager
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Publication number: 20100056469Abstract: Pesticidal mixtures comprising aminothiazoline compounds The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one aminothiazoline compound I of the Formula (I) wherein R1, R2, R3, R4, R5 and R6 are defined in the description; and 2) at least one active compound II selected from a group A comprising acetylcholine esterase inhibitors, GABA-gated chloride channel antagonists, sodium channel modulators, nicotinic acetylcholine receptor agonists/antagonists, chloride channel activators, juvenile hormone mimics, compounds affecting the oxidative phosphorylation, inhibitors of the chitin biosynthesis, moulting disruptors, inhibitors of the MET, voltage-dependent sodium channelblockers, inhibitors of the lipidsynthesis and other compounds as defined in the description, in synergistically effective amounts.Type: ApplicationFiled: February 22, 2008Publication date: March 4, 2010Inventors: Jürgen Langewald, Markus Kordes, Deborah L. Culbertson, Douglas D. Anspaugh
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Publication number: 20100056489Abstract: A method for treating a patient suffering from neuropathic pain, comprising administering to a patient in need of such treatment an effective amount of an agonist drug capable of binding to the neuronal nicotinic receptor (NNR) but which does not readily cross the blood-brain barrier.Type: ApplicationFiled: September 25, 2009Publication date: March 4, 2010Inventors: LYNNE E. RUETER, Kathy L. Kohlhaas
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Publication number: 20100041715Abstract: The invention provides certain well-defined benzamides that are useful as sphingosine-1-phosphate antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: August 12, 2009Publication date: February 18, 2010Applicant: ALLERGAN, INC.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
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Publication number: 20100040662Abstract: Fixation devices for tissue repair, for example sutures, surgical arrows, staples, darts, bolts, screws, buttons, anchors, nails, rivets, or barbed devices comprise at least one of angiogenic material; angiogenic precursor material which is capable of breaking down in vivo to form angiogenic material; or tissue-engineered material, which tissue-engineered material is capable of producing angiogenic material. In a preferred form, the material is incorporated into a polymer matrix having predetermined hydrophobicity to allow controlled release of angiogenic materials such as butyric or hydroxybutyric acid or salts thereof. Polymer matrix compositions comprising angiogenic materials and methods for tissue repair are also provided.Type: ApplicationFiled: June 15, 2009Publication date: February 18, 2010Inventors: Nicholas J. Cotton, Emma J. Wright, Steven W. Astorino, Saad Ali
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Publication number: 20100041641Abstract: The invention concerns the use an mGluR modulator, e.g. an mGluR5 modulator, for the treatment, prevention or delay of progression of cognitive dysfunction.Type: ApplicationFiled: September 10, 2007Publication date: February 18, 2010Inventors: Glatthar Ralf, Donald Johns, Daniel Umbricht
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Publication number: 20100034902Abstract: The present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity and related conditions. In particular, the present invention provides methods for measuring, detecting, diagnosing, treating, and researching salt sensitivity through measuring aberrant red blood cell based potassium efflux levels. In addition, the present invention provides methods for treating conditions involving salt sensitivity (e.g., hypertension), preventing the onset of conditions involving salt sensitivity, identifying individuals at risk for developing salt sensitivity and related conditions, identifying new types of treatment for salt sensitivity and related conditions, and evaluating the effectiveness of treatments for conditions involving salt sensitivity (e.g., hypertension).Type: ApplicationFiled: January 17, 2008Publication date: February 11, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Maria Carolina Delgado, Bertram Pitt
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Publication number: 20100029647Abstract: 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)-substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. The 3,4(,5)-substituted tetrahydropyridine compounds have the formula I wherein the substituents and symbols are as described in the specification.Type: ApplicationFiled: January 12, 2006Publication date: February 4, 2010Inventors: Keiichi Masuya, Osamu Irie, Atsuko Nihonyanagi, Atsushi Toyao, Takanori Kanazawa
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Publication number: 20100029652Abstract: The invention provides a method of treating hepatitis C, by providing compound of Formula I (shown below) in combination with a second active agent to a patient infected with the hepatitis C virus. Also provided herein are pharmaceutical combinations comprising a compound of Formula I and a second active agent. The pharmaceutical combination may be a unit dosage form or a packaged pharmaceutical composition. Packaged pharmaceutical combinations include a compound of Formula I and a second active agent in a package with instructions for using the formulation to treat a hepatitis C infection.Type: ApplicationFiled: December 17, 2007Publication date: February 4, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Mingjun Huang, Joanne Fabrycki, Wengang Yang, Xingtie Nie, Avinash Phadke, Milind Deshpande
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Publication number: 20100016377Abstract: The use of 6-(S-Cyclopropylcarbamoyl-S-fluoro-2-methyl-phenyl)-N-(2,2-dimethylproyl)-nicotinamide, which is known in the art as a p38 kinase inhibitor in the treatment or prophlaxis of one or more psychiatric disorders.Type: ApplicationFiled: June 13, 2007Publication date: January 21, 2010Inventors: Mauro Corsi, Isidore Faiferman, Emilio Merlo Pich, Emiliangelo Ratti, Paul Bryan Wren
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Publication number: 20100010012Abstract: The present invention relates to modulators of metalloproteinase activity.Type: ApplicationFiled: May 14, 2009Publication date: January 14, 2010Applicant: WyethInventors: Phaik-Eng Sum, Jerauld Stanley Skotnicki, Steve Yik-Kai Tam, Tarek Suhayl Mansour, David Brian How, Joshua James Sabatini, Jason Shaoyun Xiang, Eric Feyfant
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Publication number: 20100004296Abstract: A waterborne topical composition is designed specifically to address the treatment of acne vulgaris, rosacea, seborrheic dermatitis and other skin conditions. The composition contains effective amounts of essential components azelaic acid, niacinamide, and glycerin to create a rapidly penetrating and non-irritating compound.Type: ApplicationFiled: June 17, 2009Publication date: January 7, 2010Inventor: Christopher J. Dannaker
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Patent number: 7635788Abstract: Compounds of the formula: are described in which Z, Q, X, L, m and n assume the meanings stated in the description. The compounds (I) inhibit the production of TNF ? and may thus be useful in the treatment of inflammation and pathological conditions involving overproduction of said cytokine. They furthermore exhibit significant inhibitory activity on the proliferation of tumour cells and may thus be used for the treatment and/or prevention of tumorous, neurodegenerative or autoimmune disorders.Type: GrantFiled: June 7, 2005Date of Patent: December 22, 2009Assignee: Italfarmaco SpAInventors: Massimo Pinori, Rocco Mazzaferro, Paolo Mascagni
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Publication number: 20090306003Abstract: An improved pesticide delivery system is disclosed. The system is based on a microblend comprising (a) an amphophilic compound containing at least one hydrophilic group and at least one hydrophobic group and (b) a second compound. Compositions based on the microblend and methods of using the compositions to control pests are also disclosed.Type: ApplicationFiled: January 10, 2007Publication date: December 10, 2009Applicant: Innovation Technologies, LLCInventors: Alexander V. Kabanov, Tatiana K. Bronitch, Michael Karas, Bruce L. Frank
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Publication number: 20090306061Abstract: A method of combating phytopathogenic diseases on crop plants which comprises applying to the crop plants or the locus thereof being infested with said phytopathogenic disease an effective amount of a combination of a) 2-[?-{[(?-methyl-3-trifluoromethyl-benzyl)imino]-oxy}-o-tolyl]-glyoxalic acid methyl ester-O methyloxime (I) in association with b) a broad variety of other plant fungicides is particularly effective in combating or preventing diseases of crop plants. These combinations exhibit synergistic fungicidal activity.Type: ApplicationFiled: August 19, 2009Publication date: December 10, 2009Inventors: René Zurflüh, Neil Leadbitter
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Publication number: 20090304815Abstract: The invention relates to a method of treatment for muscular dystrophies, including Duchenne, Becker, limb-girdle, facioscapulohumeral, congenital muscular dystrophies and the like using a combination of nitric oxide-releasing and anti-inflammatory compounds.Type: ApplicationFiled: February 1, 2007Publication date: December 10, 2009Inventors: Giulio Cossu, Emilio Clementi, Silvia Brunelli
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Patent number: 7612103Abstract: Compounds of formula wherein R1 and R1? are hydrogen or deuterium, R2, R3 and R4 are hydrogen or deuterium, R5 is the residue of an amino acid, X is S or N-ALK, is piperidinyl or tetrahydropyridinyl, ALK is (C1-4)alkyl, and R6 is hydrogen, hydroxy or (C2-12)acyloxy, and their use as antimicrobials.Type: GrantFiled: July 23, 2003Date of Patent: November 3, 2009Assignee: Nabriva Therapeutics AGInventors: Heinz Berner, Gabriele Kerber
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Publication number: 20090264289Abstract: The invention relates to the use of arylcarbonic acid biphenylamides of formula (I) wherein X is halogen or methyl; n is zero, 1 or 2; Y is cyano, nitro, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-halo-alkoxy, C1-C4-alkylthio, C1-C4-haloalkylthio, C1-C4-alkoxy-iminomethyl or allyloxy-iminomethyl; m is zero to 5; Ar is an aryl radical of the formula IIa, IIb or IIc wherein R1 is hydrogen, halogen, C1-C4-alkyl or C1-C4-haloalkyl, R2 is C1-C4-alkyl, R3 is hydrogen, halogen or methyl, R4 is hydrogen, halogen or C1-C4-alkyl, R5 is C1-C4-alkyl or C1-C4-haloalkyl, Z is CH or N and R6 is halogen, C1-C4-alkyl or C1-C4-haloalkyl, for seed treatment for protecting plants after germination from the attack of foliar phytopathogenic fungi and corresponding methods of seed treatment for protecting plants after germination from the attack of foliar phytopathogenic fungi.Type: ApplicationFiled: May 2, 2007Publication date: October 22, 2009Applicant: BASF SEInventors: Jochen Dietz, Siegfried Strathmann, Reinhard Stierl, Jurith Montag
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Publication number: 20090258887Abstract: The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxy, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.Type: ApplicationFiled: September 14, 2006Publication date: October 15, 2009Inventors: Raphael Beumer, Jochen Klock, Stefan Martin Stoeckli
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Publication number: 20090258912Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: November 21, 2006Publication date: October 15, 2009Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Pierre Genix, Alain Villier, Marie-Claire Grosjean-Cournoyer
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Patent number: 7589089Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: August 23, 2007Date of Patent: September 15, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Emmanuel Pinard
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Patent number: 7589232Abstract: The present invention is related to alkynyl aryl carboxamides of Formula (I?) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia-hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I?) to modulate, notably to inhibit the activity of PTPs. (I?) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy? is an aryl, which may optionally be fused by a 3-8 membered cycloalkyl. R1 and R2 are independently from each other is selected from the group consisting of hydrogen or (C1-C6)alkyl. R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy.Type: GrantFiled: July 20, 2004Date of Patent: September 15, 2009Assignee: Laboratories Serono S.A.Inventors: Dominique Swinnen, Patrick Gerber, Jerome Gonzalez, Agnes Bombrun, Catherine Jorand-Lebrun
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Publication number: 20090227563Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: September 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
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Publication number: 20090221651Abstract: A method of preventing HIV-1 associated dendritic pathology in a brain cell, comprising contacting the cell with a therapeutically effective dose of a mitochondrial ATP-sensitive potassium channel agonist. A method of preventing HIV-1 associated dendritic pathology in a brain cell, comprising contacting the cell with a therapeutically effective dose of an inhibitor of succinate dehydrogenase. A method of preventing HIV-1 associated dendritic pathology in a brain cell, comprising contacting the cell with a therapeutically effective dose of a stimulator of production of reactive oxygen species. A model for the study of HIV-1 associated dendritic pathology, comprising a) contacting a hippocampal slice with platelet-activating factor; and b) stimulating the hippocampal slice of a) with high frequency stimulation.Type: ApplicationFiled: October 30, 2006Publication date: September 3, 2009Inventors: Matthew J. Bellizzi, Shao-Ming Lu, Harris A. Gelbard
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Publication number: 20090215838Abstract: The invention describes compositions and kits comprising at least one organic nitric oxide enhancing salt of an angiotensin ? antagonist, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia.Type: ApplicationFiled: March 9, 2006Publication date: August 27, 2009Applicant: NitroMed, Inc.Inventors: David S. Garvey, Xiong Cai, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 7579367Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: September 11, 2006Date of Patent: August 25, 2009Assignee: Purdue Pharma L.P.Inventors: Bin Shao, R. Richard Goehring, Samuel F. Victory
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Publication number: 20090197924Abstract: 2-amino-2-phenyl-alkanol ester derivatives of general formula (I) in which: R1 is H, straight or branched 1 to 4C alkyl, straight or branched 2 to 4C alkyl substituted by OH, alkoxy, alkylthio, acyloxy, NH2, alkylamino, dialkylamino, alkylcarbamoyloxy, alkoxycarbonylamino, ureido or alkylureido, R2 is a —CO—R radical in which R is H, alkyl, aryl, heterocyclyl, benzyl or heterocyclylmethyl, or R2 is a —CO—Y—R4 radical for which Y is —O—, —S—, —NH—, -Nalk- for which alk is straight or branched (1 to 4C) alkyl, and R4 is alkyl, aryl, aralkyl or heterocyclylalkyl, capable of being substituted by one or more halogen atoms or OH radicals, straight or branched (1 to 4C) alkyl, alkoxy, alkylthio, acylaminoalkylthio, alkoxycarbonyl or acylamino (1 to 4C) straight or branched, or oxo, or capable of being substituted by R5COO— in which R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by an amino acid residue, or represents an heterocyclyl radical, or R2 is alkyl (2 to 4C) substituted by OH, alkType: ApplicationFiled: January 27, 2009Publication date: August 6, 2009Applicants: Oroxcell, Alexis DenisInventors: Jean Pachot, Christophe Dini, Alexis Denis
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Publication number: 20090196906Abstract: The present invention relates to drug delivery systems comprising ocular implant, which include organic molecules, capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation, in combination with a polymer, which polymer serves to control, modify, modulate and/or slow the release of the therapeutic component into the environment of the eye in which said composite is placed.Type: ApplicationFiled: January 5, 2009Publication date: August 6, 2009Inventors: Lon T. Spada, Jane Guo Shiah, Patrick Hughes, Thomas C. Malone, Gerald W. DeVries, Jeffrey L. Edelman, Julie A. Wurster
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Publication number: 20090192172Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 8, 2005Publication date: July 30, 2009Applicant: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: 7560456Abstract: The invention relates to 3-pyridylcarboxamide derivatives of formula (I): wherein the various symbols are as defined in the description, compositions thereof, methods for controlling pests by applying same, and processes for their preparation.Type: GrantFiled: May 6, 2003Date of Patent: July 14, 2009Assignee: Merial LimitedInventors: Koichi Araki, Tetsuya Murata, Koshi Gunjima, Norihiko Nakakura, Eiichi Shimojo, Dale Robert Mitchell, Henricus Maria Martinus Bastiaans, David Stephen Carver, Daniel Allen, Christian Arnold, Waltraud Hempel, Olga Malsam, Jutta Maria Waibel
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Patent number: 7560473Abstract: The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.Type: GrantFiled: January 21, 2002Date of Patent: July 14, 2009Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A.Inventors: Hai Wang, Liuhong Yun, Huasong Feng, Fulin Li, Xingchun Tang, Huamei He, Rifang Yang, Wenyu Cui, Qixiu Gao, Gang Hu, Rusheng Zhao, Wei Liu, Chaoliang Long, Lin Wang, Xinqiang Lu, Lijun Liu, Yuan Yan