Chalcogen Or Nitrogen Bonded Directly To The Pyrazole Ring By Nonionic Bonding Patents (Class 514/407)
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Patent number: 8778837Abstract: 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: GrantFiled: November 27, 2008Date of Patent: July 15, 2014Assignee: Bayer CropScience AGInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140193347Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.Type: ApplicationFiled: September 4, 2013Publication date: July 10, 2014Applicant: CAMURUS ABInventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
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Publication number: 20140193472Abstract: The present invention relates to microcapsules, formulations comprising such microcapsules and to methods of combating phytopathogenic pests in paddy rice fields based on such microcapsules.Type: ApplicationFiled: August 16, 2012Publication date: July 10, 2014Applicant: BASF SEInventors: Christian Sowa, Gerhard Peter Dohmen, Martin Obermann, Nadine Riediger, Kristin Klappach, Manuel Schmitt, Reinhard Stierl
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Patent number: 8772328Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: October 22, 2013Date of Patent: July 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ann E. Weber
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Patent number: 8765791Abstract: The present invention relates to methods for treating cancer by administering a therapeutically effective amount of compound of formula (I), such as selective NPY5R antagonist MK-0557 (trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H), 1?-cyclohexane]-4?-carboxamide), or a pharmaceutically acceptable salt thereof, to a subject in need thereof The methods can further comprise administering a chemotherapeutic agent to the subject in need thereof.Type: GrantFiled: March 10, 2009Date of Patent: July 1, 2014Assignee: University Health NetworkInventor: Guohua Pan
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Patent number: 8765748Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 19, 2008Date of Patent: July 1, 2014Assignee: University Health NetworkInventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
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Publication number: 20140179733Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Publication number: 20140171420Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 6, 2013Publication date: June 19, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
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Publication number: 20140171469Abstract: Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: July 3, 2013Publication date: June 19, 2014Applicant: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Jason B. Ibarra, Young-Jun Shin, Brett Ullman, Ning Zou, Xi Zeng
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Patent number: 8754115Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: GrantFiled: August 31, 2011Date of Patent: June 17, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
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Publication number: 20140162997Abstract: 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 R1, R2, ring A, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: June 12, 2014Applicant: Janssen Pharmaceutica NVInventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
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Patent number: 8748341Abstract: The present invention relates to synergistic mixtures comprising, as active components, chlorfenapyr as insecticidal compound I and a fungicidal compound II selected from the group of azoxystrobin, coumethoxystrobin, coumoxystrobin, dimoxystrobin, enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, orysastrobin, pico-xystrobin, pyraclostrobin, pyrametostrobin, pyraoxystrobin, pyribencarb, trifloxysstrobin, 2-(ortho-((2,5-dimethylphenyl-oxymethylen)phenyl)-3-methoxy-acrylic acid methyl ester, 2-(2-(3-(2,6-dichlorophenyl)-1-methyl-allylideneaminooxymethyl)-phenyl)-2-methoxyimino-N-methyl-acetamide.Type: GrantFiled: September 24, 2010Date of Patent: June 10, 2014Assignee: BASF SEInventors: Markus Gewehr, Egon Haden, Lutz Brahm
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Patent number: 8748339Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.Type: GrantFiled: June 4, 2009Date of Patent: June 10, 2014Assignee: BASF SEInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden
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Publication number: 20140155452Abstract: The present invention provides compounds of Formula I: along with pharmaceutical compositions containing the same, and methods of use thereof in subjects in need of treatment.Type: ApplicationFiled: February 5, 2014Publication date: June 5, 2014Applicant: Eisai R&D Management Co., Ltd.Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
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Patent number: 8741809Abstract: The present invention relates to a novel liquid formulation for crop protection which comprises a) pyraclostrobin; b) at least one organic solvent S1 with a water solubility of less than 2 g/l at 20° C.; c) at least one organic solvent S2 with a water solubility of at least 2 g/l at 20° C., where S2 comprises at least one solvent S2.1 with a water solubility of more than 200 g/l at 20° C. and optionally at least one solvent S2.2 with a water solubility of 2 to 200 g/l at 20° C.; d) at least one anionic surface-active substance SA1; e) at least one nonionic surface-active substance SA2; and f) water. The invention also relates to the use of the crop protection formulation for treatment of plants and seed, and to corresponding methods.Type: GrantFiled: October 9, 2009Date of Patent: June 3, 2014Assignee: BASF SEInventors: Ulrike Troppmann, Wolfgang Meier, Guenter Oetter, Ulrich Steinbrenner, Tatjana Levy, Jurith Montag, Tanja Brunner, Reiner Weiler
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Patent number: 8735431Abstract: The invention relates to novel insecticidal active compound combinations comprising, firstly, anthranilamides and, secondly, further insecticidally active compounds as defined in the description, which combinations are highly suitable for controlling animal pests, such as insects.Type: GrantFiled: November 20, 2004Date of Patent: May 27, 2014Assignee: Bayer CropScience AGInventors: Christian Funke, Reiner Fischer, Rüdiger Fischer, Heike Hungenberg, Wolfram Andersch, Wolfgang Thielert, Anton Kraus
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Process for the production of particles comprising active agrochemical ingredients in amorphous form
Patent number: 8735321Abstract: An object of the present invention is a process for the preparation of particles which comprise two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is the use of an agrochemical active ingredient for inhibiting the crystallization of another agrochemical active ingredient in a preparation process for particles which comprise the two agrochemical active ingredients in amorphous form, where a melt comprising the two molten agrochemical active ingredients is emulsified in an aqueous solution and cooled. A further object is particles which comprise two agrochemical active ingredients in amorphous form. The use in plant protection is also described.Type: GrantFiled: May 6, 2009Date of Patent: May 27, 2014Assignee: BASF SEInventors: Ulrike Troppmann, Winfried Mayer, Sebastian Koltzenburg, Rafel Israels, Andreas Bauder, Ulf Schlotterbeck -
Publication number: 20140142142Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20140140973Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140142156Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.Type: ApplicationFiled: December 12, 2013Publication date: May 22, 2014Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Helen E. BLACKWELL, Christine E. McINNIS
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Patent number: 8722577Abstract: 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: GrantFiled: February 5, 2008Date of Patent: May 13, 2014Assignee: BASF SEInventors: Dirk Voeste, Egon Haden, Marco-Antonio Tavares-Rodrigues, Edson Begliomini
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Publication number: 20140128435Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicant: KARO BIO ABInventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
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Publication number: 20140128406Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140128397Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.Type: ApplicationFiled: January 20, 2012Publication date: May 8, 2014Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
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Publication number: 20140120069Abstract: The present invention describes novel amphoteric materials based on crosslinked hyaluronic acid, according to the general formula (I), and a method of preparation of said materials. Further, the invention relates to the material containing entrapped active agents (e.g. drugs, growth factors etc.) and a method of preparation thereof. Moreover, the present invention relates to the use of said materials for controlled release systems, in tissue engineering, wound dressing or tissue regeneration.Type: ApplicationFiled: April 19, 2012Publication date: May 1, 2014Applicant: CONTIPRO BIOTECH S.R.O.Inventors: Gloria Huerta-Angeles, Drahomira Chladkova, Radovan Buffa, Sofiane Kettou, Vladimir Velebny
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Publication number: 20140121103Abstract: The present invention relates to synergistic mixtures comprising at least one compound I and at least one active compound II as defined herein and to the use of these mixtures for combating phytopathogenic fungi, and to seeds coated with at least one such mixture. The invention also relates methods for combating harmful fungi using such mixtures.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: BASF SEInventors: Nadege Boudet, Wassilios Grammenos, Jochen Dietz, Egon Haden, Richard Riggs, Bernd Müller, Jan Klaas Lohmann, Jurith Montag, Ian Robert Craig
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Publication number: 20140121184Abstract: Insecticidal compositions have at least one active agent and at least one insecticide. The active agent can include perilla oil, a component found in perilla oil, or a perillaldehyde or carvone analog. The insecticide can include a pyrethrum, pyrethrin, pyrethroid, neonicotinoid, chlofenapyr, ethiprole, sulfoxoflor, carbamate, organophosphate, or organochlorine. Methods for controlling insects include contacting an insect with an effective amount of a composition described in this specification. Modified plants that produce an active agent can be contacted with an insecticide.Type: ApplicationFiled: January 7, 2014Publication date: May 1, 2014Applicant: Clarke Mosquito Control Products, Inc.Inventors: Michael Dean Willis, Marie Elizabeth Saunders, Darryl Ramoutar, Joanna Maria Szymczyk, Frances Nita Krenick, Andrea Rohrbacher
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Patent number: 8710053Abstract: A plant disease control composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and one or more QoI compounds selected from group (A) consisting of dimoxystrobin, azoxystrobin, fluoxastrobin, pyraclostrobin, kresoxim-methyl, picoxystrobin, trifloxystrobin and N-methyl-alpha-methoxyimino-2-[(2,5-dimethylphenoxy)methyl]phenylacetamide is provided by the present invention, and this composition has excellent effect for controlling a plant disease.Type: GrantFiled: April 25, 2011Date of Patent: April 29, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
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Patent number: 8703649Abstract: The present invention relates to formulation comprising at least (i) two pesticidal compounds A and B dissolved in a lactic acid ester and wherein a) both A and B have melting points below 900 C b) both A and B are selected from the following list: pyraclos-trobin, metalaxyl, mefenoxam, trifloxystrobin, imazalil, pro-chloraz and ipconazole with the proviso that A is different from B (ii) at least one pesticidal compound C present in solid particles, and having a melting point of 900 C and above, and to their use as seed treatment formulation as well as their use for plant protection, including seed and crop protection.Type: GrantFiled: July 20, 2010Date of Patent: April 22, 2014Assignee: BASF SEInventors: Rafel Israels, Katharine Klamczynski, Marco Kuhns, Ulf Schlotterbeck
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Publication number: 20140107111Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.Type: ApplicationFiled: May 18, 2012Publication date: April 17, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
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Publication number: 20140107070Abstract: This disclosure features fungicidal combinations that include a paraffinic oil and an emulsifier. The combinations can further include one or more of the following: pigments, silicone surfactants, anti-settling agents, conventional fungicides such as demethylation inhibitors (DMI) and quinone outside inhibitors (Qol) and water. The fungicidal combinations are used for controlling infection of a crop plant by a fungal pathogen.Type: ApplicationFiled: June 4, 2012Publication date: April 17, 2014Applicant: SUNCOR ENERGY INC.Inventors: Michael Fefer, Jun Liu
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Publication number: 20140105839Abstract: The present invention relates to a compound of the following formula (I): as well as its process of preparation, pharmaceutical and cosmetics composition comprising it and use thereof, notably as an inhibitor of the sodium-dependent glucose co-transporter, such as SGLT1, SGLT2 and SGLT3, in particular in the treatment or prevention of diabetes, and more particularly type-II diabetes, diabetes-related complications, such as arthritis of the lower extremities, cardiac infarction, renal insufficiency, neuropathy or blindness, hyperglycemia, hyperinsulinemia, obesity, hypertriglyceridemia, X syndrome and arteriosclerosis, as well as for its use as an anticancer, anti-infective, anti-viral, anti-thrombotic or anti-inflammatory drug, or for lightening, bleaching, depigmenting the skin, removing blemishes from the skin, particularly age spots and freckles, or preventing pigmentation of the skin.Type: ApplicationFiled: May 29, 2012Publication date: April 17, 2014Applicant: TF-CHEMInventors: Geraldine Deliencourt-Godefroy, Lenaig Lopes
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Publication number: 20140107165Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: November 22, 2013Publication date: April 17, 2014Applicant: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20140106965Abstract: The present invention relates to a composition comprising a water-insoluble pesticide and an alkoxylated polyalkyleneimine. The invention furthermore relates to a method of preparing this composition; to the use of this composition for dispersing agrochemical active substances; to a method of controlling phytopathogenic fungi and/or undesired plant growth and/or undesired insect or mite attack and/or for regulating the growth of plants, wherein the composition is allowed to act on the respective pests, their environment or the crop plants to be protected from the respective pest, on the soil and/or on undesired plants and/or on the crop plants and/or on their environment; and furthermore to seed comprising the composition.Type: ApplicationFiled: May 21, 2012Publication date: April 17, 2014Applicant: BASF SEInventors: Gerhard Schnabel, Paul Klingelhoefer
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Patent number: 8697696Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: November 2, 2011Date of Patent: April 15, 2014Assignee: Roche Palo Alto LLCInventors: Stephen Deems Gabriel, Andrew Thomas
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Publication number: 20140100258Abstract: Invented is a method of treating cardiovascular disease/injury, in a mammal, including a human, in need thereof which comprises the administration of a therapeutically effective amount of a non-peptide TPO receptor agonist to such mammal.Type: ApplicationFiled: December 9, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Connie L. ERICKSON-MILLER, Julian JENKINS
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Publication number: 20140100211Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Patent number: 8691862Abstract: The present invention relates to novel crystalline polymorphs, solvate pseudomorphs and amorphous form of 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile (fipronil). The present invention also provides methods for preparing the novel polymorphs, pseudomorphs and amorphous form, as well as insecticidal or pesticidal compositions comprising same, and methods of use thereof as pesticidal agents.Type: GrantFiled: April 27, 2011Date of Patent: April 8, 2014Assignee: Makhteshim Chemical Works Ltd.Inventor: Sharona Zamir
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Patent number: 8686018Abstract: The present invention provides compounds of Formula I: along with pharmaceutical compositions containing the same, and methods of use thereof in subjects in need of treatment.Type: GrantFiled: March 12, 2013Date of Patent: April 1, 2014Assignee: Eisai R&D Management Co., Ltd.Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
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Publication number: 20140088094Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.Type: ApplicationFiled: November 8, 2011Publication date: March 27, 2014Applicants: Merck Sharp & Dohme Corp., Lycera CorporationInventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
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Publication number: 20140088165Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 2, 2013Publication date: March 27, 2014Applicant: NOVARTIS AGInventors: Yuki Iwaki, Toshio KAWANAMI, Gary Michael Ksander, Muneto Moji
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Publication number: 20140088153Abstract: The invention relates to compounds of the general formula (I) in which the radicals A1, A2, A3, A4, L, Q, R1, T and W have the meaning given in the description and to the use of the compounds for controlling animal pests. The invention furthermore relates to processes and intermediates for preparing the compounds of formula (I).Type: ApplicationFiled: March 12, 2012Publication date: March 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Maue, Isabelle Adelt, Markus Heil, Peter Jeschke, Tobias Kapferer, Friedrich August Muehlthau, Alexander Sudau, Olga Malsam, Peter Loesel, Arnd Voerste, Ulrich Goergens
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Publication number: 20140088105Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF1) receptor antagonists.Type: ApplicationFiled: November 22, 2013Publication date: March 27, 2014Applicant: NOVARTIS AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Publication number: 20140088158Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: SANOFIInventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
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Publication number: 20140080883Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20140080702Abstract: The present invention relates to a composition comprising an agrochemical active substance and a copolymer which comprises an N-vinylcarboxamide and a diallyldialkylammonium salt incorporated into the polymer. The invention furthermore relates to a method of preparing this composition; to the use of this composition for dispersing agrochemical active substances; to a method of controlling phytopathogenic fungi and/or undesired plant growth and/or undesired insect or mite attack and/or for regulating the growth of plants, wherein the composition is allowed to act on the respective pests, their environment or the crop plants to be protected from the respective pest, on the soil and/or on undesired plants and/or on the crop plants and/or on their environment; and furthermore to seed comprising the composition.Type: ApplicationFiled: May 24, 2012Publication date: March 20, 2014Applicant: BASF SEInventors: Gerhard Schnabel, Ruth Wirschem, Paul Klingelhoefer, Lucelena Patricio Cardoso
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Publication number: 20140080884Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.Type: ApplicationFiled: June 25, 2012Publication date: March 20, 2014Applicants: Merck Sharp & Dohme Ltd., Merck Sharp & Dohme Corp.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Patent number: 8673901Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.Type: GrantFiled: August 31, 2009Date of Patent: March 18, 2014Assignee: Xention LimitedInventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
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Patent number: 8664257Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: January 26, 2011Date of Patent: March 4, 2014Assignee: SanofiInventors: Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Bodo Scheiper, Klaus Wirth
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Patent number: 8658686Abstract: Novel therapeutic agents for myeloma are provided. A therapeutic agent for multiple myeloma containing a pyrazole compound represented by the formula (1): wherein R1 is C1-C6 alkyl, C1-C6 alkyl substituted with R17, C1-C6 haloalkyl, phenyl, phenyl substituted with a R11's or the like, R2 is a hydrogen atom, C1-C6 alkyl, phenyl or phenyl optionally substituted with e R21's or the like, R3 is a hydrogen atom or the like, X is a single bond or —(CR6R7)n—, each of R4 and R5 is independently C1-C6 alkyl or the like, R6 and R7 are hydrogen atoms or C1-C6 alkyl, R8 is phenyl, phenyl optionally substituted with k R81's or the like, a tautomer of the compound or a pharmaceutically acceptable salt or solvate thereof, as an active ingredient.Type: GrantFiled: December 1, 2011Date of Patent: February 25, 2014Assignee: Nissan Chemical Industries, Ltd.Inventors: Taito Nishino, Katsuaki Miyaji, Shunsuke Iwamoto, Takumi Mikashima, Koichiro Saruhashi, Yo Kishikawa