Chalcogen Or Nitrogen Bonded Directly To The Pyrazole Ring By Nonionic Bonding Patents (Class 514/407)
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Publication number: 20150099696Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.Type: ApplicationFiled: June 26, 2012Publication date: April 9, 2015Applicant: Cadila Healthcare LimitedInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
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Patent number: 9000024Abstract: 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: February 5, 2014Date of Patent: April 7, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Mark Spyvee, Takashi Satoh, Jonathan Eric Carlson
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Patent number: 8993613Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably fipronil, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.Type: GrantFiled: April 1, 2014Date of Patent: March 31, 2015Assignee: The Hartz Mountain CorporationInventors: W. Lance Hemsarth, Keith Goldman, Ellen McGarvey
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Publication number: 20150087511Abstract: The present invention relates to synergistic mixtures comprising, as active components one insecticidal compound I selected from the group of acrinathrin, allethrin, alpha-cypermethrin, beta-cypermethrin, bifenthrin, cycloprothrin, cyfluthrin, cypermethrin, cyphenothrin, deltamethrin, dimefluthrin, esfenvalerate, etofenprox, fenpropathrin, fenvalerate, flucythrinate, imiprothrin, permethrin, prallethrin, profluthrin, pyrethrin I, pyrethrin II, resmethrin, silafluofen, tau-fluvalinate, tetramethrin, theta-cypermethrin, tralomethrin, transfluthrin and zeta-cypermethrin; and one fungicidal compound II selected from the group of azoxystrobin, coumethoxystrobin, coumoxystrobin, dimoxystrobin, enestroburin, fluoxastrobin, kresoxim-methyl, metominostrobin, orysastrobin, picoxystrobin, 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)-phenType: ApplicationFiled: December 5, 2014Publication date: March 26, 2015Inventors: Markus GEWEHR, Egon HADEN, Lutz BRAHM
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Publication number: 20150087628Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.Type: ApplicationFiled: April 10, 2013Publication date: March 26, 2015Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
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Publication number: 20150087684Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of fipronil and etofenprox as the active components, 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 mammal's skin, preferably localized over a small surface area.Type: ApplicationFiled: August 15, 2014Publication date: March 26, 2015Inventor: Larry Nouvel
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Patent number: 8987275Abstract: The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.Type: GrantFiled: February 18, 2011Date of Patent: March 24, 2015Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael Gray, Wenjun Zhou, Xianming Deng
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Publication number: 20150080375Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: October 14, 2014Publication date: March 19, 2015Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Monique Bodil Van Niel, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
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Publication number: 20150080398Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
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Publication number: 20150080397Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: September 17, 2014Publication date: March 19, 2015Inventors: Tai Wei LY, Erik Dean RAAUM
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Patent number: 8980837Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: GrantFiled: January 23, 2012Date of Patent: March 17, 2015Assignee: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Patent number: 8980294Abstract: Ready-to-use foamable pesticide compositions that contain a particulate pesticide suspended therein and applicators for dispensing such compositions. Methods for treating pests such as arthropods by contacting pests with such compositions are also provided.Type: GrantFiled: April 28, 2010Date of Patent: March 17, 2015Assignee: BASF CorporationInventors: Terrence R. Burke, Henry Wayne Moran, Jonathan D. Berger, James H. Cink
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Publication number: 20150071864Abstract: A reversely thermo-reversible hydrogel composition comprising a water soluble block copolymer comprising at least two blocks of polyethylene oxide and at least one block of polypropylene oxide, and at least one associative gelling adjuvant having water solubility less than 0.5 g/100 ml, preferably less than 0.3 g/100 ml at 20° C., and being capable of forming water soluble inter-molecular complexes with the water soluble block copolymer in water. The hydrogel composition exhibits improved gelling efficiency, enhanced solubility and/or stability for water sparely soluble and insoluble pharmaceutical agents. The hydrogel compositions are useful in a variety of pharmaceutical and cosmetic products and applications, such as esophageal, otic, vaginal, rectal, ophthalmic, treatments of disorders and imperfections of the skin, and treating and/or preventing alopecia and restoring and/or promoting hair growth.Type: ApplicationFiled: September 22, 2014Publication date: March 12, 2015Applicant: Broda Technologies Co., Ltd.Inventors: Shao Xiang LU, Jeffrey LU, Letian LIU
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Publication number: 20150064118Abstract: 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 15, 2014Publication date: March 5, 2015Inventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
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Publication number: 20150056257Abstract: The present invention relates to a method for preparing an emulsifiable granule comprising the steps of a) emulsifying water with a solution of a pesticide in a water-insoluble solvent, b) contacting the emulsion resulting from step a) and a solid dispersant containing a water-soluble polycarboxylate and a water-soluble anionic surfactant, and c) extruding the paste resulting from step b). The invention further relates to emulsifiable granules containing a water-insoluble solvent, a pesticide, which is dissolved in the water-insoluble solvent, a water-soluble polycarboxylate, and a water-soluble anionic surfactant.Type: ApplicationFiled: February 26, 2013Publication date: February 26, 2015Inventors: Claude Taranta, Thomas Bork, Jochen Schreieck, Helmut Mueller, Nadine Riediger, Clark D. Klein, Rebecca Willis, Tatjana Sikuljak, Simon Nord
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Patent number: 8962671Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, G, R10, R11, 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 24, 2012Date of Patent: February 24, 2015Assignee: SanofiInventors: Sven Ruf, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Thomas Olpp, Klaus Wirth
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Patent number: 8962524Abstract: The present invention relates to a mixture comprising [(3S,4R,4aR,6S,12R,12aS,12bS)-3-(cyclopropanecarbonyloxy)-6,12-dihydroxy-4,6a,12b-trimethyl-11-oxo-9-(pyridin-3-yl)-1,2,3,4,4a,5,6,6a,12a,12b-decahydro-11H,12H-benzo[f]pyrano[4,3-b]chromen-4-yl]methyl cyclopropanecarboxylate and a fungicidal compound II in synergistic effective amounts, to the use of this mixture for controlling pests and for improving the plant health and to plant propagation material comprising this mixture.Type: GrantFiled: May 27, 2011Date of Patent: February 24, 2015Assignee: BASF SEInventors: Matthias Pohlman, Markus Gewehr, Egon Haden, Juergen Langewald
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Patent number: 8962608Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: GrantFiled: September 21, 2012Date of Patent: February 24, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
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Publication number: 20150051177Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Inventor: Darren Orton
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Patent number: 8951934Abstract: The invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a compound of formula (I) and at least one further respiratory chain complex in inhibitor (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: December 5, 2009Date of Patent: February 10, 2015Assignee: Bayer CropScience AGInventors: Burkhard Schütz, Peter Dahmen, Ulrike Wachendorff-Neumann, Peter Herold
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Publication number: 20150038492Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: August 12, 2014Publication date: February 5, 2015Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Publication number: 20150031736Abstract: Use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of acute exacerbations of chronic obstructive pulmonary disease. Treatment may involve a single dose of the active ingredient by oral administration.Type: ApplicationFiled: March 19, 2013Publication date: January 29, 2015Inventor: Paul Andrew Ford
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Patent number: 8940730Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.Type: GrantFiled: March 16, 2010Date of Patent: January 27, 2015Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
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Publication number: 20150024032Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.Type: ApplicationFiled: July 18, 2014Publication date: January 22, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
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Publication number: 20150018374Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1 is F, Cl or Br; R2 is H or F; and R3 is Cl or Br; and (b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.Type: ApplicationFiled: January 30, 2013Publication date: January 15, 2015Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, James Francis Bereznak
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Publication number: 20150018371Abstract: Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.Type: ApplicationFiled: March 6, 2013Publication date: January 15, 2015Inventors: Roger D. Cone, Julien A. Sebag, Jacques Pantel, Savannah Y. Williams, David C. Weaver, Gary A. Sulikowski, Craig W. Lindsley, Padma S. Portonova, Chao Zhang
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Publication number: 20150011590Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles 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: ApplicationFiled: February 12, 2013Publication date: January 8, 2015Applicant: Merck Sharp & Dohme CorporationInventors: Ann E. Weber, Tesfaye Biftu
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Patent number: 8921407Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: November 13, 2012Date of Patent: December 30, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
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Patent number: 8921408Abstract: This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds alone or in combination with formamidine compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to the animal in need thereof.Type: GrantFiled: May 23, 2013Date of Patent: December 30, 2014Assignee: Merial LimitedInventors: Mark David Soll, Luiz Gustavo Cramer, Patrice Wurtz, James Pate, Natalya Shub, Loic Patrick Le Hir de Fallois, Philip Reid Timmons
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Patent number: 8921406Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: GrantFiled: August 21, 2006Date of Patent: December 30, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Alfred Hahn
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Patent number: 8921402Abstract: 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: GrantFiled: January 10, 2014Date of Patent: December 30, 2014Assignee: Karo Bio ABInventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
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Publication number: 20140378466Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: ARDEA BIOSCIENCESInventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
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Patent number: 8916601Abstract: Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.Type: GrantFiled: February 28, 2013Date of Patent: December 23, 2014Assignee: ChemoCentryx, Inc.Inventors: Xi Chen, Junfa Fan, Pingchen Fan, Antoni Krasinski, Lianfa Li, Rebecca M. Lui, Jeffrey P. McMahon, Jay P. Powers, Yibin Zeng, Penglie Zhang
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Publication number: 20140371213Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: May 19, 2014Publication date: December 18, 2014Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20140364310Abstract: The present disclosure describes a formulation including a nanoparticle including a polymer-associated strobilurin compound with an average diameter of between about 1 nm and about 500 nm; wherein the polymer is a polyelectrolyte, and a dispersant or a wetting agent. The disclosure describes various formulations and formulating agents that can be included in the formulations. Additionally, the disclosures describes application to various plants and fungi as well as advantages of the disclosed formulations.Type: ApplicationFiled: August 23, 2012Publication date: December 11, 2014Applicant: VIVE CROP PROTECTION INC.Inventors: Fugang Li, Hung Hoang Pham, Rachel Gong, Henry Galas
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Publication number: 20140364317Abstract: The present invention relates to a method for a preparation of a solid composition comprising the steps of a) dissolving a premix in a premix-solvent, or melting a premix, wherein the premix contains a pesticide and a nonionic, amphiphilic polyalkoxylate, b) solidifying the premix by removing the premix-solvent, or by cooling, and c) contacting the premix with at least one auxiliary. The invention further relates to a solid composition obtainable by said method; to a method for the preparation of an aqueous tank mix, in which a pesticide is present as suspended particles having a particle size below 1.Type: ApplicationFiled: November 29, 2012Publication date: December 11, 2014Applicant: BASF SEInventors: Claude Taranta, Thomas Bork, Jochen Schreieck, Helmut Müller, Nadine Riediger, Clark D. Klein, Rebecca Willis, Tatjana Sikuljak, Murat Mertoglu
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Publication number: 20140357671Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises fipronil, etofenprox, and an insect growth regulator as the active components, in doses and proportions which are 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: August 15, 2014Publication date: December 4, 2014Inventor: Larry Nouvel
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Patent number: 8901153Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Dow AgroSciences, LLC.Inventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul Renee LePlae, Jr., Frank Wessels, Ronald Ross, Jr., Carl DeAmicis, Peter Borromeo
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Patent number: 8895620Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more 1-(2,6-dichloro-?,?,?-trifluoroparatolyl)pyrazole compound(s) selected from Group (A) shows an excellent controlling activity on a pest. Group (A): a group consisting of acetoprole, ethiprole, fipronil, vaniliprole, pyriprole and pyrafluprole.Type: GrantFiled: October 13, 2011Date of Patent: November 25, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: So Kiguchi, Soichi Tanaka
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Patent number: 8895602Abstract: The present invention relates to a 6-pyrazolylamido-3-substituted azabicyclo[3.1.0]hexane derivatives useful as calcium channel blockers, pharmaceutically acceptable salts thereof and medical use of the calcium channel inhibiting effect of the compounds for treatment of diseases.Type: GrantFiled: August 29, 2013Date of Patent: November 25, 2014Assignee: Korea Institute of Science and TechnologyInventors: Ghil Soo Nam, Kyung Il Choi, Ae Nim Pae, Seon Hee Seo, Hyun Ah Choo, Gyo Chang Keum, Jung Hyun Kim
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Patent number: 8895603Abstract: 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: GrantFiled: June 25, 2012Date of Patent: November 25, 2014Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
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Patent number: 8889727Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is providedType: GrantFiled: January 30, 2012Date of Patent: November 18, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20140329876Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I), in which the substituents are as defined in the specification; to compounds of formula (I) for use as androgen receptor modulators. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 25, 2012Publication date: November 6, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Bharat Lagu, Chetan Pandit, Sanjita Sasmal, Thomas Ullrich
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Patent number: 8877786Abstract: 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: GrantFiled: December 2, 2013Date of Patent: November 4, 2014Assignee: Novartis AGInventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Moji
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Publication number: 20140323470Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.Type: ApplicationFiled: July 14, 2014Publication date: October 30, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
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Publication number: 20140323305Abstract: The present invention relates to the use of strobilurine type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing a mutation in the mitochondrial cytochrome b gene conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, to plant health applications, and to seeds coated with at least one such compound.Type: ApplicationFiled: December 6, 2012Publication date: October 30, 2014Applicant: BASF SEInventors: Joachim Rheinheimer, Violeta Terteryan, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Sebastian Georgios Rohrer, Wassilios Grammenos, Christian Pilger, Franz Roehl, Markus Gewehr, Gerd Stammler, Jurith Montag, Hubert Sauter
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Publication number: 20140323485Abstract: A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Darren Mark LeGrand, Roger John Taylor
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Patent number: 8871806Abstract: Methods for reducing the incidence of flea allergy dermatitis (FAD) in a companion animal are disclosed, the methods directed to inhibiting blood feeding by ectoparasites on a companion animal. The methods of the present invention involve administering a pesticide composition comprising cyphenothrin to a companion animal, specifically dogs and cats, in doses and proportions which are parasiticidally effective against a variety of ectoparasites, and in formulations which are convenient for topical application to the animal's skin, preferably localized over a small surface area. Such methods are useful in preventing and/or reducing the incidence of flea allergy dermatitis.Type: GrantFiled: June 6, 2012Date of Patent: October 28, 2014Assignee: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20140315970Abstract: The invention provides an ectoparasiticidal formulation which comprises an ectoparasiticidal agent, preferably fipronil, as the pesticidally-active ingredient, together with a crystallization inhibitor selected from the group consisting of alkyl-substituted pyrrolidones, and optionally, one or more organic solvents and/or co-solvents. Preferably, the crystallization inhibitor is N-octyl pyrrolidone, and the organic solvent, if present, preferably comprises diethylene glycol monoethyl ether. The ectoparasiticidal formulation surprisingly yields a significantly enhanced speed of kill. Methods for manufacturing the formulation, as well as methods for treating animals infested with ectoparasites, are also disclosed.Type: ApplicationFiled: April 1, 2014Publication date: October 23, 2014Applicant: THE HARTZ MOUNTAIN CORPORATIONInventors: W. Lance HEMSARTH, Keith Goldman, Ellen McGarvey