Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly To Ring Carbon Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/404)
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Publication number: 20140228420Abstract: The invention provides a method for treating ALS or suppressing the disease progress thereof, or treating symptoms caused by ALS or suppressing the disease progress thereof by administering an agent containing, as an active ingredient, 3-methyl-1-phenyl-2-pyrazolin-5-one or a physiologically acceptable salt thereof, to a patient that complies with specific criteria.Type: ApplicationFiled: September 5, 2012Publication date: August 14, 2014Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventor: Takatomo Yoneoka
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Publication number: 20140212486Abstract: The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH).Type: ApplicationFiled: January 17, 2014Publication date: July 31, 2014Applicant: TONIX PHARMACEUTICALS INC.Inventors: SETH LEDERMAN, BRUCE DAUGHERTY, LELAND J. GERSHELL, DARRYL RIDEOUT, ANDREW KAWASAKI
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Patent number: 8791049Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.Type: GrantFiled: December 13, 2010Date of Patent: July 29, 2014Assignee: Gowan Co.Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
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Publication number: 20140179637Abstract: A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.Type: ApplicationFiled: December 21, 2013Publication date: June 26, 2014Applicants: The Research Foundation for The State University of New York, Northwestern UniversityInventors: Jonathan Leis, Carol Carter
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Publication number: 20140170157Abstract: Methods of treatment for Crohn's disease and multiple sclerosis are disclosed. Also disclosed are methods for repositioning a pharmaceutical by selecting at least one target gene, gene product, or loci associated with the treatment of at least one first disease, trait, or phenotype by the pharmaceutical, identifying at least one second disease, trait, or phenotype associated with the least one target gene, gene product, or loci using genome-wide associated studies, and selecting at least one identified second disease, trait and/or phenotype based on step for treatment with the pharmaceutical.Type: ApplicationFiled: June 15, 2012Publication date: June 19, 2014Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITEDInventors: Pankaj Agarwal, Lon R. Cardon, Vincent Eugene Mooser, Philippe Sanseau
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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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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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Publication number: 20140142155Abstract: Invented is a method of treating thrombocytopenia in a human in need thereof which comprises the administration of a therapeutically effective amount of a 3?-{N?-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydropyrazol-4-ylidene]hydrazino}-2?-hydroxybiphenyl-3-carboxylic acid to such human.Type: ApplicationFiled: January 8, 2014Publication date: May 22, 2014Applicant: GlaxoSmithKline LLCInventors: SHIVAKUMAR G. KAPSI, FRANCIS XAVIER MULLER, MARY BETH WIRE
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Publication number: 20140140953Abstract: The pharmaceutically acceptable salts of bicycle-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicants: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
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Publication number: 20140107125Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: April 29, 2013Publication date: April 17, 2014Applicant: Dermira (Canada), Inc.Inventor: Dermira (Canada), Inc.
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Publication number: 20140094457Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating a genetic disease caused by premature termination codons, or other conditions that render messenger ribonucleic acid (mRNA) susceptible to nonsense mediated RNA decay, in a subject. Also disclosed is a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy. The present invention also relates to a method of identifying inhibitors of nonsense mediated RNA decay and/or inducing autophagy. The present invention further relates to a method of inhibiting nonsense mediated RNA decay and/or induction of autophagy in a subject.Type: ApplicationFiled: October 2, 2013Publication date: April 3, 2014Applicant: NEW YORK UNIVERSITYInventors: Lawrence B. Gardner, Timothy J. Cardozo, Leenus Martin
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Patent number: 8686184Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 18, 2012Date of Patent: April 1, 2014Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Patent number: 8673910Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: June 30, 2009Date of Patent: March 18, 2014Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20140075602Abstract: The present invention relates to a method comprising treating plant propagation material with at least sticker selected from specific acrylate co-copolymers, to seed dressing formulations comprising such stickers and to plant propagation material coated with such stickers.Type: ApplicationFiled: November 12, 2013Publication date: March 13, 2014Inventors: Ulf Schlotterbeck, Doris Stephan, Rafel Israels, Andreas Landes
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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: 8658684Abstract: A pharmaceutical composition comprises 3-methyl-1-phenyl-2-pyrazolin-5-one and borneol, and can be used to prepare the medicine for treating cerebrovascular diseases.Type: GrantFiled: March 3, 2009Date of Patent: February 25, 2014Assignee: Jiangsu Simcere Pharmaceutical R & D Co., Ltd.Inventors: Xiaojin Yin, Shibao Yang, Xiaoqiang Li, Zheng Jiang, Jian He, Anyuan Zhang, Xin Huang
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Publication number: 20140047572Abstract: Disclosed are transgenic non-human mammals, which useful for the screening of thrombopoietin mimetics, thrombopoietin receptor agonists, or thrombopoietin receptor antagonists active on the human thrombopoietin receptor. The transgenic non-human mammal has a genome that comprises a stably integrated transgene construct comprising a polynucleotide sequence encoding a humanized thrombopoietin receptor wherein said transgenic non-human mammal has a baseline blood platelet count corresponding to a physiological blood platelet count of a matched non-transgenic non-human mammal. The chimeric thrombopoietin receptor comprises either the transmembrane domain of a human thrombopoietin receptor or both the extracellular and transmembrane domains of a human thrombopoietin receptor operably coupled to a cytoplasmic domain of a non-human thrombopoietin receptor.Type: ApplicationFiled: March 15, 2013Publication date: February 13, 2014Applicant: University of RochesterInventors: Yuhchyau CHEN, J.H. David WU, Jane L. LIESVELD, Lin GAN
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Publication number: 20140039026Abstract: 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: ApplicationFiled: May 13, 2013Publication date: February 6, 2014Applicant: MAKHTESHIM CHEMICAL WORKS LTD.Inventor: Sharona ZAMIR
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Publication number: 20140037580Abstract: An improved thrombopoietin mimetic, the bis-(monoethanolamine) salt of 3?-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2?-hydroxy-[1,1?-biphenyl]-3-carboxylic acid.Type: ApplicationFiled: October 10, 2013Publication date: February 6, 2014Applicant: GlaxoSmithKline LLCInventor: Stephen MOORE
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Publication number: 20140038982Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.Type: ApplicationFiled: May 31, 2013Publication date: February 6, 2014Applicant: GlaxoSmithKline LLCInventor: Connie L. ERICKSON-MILLER
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Patent number: 8642637Abstract: The pharmaceutically acceptable salts of bicyclo-substituted pyrazolon azo derivatives represented by the general formula (I), their preparation methods, pharmaceutical compositions containing the same and their use as a therapeutic agent, especially as thrombopoietin (TPO) mimetics and their use as agonists of thrombopoietin receptor. The definitions of substituents in the general formula (I) are the same as the description.Type: GrantFiled: May 28, 2010Date of Patent: February 4, 2014Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.Inventors: Peng Cho Tang, Hejun Lü, Hongbo Fei, Yiqian Chen
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Patent number: 8642636Abstract: This invention provides for dimeric1-arylpyrazole compounds, of formulas (I), (II), and (III): or salts thereof, and the use of these compounds against ectoparasites such as insects, arthropods and acarina. The resulting compounds may be used in veterinary formulations such as, for example, spot-on and pour-on formulations, which may be used for treatment, controlling and preventing of parasitic infections in warm-blooded animals and birds.Type: GrantFiled: November 18, 2009Date of Patent: February 4, 2014Assignee: Merial LimitedInventor: Charles Q. Meng
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Publication number: 20140030301Abstract: The present invention relates to an aqueous pesticidal composition having excellent pesticidal activity, particularly a pesticidal composition comprising a pesticidal active ingredient, a carboxy-modified methyl methacrylate-butadiene copolymer, a surfactant and water, wherein the amount of the carboxy-modified methyl methacrylate-butadiene copolymer is 20-100 parts by weight relative to 100 parts by weight of the pesticidal active ingredient and the amount of the surfactant is 0.1-50 parts by weight relative to 100 parts by weight of the pesticidal active ingredient.Type: ApplicationFiled: March 7, 2012Publication date: January 30, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Motofumi Mizutani, Yumiko Kozuki, Maki Owaki, Masanao Takaishi, Masato Soma
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Patent number: 8637563Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.Type: GrantFiled: June 4, 2012Date of Patent: January 28, 2014Assignee: GlaxoSmithKline LLCInventor: Connie Erickson-Miller
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Patent number: 8637059Abstract: The present invention relates to mixtures comprising as active components a) carbamate derivatives of the formula (I) in which the substituents and the index have the following meaning: T is CH or N n is 0, 1 or 2 R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different when n is 2, and b) at least one compound of the formula (II).Type: GrantFiled: December 15, 2004Date of Patent: January 28, 2014Assignee: BASF SEInventors: Edson Begliomini, Sergio Zambon
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Patent number: 8629172Abstract: The present invention is directed to an implantable drug depot useful for reducing, preventing or treating post-operative pain in a patient in need of such treatment, the implantable drug depot comprising a therapeutically effective amount of clonidine or pharmaceutically acceptable salt thereof and a polymer; wherein the depot is implantable at a site beneath the skin to reduce, prevent or treat post-operative pain, and the depot is capable of releasing (i) about 5% to about 45% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a first period of up to 48 hours and (ii) about 55% to about 95% of the clonidine or pharmaceutically acceptable salt thereof relative to a total amount of the clonidine or pharmaceutically acceptable salt thereof loaded in the drug depot over a subsequent period of at least 3 days.Type: GrantFiled: April 9, 2009Date of Patent: January 14, 2014Assignees: Warsaw Orthopedic, Inc., Medtronic, Inc.Inventors: William F. McKay, Amira Wohabrebbi, Vanja Margareta King, Phillip Edward McDonald, Christopher M. Hobot, Troy Carter
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Publication number: 20140010773Abstract: This invention provides methods for treating diseases or conditions wherein the inhibition of Kit protein kinase may be beneficial, using pharmaceutical or cosmetic compositions comprising N-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine (FPL-62064) and related compounds. This invention also relates to the treatment of skin disorders, such as hyperpigmentation and cutaneous mastocytosis, and to cosmetic uses such as skin lightening.Type: ApplicationFiled: March 1, 2012Publication date: January 9, 2014Applicant: NPHARMAKON, LLCInventors: Dmitri Rebatchouk, Felix Sheinerman
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Publication number: 20130345267Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.Type: ApplicationFiled: May 30, 2013Publication date: December 26, 2013Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
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Publication number: 20130336921Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: December 19, 2013Applicant: ARDELYX, INC.Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
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Publication number: 20130338162Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 29, 2013Publication date: December 19, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
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Patent number: 8609693Abstract: The embodiments provide methods of administering a high dose or a loading dose of a TPO modulator to a subject. The embodiments further provide methods of treating thrombocytopenia and/or neutropenia in a subject. Additionally, the embodiments further provide methods of increasing platelet production and/or enhancing the number of peripheral blood stem cells in a subject.Type: GrantFiled: May 27, 2010Date of Patent: December 17, 2013Assignee: GlaxoSmithKline LLCInventors: Connie L. Erickson-Miller, Julian Jenkins
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Patent number: 8609649Abstract: One aspect of the invention relates to a method of treating or preventing a neurodegenerative disease, comprising the step of administering to a patient in need thereof a therapeutically effective amount of an inhibitor of the formation of advanced glycation end products. Another aspect of the invention relates to a proteasome activity-based screening assay to select compounds which may be useful for treating or preventing a neurodegenerative disease, and the materials used therein. Yet another aspect of the invention relates to molecules, and methods of use thereof, which bind at or adjacent to SOD-I Trp32, including molecules that bind in a site adjacent to SOD-I Trp32 whether or not it is oxidized, for treating or preventing neurodegenerative disease.Type: GrantFiled: March 20, 2008Date of Patent: December 17, 2013Assignee: Brandeis UniversityInventors: Jeffrey N. Agar, Gregory A. Petsko, Dagmar Ringe, Walter R. P. Novak
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Publication number: 20130330366Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130323283Abstract: Methods for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease in a subject in need thereof comprise administering to the subject an effective amount of a pharmaceutical composition comprising an inhibitor of a histone/protein acetyltransferase (HAT). Methods for identifying an agent useful for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease comprise (a) contacting a candidate agent with a test sample comprising Foxp3+ T regulatory cells (Tregs), and (b) comparing a function of the Foxp3+ Tregs in the test sample with that in a control sample, wherein inhibition of the function of the Foxp3+ Tregs in the test sample when compared with the control sample indicates that the candidate agent is an agent useful for treating or preventing a Foxp3+ Treg related disease.Type: ApplicationFiled: December 1, 2011Publication date: December 5, 2013Applicants: THE CHILDREN'S HOSPITAL OF PHILADELPHIA, THE JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Wayne W. Hancock, Steven M. Albelda, Philip A. Cole
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Patent number: 8586536Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: December 14, 2011Date of Patent: November 19, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20130303581Abstract: The present invention provides novel crystalline polymorphic forms of fipronil and processes for preparing the same. The present invention also provides a pesticidal composition containing a pesticidally effective amount of a crystalline form of fipronil and a method for controlling pests using a pesticidally effective amount of a crystalline form of fipronil or its composition.Type: ApplicationFiled: January 13, 2012Publication date: November 14, 2013Inventor: Keki Hormusji Gharda
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Publication number: 20130302378Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
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Publication number: 20130303492Abstract: 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: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20130296167Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: ApplicationFiled: April 17, 2013Publication date: November 7, 2013Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Heike Hungenberg, Peter Dahmen
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Publication number: 20130276352Abstract: A termite bait includes a plurality of cellulosic food material pieces palatable to termites embedded within a water resistant polyurethane foam matrix. Another termite bait includes a plurality of cellulosic food material pieces embedded within a water-absorbent polyurethane foam matrix. Yet another termite bait includes at least one cellulosic food material piece encapsulated within a water resistant polyurethane foam coating. Such termite baits can be used alone or in a monitoring device or other termite control device. Another termite control device includes a container, a cellulosic food material within the container and a water resistant polyurethane foam positioned to separate the food material from its environment. The container can contain a termite bait as described above or can include a chamber containing a cellulosic food material and at least one pocket containing a polyurethane foam barrier to reduce intrusion of water through the pocket to the food material.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Inventor: Dow AgroSciences LLC
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Publication number: 20130274278Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: June 6, 2013Publication date: October 17, 2013Inventors: Stephen M. CONDON, Yijun DENG, Matthew D. ALEXANDER, Matthew G. LAPORTE
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Publication number: 20130274307Abstract: The present invention relates to methods comprising applying to a useful plant, the locus thereof or propagation material thereof a combination of abscisic acid and a fungicidally active compound, which fungicidally active compound is a succinate dehydrogenase inhibitor, in particular for increasing the potency of a fungicidally active compound. The invention also relates to compositions comprising abscisic acid and the fungicidally active compounds as well as seeds comprising the combinations.Type: ApplicationFiled: October 21, 2011Publication date: October 17, 2013Applicant: SYNGENTA LIMITEDInventors: Elizabeth Pearson, Jose Luis Calvo, Robin Wesley, Jeremy R. Godwin, Ryan Jon Langs Ramsey, Timothy Robert Hawkes
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Publication number: 20130274227Abstract: 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: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20130261162Abstract: The present invention provides a parasiticidal formulation comprising: Fipronil, or a veterinarily acceptable derivative thereof; at least one C1-C6 alcohol co-solvent, wherein the total amount of C1-C6 alcohol is up to 8% by weight of the formulation; at least one organic solvent which is not the C1-C6 alcohol co-solvent; and at least one crystallisation inhibitor, wherein the total amount of crystallisation inhibitor is from 2 to 20% by weight of the formulation. The formulations of the invention have higher flash points than known parasiticidal formulations comprising Fipronil and therefore provide safer formulations for use in the home, storage, manufacture and distribution.Type: ApplicationFiled: March 28, 2013Publication date: October 3, 2013Applicant: Fidopharm, Inc.Inventor: Martin Benedict George DONNELLY
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Publication number: 20130261161Abstract: Fipronil co-formulations are provided herein. The formulations comprise an organic solvent, an alcohol co-solvent, and one or more antioxidants. The formulations provided herein are antiparasitic, and can be used, for example, to combat dog and cat parasites, such as, fleas and ticks.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: Velcera, Inc.Inventors: John PRESTON, David M. Petrick
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Publication number: 20130243707Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.Type: ApplicationFiled: March 28, 2013Publication date: September 19, 2013Inventors: Monique Renata GREEN, Kenton FEDDE
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Patent number: 8530508Abstract: The present invention provides methods of inhibiting human myeloid leukemia cell growth and proliferation by administering a thrombopoietin receptor agonist (TpoRA), a derivative, or variant thereof, to an individual with AML.Type: GrantFiled: October 8, 2008Date of Patent: September 10, 2013Assignee: GlaxoSmithKline LLCInventors: Alan Gewirtz, Anna Kalota, Connie L. Erickson-Miller
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Publication number: 20130231371Abstract: A spot-on pesticide composition for animals, specifically mammals, namely dogs, which composition comprises a combination of a pyrethroid and a macrocyclic lactone selected from avermectin, ivermectin, selamectin, moxidectin, milbemycin and any combination thereof, and optionally fipronil and/or 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: April 5, 2013Publication date: September 5, 2013Applicant: Sergeant's Pet Care Products, Inc.Inventors: Larry Nouvel, Donald W Kelley
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Patent number: 8524759Abstract: An improved phenylbutazone carrier composition provides increased palatability to horses. Additionally, the composition improves the bioavailability of the phenylbutazone and thus increases the horse's blood plasma levels of the medicine for the same effective dosage of the medicine.Type: GrantFiled: July 9, 2012Date of Patent: September 3, 2013Inventor: Douglas J. Gordon