1,2,4-triazoles (including Hydrogenated) Patents (Class 514/383)
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Compounds, compositions and methods for the treatment of beta-amyloid diseases and synucleinopathies
Patent number: 8829198Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: October 3, 2008Date of Patent: September 9, 2014Assignee: Proteotech IncInventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow, Lesley Larsen -
Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
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Patent number: 8829016Abstract: The present invention relates to a compound of formula 1 or 2 wherein R1 represents straight-chain or branched C2-C8 alkyl, C2-C8 alkenyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group, or C2-C4 alkynyl, optionally substituted by at least one substituent selected from the group consisting of hydroxyl, amino or C1-C6 alkyl amino group; and R2 represents hydroxyl, C1-C6 alkyl, C1-C6 alkylcarbonyl, di(C1-C6-alkyl)aminomethyl, C3-C6 heterocyclylmethyl or arylaminomethyl, wherein the aryl group is optionally substituted by at least one substituent selected from the group consisting of halogens and C1-C6 alkoxy as well as associated pharmaceutical compositions and uses of the compound or composition in therapy, in particular for the treatment of a disorder or a disease susceptible to inhibition of COX-2.Type: GrantFiled: April 20, 2012Date of Patent: September 9, 2014Assignee: King Saud UniversityInventors: Fars K. Alanazi, Awwad A Radwan, Ibrahim A. Alsarra
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Publication number: 20140248353Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.Type: ApplicationFiled: May 16, 2014Publication date: September 4, 2014Applicant: NAL Pharmaceuticals Ltd.Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
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Publication number: 20140249194Abstract: The invention discloses optically active compounds of Formula (1a) or Formula (1b), wherein R1 and R2 are independently selected from the group consisting of hydrogen and a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine; and wherein (a) R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group having a linear or branched chain having 1 to 20 carbon atoms, or (b) R3 and R4 together form a cycloalkyl ring having 3 to 10 carbon atoms fused to the thiophene ring; and wherein R5 is CN or COOR?, where R? is methyl or ethyl. The compounds of Formula (1a) or Formula (1b) may be used in pharmaceutical compositions for treating fungal infections.Type: ApplicationFiled: April 29, 2014Publication date: September 4, 2014Applicants: FDC LIMITED, COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Hanumant Bapurao BORATE, SANGESHWER PRABHAKAR SAWARGAVE, SUBHASH PRATAPRAO CHAVAN, MOHAN ANAND CHANDAVARKAR, RAMAKRISHNAN RAMACAHNDRAN IYER, AMIT CHANDRAKANT TAWTE, DEEPALI DAMODAR RAO
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Publication number: 20140249193Abstract: The present invention provides compounds that modulate protein translocation in mitochondria, compositions thereof, and methods of identifying, making and using these.Type: ApplicationFiled: April 12, 2012Publication date: September 4, 2014Applicant: The Regents of the University of CaliforniaInventors: Carla M. Koehler, Samuel A. Hasson, Kiyoko Miyata, Micheal A. Teitell, Deepa Dabir
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Patent number: 8822518Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.Type: GrantFiled: December 12, 2013Date of Patent: September 2, 2014Assignee: GlaxoSmithKline LLCInventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
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Patent number: 8822506Abstract: The present invention relates to the use of succinate dehydrogenase Inhibitors for controlling powdery mildew primary infections in crops and to a method for controlling those primary infections.Type: GrantFiled: January 29, 2010Date of Patent: September 2, 2014Assignee: Bayer Cropscience AGInventors: Gilbert Labourdette, Hélène Lachaise, Luk de Maeyer, Christian Feryn
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Publication number: 20140243194Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkynyloxy-ethyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: August 28, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
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Publication number: 20140242028Abstract: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.Type: ApplicationFiled: January 21, 2014Publication date: August 28, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Joseph Anthony Bilotta, Zhi Chen, Qingjie Ding, Shawn David Erickson, Eric Mertz, Robert James Weikert
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Patent number: 8815925Abstract: The invention relates to the use of an antimycotic agent and an epithelial cell or endothelial cell adhesion inhibitor for producing a combination drug for the topical treatment of Candida mycoses selected from vulvovaginal candidiasis, oropharyngeal candidiasis (oral thrush), diaper dermatitis (diaper thrush) and intertriginous (Candida) eczema.Type: GrantFiled: October 2, 2013Date of Patent: August 26, 2014Inventors: Christian Noe, Marion Noe-Letschnig
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Patent number: 8816070Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: GrantFiled: December 11, 2007Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
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Patent number: 8815910Abstract: 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: GrantFiled: January 4, 2013Date of Patent: August 26, 2014Assignee: 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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Patent number: 8816079Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: GrantFiled: April 27, 2011Date of Patent: August 26, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20140235441Abstract: The present invention relates to substituted 1-{2-cyclyloxy-2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-ethyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: August 21, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
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Publication number: 20140234425Abstract: The invention relates to aqueous fungicidal active substance compositions and to their use in the control of harmful microorganisms and in particular in the protection of cellulose-comprising materials, particularly wood, from infection by microorganisms, in particular those harmful fungi which can damage wood or cellulose. The active substance composition according to the invention comprises: a) at least one fungicidal organic active substance with a solubility in water of not more than 5 g/l at 25° C./1013 mbar, and b) a finely-divided polymer with an average particle size, determined by dynamic light scattering, of not more than 300 nm, in which the polymer particles comprise the active substance, the polymer being formed from ethylenically unsaturated monomers M comprising: at least 60% by weight, based on the total amount of the monomers M, of at least one neutral monoethylenically unsaturated monomer M1 with a solubility in water of not more than 30 g/l at 25° C.Type: ApplicationFiled: April 24, 2014Publication date: August 21, 2014Inventors: Reimer GOTTSCHE, Gunnar KLEIST, Joerg HABICHT, Holger SCHOPKE, Patrick AMRHEIN
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Publication number: 20140235684Abstract: A metal-salen complex compound responsive drug, which has an antidotal property capable of neutralizing cytotoxicity of a metal-salen complex compound, and an intra-corporeal behavior control system for the metal-salen complex compound are provided. This metal-salen complex compound responsive drug contains an effective amount of a metal chelating agent to suppress side effects by the metal-salen complex compound.Type: ApplicationFiled: September 19, 2012Publication date: August 21, 2014Inventors: Yoshihiro Ishikawa, Haruki Eguchi
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Publication number: 20140235660Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
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Patent number: 8809352Abstract: The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): or pharmaceutically acceptable salt thereof, as well as methods of treating a disease, disorder, or syndrome associated with Bcl-2 inhibition, particularly hyperproliferative diseases. The present invention also includes pharmaceutical compositions including compounds of formula I and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 8, 2010Date of Patent: August 19, 2014Assignee: Novartis AGInventors: Karen Miller-Moslin, Bakary-Barry Toure, Michael Scott Visser, Naeem Yusuff
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Patent number: 8809364Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: GrantFiled: April 1, 2011Date of Patent: August 19, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
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Publication number: 20140228215Abstract: This document discloses pesticidal compostions comprising molecules having the following formulas: and processes related thereto.Type: ApplicationFiled: April 23, 2014Publication date: August 14, 2014Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, William T. Lambert, Thomas C. Sparks, Vidyadhar B. Hegde
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Patent number: 8802120Abstract: Bioactive agrichemical concentrates and compositions having improved bioactivity comprising combinations of acid solutions and conventional bioactive agrichemical actives or formulations.Type: GrantFiled: September 14, 2012Date of Patent: August 12, 2014Assignee: Sciessent LLCInventor: Joseph J. Crudden
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Publication number: 20140221421Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140221922Abstract: Bioactive hydroforming luminal liner compositions are formed of an absorbable crystalline amphiphilic polyether-ester-urethane dissolved in a liquid derivative of a polyether glycol that undergoes transformation into a tissue-adhering, resilient interior cover or liner for the controlled release of its bioactive payload at clinically compromised conduits in humans as in the case of bacteria- and yeast-infected vaginal canals, esophagi, and arteries following angioplasty.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: POLY-MED, INC.Inventors: Shalaby W. Shalaby, David Ingram, Georgios Hilas, Sheila Nagatomi
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Publication number: 20140221440Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising a carboxylic acid compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and one or more kinds of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and met conazole, shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: August 23, 2012Publication date: August 7, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Atsushi Iwata, Makoto Kurahashi
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Publication number: 20140221332Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: August 7, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
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Publication number: 20140221441Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and one or more kinds of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and metconazole, shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: August 23, 2012Publication date: August 7, 2014Inventors: Atsushi Iwata, Makoto Kurahashi
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Publication number: 20140220110Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
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Patent number: 8796330Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: December 18, 2007Date of Patent: August 5, 2014Assignee: Methylgene Inc.Inventors: Robert Déziel, Alain Ajamian
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Publication number: 20140213622Abstract: The invention relates to low-dose pharmaceutical compositions comprising the aromatase inhibitor 4,4?[fluoro-(1-H-1,2,4-triazol-1-yl)methylene]bisbenzonitrile, as the active ingredient in a suitable carrier. The present invention also relates to a process for their preparation and to their use as therapeutic agents.Type: ApplicationFiled: September 6, 2012Publication date: July 31, 2014Inventors: Ann Taylor, Lloyd B. Klickstein, Jeewan Thakur
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Patent number: 8791145Abstract: The present invention provides a formulation comprising a pesticide and/or a plant growth regulator; an acyl morpholine of the formula (I) where R is H, CH3 or C2H5; and a polar aprotic co-solvent different from an acyl morpholine of formula (I). The formulation can be used in treatment of plants, and is especially well suited for use as a soluble liquid formulation.Type: GrantFiled: May 24, 2011Date of Patent: July 29, 2014Assignee: Akzo Nobel Chemicals International B.V.Inventor: Peter Westbye
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Patent number: 8791102Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: GrantFiled: October 16, 2009Date of Patent: July 29, 2014Assignee: Exelixis, Inc.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20140206730Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I): wherein each of symbols are the same as defined in the Description; or salts thereof and one or more kinds of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and metconazole, shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: August 23, 2012Publication date: July 24, 2014Inventors: Atsushi Iwata, Makoto Kurahashi
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Publication number: 20140206668Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: March 25, 2014Publication date: July 24, 2014Applicant: Dow AgroSciences LLCInventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Publication number: 20140206731Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and metconazole, shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: August 23, 2012Publication date: July 24, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Atsushi Iwata, Makoto Kurahashi
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Publication number: 20140206538Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-2-alkynyl-ethyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: July 24, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
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Publication number: 20140206706Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
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Patent number: 8785662Abstract: The present invention relates to a preservative for preserving wood comprising 5-methyl-2-trifluoromethylfuran-3-carboxylic acid anilide derivative represented by the following formula, wherein R represents an iropropyl group or an isopropoxy group as an active ingredient. The preservative for preserving wood has an excellent preservative effect on various wood-decay fungi at an extremely low dose, is economically efficient, and imposes a small burden on the environment. The present invention also relates to a method for treating wood using the preservative.Type: GrantFiled: May 12, 2010Date of Patent: July 22, 2014Assignee: SDS Biotech K.K.Inventors: Keijitsu Tanaka, Masahiro Maesawa
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Publication number: 20140200248Abstract: The present invention provides a composition for controlling plant diseases having an excellent control efficacy on plant diseases. A composition for controlling plant diseases comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of azole compounds selected from the group (A) consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole, triadimefon and metconazole, shows an excellent controlling efficacy on plant diseases.Type: ApplicationFiled: August 23, 2012Publication date: July 17, 2014Inventors: Atsushi Iwata, Makoto Kurahashi
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Patent number: 8778938Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
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Patent number: 8778835Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: July 5, 2007Date of Patent: July 15, 2014Assignee: Bayer Cropscience AGInventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20140194388Abstract: A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.Type: ApplicationFiled: May 25, 2012Publication date: July 10, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Publication number: 20140193363Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: January 15, 2014Publication date: July 10, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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Publication number: 20140187422Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-2-cyclyl-ethyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: July 3, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Müller, Wassilios Grammenos, Thomas Grote
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Publication number: 20140187423Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-hexyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: July 3, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
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Publication number: 20140187421Abstract: The present invention relates to substituted 1-{2-[2-halo-4-(4-halogen-phenoxy)-phenyl]-2-alkoxy-3-methyl-butyl}-1H-[1,2,4]triazole compounds of formula I as defined in the description, and the N-oxides, and salts thereof, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound. The invention also relates to the use of such compounds and compositions for combating harmful fungi and seed coated with at least one such compound.Type: ApplicationFiled: August 14, 2012Publication date: July 3, 2014Applicant: BASF SEInventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
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Patent number: 8765636Abstract: The present invention relates to novel active compound combinations comprising a known carboxamide, a known azole and additionally a second known azole or alternatively a known strobilurin, which combinations are highly suitable for controlling unwanted phytopathogenic fungi.Type: GrantFiled: August 29, 2012Date of Patent: July 1, 2014Assignee: Bayer Intellectual Property GmbHInventors: Peter Dahmen, Ulrike Wachendorff-Neumann, Isolde Häuser-Hahn, Hans-Ludwig Elbe, Ralf Dunkel, Anne Suty-Heinze
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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