Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
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Publication number: 20140341850Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Applicant: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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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: 20140336231Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) prothioconazole and (B) fluxapyroxad and optionally (C) a further fungicidally active compound. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungicidally of plants or crops (e.g. cereals such as wheat, barley, lye, oats, millet and triticale; soya beans; rice; corn/maize; oil seed rape including canola; beans, peas, peanuts; sugar beet, fodder beet, beetroot; potatoes; cotton), and 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: ApplicationFiled: July 22, 2014Publication date: November 13, 2014Inventor: STEPHANIE GARY
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Patent number: 8883827Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.Type: GrantFiled: June 7, 2010Date of Patent: November 11, 2014Assignee: Oslo University Hospital HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
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Patent number: 8871792Abstract: In one aspect, the invention relates to compounds having the formula X: 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: GrantFiled: June 6, 2013Date of Patent: October 28, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20140315943Abstract: A pharmaceutical composition comprising an mTOR/PI3K inhibitor, and an Hsp90 inhibitor according to the following formulae (I) and (Ia) 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 23, 2012Publication date: October 23, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Publication number: 20140309185Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
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Patent number: 8859601Abstract: The present application relates to new, substituted benzyl-1,2,4-triazolones and phenylsulfonyl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: November 26, 2009Date of Patent: October 14, 2014Assignee: Bayer Intellectual Property GmbHInventors: Ulf Brüggemeier, Ingo Flamme, Chantal Fürstner, Joerg Keldenich, Peter Kolkhof, Martina Delbeck, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Truebel
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Publication number: 20140294808Abstract: Methods of treating cancer with a compound of formulae (I) or (Ia) are disclosed. Also provided are methods of treating a cancer with a mutation in ALK or a c-MET mutation with a compound of formulae (I) or (Ia). Further provided are methods of treating non-small cell lung cancer with a mutation in ALK with a compound of formulae (I) or (Ia); a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.Type: ApplicationFiled: July 9, 2012Publication date: October 2, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Iman El-Hariry, David Proia, Vojo Vukovic
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Patent number: 8846738Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.Type: GrantFiled: January 15, 2013Date of Patent: September 30, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stefan Dutzmann, Klaus Stenzel, Manfred Jautelat
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Patent number: 8846566Abstract: PROBLEM There are provided a composition for controlling plant diseases and a method for controlling plant diseases having excellent control effect for plant diseases. SOLUTION A composition for controlling plant diseases comprising, as active ingredients, a compound represented by formula (1), wherein X1 represents a methyl group, a difluoromethyl group or an ethyl group; X2 represents a methoxy group or a methylamino group; and X3 represents a phenyl group, a 2-methylphenyl group or a 2,5-dimethylphenyl group, and at least one azole compound selected from the group consisting of bromuconazole, cyproconazole, difenoconazole, fenbuconazole, fluquinconazole, hexaconazole, imibenconazole, ipconazole, myclobutanil, prothioconazole, simeconazole, tetraconazole, triticonazole and metconazole.Type: GrantFiled: November 20, 2009Date of Patent: September 30, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Masanao Takaishi, Masato Soma
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Publication number: 20140286902Abstract: A pharmaceutical combination comprising a platinum-containing anticancer agent, and an Hsp90 inhibitor according to the following formulae (I) & (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein. Also provided is a method of treating a proliferative disorder such as cancer in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 1, 2012Publication date: September 25, 2014Inventor: David Proia
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Publication number: 20140255386Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: July 24, 2012Publication date: September 11, 2014Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTEInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20140256716Abstract: The invention relates to the use of C16-C18-carboxylic acid dibutylamides in agrochemical formulations, agrochemical formulations which comprise such compounds and the use as tank mix additives.Type: ApplicationFiled: August 10, 2012Publication date: September 11, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter Baur, Martin Steinbeck, Ingo Wetcholowsky, Thomas Auler, Alison Daniels, Rolf Pontzen
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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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Patent number: 8822519Abstract: The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype ? (PPAR?), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPAR? thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.Type: GrantFiled: August 7, 2009Date of Patent: September 2, 2014Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Chunhua Jin, Xiaoyu Liu, Zhenliang Chen, Xiaohe Zheng, Shoufeng Ming
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Publication number: 20140243381Abstract: Nitric oxide biosynthesis-inhibiting anti-inflammatory and anti-microbial compounds of Formula (3) and Formula (4) wherein R1 and R2 are independently selected from optionally substituted thienyl, optionally substituted furyl, optionally substituted —CH?CH-thienyl and optionally substituted provided that R2 is substituted with as nitro group Treatment methods utilizing the compounds, and methods of synthesis of the compounds are also disclosed.Type: ApplicationFiled: February 22, 2013Publication date: August 28, 2014Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventor: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY
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Publication number: 20140242135Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: April 25, 2012Publication date: August 28, 2014Applicant: Vanderbilt UniversityInventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
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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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Publication number: 20140228418Abstract: A pharmaceutical composition comprising an MEK inhibitor, and an Hsp90 inhibitor according to the following formulae (I) or (Ia) 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 22, 2012Publication date: August 14, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Jaime Acquaviva
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Patent number: 8802708Abstract: The present invention provides a fungicide composition having stable and high harmful bio-organism control effect on crop plants infected with plant diseases due to plant diseases. Specifically, the present invention provides a fungicide composition for agricultural or horticultural use, which comprises: (a) an indole compound represented by formula (I): wherein R1 and R2 each independently represents C1-4 alkyl, etc.; Y represents H, halogen, etc.; R3 and R4 each independently represents a hydrogen atom, alkyl, etc.; R5, R6, R7 and R8 each independently represents a hydrogen atom, alkyl, etc., and (b) at least other fungicide selected from the group consisting of Dimethomorph, Chlorothalonil, a copper compound, Iprovalicarb, Zoxamide, phosphorous acid or a salt thereof, Fluazinam, Cyazofamid, Flumorph, Benthiavalicarb-isopropyl, Ethaboxam, Methalaxyl-M and Benalaxyl-M.Type: GrantFiled: October 21, 2005Date of Patent: August 12, 2014Assignee: Ishihara Sangyo Kaisha, LtdInventor: Shigeru Mitani
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Publication number: 20140221375Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating c-Met associated cancers, in a subject in need thereof.Type: ApplicationFiled: February 10, 2014Publication date: August 7, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Zhenjian Du, Kevin Paul Foley
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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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Patent number: 8796324Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: March 21, 2012Date of Patent: August 5, 2014Assignee: Bayer Intellectual Property GmbHInventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiss, Jörg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
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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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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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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: 20140187420Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) Prothioconazole and (B) Iprodione. 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: ApplicationFiled: May 14, 2012Publication date: July 3, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Frank Göhlich, Anton Kraus, Ulrike Wachendorff-Neumann
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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: 20140171424Abstract: A method for treating hypertension in a subject in need thereof (e.g., wherein said treatment does not result in an increase in serum uric acid levels, abnormally elevated serum uric acid levels, hyperuricemia, serum uric acid levels of above 6 mg/dL, or in the development of gout in the subject), the method comprising administering to the subject: a. a thiazide diuretic; and b. an organic anion transporter 4 (OAT4) inhibitor. The thiazide diuretic is selected from hydrochlorothiazide, bendroflumethiazide, benzothiadiazine, hydroflumethiazide, clorothiazide, methyclothiazide, polythiazide, chlorthalidone, metolazone, indapamide, bumetanide, ethacrynic acid, furosemide or torsemide. The OAT4 inhibitor is 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 22, 2012Publication date: June 19, 2014Applicant: ARDEA BIOSCIENCES, INC.Inventor: Jeffrey Miner
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Patent number: 8741803Abstract: To provide a pesticidal composition which controls a pest undesirable for cultivation of a useful crop plant or a useful plant. A pesticidal composition comprising the following (component A) and the following (component B) as active ingredients: (component A): one or more compounds selected from 3-arylphenyl sulfide derivatives represented by the formula [I]: (component A): wherein R is a C2-C6 alkyl group which may be substituted, or the like, each of B0, B1, B2 and B3 which are independent of one another, is a hydrogen atom, a halogen atom or a haloalkyl group, n is an integer of from 0 to 2, and Ar is a phenyl group, a pyrazolyl group or a triazolyl group, (component B): one or more compounds selected from the group consisting of triazamate, butocarboxim, butoxycarboxim, chromafenozide, halofenozide, cyflumetofen, prallethrin, acetoprole, ethiprole, methamidophos, flonicamid, pyridalyl, flufenerim, flubendiamide, tebufenozide, fenazaquin and cyenopyrafen.Type: GrantFiled: July 31, 2008Date of Patent: June 3, 2014Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Yoshihiro Ito, Yuki Nakano
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Publication number: 20140148472Abstract: Disclosed are compounds able to modulate the activity of the GPR17 receptor in a highly specific way, which are useful in the treatment and diagnosis of diseases or dysfunctions involving the activation of said receptor. In particular, the compounds according to the invention can be used for neuroprotective and/or reparatory purposes, in cerebral, cardiac and renal ischaemia, in cerebral trauma, in chronic neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), and in demyelinating diseases such as multiple sclerosis.Type: ApplicationFiled: November 2, 2011Publication date: May 29, 2014Applicant: CENTRO CARDIOLOGICO MONZINO SpAInventors: Mariapia Abbracchio, Ivano Eberini, Chiara Parravicini, Claudia Martini, Maria Letizia Trincavelli, Simona Daniele
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Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Publication number: 20140142120Abstract: 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 cancer in a subject. Also disclosed are methods of inhibiting SCF-Skp2 activity and a method of identifying inhibitors of SCF-Skp2 activity.Type: ApplicationFiled: October 16, 2013Publication date: May 22, 2014Applicant: NEW YORK UNIVERSITYInventors: Timothy Cardozo, Michele Pagano, Lily Wu, Leslie I. Gold
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Publication number: 20140135370Abstract: Methods of treating cancer with a compound of formula (I) are disclosed. Also provided are methods of treating a cancer with a KRAS mutation or an ALK+ cancer with a compound of formula (I).Type: ApplicationFiled: November 8, 2013Publication date: May 15, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Vojo Vukovic
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Publication number: 20140135371Abstract: Chemically stable aqueous dispersions of prothioconazole and processes for preparing them are provided. The dispersions comprise prothioconazole present in an aqueous medium, and a sulfur-containing compound present in an amount effective to render the dispersion chemically stable.Type: ApplicationFiled: January 8, 2014Publication date: May 15, 2014Applicant: BAYER CROPSCIENCE LPInventors: Fred C. ROSA, Tai-Teh WU
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Publication number: 20140128338Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: November 8, 2013Publication date: May 8, 2014Applicant: ARDEA BIOSCIENCES, INC.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
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Publication number: 20140121101Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I), (B) an inhibitor of the ergosterol biosynthesis, in particular an azole compound, and (C) an inhibitor of the respiratory chain at complex III, in particular a strobilurin compound. 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: ApplicationFiled: March 28, 2012Publication date: May 1, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrike Wachendorff-Neumann, Ingo Wetcholowsky, Anton Kraus, Thomas Seitz, Jose Augusto Geraldes
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Publication number: 20140113944Abstract: The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, and generalized anxiety disorder.Type: ApplicationFiled: June 7, 2012Publication date: April 24, 2014Applicant: ELI LILLY AND COMPANYInventors: Teresa Tse Ki Man, James Allen Monn, Carlos Montero Salgado, Lourdes Prieto, David Edward Tupper, Lesley Walton
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Publication number: 20140113884Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.Type: ApplicationFiled: April 4, 2012Publication date: April 24, 2014Inventors: John David Imig, William B. Campell, John Russell Falck
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Publication number: 20140113899Abstract: An agro-horticultural agent of the present invention is intended to provide an agro-horticultural agent capable of providing, with a smaller spray amount, the same effect as compared to a conventional agro-horticultural agent. The agro-horticultural agent of the present invention includes a plurality of active ingredients and one of the plurality of active ingredients is an azole derivative represented by the following general formula (I); where: Ra and Rb each represent a predetermined hydrocarbon group and at least one of Ra and Rb has a chlorine atom or a bromine atom substituted for a hydrogen atom; Y represents a chlorine atom or a fluorine atom; and m represents 0 or 1.Type: ApplicationFiled: June 6, 2012Publication date: April 24, 2014Applicant: KUREHA CORPORATIONInventors: Hideaki Tateishi, Nobuyuki Araki, Toru Yamazaki, Taiji Miyake, Keiichi Sudo, Hisashi Kanno
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Publication number: 20140100230Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.Type: ApplicationFiled: December 10, 2013Publication date: April 10, 2014Applicant: HYDRA BIOSCIENCES, INC.Inventors: Jayhong A. Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
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Publication number: 20140100213Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: November 4, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20140100242Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.Type: ApplicationFiled: September 17, 2013Publication date: April 10, 2014Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie Bassler, Lee Swem
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Publication number: 20140100107Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I), (B) an inhibitor of the respiratory chain at complex I or II and (C1) an inhibitor of the ergosterol biosynthesis, in particular an azole compound, or (C2) an inhibitor of the respiratory chain at complex III, in particular a strobilurin compound. 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: ApplicationFiled: March 28, 2012Publication date: April 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrike Wachendorff-Neumann, Ingo Wetcholowsky, Anton Kraus, Thomas Seitz, Jose Augusto Geraldes
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Publication number: 20140080843Abstract: Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 21, 2013Publication date: March 20, 2014Inventors: Xin-Yun Huang, Christy Young Shue
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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: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Publication number: 20140066443Abstract: The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 30, 2012Publication date: March 6, 2014Inventors: Douglas C. Beshore, Robert M. Garbaccio, Scott D. Kuduk, Adam W. Johnson, Jason W. Skudlarek
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Publication number: 20140066407Abstract: The novel active compound combinations comprising 2-[2-(1-chlorocyclopropyl)-3-(2-chlorophenyl)-2-hydroxypropyl]-2,4-dihydro-[1,2,4]-triazole-3-thione of the formula and the active compound of groups (1) to (24) listed in the description have very good fungicidal properties.Type: ApplicationFiled: November 8, 2013Publication date: March 6, 2014Applicant: Bayer Intellectual Property GmbHInventors: DUTZMANN Stefan, STENZEL Klaus, JAUTELAT Manfred