1,2,4-triazoles (including Hydrogenated) Patents (Class 514/383)
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Patent number: 8697704Abstract: 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: August 11, 2011Date of Patent: April 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
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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: 20140099349Abstract: A water-based wood protection agent having a biocide-containing aqueous emulsion that contains at least one biocide active ingredient and at least one cationic emulsifier, and the at least one biocidal active ingredient is emulsified by the at least one cationic emulsifier to form active ingredient-emulsifier particles, which are each enclosed by an at least single-layered polyelectrolyte coating, so that the net charge of the enclosed particle is zero or negative.Type: ApplicationFiled: April 30, 2012Publication date: April 10, 2014Applicant: KURT OBEMEIER GMBH & CO. KGInventors: Michael Pallaske, Peter Jüngel, Sascha Hellkamp
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Publication number: 20140100255Abstract: 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: ApplicationFiled: December 12, 2013Publication date: April 10, 2014Applicant: 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: 8691235Abstract: 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: GrantFiled: April 5, 2010Date of Patent: April 8, 2014Assignee: Poly-Med, Inc.Inventors: Shalaby W Shalaby, David Ingram, Georgios T Hilas, Sheila Nagatomi
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Patent number: 8691816Abstract: 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: GrantFiled: August 14, 2009Date of Patent: April 8, 2014Assignee: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 8691858Abstract: Provided is a composition for preparing emulsion or microemulsion formulations that demonstrates favorable dilution properties without being affected by the solubilities of constituent components. The composition for preparing emulsion or microemulsion formulations contains a component (A): a polyoxyalkylene allyl phenyl ether, polyoxyalkylene aralkyl phenyl ether or polyoxyalkylene aralkenyl phenyl ether, a component (B): a polyoxyalkylene sorbitan alkylate, a component (C): a dialkylsulfosuccinate, and a component (D): an ester ether-based solvent. An emulsion or microemulsion formulation containing the composition is also provided.Type: GrantFiled: May 10, 2010Date of Patent: April 8, 2014Assignee: Nippon Soda Co., Ltd.Inventors: Shigebumi Arai, Tetsuo Kubota
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Publication number: 20140094362Abstract: In order to provide a compound that shows a strong effect on controlling a plant disease, a triazole compound of the present invention (i) is a compound in which —OH group, —R2 group, and CH2—Ar group are bonded in cis configuration with a cyclopentane, (ii) is (?)-enantiomer or (+) enantiomer, and (iii) is represented by Formula (I): (wherein R1 represents an alkyl group; R2 represents a haloalkyl group; and Ar represents a substituted/unsubstituted aromatic hydrocarbon group or a substituted/unsubstituted aromatic heterocyclic group.Type: ApplicationFiled: May 30, 2012Publication date: April 3, 2014Applicant: KUREHA CORPORATIONInventors: Taiji Miyake, Nobuyuki Araki, Toru Yamazaki
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Publication number: 20140094494Abstract: A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.Type: ApplicationFiled: September 17, 2013Publication date: April 3, 2014Applicant: Wisconsin Alumni Research FoundationInventors: Bruce Steven Klein, Brad Mark Tebbets
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Publication number: 20140080842Abstract: The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.Type: ApplicationFiled: May 11, 2012Publication date: March 20, 2014Applicant: B.R.A.I.N. Biotechnology Research and Information Network AGInventors: Michael Krohn, Dirk Sombroek
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Publication number: 20140079806Abstract: The invention relates to the use of penflufen for protecting wood and wood-comprising materials against wood-destroying basidiomycetes.Type: ApplicationFiled: September 30, 2011Publication date: March 20, 2014Applicant: LANXESS Deutschland GmbHInventors: Bernd Koop, Martin Kugler, Thomas Jaetsch, Johannes Kaulen, Tanja Gerharz
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Publication number: 20140080794Abstract: The present invention relates to the treatment of estrogen-dependent hyperproliferative uterine disorders including endometriosis, uterine fibroids, endometrial hyperplasia, uterine cancer, and their related symptoms by intravaginally administering at least two active agents selected from an aromatase inhibitor, an antiinflammatory agent, and a uterine-selective estrogen receptor antagonist. This combination therapy reduces local estrogen production, blocks local estrogen action, and suppresses inflammation locally, resulting in starvation of the estrogen-dependent diseased tissues, relief of related symptoms, and retardation of disease progression. Intravaginal delivery maximizes local inhibition of estrogen production without significantly affecting systemic circulating estrogen levels. This results in enhanced clinical efficacy and reduced side effects.Type: ApplicationFiled: July 18, 2013Publication date: March 20, 2014Inventors: Changjin Wang, Leland F. Wilson
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Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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Patent number: 8673952Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: August 7, 2012Date of Patent: March 18, 2014Assignee: F. Hoffman-La Roche AGInventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20140073503Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: ApplicationFiled: March 21, 2012Publication date: March 13, 2014Inventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen
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Publication number: 20140073678Abstract: In one aspect, the present invention discloses combinational compositions for treating users experiencing symptoms associated with a migraine or other central nervous system related pain disorder that can cause or exacerbate nausea and/or vomiting or other central nervous system related pain disorder that can cause or exacerbate nausea and/or vomiting. The combinational composition includes a first pharmaceutical active component for treating pain, and a second pharmaceutical active component for treating nausea and/or vomiting and/or vomiting in a user.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: MONOSOL RX, LLCInventors: Eric Dadey, Alexander Mark Schobel, Daniel R. Barber, Garry L. Myers
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Publication number: 20140072531Abstract: A method for preparing polymer microparticles with a reduced initial burst, and the polymer microparticles prepared thereby, the method including: contacting polymer microparticles with an alcohol aqueous solution, the polymer microparticles prepared thereby, and use for drug delivery of the polymer microparticles.Type: ApplicationFiled: November 20, 2013Publication date: March 13, 2014Applicant: SK CHEMICALS CO., LTD.Inventors: Hong Kee KIM, Kyu Ho Lee, Joon-Gyo OH, Bong-Yong Lee
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Patent number: 8669263Abstract: This disclosure concerns antimicrobial compositions and methods for immunoenhancement, for example methods of increasing production of a type I interferon (IFN) in response to pathogen infection, by administration of a TAM receptor inhibitor. In certain embodiments, the disclosure concerns methods of using a TAM receptor inhibitor to treat a viral or bacterial infection in a subject.Type: GrantFiled: March 8, 2013Date of Patent: March 11, 2014Assignee: Salk Institute for Biological StudiesInventors: Greg E. Lemke, John A. T. Young, Carla V. Rothlin, Suchita Bhattacharyya
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Patent number: 8664250Abstract: A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with these combinations. Also provided is wood treated by these combinations, and a method of treatment for composite wood.Type: GrantFiled: May 17, 2005Date of Patent: March 4, 2014Assignee: Kop-Coat, Inc.Inventors: Alan S. Ross, Brian Marks, Hans Ward
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Publication number: 20140057956Abstract: The invention relates to a copolymer having a backbone that is obtained by radical polymerisation of: a fatty body (A) comprising unsaturations and/or hydroxyl functions; and at least one monomer (B) including at least one function that can be polymerised by means of radical polymerisation and comprising either (i) at least one linear or branched alkyl chain having preferably between 16 and 44 carbon atoms, and more preferably at least 18 carbon atoms, e.g. at least 20 carbon atoms, in particular 22 carbon atoms or 44 carbon atoms, or (ii) a reactive function. The invention also relates to a method for modifying the rheological properties of an non-aqueous medium with the addition of a copolymer of the invention. The invention further relates to a composition formed totally or partially by a copolymer of the invention. Preferably, the composition is an emulsifiable composition. Furthermore, the invention relates to a composition comprising a copolymer of the invention and an emulsifying agent.Type: ApplicationFiled: April 27, 2012Publication date: February 27, 2014Applicant: RHODIA OPERATIONSInventors: Marc Balastre, Chi-Thanh Vuong
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Publication number: 20140056880Abstract: The present invention provides triazole compounds of Formula I: as further described herein. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, and a method of treating a disorder mediated, at least in part, by KSP in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of a compound of Formula I.Type: ApplicationFiled: August 28, 2013Publication date: February 27, 2014Applicant: NOVARTIS AGInventors: Tinya Abrams, Paul Barsanti, Yu Ding, David Duhl, Wooseok Han, Cheng Hu, Yue Pan
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Patent number: 8658564Abstract: The present invention relates to novel active compound combinations comprising the known fungicidally active compounds N-[2-(1,3-dimethylbutyl)phenyl]-5-fluoro-1,3-dimethyl-1H-pyrazole-4-carboxamide, metalaxyl and triazole (3), which are highly suitable for controlling unwanted phytopathogenic fungi. Moreover, the invention relates to a method for the curative or preventive treatment of phytopathogenic fungi on plants or useful plants, in particular to the treatment of seed, for example seed of cereals, and not least to the treated seed itself.Type: GrantFiled: May 28, 2008Date of Patent: February 25, 2014Assignee: Bayer Cropscience AGInventors: Anne Suty-Heinze, Peter Dahmen
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Publication number: 20140051736Abstract: The invention relates to fungicidal compositions comprising as active ingredient a combination of components A) and B) as defined in the patent claims, to a method of controlling phytopathogenic diseases on crop plants using such a composition and to a method of protecting natural substances of vegetable and/or animal origin and/or their processed forms using such a composition.Type: ApplicationFiled: September 4, 2013Publication date: February 20, 2014Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Harald WALTER, Urs NEUENSCHWANDER, Ronald ZEUN, Josef EHRENFREUND, Hans TOBLER, Camilla CORSI, Clemens LAMBERTH
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Publication number: 20140051729Abstract: Methods and compositions for treating degenerative muscle conditions are disclosed. The compositions disclosed herein include S1P promoting compositions that include an S1P promoting agent. Embodiments of the methods disclosed herein include administering therapeutically effective amounts to subjects suffering from a degenerative muscle condition, such as, for example, subjects suffering from sarcopenia and subjects suffering from muscular dystrophy, including subjects suffering from Duchenne Muscular Dystrophy and Becker Muscular Dystrophy.Type: ApplicationFiled: July 12, 2013Publication date: February 20, 2014Applicant: University of WashingtonInventors: Nicholas Ieronimakis, Hannele Ruohola-Baker, Morayma Reyes, Junlin Qi, Mario Pantoja, Karin Fischer
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Publication number: 20140050772Abstract: The biodegradable drug delivery systems described here are formulated for implantation into the nail unit and its surrounding tissues for the treatment of various nail unit conditions. The systems include non-temperature dependent phase change compositions that may be formulated as solutions, solids, semisolids, microparticles, or crystals.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: Hallux. Inc.Inventors: Frank Kochinke, Corrine Bright
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Publication number: 20140051709Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.Type: ApplicationFiled: August 16, 2012Publication date: February 20, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Sita REDDY, Lucio Comai, Nouri Neamati
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Publication number: 20140051735Abstract: The present invention relates to the use of N-phenylethylpyrazole carboxamide derivatives, in particular 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid [2-(2,4-dichlorophenyl)-2-methoxy-1-methyl-ethyl]-amide for controlling powdery mildew primary infections in crops and to a method for controlling those primary infections.Type: ApplicationFiled: August 15, 2011Publication date: February 20, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Gilbert Labourdette, Hélène Lachaise, Luk De Maeyer, Christian Feryn, Sebastian Hoffmann, Heiko Rieck
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Patent number: 8653121Abstract: An agrochemical composition comprises an azole active ingredient and an N,N-dialkyl long chain alkylamide. The N,N-dialkyl long chain alkylamide is present in sufficient amount to prevent or inhibit the crystallization of the azole derivative during the application of the composition to a locus. Preferred N,N-Dialkyl long chain alkylamide(s) comprised in the composition is/are selected from the group consisting of compounds of the formula (I): in which (a) R1 and R2 are independently normal alkyl radicals having 2 carbon atoms, and R represents an alkyl group having from 10 to 30 carbon atoms; or (b) R1 and R2 are independently normal alkyl radicals having 3 carbon atoms, and R represents an alkyl group having from 9 to 30 carbon atoms; or 20 (c) R1 and R2 are independently normal alkyl radicals having from 4 to 20 carbon atoms and R represents an alkyl group having from 6 to 30 carbon atoms.Type: GrantFiled: May 28, 2008Date of Patent: February 18, 2014Assignee: Rotam Agrochem International Co., Ltd.Inventors: Amanda Yin, Sonia Chen, Yifan Wu, Pichumani Narayanamoorthy, Chang Yuan Lo
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Patent number: 8653260Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: June 20, 2012Date of Patent: February 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
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Patent number: 8653070Abstract: 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: December 14, 2010Date of Patent: February 18, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Patent number: 8653072Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.Type: GrantFiled: January 11, 2013Date of Patent: February 18, 2014Assignee: Karo Bio ABInventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
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Publication number: 20140044799Abstract: The present invention concerns a molecular signature of cutaneous pigmentary spots, comprising the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2, and various applications of this signature. In particular, the invention concerns a method for characterizing a known or suspected pigmentary spot in a human being, comprising comparing the levels of expression in skin samples obtained from said spot and from adjacent undamaged skin, of at least one dermal gene linked to matrix remodelling or to its extracellular proteoglycan and glycoprotein components, selected from the list constituted by the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2. The invention also concerns methods for evaluating the efficacy of a pigmentary spot treatment, cosmetic and therapeutic methods for the treatment of pigmentary spots, and various modulators for said genes, and their use.Type: ApplicationFiled: April 20, 2012Publication date: February 13, 2014Applicant: L'OREALInventors: Francoise Bernerd, Christine Duval, Olivier De Lacharriere, Stephanie Nouveau, Xavier Marat
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Publication number: 20140037622Abstract: Methods of treating a head and neck cancer are disclosed.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
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Publication number: 20140039018Abstract: An fungicide capable of inhibiting the accumulation of the mycotoxin in a crop effectively and a mycotoxin accumulation inhibition method using said fungicide are provided. The mycotoxin accumulation inhibition method according to the invention is a mycotoxin accumulation inhibition method for inhibiting the accumulation of the mycotoxin in a grain after cropping comprising a first fungicide treatment step for treating the cereal plant after the flowering stage with a fungicide containing metconazole as an active ingredient.Type: ApplicationFiled: March 1, 2012Publication date: February 6, 2014Applicant: KUREHA CORPORATIONInventors: Hideaki Tateishi, Takumi Nishiuchi
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Publication number: 20140038823Abstract: The present invention relates to active compound combinations, in particular within a fungicide composition, which comprises (A) a N-cyclopropyl-N-[substituted-benzyl]-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide or thiocarboxamide derivative and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively or eradicatively 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: April 18, 2012Publication date: February 6, 2014Inventors: Peter Dahmen, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Frank Goehlich, Hendrik Helmke, Thomas Seitz, Ulrike Wachendorff-Neumann, Ingo Wetcholowsky
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Publication number: 20140038944Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts, Nicholas Sean Flinn
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Patent number: 8642585Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: GrantFiled: March 14, 2013Date of Patent: February 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
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Patent number: 8642774Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 3, 2012Date of Patent: February 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
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Patent number: 8637058Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.Type: GrantFiled: November 18, 2002Date of Patent: January 28, 2014Assignee: Isagro S.p.A.Inventors: Lucio Filippini, Marilena Gusmeroli, Alexia Elmini, Carlo Garavaglia, Luigi Mirenna
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Patent number: 8637525Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: January 25, 2011Date of Patent: January 28, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Publication number: 20140024532Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of formula I wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.Type: ApplicationFiled: September 19, 2013Publication date: January 23, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
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Publication number: 20140024641Abstract: A method of treating exposure to organophosphate agents and preventing morbidity due to such exposure through the administration of a triptan compound to a subject.Type: ApplicationFiled: January 7, 2013Publication date: January 23, 2014Inventors: David Reed HELTON, David Brian FICK, Ernest H. PFADENHAUER, James LUCOT
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Publication number: 20140024680Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: ApplicationFiled: January 9, 2013Publication date: January 23, 2014Applicant: Bayer Intellectual Property GmbHInventor: Bayer Intellectual Property GmbH
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Patent number: 8633182Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: GrantFiled: May 22, 2013Date of Patent: January 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
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Patent number: 8633232Abstract: 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: GrantFiled: May 4, 2012Date of Patent: January 21, 2014Assignee: Ardea Biosciences, Inc.Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
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Patent number: 8632767Abstract: The present invention constitutes new 3-[1-(3-haloalkyl)triazolyl]phenyl sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, R1, R2 and n are as defined in the description, to their use as acaricides and insecticides for controlling animal pests, and to processes for preparing them.Type: GrantFiled: August 19, 2010Date of Patent: January 21, 2014Assignee: Bayer Intellectual Property GmbHInventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste
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Publication number: 20140011772Abstract: The present invention relates to compositions and methods for the treating and empirically investigating conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity). In particular, the present invention provides compositions and methods for using flufenamic acid in the treatment and empirical investigation of conditions associated with neuronal dysfunction (e.g., chronic pain, epileptic neuronal activity).Type: ApplicationFiled: June 13, 2013Publication date: January 9, 2014Applicant: NORTHWESTERN UNIVERSITYInventors: Marco Martina, A. Vania Apkarian
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Publication number: 20140011794Abstract: The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.Type: ApplicationFiled: September 5, 2013Publication date: January 9, 2014Applicants: Aeouls Sciences, Inc., Duke University, National Jewish HealthInventors: James D. Crapo, Brian J. Day, Michael P. Trova, Polvina Jolicia Gauuan, Douglas B. Kitchen, Irwin Fridovich, Ines Batinic-Haberle
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Publication number: 20140010866Abstract: The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising ergopeptines, triptans, and other compounds, including salts and derivatives of these, and optionally, a hostile biophysical environment and/or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and/or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.Type: ApplicationFiled: December 29, 2011Publication date: January 9, 2014Applicant: Strategic Science & Technologies, LLCInventor: Eric T. Fossel
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Publication number: 20140010783Abstract: 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: July 2, 2013Publication date: January 9, 2014Inventors: Joseph A. Bilotta, Zhi Chen, Elbert Chin, Qingjie Ding, Shawn D. Erickson, Stephen D. Gabriel, Klaus G. Klumpp, Han Ma, Eric Mertz, Jean-Marc Plancher, Robert J. Weikert