1,2,4-triazoles (including Hydrogenated) Patents (Class 514/383)
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8962244
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: February 24, 2015
    Assignee: University of Massachusetts
    Inventor: Sean Ryder
  • Patent number: 8962661
    Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 24, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Akihiro Nishimura
  • Publication number: 20150051225
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 19, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Ishtiyaque Ahmad, Rajagopal Bakthavatchalam, Sivaramakrishna Battula, Henricus Jacobus, Maria Gijsen, Mark Wall
  • Publication number: 20150050241
    Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Fred VOLINSKY, Steven Daniel DONG
  • Publication number: 20150051203
    Abstract: A compound of structural formula (I) or (II): as HSP90 inhibitors that possess significantly improved bioavailability over comparative compounds, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 19, 2015
    Inventors: Dinesh Chimmanamada, Zachary Demko, Weiwen Ying
  • Patent number: 8957096
    Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: February 17, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
  • Patent number: 8957063
    Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
  • Publication number: 20150045327
    Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 12, 2015
    Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
  • Patent number: 8952043
    Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, 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: Grant
    Filed: January 23, 2014
    Date of Patent: February 10, 2015
    Assignee: Genetech, Inc.
    Inventors: 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
  • Publication number: 20150038540
    Abstract: An instantly wettable and rapidly disintegrating oral film dosage form without a surfactant and without a polyalcohol was achieved by combining at least one water soluble polymer that is not a copolymer of vinylpyrrolidone, at least one active agent, a copolymer of vinylpyrrolidone and titanium dioxide. In certain embodiments, the film comprises hydroxypropyl cellulose or a combination of hydroxypropyl cellulose and a polymer or copolymer of vinylpyrrolidone or a substituted vinylpyrrolidone as the water soluble polymer(s). A plasticizer, and optional additives selected from synthetic sweeteners, natural sweeteners, flavorants, antioxidants, colorants, and opacifiers, can be added to the disclosed film oral dosage forms.
    Type: Application
    Filed: July 30, 2014
    Publication date: February 5, 2015
    Applicant: IntelGenx Corp.
    Inventors: Horst G. Zerbe, Angela Angusti, Nadine Paiement
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Patent number: 8946272
    Abstract: The invention relates to crystalline forms of 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid and to its amorphous form, to processes for the preparation thereof, to compositions containing the same and their uses for the manufacture of a medicament for the treatment of the human body.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: February 3, 2015
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Patent number: 8946121
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: February 3, 2015
    Assignee: DSM IP Assets B.V.
    Inventors: Jacobus Stark, Angelique De Rijk
  • Patent number: 8946426
    Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: February 2, 2010
    Date of Patent: February 3, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Henricus Jacobus Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, François Paul Bischoff, Tongfei Wu, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge Maria Aloysius Pieters, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn, Daniel Oehlrich
  • Patent number: 8946231
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Craig M. Potteiger
  • Patent number: 8946236
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Patent number: 8946273
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: February 3, 2015
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha A. De La Rosa, Esmir Gunic, Zhi Hong, Stanley Lang, Woo-Hong Kim
  • Publication number: 20150031656
    Abstract: The present invention relates to a combination therapy for elevating testosterone levels in male mammals in which an antiestrogen or pharmaceutically acceptable salt thereof is co-administered to the mammal with an additional therapeutic agent selected from an androgen and an aromatase inhibitor. The invention is also directed to a combination therapy for treating males with hypogonadism and disorders related thereto, including reduction of muscle mass. limitation of body performance capacity, reduction of bone density, reduction of libido, reduction of potency, reduction of benign prostatic hyperplasia and infertility.
    Type: Application
    Filed: February 28, 2013
    Publication date: January 29, 2015
    Inventors: Joseph S. Podolski, Ronald D. Wiehle
  • Patent number: 8940774
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 27, 2015
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20150026842
    Abstract: This invention relates to the use of the compound flutriafol for protecting plants and plant propagation material from Sudden Death Syndrome. The use comprises applying a composition comprising flutriafol to the soil from which the plant propagation material, a plant, part of a plant and/or plant organ grow or grows at a later point in time.
    Type: Application
    Filed: July 16, 2014
    Publication date: January 22, 2015
    Inventors: James BARRENTINE, Andy BAILEY
  • Publication number: 20150024934
    Abstract: This invention relates to the use of flutriafol for controlling or preventing pathogenic damage caused by the fungi Macrophomina phaseolina in a plant propagation material, a plant, part of a plant and/or plant organ that grow or grows at a later point in time. The use comprises applying a composition of flutriafol on the plant, part of the plant, plant organ, plant propagation material or a surrounding area.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 22, 2015
    Applicant: CHEMINOVA A/S
    Inventors: James BARRENTINE, Andy BAILEY
  • Patent number: 8937094
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 20, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20150017241
    Abstract: Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.
    Type: Application
    Filed: March 6, 2014
    Publication date: January 15, 2015
    Applicant: NOVARTIS AG
    Inventors: Indrajit Ghosh, Jia-Ai Zhang
  • Publication number: 20150018402
    Abstract: The present invention relates to non-aqueous pesticidal dispersible concentrate formulations comprising from about 2 to about 10% of at least one pesticidal agent, from about 15 to about 25% of hexylene glycol, from about 65 to about 75% of propylene glycol, a hydrophobic silica, and a surfactant, wherein the weight percentages are based on the total weight of the formulation. Formulations of the present invention have superior storage stability but are non-phytotoxic to seeds when used as a seed treatment. The present invention also relates to ready-to-use products made from the concentrated formulations of the present invention. Further, the present invention includes methods of using the pesticidal dispersible concentrate formulations and ready-to-use products to achieve superior plant protection and disease control.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 15, 2015
    Inventors: Jane Liu, Toshiya Ogawa, Christopher B. Meador, Michael Seitz, Dair McDuffee, Karen S. Arthur
  • Patent number: 8933111
    Abstract: The invention provides a crystalline form of (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(1H-[1,2,3]triazole-4-carbonyl)amino]pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester or its tautomer. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: January 13, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Miroslav Rapta
  • Publication number: 20150011573
    Abstract: Adjuvant compositions are provided which comprise at least one terpenic alkoxylate and at least one agrochemical active ingredient.
    Type: Application
    Filed: January 18, 2013
    Publication date: January 8, 2015
    Applicants: SYNGENTA PARTICIPATIONS AG, SYNGENTA LIMITED
    Inventors: David Stock, Philip Taylor, Richard Brian Perry, Julia Lynn Ramsey, Gordon Alastair Bell, Emma Jane Ashford
  • Publication number: 20150010635
    Abstract: Controlled release particles are obtained by dissolving a hydrophobic antibiotic compound with a hydrophobic polymerizable vinyl monomer to prepare a hydrophobic solution, blending water with an emulsifier to prepare an aqueous emulsifier solution, emulsifying the hydrophobic solution in the aqueous emulsifier solution, and polymerizing the polymerizable vinyl monomer by mini-emulsion polymerization in the presence of a polymerization initiator, thereby producing a polymer containing an antibiotic compound and having an average particle size of below 1 ?m.
    Type: Application
    Filed: December 27, 2012
    Publication date: January 8, 2015
    Applicant: Japan EnviroChemicals, Ltd.
    Inventors: Junji Oshima, Hideaki Inoue
  • Publication number: 20150010619
    Abstract: 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: Application
    Filed: September 26, 2014
    Publication date: January 8, 2015
    Applicant: Strategic Science & Technologies, LLC
    Inventor: Eric T. Fossel
  • Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Publication number: 20150011592
    Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.
    Type: Application
    Filed: October 24, 2013
    Publication date: January 8, 2015
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Gregor BAHRENBERG, Thomas CHRISTOPH, Klaus SCHIENE, Jean DE VRY, Nils DAMANN, Sven FRORMANN, Bernhard LESCH, Jeewoo LEE, Yong-Soo KIM, Myeong-Seop KIM, Derek SAUNDERS, Hannelore STOCKHAUSEN
  • Patent number: 8921406
    Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.
    Type: Grant
    Filed: August 21, 2006
    Date of Patent: December 30, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Alfred Hahn
  • Patent number: 8921359
    Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: December 30, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Patent number: 8916598
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: December 23, 2014
    Assignee: Proteotech Inc
    Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow
  • Patent number: 8916502
    Abstract: An agent for improving lawn grass quality, which is excellent in promoting dwarfing of lawn grass, making the stem sturdy, increasing the leaf count, and improving greenness, is provided. An agent for improving lawn grass quality containing, as active ingredients, 5-aminolevulinic acid represented by formula (1): R2R1NCH2COCH2CH2COR3??(1) wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryl group or an aralkyl group; and R3 represents a hydroxyl group, an alkoxy group, an acyloxy group, an alkoxycarbonyloxy group, an aryloxy group, an aralkyloxy group or an amino group, or a derivative thereof or a salt of the acid or the derivative, and a gibberellin biosynthesis inhibitor.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: December 23, 2014
    Assignee: Cosmo Oil Co., Ltd.
    Inventors: Yasutomo Takeuchi, Shigeyuki Funada
  • Patent number: 8916597
    Abstract: (1) Use of pyraclostrobin of the formula I as safener for (2) triticonazole of the formula II or salts or adducts thereof for controlling harmful fungi. The use of the compounds I and II in a process for controlling harmful fungi using mixtures of the compounds I and II and the use of the compounds I and II for preparing such mixtures, and also compositions comprising such mixtures.
    Type: Grant
    Filed: November 6, 2006
    Date of Patent: December 23, 2014
    Assignee: BASF SE
    Inventors: Hendrik Ypema, Andreas Hopf, Nathan Froese, Reinhard Stierl
  • Patent number: 8916183
    Abstract: 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: Grant
    Filed: January 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Lindsey G. Fischer, Gary D. Crouse, Thomas C. Sparks, Erich W. Baum
  • Publication number: 20140371213
    Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.
    Type: Application
    Filed: May 19, 2014
    Publication date: December 18, 2014
    Applicant: ASTEX THERAPEUTICS, LTD.
    Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140370320
    Abstract: According to the present invention there is provided a preservative formulation for use in treating wood or other cellulosic formulations, said formulation comprising: at least one biocidal metal compound; at least one organic compound; and a carrier. Preferably, the preservative formulation is copper/(tebuconazole/propiconazole) in a ratio of about 1:3 w/w; the carrier is preferably aqueous or spirit-based.
    Type: Application
    Filed: December 19, 2012
    Publication date: December 18, 2014
    Inventors: David Humphrey, Brett Skewes
  • Publication number: 20140371066
    Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1 and R2 are as defined in the description, and the active compound groups (2) to (24) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL, Hans-Ludwig ELBE, Heiko RIECK, Anne SUTY-HEINZE
  • Publication number: 20140364317
    Abstract: The present invention relates to a method for a preparation of a solid composition comprising the steps of a) dissolving a premix in a premix-solvent, or melting a premix, wherein the premix contains a pesticide and a nonionic, amphiphilic polyalkoxylate, b) solidifying the premix by removing the premix-solvent, or by cooling, and c) contacting the premix with at least one auxiliary. The invention further relates to a solid composition obtainable by said method; to a method for the preparation of an aqueous tank mix, in which a pesticide is present as suspended particles having a particle size below 1.
    Type: Application
    Filed: November 29, 2012
    Publication date: December 11, 2014
    Applicant: BASF SE
    Inventors: Claude Taranta, Thomas Bork, Jochen Schreieck, Helmut Müller, Nadine Riediger, Clark D. Klein, Rebecca Willis, Tatjana Sikuljak, Murat Mertoglu
  • Publication number: 20140364308
    Abstract: There is provided a microcapsule for plant disease control in which a core material containing a fungicidal active ingredient is enclosed within a shell material; wherein the microcapsule satisfies the following conditions (1) and (2), is a formulation that withstands physical impacts, drying and diluting, and is suitable for seed treatment using a stirring type machine, and the durability of control of diseases of crops and the safety for the crops can be improved more efficiently by the microcapsule of the present invention; Condition (1): D50/T?230; Condition (2): (D90?D10)/D50?2.5; and wherein in the formulae of conditions (1) and (2), T represents the shell thickness (?m) of the microcapsule, and D10, D50 and D90 respectively represent the 10%, 50% and 90% cumulative volume particle diameter (?m) of the microcapsule.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 11, 2014
    Inventors: Takuya Tanaka, Nobuhito Ueda
  • Publication number: 20140364408
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 8906885
    Abstract: Methods of treating cancer with a compound of formulae (I) or (1a) 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 (1a). Further provided are methods of treating non-small cell lung cancer with a mutation in ALK with a compound of formulae (I) or (1a); a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: December 9, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Iman El-Hariry, David Proia, Vojo Vukovic
  • Publication number: 20140357649
    Abstract: The present invention relates to novel phenyl(oxy/thio)alkanol derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: August 13, 2014
    Publication date: December 4, 2014
    Inventors: Carl Friedrich NISING, Klaus Kunz, Jörg Nico Greul, Hendrick Helmke, Gorka Peris, Jürgen Benting, Peter Dahmen, Isolde Hauser-Hahn, Ines Heinemann, Christian Paulitz, Dirk Schmutzler, Ulrike Wachendorff-Neumann, Tomoki Tsuchiya, Christoph Andreas Braun, Ruth Meissner, Thomas Knobloch
  • Patent number: 8901125
    Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: Grant
    Filed: June 19, 2013
    Date of Patent: December 2, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James Macdonald, Han Min Tong, Miguel Angel Pena-Piñón, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil
  • Patent number: 8901156
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 2, 2014
    Assignee: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Publication number: 20140349918
    Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Applicants: Singapore Health Services Pte Ltd., Agency for Science, Technology and Research
    Inventors: Hanxun Zou, Lakshminiarayan Rajanmani, Lei Zhou, Chang Chui Charles Tang, Jun Jie Koh, Tiang Hwee Donald Tan, Chandra Verma, Roger W. Beuerman, Shouping Liu, Saraswathi Padmanabhan