1,2,4-triazoles (including Hydrogenated) Patents (Class 548/262.2)
  • Patent number: 10336737
    Abstract: Described herein is the development of an arenophile-mediated, nickel-catalyzed dearomative trans-1,2-carboamination protocol. A range of readily available aromatic compounds was converted to the corresponding dienes using Grignard reagents as nucleophiles. This strategy provided products with exclusive trans-selectivity and high enantioselectivity was observed in case of benzene and naphthalene. The utility of this methodology was showcased by controlled and stereoselective preparation of small, functionalized molecules. A concise synthesis of (+)-pancratistatin and (+)-7-deoxypancratistatin from benzene using an enantioselective, dearomative carboamination strategy has been achieved. This approach, in combination with the judicious choice of subsequent olefin-type difunctionalization reactions, permits rapid and controlled access to a hexasubstituted core. Finally, minimal use of intermediary steps as well as direct, late stage C-7 hydroxylation provides both natural products in six and seven operations.
    Type: Grant
    Filed: June 18, 2018
    Date of Patent: July 2, 2019
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: David Sarlah, Lucas William Hernandez, Jola Pospech
  • Patent number: 9814236
    Abstract: An agricultural or horticultural chemical according to the present invention is an agricultural or horticultural chemical containing a plurality of active ingredients, the agricultural or horticultural chemical comprises, as one of the active ingredients, an azole derivative represented by general formula (I) below, and can be used as a plant disease controlling agent that can reduce the content of an active ingredient, (In the general formula, R1 represents an alkyl group having from 1 to 6 carbons, R2 represents a hydrogen atom, an alkyl group having from 1 to 3 carbons, an alkenyl group or an alkynyl group having from 2 to 3 carbons, A represents a nitrogen atom or a methine group, Y1 represents a halogen atom, and n represents either 0 or 1).
    Type: Grant
    Filed: October 8, 2014
    Date of Patent: November 14, 2017
    Assignee: Kureha Corporation
    Inventors: Taiji Miyake, Nobuyuki Araki
  • Patent number: 9750254
    Abstract: An agricultural or horticultural chemical according to the present invention is an agricultural or horticultural chemical containing a plurality of active ingredients, the agricultural or horticultural chemical comprises, as one of the active ingredients, an azole derivative represented by general formula (I) below, and can be used as a plant disease controlling agent that can reduce the content of an active ingredient: wherein, R1 represents an alkyl group having from 1 to 6 carbons, R2 represents a hydrogen atom, an alkyl group having from 1 to 3 carbons, an alkenyl group or an alkynyl group having from 2 to 3 carbons, A represents a nitrogen atom or a methine group, Y1 represents a halogen atom, and n represents either 0 or 1.
    Type: Grant
    Filed: October 8, 2014
    Date of Patent: September 5, 2017
    Assignee: KUREHA CORPORATION
    Inventors: Taiji Miyake, Nobuyuki Araki
  • Patent number: 9394311
    Abstract: The present invention provides compounds of formula (Ia) and (Ib) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: July 19, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Bernd Kuhn, Christian Lerner, Markus Rudolph, Herve Schaffhauser
  • Patent number: 9150524
    Abstract: The present invention relates to an improved process for the preparation of Letrozole (I) and its synthetic intermediate 4-[(1-(1,2,4-triazoly)methyl]benzonitrile (III). In particular, it relates to a process to prepare Letrozole and its intermediate (III) substantially free from regioisomeric impurities. The present invention further relates to acid addition salts of 4-[(1-(1,2,4-triazoly)methyl]benzonitrile (III) such as the oxalate salt, and also to Letrozole (I), the intermediate (III) and salts thereof preparable by the processes of the present invention.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 6, 2015
    Assignee: Generics [UK] Limited
    Inventors: Vinayak Govind Gore, Vinay Kumar Shukla, Sandeep Mekde, Suresh Hasbe, Shreyas Bhandari, Dhananjay Shinde, Madhukar Shaligram Patil
  • Patent number: 9035069
    Abstract: Provided is an azole derivative superior in disease-controlling activity contained as an active ingredient in agricultural or horticultural chemical agents. The azole derivative according to the present invention is represented by the following General Formula (I): (in Formula (I), R1 represents an unsubstituted or substituted C1-C6-alkyl group; R2 represents a carbonyl group-containing functional group, wherein the carbon atom in the carbonyl group is bound to the carbon atom in the cyclopentane ring substituted with R1 and to a hydrogen atom, a hydroxyl group, R3, OR3, or NR3R4; R3 and R4 each represent a C1-C6-alkyl group, a C2-C6-alkenyl group, or a C2-C6-alkynyl group; Y represents a halogen atom, a C1-C4-alkyl group, a C1-C4-haloalkyl group, a C1-C4-alkoxy group, a C1-C4-haloalkoxy group, a phenyl group, a cyano group, or a nitro group; m is 0 to 5; and A represents a nitrogen atom or a methine group).
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: May 19, 2015
    Assignee: Kureha Corporation
    Inventors: Nobuyuki Araki, Taiji Miyake, Eiyu Imai, Emiko Obata
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20150119579
    Abstract: Generation of by-product is reduced by producing a triazolylmethyl cycloalkanol derivative by reacting a cycloalkanone derivative and an alkali metal salt of 1,2,4-triazole in the presence of a sulfur ylide at a reaction temperature of higher than 110° C. and 140° C. or lower.
    Type: Application
    Filed: March 5, 2013
    Publication date: April 30, 2015
    Inventors: Takashi Oohashi, Nobuyuki Araki, Takashi Shimokawara
  • Patent number: 8981111
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Marie-Claire Grosjean-Cournoyer, Daniela Portz, Rachel Rama, Philippe Rinolfi, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Patent number: 8980886
    Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
  • Patent number: 8969248
    Abstract: The present invention relates to novel 5-iodotriazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: March 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hendrik Helmke, Carl Friedrich Nising, Gorka Peris, Pierre Cristau, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • 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: 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
  • 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
  • Publication number: 20140336389
    Abstract: In order to manufacture a higher yield of a 4-benzyl-1-methyl-6-oxabicyclo[3,2,0]heptane derivative, the present invention is a method for manufacturing a compound represented by General Formula (I) which includes a step for reducing a compound represented by General Formula (II) using a hydride-type reducing agent in an aprotic solvent having an amide bond.
    Type: Application
    Filed: November 5, 2012
    Publication date: November 13, 2014
    Applicant: Kureha Corporation
    Inventor: Hisashi Kanno
  • Publication number: 20140315967
    Abstract: In order to provide a compound which exhibits a high controlling effect against plant diseases and is able to reduce phytotoxicity, the present invention is a triazole derivative represented by General Formula (I), the azole derivative being a (?)-enantiomer or (+)-enantiomer having an —R1 group, hydroxy group, and substituted or unsubstituted benzyl group bonded to a cyclopentane ring in cis-form.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 23, 2014
    Inventors: Nobuyuki Araki, Taiji Miyake, Emiko Obata
  • Patent number: 8859607
    Abstract: The present invention relates to crystalline complexes comprising at least one agriculturally active organic compound A having at least one functional moiety which is capable as serving as a hydrogen acceptor in a hydrogen bond and thiophanate-methyl.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: October 14, 2014
    Assignee: BASF SE
    Inventors: Rafel Israels, Heidi Emilia Saxell, Matthias Bratz, Marco Kuhns, Peter Erk
  • Patent number: 8822519
    Abstract: 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: Grant
    Filed: August 7, 2009
    Date of Patent: September 2, 2014
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Chunhua Jin, Xiaoyu Liu, Zhenliang Chen, Xiaohe Zheng, Shoufeng Ming
  • Patent number: 8748358
    Abstract: Provided is an additive for lubricating oils which enhances frictional characteristics of slide parts in internal combustion engines and driving system transmission engines and which exhibit an excellent fuel consumption reducing effect. The above additive for lubricating oils comprises a heterocyclic compound having a heterocyclic skeleton originating in a compound selected from pyridines, pyrroles, pyrimidines, pyrazoles, pyridazines, indazoles, pyrazines, triazines, triazoles, tetrazoles, oxazoles, oxadiazoles, thiazoles, thiadiazoles, furans, dioxanes, pyrans and thiophenes. A lubricating oil composition containing the above additive for lubricating oils is effectively used for various low friction slide members, antifriction bearings and slide bearings.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: June 10, 2014
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Hiroaki Koshima, Hideki Kamano
  • Publication number: 20140155262
    Abstract: The present invention relates to substituted 2-[2-halogenalkyl-4-(phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof, their preparation and intermediates for preparing them. The invention also relates to the use of these compounds for combating harmful fungi and seed coated with at least one such compound and also to compositions comprising at least one such compound.
    Type: Application
    Filed: July 12, 2012
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Mueller, Wassilios Grammenos, Thomas Grote
  • Patent number: 8742133
    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: Grant
    Filed: August 13, 2008
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Lijun Sun, Keizo Koya, Dinesh U. Chimmanamada, Shijie Zhang, Teresa Kowalcyzk-Przewloka, Hao Li
  • Patent number: 8742130
    Abstract: The present invention provides new hydrate forms of triazole, triazole alkaline salt, and alkali doped 1,2,4-triazole. The present invention also discloses processes for manufacturing new hydrate forms of triazole, triazole alkaline salt, and alkali-doped 1,2,4-triazole. The present invention also relates to compositions for different applications of new hydrate forms of triazole, triazole alkaline salt, and alkali doped 1,2,4-triazole. In addition, the present invention provides co-crystal form of triazole with acid, and methods of preparing thereof.
    Type: Grant
    Filed: November 1, 2012
    Date of Patent: June 3, 2014
    Assignee: Fujifilm Planar Solutions, LLC
    Inventors: Deepak Mahulikar, Luling Wang
  • Patent number: 8728978
    Abstract: Suggested are biocide compositions, comprising (a) esters based on ketocarboxylic acids, (b) biocides, and optionally (c) oil components or co-solvents and/or (d) emulsifiers. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. over a longer period.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: May 20, 2014
    Assignee: Cognis IP Management GmbH
    Inventors: Joaquin Bigorra Llosas, Stéphanie Merlet, Ramon Valls, Stefan Busch
  • Patent number: 8722717
    Abstract: The present invention constitutes new 3-triazolylphenyl-substituted sulphide derivatives of the formula (I) in which A1, A2, B0, B1, B2, B3, X, 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: Grant
    Filed: August 19, 2010
    Date of Patent: May 13, 2014
    Assignee: Bayer CropScience AG
    Inventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste, Ulrich Görgens
  • Publication number: 20140121382
    Abstract: The present invention provides new hydrate forms of triazole, triazole alkaline salt, and alkali doped 1,2,4-triazole. The present invention also discloses processes for manufacturing new hydrate forms of triazole, triazole alkaline salt, and alkali-doped 1,2,4-triazole. The present invention also relates to compositions for different applications of new hydrate forms of triazole, triazole alkaline salt, and alkali doped 1,2,4-triazole. In addition, the present invention provides co-crystal form of triazole with acid, and methods of preparing thereof.
    Type: Application
    Filed: November 1, 2012
    Publication date: May 1, 2014
    Applicant: FUJIFILM PLANAR SOLUTIONS, LLC
    Inventors: Deepak Mahulikar, Luling Wang
  • Patent number: 8710089
    Abstract: The present invention provides novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: April 29, 2014
    Assignees: Zentaris GmbH, Le Centre National de la Recherche Scientifique, University of Montpellier I, University of Montpellier II
    Inventors: Daniel Perrissoud, Jean Martinez, Aline Moulin, Jean-Alain Fehrentz, Damien Boeglin, Luc Demange
  • Patent number: 8710055
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: April 29, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Steffen Steurer
  • Publication number: 20140113815
    Abstract: In order to provide a novel azole derivative, an azole derivative of the present invention is an azole derivative represented by a general formula (V?). (where R6 and R7 independently represent a hydrogen atom, a C1-C4 alkyl group, a phenyl group, or a benzyl group; X represents a halogen atom, a C1-C4 alkyl group, a haloalkyl group, an alkoxy group or a haloalkoxy group, a phenyl group, a cyano group, or a nitro group; m represents an integer of 0 to 5; and A represents a nitrogen atom or a methyne group.
    Type: Application
    Filed: June 6, 2012
    Publication date: April 24, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Toru Yamazaki, Emiko Obata, Taiji Miyake, Hisashi Kanno
  • Patent number: 8691998
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 8, 2014
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam S. Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Publication number: 20140094362
    Abstract: 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: Application
    Filed: May 30, 2012
    Publication date: April 3, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Taiji Miyake, Nobuyuki Araki, Toru Yamazaki
  • Patent number: 8653121
    Abstract: 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: Grant
    Filed: May 28, 2008
    Date of Patent: February 18, 2014
    Assignee: Rotam Agrochem International Co., Ltd.
    Inventors: Amanda Yin, Sonia Chen, Yifan Wu, Pichumani Narayanamoorthy, Chang Yuan Lo
  • Publication number: 20140039018
    Abstract: 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: Application
    Filed: March 1, 2012
    Publication date: February 6, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Hideaki Tateishi, Takumi Nishiuchi
  • Patent number: 8642585
    Abstract: 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: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • Patent number: 8632767
    Abstract: 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: Grant
    Filed: August 19, 2010
    Date of Patent: January 21, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Bernd Alig, Stefan Antons, Reiner Fischer, Norbert Lui, Adeline Köhler, Arnd Voerste
  • Patent number: 8632914
    Abstract: The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1?-R3?, R8-R11, X, X?, X?, Y, Y? and Y? are as defined in the disclosure.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: January 21, 2014
    Assignee: University Health Network
    Inventors: Ian E. Crandall, Walter A. Szarek, Jason Z. Vlahakis
  • Patent number: 8633232
    Abstract: 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: Grant
    Filed: May 4, 2012
    Date of Patent: January 21, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Esmir Gunic, Jean-Luc Girardet, Jean-Michel Vernier, Martina E. Tedder, David A. Paisner
  • Patent number: 8618144
    Abstract: 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: Grant
    Filed: April 28, 2010
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Patent number: 8614168
    Abstract: The invention relates to the use of at least one compound, selected from the group consisting of tebuconazole, epoxiconazole, metconazole, cyproconazole, prothioconazole and any mixtures thereof, for increasing the resistance of plants to abiotic stress factors.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: December 24, 2013
    Assignee: Monheim
    Inventors: Jan Dittgen, Isolde Häuser-Hahn, Heinz Kehne, Stefan Lehr, Jörg Tiebes, Marco Busch
  • Patent number: 8569350
    Abstract: Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: October 29, 2013
    Assignee: Rutgers, The State University of New Jersey
    Inventors: William J. Welsh, Youyi Peng, Xin Wang, Susan M. Keenan, Qiang Zhang, Sonia Arora
  • Patent number: 8568756
    Abstract: 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: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8551980
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: October 8, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Benjamin Bader, Philip Lienau, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner
  • Patent number: 8552043
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having N-(?-mercaptoacetyl) p amino benzoic acid derivatives. are provided, where Q is CO2H, or a salt or ester thereof, or a C(O) N-linked amino acid. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: October 8, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Martha De La Rosa, Zhi Hong, Stanley Lang
  • Patent number: 8546434
    Abstract: 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: Grant
    Filed: April 13, 2011
    Date of Patent: October 1, 2013
    Assignee: Novartis AG
    Inventors: Tinya Abrams, Paul Barsanti, Yu Ding, David Duhl, Wooseok Han, Cheng Hu, Yue Pan
  • Patent number: 8546436
    Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: October 1, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Laszlo R. Treiber, Gabriel Galvin, Irina Zamansky, Jean-Luc Girardet
  • Patent number: 8546435
    Abstract: The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: October 1, 2013
    Assignees: AEterna Zentaris GmbH, Centre National de la Recherche Scientifique, University of Montpellier I, University of Montpellier II
    Inventors: Babette Aicher, Gilbert Mueller, Klaus Paulini, Lars Blumenstein, Peter Schmidt, Matthias Gerlach, Michael Teifel, Jean Martinez, Jean-Alain Fehrentz, Anne-Laure Blayo
  • Patent number: 8546437
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of 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: Grant
    Filed: June 30, 2011
    Date of Patent: October 1, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
  • Patent number: 8524754
    Abstract: Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: September 3, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Irina Zamansky, Jean-Luc Girardet, Gabriel Galvin
  • Publication number: 20130225644
    Abstract: Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 29, 2013
    Applicant: Zealand Pharma A/S
    Inventor: Zealand Pharma A/S
  • Patent number: 8513436
    Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: August 20, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick