Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/376.1)
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Publication number: 20150141477Abstract: The present invention relates to compounds of the formula (I), wherein the residues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 16, 2013Publication date: May 21, 2015Inventors: Marc Nazare, Detlef Kozian, Andreas Evers, Werngard Czechtizky
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Patent number: 9035071Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: December 19, 2012Date of Patent: May 19, 2015Assignee: Allergan, Inc.Inventors: Jussi J. Kangasmetsa, William R. Carling, Jose L. Martos, David F. Woodward, Jenny W. Wang
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Patent number: 9023874Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: Merial, Inc.Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Publication number: 20150119438Abstract: The present invention provides 3-{1-[5-chloro-2-(2-ethylbutoxy)benzyl]-5-methyl-1H-pyrazol-3-yl}propanoicacid in crystalline form. The present invention further provides methods for treating disorders associated with DP1, FP, TP, EP1 and EP4 prostaglandin (PG) receptors.Type: ApplicationFiled: October 31, 2014Publication date: April 30, 2015Inventors: Ke Wu, Gyorgy F. Ambrus
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Publication number: 20150087833Abstract: An alkyl phenyl sulfide derivative represented by the general formula [I] or an agriculturally acceptable salt thereof, and a pest control agent containing the derivative or the salt as an active ingredient. [in the above formula, R1 is, for example, a C1˜C6 alkyl group which is mono- or poly-substituted with halogen atom; R2 is, for example, a halogen atom or a C1˜C6 alkyl group; R3 is, for example, a hydrogen atom or a halogen atom; and R4 is, for example, a hydrogen atom or a C1˜C12 alkyl group.] The derivative or the salt has an excellent pest control effect.Type: ApplicationFiled: April 11, 2013Publication date: March 26, 2015Applicants: IHARA CHEMICAL INDUSTRY CO., LTD., KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Kei Domon, Keiji Toriyabe, Yutaka Ogawa, Junichiro Bessho, Kei Kawamoto, Akira Watanabe, Masaaki Komatsu, Takeshi Matsuda, Seisuke Ito
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Publication number: 20150080446Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: September 16, 2014Publication date: March 19, 2015Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
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Patent number: 8957066Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.Type: GrantFiled: March 15, 2013Date of Patent: February 17, 2015Assignee: Biomarin Pharmaceutical Inc.Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
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Publication number: 20150045399Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.Type: ApplicationFiled: September 2, 2014Publication date: February 12, 2015Applicant: Alexar Therapeutics, Inc.Inventor: Raju Mohan
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Patent number: 8952042Abstract: The present invention relates to compounds of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: GrantFiled: August 19, 2010Date of Patent: February 10, 2015Assignee: Phenex Pharmaceuticals AGInventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
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Publication number: 20150025120Abstract: A compound represented by the following formula: or a pharmaceutically acceptable salt thereof, and pharmaceutical use thereof.Type: ApplicationFiled: June 30, 2014Publication date: January 22, 2015Inventors: Takahisa MOTOMURA, Takuya MATSUO, Gakujun SHOMI, Masafumi INOUE
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Patent number: 8937083Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: October 24, 2012Date of Patent: January 20, 2015Assignee: DowAgroSciences, LLCInventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul Renee LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
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Patent number: 8901153Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Dow AgroSciences, LLC.Inventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul Renee LePlae, Jr., Frank Wessels, Ronald Ross, Jr., Carl DeAmicis, Peter Borromeo
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Patent number: 8889727Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is providedType: GrantFiled: January 30, 2012Date of Patent: November 18, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Patent number: 8877795Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and thereby decreasing aggregate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: GrantFiled: May 5, 2011Date of Patent: November 4, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Isabella A. Graef, Mamoun Alhamadsheh
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Publication number: 20140323303Abstract: The present invention relates to a compound of formula (I): wherein: X is methyl or chlorine; R1 is methyl or chlorine; R2 is hydrogen, methyl, ethyl, n-propyl, cyclopropyl, vinyl, ethynyl, fluorine, chlorine, bromine, methoxy, ethoxy or fluoromethoxy; and G, R3, R4, R5 and R6 are as defined herein; wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.Type: ApplicationFiled: November 30, 2012Publication date: October 30, 2014Applicants: Syngenta Participations AG, Syngenta LimitedInventors: Alaric James Avery, Mangala Mahadev Phadte, James Nicholas Scutt, John Benjamin Taylor, Russell Colin Viner, Jeffrey Steven Wailes
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Publication number: 20140323538Abstract: Compounds according to formula I: wherein Ar is a fused aryl group, R1 is selected from alkyl and aryl amides, CF3, and CH2OH, and R2 is selected from hydrogen, —C(?O)CH2NH2, and —C(?O)CH2CH2NH2 are described. The compounds are effective for inhibiting p21-activated kinases, and can be used for prevention and treatment of cancer.Type: ApplicationFiled: March 31, 2014Publication date: October 30, 2014Applicant: Ohio State Innovation FoundationInventors: Ching-Shih Chen, Matthew David Ringel, Motoyashi Saji, Yihui Ma
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Publication number: 20140309206Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.Type: ApplicationFiled: June 27, 2014Publication date: October 16, 2014Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
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Patent number: 8859606Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: January 21, 2013Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
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Publication number: 20140296316Abstract: A compound represented by the formula (J): or a crystal thereof, or a compound represented by the formula (Q): or a crystal thereof.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: JAPAN TOBACCO INC.Inventor: Takahisa Motomura
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Publication number: 20140288074Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, fungicides: wherein Q1, R1, R1a, R2, R3 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: March 21, 2014Publication date: September 25, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: ANDREW EDMUND TAGGI, Jeffrey Keith Long, Moumita Kar
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Publication number: 20140243362Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.Type: ApplicationFiled: September 25, 2012Publication date: August 28, 2014Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
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Publication number: 20140235689Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R1, R1a, R2, R3, R4, Q1 and Q2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: February 19, 2014Publication date: August 21, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventor: MOUMITA KAR
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Patent number: 8809351Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.Type: GrantFiled: February 6, 2013Date of Patent: August 19, 2014Assignee: Innovative Med Concepts, LLC.Inventor: William L. Pridgen
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Publication number: 20140221448Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Amy X. Ding
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Publication number: 20140179751Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of proteins particularly proteins that tend to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of proteins and thereby decreasing aggregate formation by these proteins. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: ApplicationFiled: March 14, 2013Publication date: June 26, 2014Inventors: Isabella A. Graef, Mamoun M. Alhamadsheh
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Patent number: 8754115Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: GrantFiled: August 31, 2011Date of Patent: June 17, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Jeffrey Keith Long, Paula Louise Sharpe, Amy X Ding
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Patent number: 8735398Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: GrantFiled: November 7, 2012Date of Patent: May 27, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Publication number: 20140121258Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxyl}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula (I). Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: July 1, 2011Publication date: May 1, 2014Applicant: ALLERGAN, INC.Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
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Patent number: 8658647Abstract: A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.Type: GrantFiled: November 21, 2011Date of Patent: February 25, 2014Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Su-Lin Lee, Samuel K. Kulp
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Publication number: 20140038923Abstract: The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay.Type: ApplicationFiled: December 12, 2011Publication date: February 6, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Karen Wagner, Christophe Morisseau, Aaron Wecksler, Guodong Zhang
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Publication number: 20140031553Abstract: The use of thiazole-4-carboxylic esters and thioesters of the formula (I) in which R1, R2, R3, R4, R5, R6, R7, Y1, Y2, Y3, W, X and G have the meanings given in the description, and also of agrochemically active salts thereof, as fungicides.Type: ApplicationFiled: September 27, 2013Publication date: January 30, 2014Inventors: Pierre CRISTAU, Stefan HERRMANN, Nicola RAHN, Arnd VOERSTE, Ulrike WACHENDORFF-NEUMANN, Tomoki TSUCHIYA
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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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Publication number: 20130317003Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).Type: ApplicationFiled: March 15, 2013Publication date: November 28, 2013Inventor: Repligen Corporation
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Publication number: 20130317074Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is providedType: ApplicationFiled: January 30, 2012Publication date: November 28, 2013Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Publication number: 20130289283Abstract: An improved oxidation process for preparing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulphinyl-pyrazole, of formula (I) is described. The process includes admixing 5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylthiopyrazole of formula (II) with dichloroacetic acid and hydrogen peroxide in the presence of a strong acid.Type: ApplicationFiled: June 25, 2013Publication date: October 31, 2013Inventors: Anat Levin, Michael Grabarnick
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Publication number: 20130281455Abstract: Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], wherein the symbols have the meanings stated in the description, and agrochemically active salts thereof and the use thereof for the control of undesired microorganisms in the protection of plants and materials and for the reduction of mycotoxins in plants and plant parts and methods for the production of compounds of the formula [I-a] and [I-b].Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Inventors: Alexander SUDAU, Mazen ES-SAYED, Christoph Andreas BRAUN, Ruth MEISSNER, Catherine SIRVEN, Jürgen BENTING, Peter DAHMEN, Daniela PORTZ, Ulrike WACHENDORFF-NEUMANN, Philippe DESBORDES, Samir BENNABI, Christophe CATHERIN, Anne-Sophie REBSTOCK, Marie-Claire GROSJEAN-COURNOYER, Hiroyuki HADANO, Thomas KNOBLOCH, Philippe RINOLFI
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Publication number: 20130274240Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.Type: ApplicationFiled: November 5, 2012Publication date: October 17, 2013Inventor: JAPAN TOBACCO INC.
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Publication number: 20130253028Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: May 20, 2013Publication date: September 26, 2013Applicant: ALLERGAN, INC.Inventors: WILLIAM R. CARLING, JOSE L. MARTOS, DAVID F. WOODWARD, JENNY W. WANG, JUSSI J. KANGASMETSA
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Publication number: 20130253004Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: December 6, 2011Publication date: September 26, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Thomas Jon Seiders, Bowei Wang, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots
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Publication number: 20130203777Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and therby decreasing aggegate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: ApplicationFiled: May 5, 2011Publication date: August 8, 2013Inventors: Isabella A. Graef, Mamoun Alhamadsheh
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Patent number: 8492424Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: June 28, 2011Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: William R. Carling, Jose L. Martos, David F. Woodward, Jenny W. Wang, Jussi J. Kangasmetsa
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Publication number: 20130177529Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.Type: ApplicationFiled: November 15, 2012Publication date: July 11, 2013Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
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Publication number: 20130165666Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: December 19, 2012Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130143870Abstract: 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: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130143940Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein Q1, Q2, R1, R2, R4, R5 and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 31, 2011Publication date: June 6, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Mary Ann Hanagan, Eric Allen Marshall, Paula Louise Sharpe, Amy X. Ding
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Publication number: 20130131135Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: January 21, 2013Publication date: May 23, 2013Applicant: ALLERGAN, INC.Inventor: Allergan, Inc.
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Patent number: 8383654Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: GrantFiled: November 16, 2009Date of Patent: February 26, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Brian Andrew Stearns, Timothy Parr
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Publication number: 20120289403Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: ApplicationFiled: November 11, 2010Publication date: November 15, 2012Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Patent number: 8309740Abstract: The present invention relates to a method for one-pot synthesis of ionic liquid with fluoroalkyl group, more particularly to a method for one-pot synthesis of ionic liquid with fluoroalkyl group represented by the following Chemical Formula 1 by adding and reacting a nitrogen-containing compound, a Brønsted acid of the formula YH and a fluoroolefin compound of the formula CFR1?CR2R3 in a single reactor: wherein represents a nitrogen-containing compound; Y? represents an anion of the Brønsted acid; and R1, R2 and R3, which may be same or different, represent hydrogen, fluorine, C1-C10 alkyl or C1-C10 fluoroalkyl having from 1 to 23 fluorine atoms.Type: GrantFiled: August 15, 2008Date of Patent: November 13, 2012Assignee: Korea Institute of Science and TechnologyInventors: Hyun Joo Lee, Dong Jin Suh, Byoung Sung Ahn, Hong Gon Kim, Chang Soo Kim, Hoon Sik Kim
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Publication number: 20120264790Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 1, 2012Publication date: October 18, 2012Applicant: SANOFIInventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK