Chalcogen Or Nitrogen Bonded Directly To The Pyrazole Ring By Nonionic Bonding Patents (Class 514/407)
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Publication number: 20140051740Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: October 22, 2013Publication date: February 20, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Tesfaye Biftu, Ann E. Weber
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Patent number: 8653128Abstract: A stable liquid pharmaceutical formulation containing an N-phenylpyrazole derivative, a crystallization inhibitor/viscolizer and a solvent/co-solvent system comprised of a glycol ether solvent and at least one mono alkyl ester co-solvent; and the use of such a formulation for the prevention and/or treatment of infestations with fleas and ticks.Type: GrantFiled: March 23, 2012Date of Patent: February 18, 2014Inventor: Jugal K. Taneja
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Patent number: 8653112Abstract: The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: GrantFiled: October 6, 2010Date of Patent: February 18, 2014Assignee: Karo Bio ABInventors: Joakim Löfstedt, Xiongyu Wu, Lars Krüger
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Publication number: 20140045906Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: August 7, 2013Publication date: February 13, 2014Inventors: Melissa Fleury, Adam D. Hughes
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as 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 said compounds.Type: ApplicationFiled: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Patent number: 8642626Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.Type: GrantFiled: July 29, 2011Date of Patent: February 4, 2014Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
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Patent number: 8642636Abstract: This invention provides for dimeric1-arylpyrazole compounds, of formulas (I), (II), and (III): or salts thereof, and the use of these compounds against ectoparasites such as insects, arthropods and acarina. The resulting compounds may be used in veterinary formulations such as, for example, spot-on and pour-on formulations, which may be used for treatment, controlling and preventing of parasitic infections in warm-blooded animals and birds.Type: GrantFiled: November 18, 2009Date of Patent: February 4, 2014Assignee: Merial LimitedInventor: Charles Q. Meng
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Publication number: 20140031205Abstract: The present invention relates to an agrochemical composition containing a pesticide and a copolymer, which contains in polymerized form at least 20 wt % vinylimidazol and/or a quaternized vinylimidazol, an acidic comonomer, and a hydrophobic comonomer, which comprises C1-22 alkyl (meth)acrylate, mono C1-22 alkyl terminated poly(ethylene glycol) (meth)acrylate, vinyl ester of aliphatic C1-32 carboxylic acids, or vinyl C1-4 alkyl ether. It further relates to a method for preparing said composition by mixing the pesticide and the copolymer; and to a use of said copolymer as dispersing agent in a composition containing a pesticide.Type: ApplicationFiled: April 2, 2012Publication date: January 30, 2014Applicant: BASF SEInventors: Murat Mertoglu, Stefan Fischer, Son Nguyen Kim
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Publication number: 20140031406Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Izumi SASAKI, Tomohiro TOYODA, Hidefumi YOSHINAGA, Itaru NATSUTANI, Yoko TAKAHASHI
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Publication number: 20140031331Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: September 19, 2013Publication date: January 30, 2014Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
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Patent number: 8637059Abstract: The present invention relates to mixtures comprising as active components a) carbamate derivatives of the formula (I) in which the substituents and the index have the following meaning: T is CH or N n is 0, 1 or 2 R is halogen, C1-C4-alkyl or C1-C4-haloalkyl, it being possible for the radicals R to be different when n is 2, and b) at least one compound of the formula (II).Type: GrantFiled: December 15, 2004Date of Patent: January 28, 2014Assignee: BASF SEInventors: Edson Begliomini, Sergio Zambon
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Patent number: 8637060Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: GrantFiled: October 5, 2011Date of Patent: January 28, 2014Assignee: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Publication number: 20140024693Abstract: A topical composition comprising: fipronil or a pharmaceutically acceptable salt thereof; at least one surfactant and at least one crystallization inhibitor for the treatment and protection of animals which are infested with parasites.Type: ApplicationFiled: July 12, 2013Publication date: January 23, 2014Inventors: Geena MALHOTRA, Amar Lulla, Martin Benedict George Donnelly
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Patent number: 8633237Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.Type: GrantFiled: April 8, 2010Date of Patent: January 21, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Kevin J. Gillen, Jonathan Gillespie, Craig Jamieson, John K. F. MacLean, Elizabeth M. Moir, Zoran Rankovic
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Publication number: 20140013654Abstract: Ready-to-use foamable pesticide compositions that contain a particulate pesticide suspended therein and applicators for dispensing such compositions. Methods for treating pests such as arthropods by contacting pests with such compositions are also provided.Type: ApplicationFiled: September 17, 2013Publication date: January 16, 2014Inventor: Terrence R. Burke
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Patent number: 8623876Abstract: Substituted pyrrolo-pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with dysregulated protein kinase activity, like cancer.Type: GrantFiled: June 13, 2012Date of Patent: January 7, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri
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Publication number: 20140005245Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests wherein A1, A2, A3, A4, R1, R2, G1, Q1 and Q2 are as defined in claim 1; or salts or N— oxides thereof.Type: ApplicationFiled: February 7, 2012Publication date: January 2, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold, Thomas Pitterna
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Publication number: 20140005231Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein L is —C(R12a)R12b—C(R13a)R13b—, wherein the carbon atom bonded to R12a and R12b is also bonded to the carboxamide nitrogen atom in Formula 1; or 1,2-phenylene optionally substituted with up to 4 substituents independently selected from halogen and C1-C2 alkyl; and A, Z, R1, R2, n, G and Q 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. Also disclosed are methods for controlling a phytophagous nematode comprising contacting the nematode or its environment with a nematocidally effective amount of a compound of Formula 1 wherein L is —C(R12a)R12b—C(R13a)R13b; and A, Z, R1, R2, n, G and Q are as defined in the disclosure.Type: ApplicationFiled: June 19, 2013Publication date: January 2, 2014Inventors: JAMES FRANCIS BEREZNAK, Steven Gutteridge, Ravisekhara P. Reddy, Andrew Edmund Taggi, Matthew James Campbell, Moumita Kar, Johan A. J. Desaeger
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Patent number: 8617582Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: GrantFiled: October 5, 2011Date of Patent: December 31, 2013Assignee: Sergeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Patent number: 8618022Abstract: The present invention relates to a process for preparing an aqueous suspension of an organic pesticide compound, which has a solubility in water of not more than 2 g/l at 20° C. and a melting point of not more than 110° C. and which is capable of forming at least one crystalline modification, wherein the organic pesticide compound is present in the form of essentially crystalline particles, which process comprises: a) providing an aqueous emulsion of the organic pesticide compound, wherein the organic pesticide compound is present in the form droplets of an amorphous form of the organic pesticide compound, and b) addition of an aqueous suspension of said organic pesticide compound, wherein the organic pesticide compound is present in the form of essentially crystalline particles, wherein the addition in step b) is performed at a temperature below the melting temperature of the crystalline form of the organic pesticide compound.Type: GrantFiled: July 13, 2010Date of Patent: December 31, 2013Assignee: BASF SEInventor: Charles W. Finch
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Patent number: 8618155Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: GrantFiled: August 9, 2010Date of Patent: December 31, 2013Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Patent number: 8614206Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: September 26, 2012Date of Patent: December 24, 2013Assignee: F. Hoffmann-La Roche AGInventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
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Patent number: 8614213Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing (CRF1) receptor antagonists.Type: GrantFiled: August 5, 2009Date of Patent: December 24, 2013Assignee: Novartis AGInventors: David Beattie, Andrew James Culshaw, Lisa Rooney, Emily Stanley
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Patent number: 8614243Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: GrantFiled: June 8, 2010Date of Patent: December 24, 2013Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Patent number: 8614244Abstract: A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.Type: GrantFiled: September 22, 2010Date of Patent: December 24, 2013Assignee: Segeant's Pet Care Products, Inc.Inventor: Larry Nouvel
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Patent number: 8604022Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: January 26, 2012Date of Patent: December 10, 2013Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas, David Buttar
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Publication number: 20130324557Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.Type: ApplicationFiled: November 4, 2011Publication date: December 5, 2013Applicant: SENOMYX, INC.Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
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Publication number: 20130324536Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 8, 2011Publication date: December 5, 2013Applicant: Lycera CorporationInventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
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Publication number: 20130324457Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.Type: ApplicationFiled: May 15, 2013Publication date: December 5, 2013Applicants: AVENTIS AGRICULTURE, MERIAL LIMITEDInventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons, William Glenn Cawthorne, Jr., Alberto Perez de Leon
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Patent number: 8598200Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: November 30, 2011Date of Patent: December 3, 2013Assignee: Pfizer Inc.Inventors: Amy B Dounay, Laura McAllister, Vinod D Parikh, Suobao Rong, Patrick R Verhoest
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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
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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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Patent number: 8586594Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.Type: GrantFiled: May 31, 2012Date of Patent: November 19, 2013Assignee: AbbVie Inc.Inventors: Andrew J. Souers, Ju Gao, Todd M. Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Patent number: 8580837Abstract: The present invention provides a parasiticidal formulation comprising: Fipronil, or a veterinarily acceptable derivative thereof; at least one C1-C6 alcohol co-solvent, wherein the total amount of C1-C6 alcohol is up to 8% by weight of the formulation; at least one organic solvent which is not the C1-C6 alcohol co-solvent; and at least one crystallization inhibitor, wherein the total amount of crystallization inhibitor is from 2 to 20% by weight of the formulation. The formulations of the invention have higher flash points than known parasiticidal formulations comprising Fipronil and therefore provide safer formulations for use in the home, storage, manufacture and distribution.Type: GrantFiled: March 18, 2010Date of Patent: November 12, 2013Assignee: Fidopharm, Inc.Inventor: Martin Benedict George Donnelly
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Patent number: 8580838Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38?, and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: GrantFiled: February 25, 2013Date of Patent: November 12, 2013Assignee: Novartis AGInventors: Hengyuan Lang, Olga M. Fryszman, Edcon Chang, Jiong Lan, Yunfeng Fang
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Publication number: 20130296355Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Patent number: 8569353Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: GrantFiled: July 14, 2011Date of Patent: October 29, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Izumi Sasaki, Tomohiro Toyoda, Hidefumi Yoshinaga, Itaru Natsutani, Yoko Takahashi
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Publication number: 20130281366Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: December 26, 2011Publication date: October 24, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
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Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20130274256Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.Type: ApplicationFiled: October 11, 2012Publication date: October 17, 2013Applicant: SEQUOIA SCIENCES, INC.Inventor: Sequoia Sciences, Inc.
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Publication number: 20130269064Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: November 18, 2011Publication date: October 10, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
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Publication number: 20130267543Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 8, 2011Publication date: October 10, 2013Applicants: CHAPERONE THERAPEUTICS, INC., DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
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Patent number: 8551912Abstract: A composition suitable for control of diseases caused by phytopathogens comprising (A) a compound of Formula (I) wherein R1 is difluoromethyl or trifluoromethyl and X is chloro, fluoro or bromo; and (B) at least one compound selected from compounds known for their fungicidal activity; and a method of controlling diseases on useful plants, especially rust diseases on soybean plants.Type: GrantFiled: April 23, 2008Date of Patent: October 8, 2013Assignee: Syngenta Crop Protection LLCInventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
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Patent number: 8552050Abstract: The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.Type: GrantFiled: August 18, 2008Date of Patent: October 8, 2013Assignee: Beth Israel Deaconess Medical CenterInventors: Lewis C. Cantley, Matthew G. Vander Heiden, Heather R. Christofk
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Publication number: 20130261120Abstract: The present invention relates to: *combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; *use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and *a kit comprising such a combination.Type: ApplicationFiled: September 29, 2011Publication date: October 3, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Florian Pühler, Marion Hitchcock
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Publication number: 20130261158Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.Type: ApplicationFiled: July 30, 2009Publication date: October 3, 2013Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
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Patent number: 8546304Abstract: The present invention relates to plant-protecting active ingredient mixtures comprising, as active components, a neonicotinoid and one or two fungicides selected from pyraclostrobin and boscalid, in synergistically effective amounts and to a method of improving the health of plants by to the plants or the locus thereof by applying said mixtures.Type: GrantFiled: August 15, 2011Date of Patent: October 1, 2013Assignee: BASF SEInventors: Dirk Voeste, Martin P. Mascianica, Hendrik Ypema, Henry Van Tuyl Cotter