Hetero Ring Is Six-membered Consisting Of Three Nitrogens And Three Carbon Atoms Patents (Class 514/241)
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Synthesis of two-photon absorbing polyhydroxy diphenylamino-dialkylfluorene-1,3,5-triazine molecules
Patent number: 8895730Abstract: A method of synthesizing a two-photon active tris(diarylamino-9,9-di(R)fluorenyl)-1,3,5-triazine compound having the structure: where Y is hydrogen, a thermally self-polymerizable acrylic, or a methacrylic group; R is an alkyl group of the formula —CmH2m+1, wherein the subscript m ranges from 1 to 6, or an alkylether group of the formula —(CH2CH2O)pMe, wherein the subscript p ranges from 1 to 5; R? is an alkyl group; and the R?—(OY)x groups are attached to the phenyl rings of the triarylamine moiety either in a para position or a meta position and the subscript x ranges from 1 to 3. The compound may be synthesized by (a) synthesizing a diarylamine intermediate, (b) synthesizing a brominated 1,3,5-triazine intermediate as a three-arm core structure, and (c) forming the two-photon active tris(diarylamino-9,9-di(R)fluorenyl)-1,3,5-triazine compound by covalently joining the diarylamine and each arm of the three-arm core structure and removing the acetone protecting groups.Type: GrantFiled: October 7, 2013Date of Patent: November 25, 2014Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton -
Patent number: 8889677Abstract: 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, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8889679Abstract: Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.Type: GrantFiled: May 21, 2010Date of Patent: November 18, 2014Assignee: Dow Global Technologies LLCInventor: Bei Yin
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Publication number: 20140335174Abstract: The present invention provides a dry-coated tablet comprising: an inner core containing, as active ingredients, (a) tegafur, (b) gimeracil, and (c) oteracil potassium; and an outer shell.Type: ApplicationFiled: May 24, 2012Publication date: November 13, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Takumi Okamoto, Takashi Yoshizawa, Yoshito Ohnishi
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Publication number: 20140329674Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 3, 2014Publication date: November 6, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140329884Abstract: The present invention provides novel 1,3,5-triazinane-2,4,6-trione derivatives, such as compounds of any one of Formulae (I) and (II), and salts thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, or plasmid DNA). The present invention also provides methods and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, and lung diseases.Type: ApplicationFiled: May 1, 2014Publication date: November 6, 2014Inventors: Yizhou Dong, Akinleye C. Alabi, Hao Yin, Joseph R. Dorkin, Delai Chen, Robert S. Langer, Daniel Griffith Anderson, Ahmed A. Eltoukhy
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Publication number: 20140315839Abstract: Provided is a pest control composition containing a novel iminopyridine derivative and other pest control agents. Provided is a pest control composition containing an iminopyridine derivative represented by the following Formula (I) and at least one of other pest control agents: [in the formula (I), Ar represents a 5- to 6-membered heterocycle which may be substituted, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents hydrogen, halogen and the like, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z)].Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Ryo HORIKOSHI, Yasumichi ONOZAKI, Satoshi NAKAMURA, Masahiro NOMURA, Makoto MATSUMURA, Masaaki MITOMI
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Patent number: 8864853Abstract: An additive mixture for fuels including a) at least one N-formal, b) at least one antioxidant and c) at least one corrosion inhibitor. The additive mixture ensures that the additized fuels and lubricants have biocidal and corrosion-inhibiting additization, especially when they include proportions of renewable raw materials, such as biodiesel, and when they are in contact with copper-containing surfaces.Type: GrantFiled: June 21, 2010Date of Patent: October 21, 2014Assignee: l'Air Liquide Societe Anonyme pour l'etude et L'exploitation des Procedes Georges ClaudeInventors: Wolfgang Beilfuss, Ralf Gradtke, Jennifer Knopf, Ingo Krull
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Publication number: 20140296068Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.Type: ApplicationFiled: October 24, 2012Publication date: October 2, 2014Applicant: DOW AGROSCIENCES LLCInventors: Negar Garizi, Tony K. Trullinger, Ricky Hunter, Yu Zhang, Noormohamed M. Niyaz, Daniel Knueppel, Christian T. Lowe, Ann M. Buysse
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Patent number: 8846910Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: GrantFiled: July 8, 2013Date of Patent: September 30, 2014Assignee: Ranbaxy Laboratories LimitedInventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranadheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
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Patent number: 8841294Abstract: The invention relates to insecticidal and acaricidal mixtures comprising certain cyclic ketoenols and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.Type: GrantFiled: January 6, 2005Date of Patent: September 23, 2014Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 8828908Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.Type: GrantFiled: May 27, 2008Date of Patent: September 9, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
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Patent number: 8816073Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.Type: GrantFiled: July 8, 2013Date of Patent: August 26, 2014Assignee: Ranbaxy Laboratories LimitedInventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranadheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Sricastava
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Patent number: 8809379Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.Type: GrantFiled: January 14, 2009Date of Patent: August 19, 2014Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Ling Li, Wenkui K. Fang, Janet A. Takeuchi, Smita Bhat
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Publication number: 20140221203Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically 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: George Philip LAHM, Renee Marie LETT, Brenton Todd SMITH, Benjamin Kenneth SMITH, Clarice Anne TYLER
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Patent number: 8785628Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: March 2, 2010Date of Patent: July 22, 2014Assignee: UCB Pharma, S.A.Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
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Patent number: 8772480Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: GrantFiled: November 19, 2012Date of Patent: July 8, 2014Assignee: Amgen Inc.Inventors: Kristin L. Andrews, Yunxin Y. Bo, Shon Booker, Victor J. Cee, Noel D'Angelo, Bradley J. Herberich, Fang-Tsao Hong, Claire L. M. Jackson, Brian Alan Lanman, Hongyu Liao, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Anthony B. Reed, Adrian Leonard Smith, Seifu Tadesse, Nuria A. Tamayo, Bin Wu, Ryan Wurz, Kevin C. Yang
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Patent number: 8765753Abstract: A process is described for the preparation of s-triazine derivatives of the formula in which R is a C1-C12-alkyl radical, by reacting a cyanuric acid halide with a p-aminobenzoic acid ester, which comprises a C6-C12-alkyl radical as radical of the ester alcohol, in a molar ratio of 1:3 to 1:5 in a xylene isomer mixture as solvent. 10 The process is characterized in that the solvent is used in amounts of from 0.6 to 2.1 mol/l.Type: GrantFiled: March 21, 2012Date of Patent: July 1, 2014Assignee: BASF SEInventor: Rudi Kroner
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Patent number: 8748426Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: GrantFiled: December 30, 2010Date of Patent: June 10, 2014Assignee: Piramal Enterprises LimitedInventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Patent number: 8747873Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems.Type: GrantFiled: November 15, 2013Date of Patent: June 10, 2014Assignee: Dow Global Technologies LLCInventors: Bei Yin, Freddie L. Singleton
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Patent number: 8747999Abstract: The present invention related to (micro-or nano-) capsules that have two different functional groups on the outer shell of the particles that allow deposition onto the textile surfaces (i.e. exhibit substantivity) and subsequent covalent bonding of the particles onto the textile (i.e. are reactive towards the fiber).Type: GrantFiled: November 20, 2006Date of Patent: June 10, 2014Assignee: BASF SEInventors: Bryan David Grey, Kishor Kumar Mistry, Chun-tian Zhao
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Patent number: 8748427Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems.Type: GrantFiled: November 15, 2013Date of Patent: June 10, 2014Assignee: Dow Global Technologies LLCInventors: Bei Yin, Freddie L. Singleton
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Patent number: 8742101Abstract: This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.Type: GrantFiled: November 13, 2008Date of Patent: June 3, 2014Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Richard Storer, Gilles Gosselin, David Dukhan, Frederic Leroy
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Publication number: 20140135334Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems.Type: ApplicationFiled: November 15, 2013Publication date: May 15, 2014Inventors: Bei Yin, Freddie L. Singleton
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Patent number: 8710174Abstract: A polymer containing a triazine ring-containing repeating unit structure represented by, for example, formula (23) or (24), which alone can achieve high heat resistance, high transparency, high refraction index, high solubility, and low volume shrinkage, without adding a metal oxide.Type: GrantFiled: September 6, 2013Date of Patent: April 29, 2014Assignee: Nissan Chemical Industries, Ltd.Inventors: Naoya Nishimura, Taku Kato, Masaaki Ozawa, Masahiro Hida, Yasuyuki Koide
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20140105893Abstract: A method for predicting a therapeutic effect of chemotherapy with a combination drug containing tegafur, gimeracil, and oteracil potassium in a gastric cancer patient by: (1) measuring an expression level of epidermal growth factor receptor (EGFR) in a biological sample obtained from the patient; (2) comparing the expression level of EGFR obtained in step (1) with a corresponding predetermined cut-off point; and (3) predicting that the patient is likely to sufficiently respond to chemotherapy when a tegafur, gimeracil, and oteracil potassium combination drug is used with an EGFR inhibitor, when the step (2) comparison reveals that the expression level of EGFR is greater than the cut-off point, or predicting that the patient is likely to sufficiently respond to chemotherapy when a tegafur, gimeracil, and oteracil potassium combination drug is used alone, when the step (2) comparison reveals that the expression level of EGFR is not greater than the cut-off point.Type: ApplicationFiled: May 15, 2012Publication date: April 17, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Takashi Kobunai, Hitoshi Saito, Teiji Takechi
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Patent number: 8697754Abstract: Biocidal compositions and their use in aqueous media, such as metalworking fluids, the compositions comprising a biocidal agent; and a non-biocidal primary amino alcohol compound of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein.Type: GrantFiled: April 29, 2009Date of Patent: April 15, 2014Inventors: Patrick E. Brutto, Charles E. Coburn, G. David Green, Bonnie A. Pyzowski, Raymond J. Swedo, John Pohlman
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Patent number: 8697697Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.Type: GrantFiled: January 3, 2012Date of Patent: April 15, 2014Assignee: Kinentia Biosciences LLCInventors: David Fairfax, Russell Joseph Deorazio
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Patent number: 8691983Abstract: The invention provides compositions that include crosslinking agents having multiple photoactivatable groups, such as diaryl ketones, or a diaryl ketone, such as benzophenone, and at least one polymerizable monomer, such as a zwitterionic monomer. The compositions are useful as surface coating agents that provide brush type polymeric coatings. These polymeric coatings can be used on medical devices, such as artificial joints, to reduce wear and tear between the components of the joint and thus reduce or eliminate debris generated by friction between the joint components.Type: GrantFiled: March 1, 2010Date of Patent: April 8, 2014Assignee: Innovative Surface Technologies, Inc.Inventors: Jie Wen, Laurie R. Lawin, Patrick Guire
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Publication number: 20140073644Abstract: A biocidal composition comprising 2,2-dibromomalonamide and an aldehyde-based biocidal compound, and its use for the control of microorganisms in aqueous and water-containing systems.Type: ApplicationFiled: November 15, 2013Publication date: March 13, 2014Inventors: Bei Yin, Freddie L. Singleton
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Patent number: 8669253Abstract: Inhibition of geranylgeranylation of Rho GTPases and heterotrimeric G-proteins in the aqueous outflow pathway increases aqueous humor outflow, possibly through the tissue relaxation, and through altered cell adhesive interactions and actin cytoskeletal organization in cells of the outflow pathway. In addition, such inhibition is useful for treating age-related macular degeneration. The GGTase-I enzyme is a molecular target for lowering increased ocular pressure in glaucoma patients.Type: GrantFiled: March 12, 2007Date of Patent: March 11, 2014Assignee: Duke UniversityInventors: Vasantha P. Rao, Patrick J. Casey, Peifeng Deng, Yuri K. Peterson
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Publication number: 20140038966Abstract: This invention provides an antitumor agent comprising a combination drug containing tegafur, gimeracil, and oteracil potassium, characterized by being repeatedly administered to a patient once a day every other day, four days a week, at a dose such that the tegafur is administered in an amount of 80 mg or more/dose when the patient has a body surface area of less than 1.25 m2, in an amount of 100 mg or more/dose when the patient has a body surface area of 1.25 to 1.5 m2, or in an amount of 120 mg or more/dose when the patient has a body surface area of not less than 1.5 m2.Type: ApplicationFiled: January 30, 2012Publication date: February 6, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Tetsuhiko Shirasaka, Hiroki Yamaue, Susumu Yamamitsu
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Publication number: 20140038968Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: October 17, 2012Publication date: February 6, 2014Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz
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Publication number: 20140038965Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comparing cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: February 6, 2014Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20140024651Abstract: Provided are decontamination compositions that include an ammonium compound, a ferric/ferrocyanide compound, a polyaminocarboxylic acid compound and a polycarboxylic compound. Depending on the mode of application, the compositions can be used as foams, liquids, gels, strippable coatings, mists, or in other forms. Also provided are kits that include such components in whole or in part along with an optional dispersing device for use of the decontamination composition.Type: ApplicationFiled: October 16, 2012Publication date: January 23, 2014Applicant: Her Majesty the Queen in Right Canada, as Represented by the Minister of EnvironmentInventors: Konstantin Volchek, Pervez Azmi, Wenxing Kuang, Carl E. Brown
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Publication number: 20130345050Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: ApplicationFiled: August 29, 2013Publication date: December 26, 2013Applicant: Bayer Intellectual Property GmbHInventors: Lutz ASSMANN, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20130345222Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: May 17, 2013Publication date: December 26, 2013Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Patent number: 8614201Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: June 4, 2010Date of Patent: December 24, 2013Assignee: Janssen Pharmaceutica NVInventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
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Publication number: 20130324541Abstract: The present invention relates to an agent for potentiating an antitumor activity of a chemotherapeutic agent against a cancer containing cancer stem cells, which contains at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof. In addition, the present invention relates to an agent for treating a cancer containing cancer stem cells, which contains a combination of a chemotherapeutic agent and at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof. Furthermore, the present invention relates to an agent for preventing metastasis or recurrence of a cancer containing cancer stem cells, which contains a combination of a chemotherapeutic agent and at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof.Type: ApplicationFiled: August 13, 2013Publication date: December 5, 2013Applicant: Kurume UniversityInventors: Shinobu NISHITANI, Hirohisa Yano
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Patent number: 8592370Abstract: The invention relates to a composition for use as a medicament comprising insulin in combination with at least one compound of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof. Another object of the invention concerns a pharmaceutical composition comprising as active ingredients effective amounts of insulin and at least one compound of formula (I), together with pharmaceutically tolerable adjuvants, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with insulin resistance. The invention also relates to a pharmaceutical package comprising insulin in a first dosage unit and at least one compound of formula (I) in a second dosage unit.Type: GrantFiled: November 13, 2009Date of Patent: November 26, 2013Assignee: Poxel S.A.S.Inventors: Didier Mesangeau, Daniel Cravo, Annick Audet
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Publication number: 20130303516Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.Type: ApplicationFiled: January 25, 2012Publication date: November 14, 2013Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
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Patent number: 8580958Abstract: Provided are novel 2PA-active monomers of the formula: wherein Y?H, acrylic or methacrylic moiety; R is a linear or branched alkyl group, —CmH2m+1, where m=1-6 or an alkylether group, —(CH2CH2O)pMe, where p=1-5. The number of R?—(OH)x groups, attached to the phenyl rings of the triarylamine moiety either in a para or a meta position, could be 3 or 6 per molecule, or mixtures of molecules containing 3, 4, 5, 6 in various ratios and wherein x=1, 2, or 3. R? is a linear or branched alkyl group such as —CmH2m, where m=1-6, i.e. linear —(CH2)m, where m=2-6, or branched alkyl group such as —CH2CH(R?)—, where R??—(CH2)lCH3, where l=2-6.Type: GrantFiled: September 22, 2011Date of Patent: November 12, 2013Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton
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Publication number: 20130245020Abstract: A synergistic antimicrobial composition. The composition contains at least two components. The first component is ortho-phenylphenol or its alkali metal or ammonium salts. The second component is 4,4-dimethyloxazolidine (DMOZ).Type: ApplicationFiled: April 19, 2013Publication date: September 19, 2013Applicant: DOW GLOBAL TECHNOLOGIES LLCInventor: Bei Yin
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Patent number: 8524896Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.Type: GrantFiled: March 2, 2009Date of Patent: September 3, 2013Assignee: Syngenta Crop Protection LLCInventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
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Patent number: 8518942Abstract: This invention provides novel caspase inhibitors useful for prophylaxis or treatment of a number of pathologies, including, for example, Huntington's disease. In certain embodiments the inhibitors include inhibitors of casepase-3 and/or casepase-6.Type: GrantFiled: August 6, 2009Date of Patent: August 27, 2013Assignees: Buck Institute for Research on Aging, The Regents of the University of CaliforniaInventors: Lisa M. Ellerby, Jonathan A. Ellman, Melissa J. Leyva
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Patent number: 8518941Abstract: An extreme temperature decontamination composition such as a solution for destroying microorganisms, chemical warfare and bioterrorism agents is utilized that generally does not freeze at low temperatures down to about minus 25° F. and also has no significant evaporation or decomposition at temperatures up to about 120° F. The solution is effective against nerve agents and vesicants such as VX and HD, and various biological agents. The composition comprises a metallic salt of dichloroisocyanuric acid or dibromoisocyanuric acid, an aqueous solvent system comprising polar compounds such as water and an alkyl glycol, and a quasi hydrophilic compound. The composition can be formulated as a one part system wherein all components are blended together.Type: GrantFiled: August 19, 2010Date of Patent: August 27, 2013Assignee: American Sterilizer CompanyInventors: Herbert J. Kaiser, Daniel A. Klein, Anchalee Thanavaro, Miranda Chevon Shaver
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Patent number: 8501939Abstract: Compounds of the general formula (I): in which inter alia Q1 represents —NR1R3, —OR1 or —SR1 and Q2 represents —NR2R4, —OR2 or —SR2, and A represents the point of attachment to a support matrix, are useful as protein binding ligands when (a) at least one of R1, R2, R3 and R4 includes an alkyl group —CnH2n+1 in which n is greater than or equal to 7; (b) at least two of R1, R2, R3 and R4 independently include an alkyl group —CnH2n+1 or a cycloalkyl group —CnH2n?1 in which n is greater than or equal to 4; or (c) at least three of R1, R2, R3 and R4 independently include a C1-12 alkyl group substituted by —NR5R6 or aryl.Type: GrantFiled: June 8, 2006Date of Patent: August 6, 2013Assignee: Prometic Biosciences LimitedInventors: Jason Richard Betley, James Christopher Pearson, Helen Rosemary Tatton, Ben Martin Beacom
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Publication number: 20130178474Abstract: The present invention is directed to a water treatment composition, containing 50-99.9 wt. % of particulate halogen-releasing compound; and 0.1-10 wt. % of granular fluoropolymer, wherein all weight percentages are based on the total weight of the composition. The present invention is also directed to a water treatment composition, containing 50-99 wt. % of particulate halogen-releasing compound; 1-10 wt. % of aluminum sulfate; 0.5-15 wt. % of a sulfate salt selected from the group consisting of copper sulfate, zinc sulfate, and combinations thereof; and 0.1-10 wt. % of particulate polytetrafluoroethylene polymer, wherein all weight percentages are based on the total weight of the composition. One particular halogen-releasing compound is trichloroisocyanuric acid.Type: ApplicationFiled: September 20, 2012Publication date: July 11, 2013Applicant: Arch Chemicals, Inc.Inventors: Michael J. Unhoch, Nicole Wise, Derek Francis Parish
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Patent number: 8481534Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 25, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth