Carbocyclic Ring Attached Indirectly To The Morpholine Ring By Nonionic Bonding Patents (Class 514/239.5)
  • Patent number: 10292934
    Abstract: An object of the present application is to provide an orally-disintegrating tablet having excellent tablet hardness and disintegrability, and including a disintegrative particulate composition. This invention relates to a disintegrative particulate composition comprising the four components consisting of a first disintegrator component of an acid-type carboxymethylcellulose, a second disintegrator component other than the acid-type carboxymethylcellulose, an excipient of a sugar or sugar alcohol, and crystalline cellulose; and to an orally-disintegrating tablet, including the disintegrative particulate composition and a medicinal ingredient.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: May 21, 2019
    Assignees: DAICEL CORPORATION, NICHIRIN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takahiro Hiramura, Kiyoshi Ikura, Sae Ishikawa, Tomohito Okabayashi, Naohiro Hashikawa, Tetsuro Morita, Kimiko Ikeda
  • Patent number: 9968613
    Abstract: The present invention provides methods for reducing loss of muscle strength, muscle mass, or Type I muscle fibers in an immobilized limb by administering (E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: May 15, 2018
    Assignee: VTV THERAPEUTICS LLC
    Inventors: Maria Carmen Valcarce Lopez, Eliot Ohlstein
  • Patent number: 9855274
    Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: January 2, 2018
    Assignee: vTv Therapeutics LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Patent number: 9663481
    Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: May 30, 2017
    Assignee: vTv Therapeutics LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Patent number: 9511073
    Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: December 6, 2016
    Assignee: TAXIS Pharmaceuticals, Inc.
    Inventors: David John Haydon, Lloyd George Czaplewski, Neil Robert Stokes, David Davies, Ian Collins, James T. Palmer, Jeffrey Peter Mitchell, Gary Robert William Pitt, Daniel Offermann
  • Patent number: 9468644
    Abstract: Suggested is a non-therapeutic aqueous composition for topical application, comprising (a) at least one solid active agent having at 20° C. a solubility in water (20° dH) of less than 5 g/L; (b) at least one 1,2-alkandiol having 4 to 12 carbon atoms; and (c) at least one aliphatic alcohol having 2 to 4 carbon atoms.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: October 18, 2016
    Assignee: Symrise AG
    Inventor: Cecile Kalem
  • Publication number: 20150133527
    Abstract: Methods are provided herein for treating cardiac arrhythmias, such as for treating an arrhythmia syndrome, for example Brugada syndrome, in a subject. In some embodiments, the methods include selecting a subject with Brugada syndrome and administering to the subject an effective amount of an agent that increases the expression or activity of SIRT1 in the subject. In some embodiments, the agent increases Nav1.5 activation. In some embodiments, the agent increases the expression or activity of SRIT1 and increases Nav1.5 activation.
    Type: Application
    Filed: May 6, 2013
    Publication date: May 14, 2015
    Inventors: Barry London, Kaikobad J. Irani
  • Publication number: 20150133297
    Abstract: The present invention relates to new antifungal compositions and their use in the treatment of agricultural products.
    Type: Application
    Filed: April 25, 2013
    Publication date: May 14, 2015
    Inventors: Jacobus Stark, Eva Louise Wilhelmine Sack
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • Patent number: 8993568
    Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.
    Type: Grant
    Filed: January 24, 2013
    Date of Patent: March 31, 2015
    Assignee: Eli Lilly and Company
    Inventors: Maria Rosario Gonzalez-Garcia, Maria Carmen Fernandez
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20150072985
    Abstract: The present invention provides methods for treating muscle atrophy by administering a PPAR? agonist.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 12, 2015
    Inventors: Maria Carmen Valcarce Lopez, Eliot Ohlstein
  • Patent number: 8962624
    Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: February 24, 2015
    Assignee: University of Kansas
    Inventors: Emily Scott, Anuradha Roy
  • Publication number: 20150038512
    Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, or reduce biofilms, or to inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
    Type: Application
    Filed: October 6, 2014
    Publication date: February 5, 2015
    Inventors: Ryan Looper, Dustin Williams, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hariprasada R. Kanna Reddy
  • Publication number: 20150018331
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Publication number: 20140378460
    Abstract: This invention relates to the use sigma-2 receptor antagonists, and of pharmaceutical compositions comprising such compounds, in methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology and more broadly treating with such compounds and compositions neurodegenerative diseases and disorders associated with Abeta pathology. This invention also relates to methods for screening compounds for activity in inhibiting cognitive decline on the basis of their ability to bind to a sigma-2 receptor.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Publication number: 20140371316
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: November 23, 2012
    Publication date: December 18, 2014
    Inventors: Jill S. FABRICANT, Iraj LALEZARI
  • Publication number: 20140348774
    Abstract: The present inventions relate to a number of fields including wound healing, a waterless antibacterial disinfectant, a surgical scrub, insect repellant, and methods of treating traumatic injuries, particularly those on the battlefield where there is a need to stabilize the patient and prevent infection.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Aurora Pharmaceutical, LLC
    Inventors: Michael Strobel, Gene Komer
  • Patent number: 8895552
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: November 25, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20140335201
    Abstract: The present invention provides a composition comprising a combination of components A) and B), wherein component A) is a compound of formula (I) and the component (B) is a further fungicide, insecticide or herbicide.
    Type: Application
    Filed: April 9, 2012
    Publication date: November 13, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Ulrich Johannes Haas, Dietrich Hermann, Gabriel Didier Scalliet, Kurt Nebel, Long Lu, Jianzhong Yang, Qiang Lu, Thomas James Hoffman, Renaud Beaudegnies, Werner Zambach, Olivier Jacob
  • Publication number: 20140329675
    Abstract: 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: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140323470
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: CHIESI FARMACEUTICI S.p.A.
    Inventors: Monique Bodil VAN NIEL, Nicholas Charles Ray, Lilian Alcaraz, Terry Aaron Panchal, Andrew Stephen Robert Jennings, Elisabetta Armani, Andrew Peter Cridland, Christopher Hurley
  • Publication number: 20140314882
    Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 23, 2014
    Inventors: Frederick P. ROTH, Murat COKOL, Hon Nian CHUA
  • Publication number: 20140296241
    Abstract: The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.
    Type: Application
    Filed: October 15, 2012
    Publication date: October 2, 2014
    Inventors: Irving W. Wainer, Ruin Moaddel, Michel Bernier, Carlos A. Zarate, Marc C. Torjman, Michael E. Goldberg, Mary J. Tanga
  • Publication number: 20140256731
    Abstract: Pleuromutilin derivative compounds of the following formula, and uses thereof for the treatment of diseases mediated by microbes, are disclosed:
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Applicant: NABRIVA THERAPEUTICS AG
    Inventors: Rosemarie MANG, Werner HEILMAYER, Rudolf BADEGRUBER, Dirk B. STRICKMANN, Rodger NOVAK, Mathias FERENCIC, Atchyuta Rama Chandra Murty BULUSU
  • Publication number: 20140206692
    Abstract: The invention is directed to formulations of bioactive compounds of limited water solubility, inhibitors of focal adhesion kinase (FAK) of the 2,4-diaminopyridine class, adapted for oral administration to patients. The formulations are self-emulsifying in the gastrointestinal tract of the patients, providing enhanced absorption and bioavailability of the bioactive compounds as dispersions or emulsions in an oil base. For example, esters of PEG-ylated glycerol can be used as the oil, in conjunction with surfactants such as lecithin and TEPG succinate and solubilizers such as PEG 400 to provide useful oral formulations for administration to patients having a malcondition wherein inhibition of FAK is medically indicated, such as cancer or arthritis.
    Type: Application
    Filed: August 14, 2013
    Publication date: July 24, 2014
    Inventors: Andrew Xian Chen, Yali J. Tsai
  • Patent number: 8772290
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: July 8, 2014
    Assignee: Oscotech Inc.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Publication number: 20140187557
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 3, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Publication number: 20140187554
    Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
    Type: Application
    Filed: May 16, 2012
    Publication date: July 3, 2014
    Applicant: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
  • Patent number: 8748347
    Abstract: The present invention relates to methods, use and compositions for combating harmful fungi and bacteria in plants. More specifically, it relates to methods and compositions for controlling, preventing, or treating plant pathogens using UV filters for combating phytotoxin-producing fungi and/or bacteria, in particular, for combating harmful fungi and/or bacteria producing photodynamically active phytotoxins.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: June 10, 2014
    Assignee: BASF SE
    Inventors: Richard Riggs, Dieter Strobel, Jochen Prochnow, Helmut Herrmann, Michael Ishaque, Christian Bittner
  • Publication number: 20140155261
    Abstract: 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: Application
    Filed: May 4, 2012
    Publication date: June 5, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140113899
    Abstract: An agro-horticultural agent of the present invention is intended to provide an agro-horticultural agent capable of providing, with a smaller spray amount, the same effect as compared to a conventional agro-horticultural agent. The agro-horticultural agent of the present invention includes a plurality of active ingredients and one of the plurality of active ingredients is an azole derivative represented by the following general formula (I); where: Ra and Rb each represent a predetermined hydrocarbon group and at least one of Ra and Rb has a chlorine atom or a bromine atom substituted for a hydrogen atom; Y represents a chlorine atom or a fluorine atom; and m represents 0 or 1.
    Type: Application
    Filed: June 6, 2012
    Publication date: April 24, 2014
    Applicant: KUREHA CORPORATION
    Inventors: Hideaki Tateishi, Nobuyuki Araki, Toru Yamazaki, Taiji Miyake, Keiichi Sudo, Hisashi Kanno
  • Publication number: 20140113012
    Abstract: The present invention provides compounds and compositions for the amelioration of arthritis and joint injuries by inducing mesenchymal stem cells into chondrocytes.
    Type: Application
    Filed: March 26, 2012
    Publication date: April 24, 2014
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Peter Schultz, Laure Bouchez
  • Publication number: 20140094465
    Abstract: The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: June 5, 2012
    Publication date: April 3, 2014
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Publication number: 20140094445
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140079806
    Abstract: The invention relates to the use of penflufen for protecting wood and wood-comprising materials against wood-destroying basidiomycetes.
    Type: Application
    Filed: September 30, 2011
    Publication date: March 20, 2014
    Applicant: LANXESS Deutschland GmbH
    Inventors: Bernd Koop, Martin Kugler, Thomas Jaetsch, Johannes Kaulen, Tanja Gerharz
  • Publication number: 20140072536
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of Nevada
    Inventors: Ryan Wuebbles, Dean Burkin
  • Publication number: 20140066446
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 6, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Publication number: 20140045851
    Abstract: A method of inhibiting formation of cancerous metabolites, of inhibiting cytochrome P450 2A13 from forming carcinogen metabolites, and/or inhibiting formation of cancerous lung cells in a subject can include: providing a morpholine compound that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6; administering a therapeutically effective amount of the morpholine compound or derivative to the subject. The morpholine compound or derivative can be substantially more selective for interacting with the cytochrome P450 2A13 over the cytochrome P450 2A6. The morpholine compound or derivative can also be substantially non-interactive with other physiological components. The morpholine compound or derivative can include a structure that selectively interacts with cytochrome P450 2A13 over cytochrome P450 2A6, such as Compounds 1-34 of Formulas A-D.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 13, 2014
    Applicant: University of Kansas
    Inventors: Emily Scott, Anuradha Roy
  • Publication number: 20140038945
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds ate inhibitors of PDE4function and are useful for improving cognitive function in animals.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 6, 2014
    Applicant: DART NEUROSCIENCE (CAYMAN) LTD
    Inventors: Terence P. Keenan, Alan P. Kaplan
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20140031290
    Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
  • Patent number: 8637058
    Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: January 28, 2014
    Assignee: Isagro S.p.A.
    Inventors: Lucio Filippini, Marilena Gusmeroli, Alexia Elmini, Carlo Garavaglia, Luigi Mirenna
  • Publication number: 20140024645
    Abstract: Phenoxy acetic acids and phenyl propionic acids and their use in treating type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, or obesity are provided herein. The present compounds are activators of PPAR? and may be useful for treating conditions mediated by the same.
    Type: Application
    Filed: September 3, 2013
    Publication date: January 23, 2014
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
  • Publication number: 20140024532
    Abstract: 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: Application
    Filed: September 19, 2013
    Publication date: January 23, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Hans Tobler, Harald Walter, Ulrich Johannes Haas
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Publication number: 20140005196
    Abstract: This invention offers an effective method of inhibiting the expression of apolipoprotein E by mammalian cells. Apolipoprotein E is a protein that plays a significant role in the development of Alzheimer's Disease in humans. The method comprises administering an effective amount of a triarylmethyl amine compound having the general formula: wherein the R1 group may comprise acyclic amines and aliphatic amines. The R2 group may comprise one of three aryl varieties: aryl, substituted aryl, or heterocycle. Triarylamine compounds inhibit apolipoprotein E expression in mammalian cells. In one aspect of the invention the mammalian cells may be human cells, and more specifically may be human brain cells.
    Type: Application
    Filed: June 28, 2012
    Publication date: January 2, 2014
    Applicants: California State University Fullerton, California State University Fresno
    Inventors: Santanu Maitra, Nilay Patel
  • Patent number: 8609658
    Abstract: The invention provides well defined N,N-dialkylalkenyl ester compounds for treating glaucoma or ocular hypertension. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: December 17, 2013
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old
  • Publication number: 20130296271
    Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cell
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: SDS Biotech K.K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki