Ring Sulfur In The Additional Hetero Ring Patents (Class 514/342)
  • Patent number: 8883832
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Grant
    Filed: March 3, 2013
    Date of Patent: November 11, 2014
    Assignee: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Patent number: 8883834
    Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: November 11, 2014
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Patent number: 8882988
    Abstract: The potentiometric device and method selective for pioglitazone relates to the detection of pioglitazone in urine, in other liquid biological samples, and in pharmaceutical preparations for quality control testing and the like, and particularly to the use of a potentiometric sensor for potentiometric detection and measurement of the concentration of pioglitazone. The potentiometric sensor includes a plasticized polyvinyl chloride (PVC) matrix membrane having an ionophore impregnated or embedded therein. The ionophore is an iodobismuth anion in which the iodobismuth anion forms a complex with pioglitazone. The polymer membrane is plasticized with either ortho-nitrophenyl octyl ether (NPOE) or dioctyl phthalate (DOP).
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: November 11, 2014
    Assignee: UMM Al-Qura University
    Inventor: Amr Lotfy Saber Hefny
  • Patent number: 8883828
    Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: November 11, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
  • Patent number: 8883180
    Abstract: 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: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8883793
    Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: November 11, 2014
    Assignee: Development Center for Biotechnology
    Inventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
  • Publication number: 20140329863
    Abstract: Described herein are novel compositions and methods of treatment addressing diseases such as neurodegenerative diseases, including prion diseases and Alzheimer's disease.
    Type: Application
    Filed: February 26, 2014
    Publication date: November 6, 2014
    Applicant: The Regents of the University of California
    Inventors: Adam R. Renslo, Alejandra Gallardo-Godoy, Michael B. Silber, Stanley B. Prusiner, Kurt Giles, Zhe Li, R. Jeffrey Neitz
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Publication number: 20140323525
    Abstract: What are described are novel active compound combinations comprising a known oxime ether derivative (trifloxystrobin) and imidacloprid, which combinations are highly suitable for controlling phytopathogenic fungi and insects.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 30, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Ulrike WACHENDORFF-NEUMANN, Astrid MAULER-MACHNIK, Christoph ERDELEN, Hirohisa OHTAKE
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Publication number: 20140322165
    Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
  • Publication number: 20140323423
    Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.
    Type: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Patent number: 8865747
    Abstract: The present invention is directed to pioglitazone, or a pharmaceutically acceptable salt thereof, as well as a pharmaceutical composition comprising pioglitazone, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient, for use in the treatment and/or prevention of an adrenoleukodystrophy.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: October 21, 2014
    Assignees: Fundació Institute D'Investigació Biomėdica de Bellvitge (IDIBELL), Fundació Institució Catalana de Recerca I Estudis Avançats (ICREA), Fondation ELA
    Inventor: Aurora Pujol Onofre
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Publication number: 20140309237
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Publication number: 20140302022
    Abstract: The invention relates to the use of compounds of formula (I) in the treatment of warm-blooded animal target of VEGF-driven angiogenic diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical compositions comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.
    Type: Application
    Filed: October 31, 2012
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventor: Christian Rene Schnell
  • Publication number: 20140303213
    Abstract: The present invention relates to the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures, for example, but not limited to, heterocyclic, phenyl or benzyl ring structures with or without substitutions and are described in detail herein. Also provided are methods for the treatment and/or prevention of one or more metabolic disorders, for example, obesity or diabetes, utilizing fatostatin A and/or a derivative and/or analog thereof and/or the A-B-C tripartite compounds.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Mizuki Watanabe
  • Patent number: 8853409
    Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.
    Type: Grant
    Filed: June 11, 2012
    Date of Patent: October 7, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Indrani W. Gunawardana, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner, Eli M. Wallace
  • Patent number: 8853246
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: October 7, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, Jr., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Patent number: 8853126
    Abstract: The present invention relates to compositions for controlling plant pests containing the compound of the formula (I) in a mixture with specified fungicidally active compounds.
    Type: Grant
    Filed: February 29, 2012
    Date of Patent: October 7, 2014
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christoph Eredelen, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Kraemer
  • Patent number: 8853127
    Abstract: The present invention provides a composition for controlling pests comprising, as active ingredients, ethaboxam and a neonicotinoid compound represented by formula (1); and so on.
    Type: Grant
    Filed: December 18, 2012
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Makoto Kurahashi, Yuichi Matsuzaki
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Publication number: 20140296239
    Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 27, 2014
    Publication date: October 2, 2014
    Applicant: SANOFI
    Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
  • Publication number: 20140296295
    Abstract: The present application relates to novel 2-alkoxy-substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Walter HÜBSCH, Daniel MEIBOM, Alexandros VAKALOPOULOS, Barbara ALBRECHT-KÜPPER, Peter NELL, Katja ZIMMERMANN, Frank SÜßMEIER, Joerg KELDENICH
  • Publication number: 20140296064
    Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.
    Type: Application
    Filed: July 13, 2012
    Publication date: October 2, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
  • Publication number: 20140296299
    Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.
    Type: Application
    Filed: June 6, 2014
    Publication date: October 2, 2014
    Applicant: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20140287916
    Abstract: A compound of formula (I), wherein R1 to R4 are, for example, each hydrogen, R5 is, for example, an unsubstituted aromatic 6-membered heterocycle; R6 is, for example, hydrogen; R7 is, for example, hydrogen, cyano, hydroxyl, formyl, C1-C4-alkyl, C1-C4-alkoxy, C2-C4-alkenyl, or C2-C4-alkynyl; and A1 to A5 are, independently selected, from, for example, N, and C—H; and its use as a pesticidal agent.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Olivier Loiseleur, Thomas Pitterna, Anthony Cornelius O'Sullivan, Torsten Luksch
  • Publication number: 20140286931
    Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Chengzhi Zhang
  • Patent number: 8841328
    Abstract: The present invention relates to the use of selective insecticidal compositions, characterized by an effective amount of an active compound combination comprising (a) (1) at least one haloalkylnicotinic acid derivative of the formula (I) in which AA and R1A are as defined in the description, or (2) at least one phthalic acid diamide of the formula (II) in which XB, R1B, R2B, R3B, L1B, L2B and L3B are as defined in the description, or (3) at least one anthranilamide of the formula (III) in which A1C, A2C, XC, R1C, R2C, R3C, R4C, R5C, R7C, R8C and R9C are as defined in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description, in particular cloquintocet-mexyl, isoxadifen-ethyl and mefenpyr-diethyl for controlling insects and/or arachnids, and a method for controlling insects and/or arachnids using the compositions.
    Type: Grant
    Filed: December 3, 2013
    Date of Patent: September 23, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Rüdiger Fischer, Christian Funke, Achim Hense, Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert, Udo Reckmann, Lothar Willms, Christian Arnold
  • Publication number: 20140275179
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
  • Publication number: 20140275089
    Abstract: The present invention relates to a pharmaceutical combination comprising a 2-carboxamide cycloamino urea derivative compound of formula (I) and inhibitors of Heat Shock Protein 90, and the uses of such combinations in the treatment of proliferative diseases, more specifically PI3K dependent diseases, more specifically PI3K-alpha dependent diseases.
    Type: Application
    Filed: October 11, 2012
    Publication date: September 18, 2014
    Inventors: Xizhong Huang, Cornelia Quadt, Hui-Qin Wang, Christine Fritsch, Christian René Schnell
  • Publication number: 20140275180
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Publication number: 20140275178
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
  • Publication number: 20140275103
    Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Kevin Peters, Robert Shalwitz, John Janusz, Alexander Smith
  • Patent number: 8835475
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: September 16, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • Patent number: 8835427
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: September 16, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
  • Patent number: 8835435
    Abstract: Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: September 16, 2014
    Assignee: AB Science
    Inventors: Marco Ciufolini, Camille Wermuth, Bruno Giethlen, Alain Moussy
  • Patent number: 8835644
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: September 16, 2014
    Assignee: University of Virginia Patent Foundation
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
  • Publication number: 20140256728
    Abstract: The present invention relates to the use of predominantly known pyridyl carboxamide derivatives as nematicides, compositions containing such compounds and methods for the control of nematodes.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 11, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jörg Nico Greul, Heiko Rieck, Christian Paulitz, Matthias Riedrich, Ralf Dunkel, Arianna Martelletti, Alexander Sudau, Peter Lösel, Olga Malsam, Arnd Voerste, Hans-Georg Schwarz, Ulrich Görgens, Kerstin Ilg, Michael Maue, Pierre-Yves Coqueron, Philippe Desbordes, Philippe Meresse, Stephanie Gary, Pierre Cristau, David Bernier
  • Publication number: 20140256736
    Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
  • Publication number: 20140256772
    Abstract: Pharmaceutical formulations comprising solid pharmaceutically acceptable organic acids, such as maleic acid or tartaric acid, that inhibit the disproportionation of pharmaceutically acceptable acid salts of active pharmaceutical ingredients, and methods of manufacturing such pharmaceutical compositions. The pharmaceutically acceptable acid salt of the active pharmaceutical ingredient has a pKa of less than about 6.0, and wherein the solid pharmaceutically acceptable organic acid has a pKa of less than about 4.0 and an aqueous solubility in the range of about 500 to about 2000 milligrams per milliliter. A pharmaceutical formulation comprising a pharmaceutical acceptable acid salt of pioglitazone, a solid pharmaceutically acceptable organic acid selected from the group consisting of maleic acid or tartaric acid, and an excipient that promotes disproportionation, wherein the ratio by weight of the solid pharmaceutically acceptable organic acid to excipient is from about 1:6 to about 1:1.
    Type: Application
    Filed: October 8, 2012
    Publication date: September 11, 2014
    Inventors: Christopher T. John, Paul A. Harmon
  • Publication number: 20140248357
    Abstract: A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.
    Type: Application
    Filed: April 7, 2014
    Publication date: September 4, 2014
    Applicant: PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED
    Inventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
  • Publication number: 20140248362
    Abstract: Provided is a sustained-release preparation containing pioglitazone or a salt thereof as an active ingredient and showing superior sustainability. A sustained-release preparation containing pioglitazone or a salt thereof, which shows a dissolution ratio of pioglitazone of average 25-58% at the 2-hour time point, and average 60-100% at the 4-hour time point, in a dissolution test according to the 50 rpm USP Paddle Method and using pH 2.0 KCl/HCl buffer at 37° C. as a test solution.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 4, 2014
    Inventors: Yutaka Tanoue, Yusuke Murakawa, Yumiko Ishii, Kaoru Takenaka
  • Publication number: 20140249100
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: March 3, 2013
    Publication date: September 4, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
  • Publication number: 20140249154
    Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • Publication number: 20140249024
    Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.
    Type: Application
    Filed: July 13, 2012
    Publication date: September 4, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
  • Publication number: 20140243326
    Abstract: The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests.
    Type: Application
    Filed: May 9, 2014
    Publication date: August 28, 2014
    Applicant: Bayer CropScience Ag
    Inventors: Wolfram Andersch, Heike Hungenberg, Wolfgang Thielert
  • Publication number: 20140243340
    Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: AbbVie Inc.
    Inventors: Larry L. Klein, Hui-Ju CHEN, Ming C. YEUNG, Charles A. Flentge, John T. Randolph, Peggy Huang, Douglas K. Hutchinson, Dale J. Kempf