The Ring Is A Benzene Ring Patents (Class 514/485)
  • Patent number: 10245239
    Abstract: Compositions having synergistic combinations of astaxanthin with a tomato extract lycopene, and optionally with carnosic acid and/or lutein. Compositions having synergistic combinations of the aforementioned compounds, which may be used, inter alia, to inhibit/suppress inflammation via the suppression of the expression of anti-inflammatory mediators or via the suppression of the secretion of anti-inflammatory mediators from macrophages at a site of inflammation.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: April 2, 2019
    Assignee: LYCORED LTD.
    Inventors: Rachel Levy, Nurit Hadad, Tanya Sedlov, Morris Zelkha
  • Patent number: 10195173
    Abstract: The specification provides compositions and methods to treat neurodegenerative diseases.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: February 5, 2019
    Assignees: Children's Medical Center Corporation, The General Hospital Corporation, President and Fellows of Harvard College
    Inventors: Clifford J. Woolf, Brian Wainger, Evangelos Kiskinis, Kevin Eggan
  • Patent number: 9096491
    Abstract: A process for the preparation of a prodrug of 5-aminosalicylic acid, namely 2-butanoyloxy-5-amino-benzoic acid, and solid forms of such compound are described.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: August 4, 2015
    Assignee: CHEMI S.P.A.
    Inventors: Maurizio Zenoni, Umberto Ciambecchini, Lorenzo De Ferra, Stefano Turchetta, Vincenzo De Sio
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20150098902
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20150031688
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 29, 2015
    Inventor: Shaker A. Mousa
  • Patent number: 8916133
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: December 23, 2014
    Assignee: SciFluor Life Sciences, LLC
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20140343138
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 14, 2014
    Publication date: November 20, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
  • Publication number: 20140336252
    Abstract: The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
    Type: Application
    Filed: October 23, 2012
    Publication date: November 13, 2014
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Fei Chen, Yangming Zhang, Pingzheng Zhou, Haining Hu, Haiyan Xu, Sheng Liu
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Patent number: 8865641
    Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: October 21, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Publication number: 20140303122
    Abstract: By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 9, 2014
    Applicant: AJINOMOTO CO., INC.
    Inventors: Masayuki SUGIKI, Toru Okamatsu, Sayaka Asari, Yayoi Kawato, Toshihiro Hatanaka, Tetsuo Yano, Yukie Seki, Naohiro Miyamura, Hiroaki Nagasaki, Yuzuru Eto, Reiko Yasuda
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Publication number: 20140155368
    Abstract: Methods and combination pharmaceuticals for treating bronchospastic medical conditions by utilizing the electrophysiology of proteinacious channels in lipid membranes of mammalian cells. The combination pharmaceuticals include at least one ?-adrenergic receptor agonist, and at least one composition adapted to effect the electrophysiology of Kv7 potassium channels of a lipid membrane of an airway smooth muscle cell. The pharmaceutical may be administered to a living body in a therapeutic amount sufficient to activate the Kv7 potassium channels of an airway smooth muscle cell.
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: Loyola University Chicago
    Inventor: Kenneth L. Byron
  • Patent number: 8697746
    Abstract: A solid dispersion comprising ((1S)-1-((((1S)-1-benzyl-2,3-dioxo-3-(cyclopropylamino)propyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester made amorphous in the presence of a water-soluble cellulosic polymer has improved storage stability. The solid dispersion also has improved solubility for an improved bioavailability.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: April 15, 2014
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Andrew Xian Chen, John Fan, Masazumi Yamaguchi
  • Publication number: 20140066500
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema BHAT
  • Publication number: 20140024709
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: September 26, 2013
    Publication date: January 23, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Kouacou ADIEY
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20130287686
    Abstract: The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 31, 2013
    Applicant: SCIFLUOR LIFE SCIENCES, LLC
    Inventors: Mark E. Duggan, Takeru Furuya, D. Scott Edwards, Ajay Purohit
  • Publication number: 20130267590
    Abstract: Stable premixes comprising retigabine, or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable carrier, and process for preparing the same are disclosed. Stable premixes comprising retigabine, or pharmaceutically acceptable salts thereof, and at least one pharmaceutically acceptable inorganic carrier, and processes for preparing the same and incorporating them in compositions that are employed for therapeutic uses and methods of treatment.
    Type: Application
    Filed: September 13, 2012
    Publication date: October 10, 2013
    Applicant: Dr. Reddy's Laboratories Limited
    Inventors: Snehalatha Movva, Mary Tom Teenu, Badri Narayanan Vishwanathan
  • Publication number: 20130217660
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 12, 2011
    Publication date: August 22, 2013
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • Patent number: 8481571
    Abstract: A method of treating coronavirus infection. The method includes administering to a subject suffering from or being at risk of suffering from such infection an effective amount of a compound of formula (I). Each variable in this formula is defined in the specification.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: July 9, 2013
    Assignee: Academia Sinica
    Inventors: Chi-Huey Wong, Chung-Yi Wu, Jia-Tsrong Jan
  • Publication number: 20130131164
    Abstract: The invention relates to retigabine with improved color quality, and to processes for preparing the same. In addition, the invention relates to a process for drying wet retigabine. Also, the invention relates to stabilized or substantially stabilized retigabine in solid state, or a mixture or pharmaceutical formulation comprising the same. Further, the invention also relates to an improved process for preparing retigabine.
    Type: Application
    Filed: February 18, 2011
    Publication date: May 23, 2013
    Applicant: MEDICHEM, S.A.
    Inventors: Ernesto Duran Lopez, Jordi Bosch I Lladó, Judit Serra Miralles
  • Publication number: 20130123287
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Publication number: 20130109751
    Abstract: The present invention relates to the use of LSD-1 enzyme inhibitors in the osteogenic differentiation of cells capable to differentiate into osteoblasts, especially mesenchymal stem cells, adult stem cells, and cells with osteogenic potential
    Type: Application
    Filed: October 24, 2012
    Publication date: May 2, 2013
    Applicant: MESOGENICS S.R.L.
    Inventor: MESOGENICS S.R.L.
  • Publication number: 20130102570
    Abstract: A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 25, 2013
    Applicant: AJINOMOTO CO., INC.
    Inventor: AJINOMOTO CO., INC
  • Publication number: 20130096092
    Abstract: Disclosed are inhibitors of retroviral growth of formula (I), that are useful in treatment of retroviral infections such as HIV. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, a method for inactivating a virus, a method for dissociating a metal ion from a zinc finger-containing protein, and a method for inhibiting the transmission of a virus.
    Type: Application
    Filed: June 10, 2011
    Publication date: April 18, 2013
    Applicants: Health and Human Services
    Inventors: Daniel Appella, Ettore Appella, John K. Inman, Lisa M. Miller Jenkins, Ryo Hayashi, Deyun Wang
  • Publication number: 20130079399
    Abstract: The present invention refers to the compounds corresponding to the following general formula (I): wherein: R?C4-C8 alkanoyl; and X?NH—R1 where R1?H, or an amine protecting group; and/or the pharmaceutically acceptable salts thereof. Preferred compounds according to the present invention are represented by the following formula (Ia): wherein: R?C4-C8 alkanoyl; and/or the pharmaceutically acceptable salts thereof. In a preferred embodiment, an object of the present invention is to provide 5-amino-2-(butyryloxy)benzoic acid and/or the pharmaceutically acceptable salts thereof, preferably hydrochloride salt. A further object of the present invention is represented by the use of the compounds of formula (Ia), in particular 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof, as a medicament and by the use thereof for the treatment of intestinal inflammatory diseases.
    Type: Application
    Filed: November 21, 2012
    Publication date: March 28, 2013
    Applicant: SOFAR SPA
    Inventor: Carla LABRUZZO
  • Publication number: 20130072491
    Abstract: An object is to provide a CaSR agonist agent that has excellent CaSR agonist effects, and particularly, a pharmaceutical product that can prevent or remedy diabetes or obesity by the effect of CaSR activation. The aforementioned object is achieved by a composition that contains a compound represented by the following General Formula (I) or a salt thereof (refer to the Description for the definitions of the symbols used in the formula).
    Type: Application
    Filed: August 31, 2012
    Publication date: March 21, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Reiko YASUDA, Yuzuru Eto, Yoshiro Kitahara
  • Publication number: 20120322719
    Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 20, 2012
    Applicant: The Feinstein Institute For Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Publication number: 20120225912
    Abstract: The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer.
    Type: Application
    Filed: July 30, 2010
    Publication date: September 6, 2012
    Inventors: Jack Tuszynski, Jonathan Y. Mane, John Torin Huzil, Boguslaw Tomanek, Dorota Bartusik
  • Publication number: 20120172426
    Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.
    Type: Application
    Filed: July 1, 2011
    Publication date: July 5, 2012
    Applicant: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Kouacou Adiey
  • Publication number: 20120122973
    Abstract: The invention relates to dry processes for the production of oral dosage forms, especially tablets, containing retigabine and adhesion promoter. In addition, the invention relates to compacted intermediates containing retigabine and an adhesion promoter. Finally, the invention relates to single-dose and multiple-dose containers, preferably sachets and stick-packs, containing the intermediate of the invention.
    Type: Application
    Filed: March 17, 2010
    Publication date: May 17, 2012
    Applicant: ratiopharm GmbH
    Inventors: Jana Paetz, Katrin Rimkus
  • Patent number: 8158814
    Abstract: An object of the present invention is to provide insecticides having high effectiveness.
    Type: Grant
    Filed: August 23, 2004
    Date of Patent: April 17, 2012
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba, Atsuko Kawahara
  • Publication number: 20120071522
    Abstract: A composition includes (a) a matrix, (b) a biocide, and (c) an antioxidant, in which said biocide exhibits thermal stability at matrix processing temperatures up to 250° C.
    Type: Application
    Filed: November 23, 2011
    Publication date: March 22, 2012
    Applicant: ISP Investments Inc.
    Inventor: Joseph P. BARTKO
  • Publication number: 20120058183
    Abstract: The invention relates to tablets, especially tablets with modified release, containing (a) retigabine and a combination of (b) water-soluble excipient and (c) non-water-soluble excipient; and a process for producing them.
    Type: Application
    Filed: March 17, 2010
    Publication date: March 8, 2012
    Applicant: ratiopharm GmbH
    Inventors: Sandra Brueck, Katrin Rimkus
  • Publication number: 20120046358
    Abstract: A method for preventing and treating prostatic diseases and skin cancer using naturally or artificially synthesized isothiocyanates compounds or the derivatives or metabolites thereof.
    Type: Application
    Filed: September 13, 2011
    Publication date: February 23, 2012
    Applicant: WUXI JC PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Jingcai Cheng, Jenwei Chiao, Haiya Jin, Chengjuan Zhong
  • Publication number: 20120016020
    Abstract: A solid dispersion comprising ((1S)-1-((((1S)-1-benzyl-2,3-dioxo-3-(cyclopropylamino)propyl)amino)carbonyl)-3-methylbutyl)carbamic acid 5-methoxy-3-oxapentyl ester made amorphous in the presence of a water-soluble cellulosic polymer has improved storage stability. The solid dispersion also has improved solubility for an improved bioavailability.
    Type: Application
    Filed: July 13, 2011
    Publication date: January 19, 2012
    Applicant: SENJU PHARMACEUTICAL CO., LTD.
    Inventors: Andrew Xian CHEN, John FAN, Masazumi YAMAGUCHI
  • Publication number: 20110136878
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Application
    Filed: June 29, 2009
    Publication date: June 9, 2011
    Applicant: Mitsui Chemicals Agro., Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20110104057
    Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.
    Type: Application
    Filed: May 13, 2009
    Publication date: May 5, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludger Dinkelborg, Keith Graham, Mathias Berndt, Norman Koglin, Heribert Schmitt-Willich, Matthias Friebe, Lutz Lehmann
  • Publication number: 20100323016
    Abstract: A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours. A method of treating a disorder characterized by nervous system hyperexcitability includes administering to a subject an effective amount of these pharmaceutical formulations.
    Type: Application
    Filed: January 21, 2010
    Publication date: December 23, 2010
    Inventor: Biljana Nadjsombati
  • Publication number: 20100323015
    Abstract: A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl) carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours. A method of treating a disorder characterized by nervous system hyperexcitability includes administering to a subject an effective amount of these pharmaceutical formulations.
    Type: Application
    Filed: January 20, 2010
    Publication date: December 23, 2010
    Inventor: Biljana Nadjsombati
  • Publication number: 20100261788
    Abstract: Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.
    Type: Application
    Filed: June 22, 2010
    Publication date: October 14, 2010
    Inventors: John C. Reed, Maurizio Pellecchia
  • Patent number: 7795304
    Abstract: The invention relates to hydroxamic acid derivatives having carbamate linkage with the structural formula that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous systems (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: September 14, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sandro Belvedere, Christopher Laurence Hamblett, Thomas A. Miller, David J. Witter, Jiaming Yan
  • Publication number: 20100215589
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
    Type: Application
    Filed: March 31, 2010
    Publication date: August 26, 2010
    Applicant: SEPRACOR INC.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20100190829
    Abstract: Described are compounds that bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.
    Type: Application
    Filed: June 20, 2008
    Publication date: July 29, 2010
    Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishchenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao
  • Publication number: 20100130601
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, R1, R2, R3, G1, G2, G3 and Q are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: February 26, 2008
    Publication date: May 27, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Pierre Jung, Christopher Richard Ayles Godrey, William Lutz, Peter Maienfisch, Andre Stoller, Werner Zambach
  • Publication number: 20100120906
    Abstract: A modified release pharmaceutical formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix including hydroxypropylmethylcellulose (HPMC), about 1.0-10% of an anionic surfactant, and an enteric polymer. The pharmaceutical formulation produces a sustained plasma concentration of retigabine following administration to a subject for 4-20 hours longer than the time required for in vitro release of 80% of retigabine. A formulation includes about 30-70% N-(2-amino-4-(fluorobenzylamino)-phenyl)carbamic acid ethyl ester (retigabine), or a pharmaceutically acceptable salt, solvate or hydrate thereof, about 5-30% of a drug delivery matrix, and an agent for retarding release in the gastric environment. The plasma concentration vs. time profile of this formulation is substantially flat over an extended period lasting for about 4 hours to about 36 hours.
    Type: Application
    Filed: July 17, 2009
    Publication date: May 13, 2010
    Applicant: VALEANT PHARMACEUTICALS INTERNATIONAL
    Inventor: Biljana Nadjsombati
  • Patent number: 7704519
    Abstract: A composition for application to exterior surfaces, such as trees, so as to prevent animal damage to the exterior surface, has asphalt and denatonium benzoate mixed together. The denatonium benzoate is 1% to 50% by weight of the total composition. The asphalt is between 50% and 60% of the total composition. Naphtha and dimethyl ether are further components of the total composition. The composition is sprayable onto the exterior surface.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: April 27, 2010
    Inventor: John Baldwin