Chalcogen Bonded Directly To Ring Carbon Of The Six-membered Hetero Ring Patents (Class 546/290)
  • Patent number: 10570095
    Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: February 25, 2020
    Assignee: Ardea Biosciences, Inc.
    Inventors: Li-Tain Yeh, Barry D. Quart
  • Patent number: 10550084
    Abstract: The present invention includes novel substituted 1-hydroxy-pyridin-2(1H)-ones, which can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention inhibit HBV RNAse H activity.
    Type: Grant
    Filed: November 29, 2018
    Date of Patent: February 4, 2020
    Assignee: Arbutus Biopharma Corporation
    Inventors: Ramesh Kakarla, Bruce D. Dorsey
  • Patent number: 10351563
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: July 16, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventor: Guanglin Luo
  • Patent number: 10047050
    Abstract: 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: August 14, 2018
    Assignee: ARDEA BIOSCIENCES, INC.
    Inventors: Li-Tain Yeh, Barry D. Quart
  • Patent number: 9968537
    Abstract: The present invention discloses a stable biocidal composition with enhanced antifungal activity at low concentration of active (s) and a process for preparing the same. The composition comprises: zinc pyrithione, C8-C18 quaternary ammonium salt (preferably cetylpyridinium chloride), water miscible glycol/polyol/glycol ether/lactam, organic amine and/or alkanol amine. The composition can be formulated into: hair care formulations, antidandruff hair care formulations, water based paints, coatings, adhesives, hard surface cleaners, fabric care compositions, wood products, plastic products and medical products. The biocidal compositions and the resulting formulations are transparent or opaque and are stable at varying pH and humidity conditions.
    Type: Grant
    Filed: September 2, 2014
    Date of Patent: May 15, 2018
    Inventors: Vineet Sharma, Ashutosh Agarwal
  • Patent number: 9926277
    Abstract: Provided herein are pyridone compounds, for example, a compound 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 proliferative disease.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: March 27, 2018
    Assignee: BioTheryX, Inc.
    Inventors: Robert Sullivan, Sara Howard, Leah Fung, Kyle W. H. Chan, Frank Mercurio
  • Patent number: 9846263
    Abstract: The present invention provides a metal oxide dispersion comprises a metal oxide, a millbase and a dispersant. The dispersant in the metal oxide is selected from a group consisting of a phosphoric acid polyester copolymer, a trimethoxysilane compound, a triethoxysilanes compound, dimethylamino ethyl methacrylate (DMAEMA) and a combination thereof, and the dispersion is substantially free of water. The metal oxide dispersion of the invention is useful for manufacturing an inkjet ink to provide a high-quality color image on a contact lens or a mold so as to produce a colored contact lens.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: December 19, 2017
    Assignee: Novartis AG
    Inventors: Richard Charles Breitkopf, Rahul Panicker
  • Patent number: 9458108
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: August 17, 2015
    Date of Patent: October 4, 2016
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Stepan Vyskocil, Gabriel S. Weatherhead
  • Patent number: 9233936
    Abstract: The invention concerns a new process for the preparation of bosentan or bosentan monohydrate by reaction of compound of Formula II with ethylene glycol in the presence of potassium bases and the potassium salt of bosentan.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: January 12, 2016
    Assignee: SIFAVITOR S.R.L.
    Inventors: Giancarlo Biffi, Lazzaro Feliciani, Enrico Viscardi
  • Patent number: 9181188
    Abstract: This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: November 10, 2015
    Assignee: Bayer Healthcare LLC
    Inventors: Jacques Dumas, William J. Scott, Du-Schieng Chien, Ala Nassar, Wendy Lee, Susan Bjorge, Laszlo L. Musza, Bernd Riedl
  • Patent number: 9126905
    Abstract: The present invention relates to a process for manufacturing fluoroaromatics of formula (I), A-F ??(I) comprising step a) diazotization of aminoaromatics of formula (II) in anhydrous HF with an aqueous solution of a diazotizing agent; followed by step b) thermic decomposition of the diazonium salt of formula (III) resulting from step a); wherein the variables are defined according to the description.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: September 8, 2015
    Assignee: BASF SE
    Inventors: Michael Rack, Maximilian Dochnahl, Volker Maywald, Bernd Wolf, Joachim Gebhardt, Timo Frassetto, Uwe Josef Vogelbacher, Roland Götz
  • Patent number: 9062001
    Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 30, 2014
    Date of Patent: June 23, 2015
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 9035063
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: December 9, 2014
    Date of Patent: May 19, 2015
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck Eidam, Huiping Amy Guan, Chengde Wu, Mui Cheung
  • Publication number: 20150126562
    Abstract: Disclosed herein are methods of administering deuterated pirfenidone and kits thereof.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventor: Chengzhi Zhang
  • Publication number: 20150111899
    Abstract: The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Williamson Z. Bradford, Javier Szwarcberg
  • Patent number: 9006450
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: April 14, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz, Heike Neubauer, Bernd Nosse
  • Publication number: 20150065720
    Abstract: A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sabine M. Pyles, Michael Cyr, Ramachandran Radhakrishnan
  • Patent number: 8969576
    Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: March 3, 2015
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 8969575
    Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: March 3, 2015
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 8969347
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: March 3, 2015
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Patent number: 8946437
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 3, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takashi Nakagawa, Makoto Sakamoto, Kazuya Yamaguchi, Yuki Terauchi, Masamichi Shirakura, Yasuo Harada, Yutaka Kojima, Takumi Sumida
  • Patent number: 8940375
    Abstract: The present invention relates to a liquid-crystal (LC) display of the PS (polymer stabilized) or PSA (polymer sustained alignment) type, and to polymerizable compounds and LC media for use in PS (polymer stabilized) and PSA displays.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: January 27, 2015
    Assignee: Merck Patent GmbH
    Inventors: Matthias Bremer, Georg Bernatz
  • Patent number: 8937071
    Abstract: This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung c
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 20, 2015
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Hilary Schenck Eidam, Kaushik Raha, Zhen Gong, Huiping Amy Guan, Chengde Wu, Haiying Yang, Haiyu Yu, Zhiliu Zhang, Mui Cheung
  • Patent number: 8907101
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: December 9, 2014
    Assignees: Pfizer Limited, Icagen, Inc.
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Publication number: 20140350060
    Abstract: The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Williamson Z. Bradford, Javier Szwarcberg
  • Patent number: 8895568
    Abstract: The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-oxy- or sulfanyl) pteridines and 1- or 2-(4 Jheteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products. The disclosure provides compounds of Formula (I-A) and Formula (I-B).
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: November 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: William K. Brewster, David A. Demeter, W. Randal Erickson, Christian T. Lowe, Carla J. R. Klittich, Jaime S. Nugent, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao, Carla N. Yerkes, Yuanming Zhu
  • Patent number: 8871760
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, and R3 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Christine E. Brotherton-Pleiss, Ralph New Harris, III, Bradley E. Loe, Francisco Javier Lopez-Tapia, Pankaj D. Rege, David Bruce Repke, Russell Stephen Stabler, Keith Adrian Murray Walker
  • Patent number: 8865908
    Abstract: Process for the preparation of a N-[2-(2-pyridinyl)ethyl]carboxamide derivative of general formula (I) or a salt thereof Intermediate of general formula (II) Intermediate of general formula (III)
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 21, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Frederic Lhermitte, Pierre-Yves Coqueron, Philippe Desbordes, Thomas Himmler
  • Patent number: 8859573
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: October 14, 2014
    Assignee: Glaxo Group Limited
    Inventors: Zehong Wan, Xiaomin Zhang, Jian Wang, Cheng Peng, Yun Jin, Yimin Hu
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140221660
    Abstract: A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: INTERMUNE, INC.
    Inventors: Sabine M. Pyles, Michael Cyr, Ramachandran Radhakrishnan
  • Patent number: 8795700
    Abstract: New pesticidal compositions comprising pyriproxyfen and methyl esters of C16-C18 fatty acids and having low volatile organic compound (VOC) content are provided. Methods of use and ready-to-use products are also provided.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: August 5, 2014
    Assignee: Valent U.S.A., Corporation
    Inventors: Evelyn Jean Taylor, Humberto Benito Lopez
  • Patent number: 8791266
    Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: July 29, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Shinji Kawata, Koji Matsumoto, Maki Niijima, Taichi Takahashi
  • Patent number: 8779148
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: July 15, 2014
    Assignee: Pfizer Inc.
    Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
  • Patent number: 8754229
    Abstract: 3-alkoxy, thioalkyl and amino-4-amino-6-(substituted)picolinic acids having a halogen, alkyl or mono-, di- tri- and tetra-substituted aryl substituents in the 6-position, and their acid derivatives, are herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: June 17, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jeffrey B. Epp, Christian T. Lowe, James M. Renga, Paul R. Schmitzer, Joseph D. Eckelbarger, Katherine A. Guenthenspberger, Thomas L. Siddall, Carla N. Yerkes, Lindsey Gayle Fischer, Natalie Christine Giampietro, Jeremy Kister, Joshua Roth
  • Patent number: 8754230
    Abstract: Disclosed herein is a process for preparing a compound of Formula (I), comprising the steps of: (a) reacting an aniline compound of Formula (II) and an carboxylic acid compound of Formula (III) or an activated carboxylic acid compound thereof, to provide a compound of Formula (IV); and (b) converting said protected amine group attached to said compound of Formula (IV) to an amine group to provide said compound of Formula (I); wherein PAm is a protected amine group. Processes to prepare the compounds of Formulae (II), (III), and (IV) are also disclosed.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert C. Livingston, William P. Gallagher, Robert M. Borzilleri, Zhen-Wei Cai
  • Patent number: 8748620
    Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: June 10, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Shinji Kawata, Koji Matsumoto, Maki Niijima, Taichi Takahashi
  • Patent number: 8748621
    Abstract: The present invention relates to a method of treating, ameliorating, or controlling a condition in a mammal, including a human, wherein the condition is selected from the group consisting of anxiety disorders, psychotic disorders, substance-dependence related disorders, mood disorders, epilepsy or convulsive disorders, idiopathic Parkinson's disease, and Alzheimer's disease, wherein the method comprises administering to the mammal an effective amount of a compound of Formula (I) wherein all radicals are as defined in the application and claims. In particular, such conditions are central nervous system disorders selected from the group of anxiety, schizophrenia, depression, and epilepsy.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: June 10, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma, SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
  • Patent number: 8741927
    Abstract: The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 3, 2014
    Assignee: LG Life Sciences Ltd.
    Inventors: Bong Chan Kim, Kyu Young Kim, Hee Bong Lee, Ji Eun An, Kyu Woong Lee
  • Patent number: 8741936
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: June 3, 2014
    Assignee: Intermune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 8716421
    Abstract: This invention discloses and claims a series of polycyclic monomers and polymers useful in the production of optical waveguides. The polymers of the invention comprise one or more repeating units represented by the formula (IV): Wherein m, X, R1 and R2 are as defined herein. The films formed from the polymers of this invention exhibit significant changes in refractive index (greater than or equal to 0.5%) after exposure to suitable actinic or thermal energy thereby having superior optical transmission performance, which is of importance for modern optical applications such as wave guiding and optical data storage.
    Type: Grant
    Filed: May 23, 2013
    Date of Patent: May 6, 2014
    Assignees: Promerus, LLC, Sumitomo Bakelite Co., Ltd
    Inventors: Kazuyoshi Fujita, Nanae Kawate, Mari Ueda, Larry F Rhodes
  • Patent number: 8703802
    Abstract: An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.
    Type: Grant
    Filed: May 19, 2011
    Date of Patent: April 22, 2014
    Assignee: Targacept, Inc.
    Inventors: Gary Maurice Dull, John Genus, Tommi Ratilainen, Per Olof Ryberg, Janna Hellström, Niklas Wahlström, Thomas Wännman
  • Publication number: 20140107040
    Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 8673901
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: March 18, 2014
    Assignee: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Publication number: 20140038963
    Abstract: The present disclosure provides methods for identifying therapeutic agents that are multifunctional radical quenchers. It also provides compounds of formula (I), (II), or (II-A): and pharmaceutically acceptable salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 4, 2012
    Publication date: February 6, 2014
    Inventors: Sidney Hecht, Omar Khdour, Sandipan Roy Chowdhury, Poulami Talukder
  • Patent number: 8642629
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: February 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Eric Mertz, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Patent number: 8629278
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: January 14, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier
  • Patent number: 8624034
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: January 7, 2014
    Assignee: Pfizer Inc.
    Inventors: Usa Reilly, Michael Melnick, Matthew F. Brown, Mark S. Plummer, Justin Montgomery, Ye Che, Loren Price
  • Patent number: 8623942
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya