Both Nitrogens Bonded Directly To The Same Acyclic Hydrocarbon Group Patents (Class 546/163)
  • Patent number: 11578041
    Abstract: Two crystals of (S)-(+)-hydroxychloroquine sulfate. One crystal features diffraction peaks at 12.3±0.1°, 13.1±0.1°, 17.9±0.1°, 22.8±0.1°, 23.4±0.1°, 25.1±0.1°, and 26.3±0.1° as 2? angles in a powder X-ray diffraction pattern. The other crystal features diffraction peaks at 12.8±0.1°, 14.5±0.1°, 16.7±0.1°, 17.6±0.1°, 20.2±0.1°, 21.4±0.1°, 23.8±0.1°, 25.7±0.1°, and 26.0±0.1° as 2? angles in a powder X-ray diffraction pattern. Also disclosed are methods of preparing crystals of (S)-(+)-hydroxychloroquine sulfate.
    Type: Grant
    Filed: December 31, 2020
    Date of Patent: February 14, 2023
    Assignee: Genovate Biotechnology Co. Ltd.
    Inventors: Jen Chen, Nai-tung Yao
  • Patent number: 9040558
    Abstract: The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: May 26, 2015
    Assignee: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dager, Shanavas Alikunju
  • Patent number: 9029378
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Grant
    Filed: July 25, 2012
    Date of Patent: May 12, 2015
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20150079622
    Abstract: Disclosed herein are compounds, compositions, methods, and kits for detecting reactive oxygen species (ROS) by conventional fluorescence microscopy, fluorescence spectroscopy, flow cytometry, and/or high content imaging. The compounds disclosed herein are novel reduced nucleic acid binding cyanine dyes, which dyes are probes for detecting ROS and measuring oxidative stress in cells either in vitro and/or in vivo. Also described herein are processes for preparing novel reduced dyes, i.e., ROS probes, for use in the disclosed compositions, methods and kits.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 19, 2015
    Inventors: Yi-Zhen Hu, Aimei Chen, Hee Chol Kang, Kyle Gee, Bhaskar Mandavilli
  • Publication number: 20150064788
    Abstract: The present invention relates to a method for transducing a target cell, the method comprising the step of contacting a target cell with a retroviral vector and a poloxamer having a molecular weight of 12.8 kDa to about 15 kDa. Further, the invention relates to the use of a poloxamer as defined herein, optionally in combination with a polycationic substance as defined herein, for transducing a target cell with a retroviral vector and a kit comprising a retroviral vector, a poloxamer as defined herein and, optionally, instructions for use.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 5, 2015
    Inventors: Natasa Anastasov, Ines Höfig, Christian Thirion
  • Publication number: 20150057279
    Abstract: This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Publication number: 20150051245
    Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating cell proliferative disorders, especially cancer.
    Type: Application
    Filed: November 13, 2012
    Publication date: February 19, 2015
    Inventors: William G. Cance, Ravindra K. Pandey, Elena V. Kurenova, Manivannan Ethirajan
  • Publication number: 20150004597
    Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 1, 2015
    Inventors: Jolene BRADFORD, Ching-Ying CHEUNG, Shih-Jung HUANG, Patrick PINSON, Stephen YUE
  • Publication number: 20140350262
    Abstract: The present invention relates to organophosphate-inhibited acetylcholinesterase (AChE) reactivators with central nervous system (CNS) bioavailability and their associated methods of preparation including their use for treatment of exposure to AChE inhibitors such as an organophosphate (OP) insecticides and nerve agents.
    Type: Application
    Filed: May 22, 2014
    Publication date: November 27, 2014
    Applicant: Southwest Research Institute
    Inventors: William E. BAUTA, William R. CANTRELL, JR., Michael W. TIDWELL
  • Publication number: 20140350048
    Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.
    Type: Application
    Filed: January 14, 2013
    Publication date: November 27, 2014
    Inventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
  • Patent number: 8889863
    Abstract: The present invention provides methods and intermediates are provided for the preparation of (?)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use in these and other reactions are also provided.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: November 18, 2014
    Assignee: Vanderbilt University
    Inventors: Jeffrey N. Johnston, Tyler A. Davis
  • Patent number: 8871228
    Abstract: The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: October 28, 2014
    Inventor: Oh-Young Yeo
  • Patent number: 8871939
    Abstract: A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: October 28, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Sigridur Soley Kristjansdottir, Rafael Shapiro, Matthew Richard Oberholzer
  • Publication number: 20140296215
    Abstract: The present disclosure provides pharmaceutical compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The pharmaceutical compositions, pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The pharmaceutical compositions and pharmaceutical preparations may include one or more cyanoquinoline-containing compounds of the embodiments, or an analog or derivative thereof.
    Type: Application
    Filed: May 25, 2012
    Publication date: October 2, 2014
    Applicant: The Regents of the University of California
    Inventors: Alan S. Verkman, Puay-Wah Phuan, Mark J. Kurth, John Knapp
  • Patent number: 8802701
    Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1=H, CF3, CH3, OCH3, NH2, halogen; R2=H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3=H, m-OC6H4CF3, NH2; R4=H, CH3, OCH3, NH2, halogen; R5=H, CH3, CF3, NH2, halogen; R6=H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7=(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8=CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: August 12, 2014
    Assignee: Fundação Oswaldo Cruz
    Inventors: Nubia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
  • Publication number: 20140148458
    Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
  • Publication number: 20140107097
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
  • Publication number: 20140050696
    Abstract: The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.
    Type: Application
    Filed: April 26, 2012
    Publication date: February 20, 2014
    Inventors: Ravi K. Amaravadi, Jeffrey Winkler
  • Publication number: 20140038948
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Publication number: 20140011839
    Abstract: Compositions and methods for the treatment, as well as the inhibition and prevention, of an infection of the papillomavirus and the epithelial lesions, namely, the warts of the skin and mucosal surfaces, associated therewith, in a mammalian host, as well as methods of inhibiting the replication of a papillomavirus in an infected cell, are provided. The compositions comprise a therapeutically effective amount of an active ingredient comprising at least one compound selected from the group consisting of chloroquine, hydroxychloroquine, amodiaquine, or in each case, a pharmaceutically acceptable salt thereof. The methods comprise topically administering a therapeutically and/or antivirally effective amount of such a compound to a mammalian host, such as a human being, in need of such treatment, although alternatively other routes of administration may be used, including but not limited to transdermal, transmucosal, respiratory, and by injection.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 9, 2014
    Inventor: Justice E. OBI
  • Publication number: 20130331571
    Abstract: The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.
    Type: Application
    Filed: February 21, 2012
    Publication date: December 12, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Minoru Moriya, Hiroshi Ohta, Shuji Yamamoto, Kumi Abe, Yuko Araki, Xiang-Min Sun, Daisuke Wakasugi
  • Publication number: 20130310365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: Janssen Pharmaceutical NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20130217671
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Raymond Huntley, Joel R. Walker, Helene Decomez
  • Patent number: 8440595
    Abstract: Fungicidal compounds of the general formula (I), wherein the substituents are as defined in claim 1.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: May 14, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Laura Quaranta, Fiona Murphy Kessabi, Renaud Beaudegnies, Hans-Georg Brunner, Fredrik Cederbaum
  • Patent number: 8415272
    Abstract: Compounds of the general Formula (1) wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: April 9, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Fiona Murphy Kessabi, Laura Quaranta, Renaud Beaudegnies, Hans-Georg Brunner, Fredrik Cederbaum
  • Patent number: 8415475
    Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: April 9, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Ismet Dorange, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
  • Publication number: 20130085159
    Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1?H, CF3, CH3, OCH3, NH2, halogen; R2?H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3?H, m-OC6H4CF3, NH2; R4?H, CH3, OCH3, NH2, halogen; R5?H, CH3, CF3, NH2, halogen; R6?H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3) (CH2)3NH2; R7?(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8?CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.
    Type: Application
    Filed: November 27, 2012
    Publication date: April 4, 2013
    Applicant: Fundação Oswaldo Cruz
    Inventor: Fundação Oswaldo Cruz
  • Patent number: 8399674
    Abstract: The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: March 19, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Publication number: 20130029995
    Abstract: Substituted bicyclic aromatic carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds, and a method of using these compounds in the treatment and/or inhibition of pain and further diseases and/or disorders mediated at least in part via the vanilloid receptor 1 (VR1/TRPV1).
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Thomas CHRISTOPH, Bernhard LESCH, Jeewoo LEE
  • Publication number: 20130030180
    Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).
    Type: Application
    Filed: December 13, 2010
    Publication date: January 31, 2013
    Applicant: GeneCode AS
    Inventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
  • Publication number: 20130011448
    Abstract: The present invention relates to a system for intracellular cargo delivery comprising: D(n)BAC wherein: Component D is a amine-containing compound; n is a number of amines between 2-6, Component B is a di-, tri or tetra ring system, such as quinoline or naphthalene derivatives which may contain several hetero atoms chosen from N, S, O and P; Component A is an aliphatic linear or branched hydrophobic chain of at least 4 carbon atoms preferably an epoxide, alkyl halide or an acrylamide with 6-30 carbon atoms or a derivative thereof; and Component C is an optional targeting moiety, such as homing peptide or aptamer, wherein components D, B, A and C may be coupled to each other via spacer(s). It also relates to the use of the system in diagnosis of diseases, as research tool and as a targeting system, a composition comprising the system and especially a pharmaceutical composition, a material covered with the system and a material having the delivery systems within the material.
    Type: Application
    Filed: March 15, 2011
    Publication date: January 10, 2013
    Applicant: GE HEALTHCARE BIO-SCIENCES AB
    Inventor: Ulf Tedebark
  • Patent number: 8324244
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: September 28, 2010
    Date of Patent: December 4, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Eric Dowdy, Xi Chen, Steven Pfeiffer
  • Publication number: 20120288855
    Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.
    Type: Application
    Filed: July 26, 2012
    Publication date: November 15, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
  • Patent number: 8299256
    Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: October 30, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jorge Eduardo Vialard, Patrick René Angibaud, Laurence Anne Mevellec, Christophe Meyer, Eddy Jean Edgard Freyne, Isabelle Noëlle Constance Pilatte, Bruno Roux, Elisabeth Thérèse Jeanne Pasquier, Xavier Marc Bourdrez, Christophe Denis Adelinet, Laurence Françoise Bernadette Marconnet-Decrane, Jacqueline Anne Macritchie, James Edward Stewart Duffy, Andrew Pate Owens, Pierre-Henri Storck, Virginie Sophie Poncelet
  • Publication number: 20120264810
    Abstract: Compositions, methods and compounds useful for enhancing the uptake of a lipid particle b\ a cell are described In particular embodiments, the methods of the invention include contacting a cell with a lipid particle and a compound that binds a Na+/K+ ATPase to enhance uptake of the lipid particle b\ the cell Related compositions useful in practicing methods include lipid particles comprising a conjugated compound that enhances uptake of the lipid particles b\ the cell The methods and compositions are useful in delivering a therapeutic agent to a cell, e g for the treatment of a disease or disorder in a subject
    Type: Application
    Filed: September 22, 2010
    Publication date: October 18, 2012
    Applicant: The University of British Columbia
    Inventors: Paulo J.C. Lin, Yuen Yi c. Tam, Srinivasulu Masuna, Marco A. Ciufolini, Michel Roberge, Pieter R. Cullis
  • Patent number: 8283361
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: October 9, 2012
    Assignee: AstraZeneca AB
    Inventors: Allison Laura Choy, Pamela Hill, John Irvin Manchester, Brian Sherer
  • Patent number: 8263623
    Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 11, 2012
    Assignee: Pfizer Inc.
    Inventors: Lyn Howard Jones, Dannielle Frances Roberts, Ross Sinclair Strang
  • Publication number: 20120214803
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 23, 2012
    Applicant: VIFOR (INTERNATIONAL) AG
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Chrostopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Publication number: 20120165276
    Abstract: Disclosed are compounds having at least one quaternary alkyl ammonium functionality. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.
    Type: Application
    Filed: May 6, 2008
    Publication date: June 28, 2012
    Applicant: Mpex Pharmaceuticals, Inc.
    Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
  • Patent number: 8193361
    Abstract: Compounds of the formula wherein the substituents are as defined in the claims, are useful as fungicides.
    Type: Grant
    Filed: November 29, 2005
    Date of Patent: June 5, 2012
    Assignees: Syngenta Limited, Syngenta Crop Protection LLC
    Inventors: Patrick Jelf Crowley, Roger Salmon, Ewan James Turner Chrystal, Olivia Anabelle Sageot, Laura Quaranta, Hans-Georg Brunner, Renaud Beaudegnies, Fredrik Cederbaum, Fiona Murphy Kessabi
  • Patent number: 8188284
    Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 8183380
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Publication number: 20120108633
    Abstract: The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.
    Type: Application
    Filed: June 18, 2010
    Publication date: May 3, 2012
    Inventor: Oh-Young Yeo
  • Publication number: 20120100555
    Abstract: This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in Plasmodium isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.
    Type: Application
    Filed: June 28, 2010
    Publication date: April 26, 2012
    Inventors: Martin James Lear, Kevin Shyong Wei Tan
  • Publication number: 20120095045
    Abstract: The present invention relates to an injectable anticancer composition for local administration comprising hydroxychloroquine. The anticancer composition shows an IC50 value against sarcoma-180 cells, which is about 10 times lower than cisplatin, as determined by the MTT assay in vitro, suggesting that the anticancer composition has an excellent cytotoxic effect. Also, the anticancer composition shows dose-dependent effects against solid cancer induced by sarcoma-80 cells in vivo. In addition, the anticancer composition has the effect of extending the life expectancy of patients having ascites cancer induced by sarcoma-80 cells.
    Type: Application
    Filed: June 18, 2010
    Publication date: April 19, 2012
    Inventor: Oh-Young Yeo
  • Publication number: 20120088915
    Abstract: The present invention provides methods and intermediates are provided for the preparation of (?)-Nutlin-3. Methods and intermediates are also provided for the enantioselective addition of aryl nitromethanes to aldimines. Bis(amidine) catalysts for the use in these and other reactions are also provided.
    Type: Application
    Filed: July 14, 2011
    Publication date: April 12, 2012
    Inventors: Jeffrey N. Johnston, Tyler A. Davis
  • Patent number: 8138346
    Abstract: The present invention provides process for synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones of the Formula A. The substituents R, R5, R6, R7, R8 and R9 are defined herein. The invention also provides novel synthetic intermediates useful in the synthesis of 8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and 8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones.
    Type: Grant
    Filed: March 4, 2011
    Date of Patent: March 20, 2012
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Barton James Bradbury, Jason Allan Wiles, Akihiro Hashimoto, Qiuping Wang, Edlaine Lucien, Godwin Pais, Ha Young Kim
  • Publication number: 20110312936
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui
  • Patent number: 8071777
    Abstract: The present invention refers to new compounds derived from artesunate salts with quinolines represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III) depending on the radicals substituted in X (formula II), the relation X to Y (formula III) may vary from 1:1 to 1:7, because the amount of Y depends on the amount of N available in X for the formation of the salt. The radicals R1, R2, R3, R4, R5, e R6 in the general formula (II) are represented by: R1?H, CF3, CH3, OCH3, NH2, halogen; R2?H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3?H, m-OC6H4CF3, NH2; R4?H, CH3, OCH3, NH2, halogen; R5?H, CH3, CF3, NH2, halogen; R6?H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7?(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3(CH2)6, (CH2)8, (CH2)10, (CH2)12; R8?CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: December 6, 2011
    Assignee: Fundação Oswaldo Cruz - FIOCRUZ
    Inventors: Núbia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli