Nitrogen In Substituent Q Patents (Class 564/86)
  • Patent number: 9108986
    Abstract: Provided are a novel chiral iridium(III) complex; and a method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines from 2-substituted-quinolines with the use of the chiral iridium(III) complex through a more economical and easy production process.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: August 18, 2015
    Assignee: HAMARI CHEMICALS, LTD.
    Inventors: Sadayuki Maeda, Tatsunori Sato, Yasuhiko Kawano, Toshio Miyawaki
  • Publication number: 20150136611
    Abstract: Reaction products of guanidine compounds or salts thereof, polyepoxide compounds and polyhalogen compounds may be used as levelers in metal electroplating baths, such as copper electroplating baths, to provide good throwing power. Such reaction products may plate with good surface properties of the metal deposits and good physical reliability.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 21, 2015
    Inventors: Julia KOZHUKH, Zuhra I. NIAZIMBETOVA, Maria Anna RZEZNIK
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150073054
    Abstract: Disclosed herein are Furin/PC inhibitors for inhibiting Furin and other Propprotein Convertases. Method of making the Furin/PC inhibitors, chemical and biological characterization of the Furin/PC inhibitors, and the use of the Furin/PC inhibitors to treat infectious diseases, cancers, and inflammatory/autoimmune disorders, are also disclosed.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 12, 2015
    Inventors: Alex Strongin, Maurizio Pellecchia, Elisa Barile
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Publication number: 20140378681
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: February 26, 2013
    Publication date: December 25, 2014
    Applicant: Siga Technologies Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey, Jack H. Nunberg, Celestine Johnson Thomas
  • Publication number: 20140357634
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
  • Publication number: 20140336178
    Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
    Type: Application
    Filed: April 29, 2014
    Publication date: November 13, 2014
    Applicants: The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
  • Patent number: 8871208
    Abstract: A method for treating a patient suffering from inflammation, chronic inflammation, pain, rheumatoid arthritis (RA), osteoarthritis and osteoporosis, comprising administering an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: October 28, 2014
    Assignee: AbbVie Inc.
    Inventors: Peer B. Jacobson, Lisa M. Olson, Sreeinvasarao Vepachedu
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Publication number: 20140256743
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Applicants: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Patent number: 8815485
    Abstract: A compound that can improve azo pigment dispersibility in a non-water-soluble solvent. The compound is represented by formula (1): wherein R1 to R4 represent hydrogen or halogen; R5 to R9 represent hydrogen, COOR17 or CONR18R19, and at least one of R5 to R9 represents COOR17 or CONR18R19, where R17 to R19 represent hydrogen or an alkyl group having 1 to 3 carbons; R10 represents an alkyl group having 1 to 6 carbons or a phenyl group; R11 to R15 represent a hydrogen, L1R20 or L2R21R22, and at least one of R11 to R15 represents L1R20 or L2R21R22, where L1 represents a divalent linking group, L2 represents a trivalent linking group, and R20 to R22 represent an alkyl group having 8 or more carbons or an alkenyl group having 8 or more carbons; and R16 represents an alkyl group having 1 to 6 carbons or a phenyl group.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 26, 2014
    Assignee: Canon Kabushiki Kaisha
    Inventors: Masatake Tanaka, Masashi Kawamura, Yuki Hasegawa, Takayuki Toyoda, Yasuaki Murai, Masashi Hirose, Takeshi Miyazaki
  • Publication number: 20140234939
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 21, 2014
    Applicant: Northwestern University
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Publication number: 20140221591
    Abstract: There is provided a copolymer having the general structure below, wherein a, b, and d are molar ratios varying between about 0.01 and about 0.90 and c is a molar ratio varying between about 0.01 and about 0.90; A1 represents monomer units comprising a cyano-containing pendant group in which the cyano is not directly attached to the backbone of the copolymer; A2 represents monomer units comprising two or more hydrogen bonding sites; A3 represents monomer units that increase solubility in organic solvents; and A4 represents monomer units that increase solubility in aqueous alkaline solutions. There is also provided a near-infrared radiation-sensitive coating composition comprising this copolymer as well as a positive-working thermal lithographic printing plate comprising a near-infrared radiation-sensitive coating comprising this copolymer, a method of producing such a printing plate, and finally a method of printing using such a printing plate. Formula (I).
    Type: Application
    Filed: September 14, 2010
    Publication date: August 7, 2014
    Applicant: MYLAN GROUP
    Inventors: My T. Nguyen, Akha Phan, Viet-Thu Nguyen-Truong, Marc-André Locas
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8784879
    Abstract: In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt % tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt % polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1-20 wt % of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt % of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: July 22, 2014
    Assignee: Corium International, Inc.
    Inventors: Parminder Singh, Eun Soo Lee, Amit K. Jain
  • Publication number: 20140200225
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 17, 2014
    Applicant: ORION CORPORATION
    Inventors: Rajeev GOSWAMI, Anil Kumar VUPPALA, Ramesh VELUDANDI, Ramesh SISTLA, Chakshusmathi GHADIYARAM, Muralidhara RAMACHANDRA
  • Patent number: 8778838
    Abstract: The present invention relates to aqueous concentrate formulations for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its anhydrate; N-(phosphonomethyl)glycine in the form of its free acid, in the form of the ammonium salt or a substituted ammonium salt or a mixture thereof; at least two different non-ionic surfactants with at least one of them comprising an ethylene oxide polymer moiety or an ethylene oxide/C3-C4-alkylene oxide block copolymer moiety, and water; wherein the pH-value of the formulation is below 6.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: July 15, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Sven Adam, Klaus Kolb, Juergen Jakob, Bernd Sievernich, Joerg Steuerwald, Steven Bowe, Joseph Zawierucha, Rex Liebl
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20140170067
    Abstract: The present invention relates to novel compounds of formulae (I) and (II) which are useful in the prevention, treatment and diagnosis, in vivo diagnosis of diseases or disorders related to S1P receptors, in particular, in diseases which are connected to the regulatory function of sphingosine-1-phosphate (S1P) and its analogues, such as inflammation, pain, autoimmune diseases and cardiovascular diseases.
    Type: Application
    Filed: August 16, 2012
    Publication date: June 19, 2014
    Applicant: WESTFAELISCHE WILHELMS-UNIVERSITAET MUENSTER
    Inventors: Guenter Haufe, Bodo Levkau, Michael Schaefers, Stefani Silke Schilson, Petra Keul
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140094445
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 15, 2012
    Publication date: April 3, 2014
    Applicant: University of Utah Research Foundation
    Inventors: Hariprasad Vakayalapati, Venkataswamy Soma, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140066504
    Abstract: Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 6, 2014
    Inventor: Daryl W. HOCHMAN
  • Patent number: 8653141
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: February 18, 2014
    Assignee: AbbVie Inc.
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Patent number: 8653002
    Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: February 18, 2014
    Assignee: BASF SE
    Inventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
  • Patent number: 8642809
    Abstract: The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PURC) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PURE) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PURF) optional purification; (HAF) hydroxamic acid formation; and (PURG) optional purification.
    Type: Grant
    Filed: September 23, 2008
    Date of Patent: February 4, 2014
    Assignee: Topotarget UK Ltd.
    Inventors: Helge A. Reisch, Peter Leeming, Prasad S. Raje
  • Publication number: 20140031395
    Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: January 30, 2014
    Applicant: Bionomics Limited
    Inventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
  • 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: 20140018326
    Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 27, 2011
    Publication date: January 16, 2014
    Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130289280
    Abstract: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
    Type: Application
    Filed: May 7, 2013
    Publication date: October 31, 2013
    Applicants: TRANSFORM PHARMACEUTICALS, INC., UNIVERSITY OF SOUTH FLORIDA
    Inventors: University of South Florida, Transform Pharmaceuticals, Inc.
  • Publication number: 20130287841
    Abstract: The invention relates to medicine, and specifically to synthetic biologically active derivatives of carbopentoxysulfanilic acid. The novel substance comprises a (2,6-dichlorophenyl)amide salt of carbopentoxysulfanilic acid of general formula: where X is Na, K, NH4; the drug may be contained in tablets, including sublingual tablets, or in capsules, or in suppositories, or in drops, or in mixtures, or in ointments, creams or other forms for application to the skin and mucosae, or in an oral-buccal film, or in a spray, or in a liquid for parenteral administration, or in chewing gum. A preparation having pronounced activity against herpes viruses is thus produced.
    Type: Application
    Filed: January 28, 2011
    Publication date: October 31, 2013
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets, Viktor Iosifovich Krutikov
  • Publication number: 20130261132
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 3, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedso, Lars Kristian Albert BlÆher
  • Patent number: 8546602
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: October 1, 2013
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
  • Publication number: 20130251673
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 21, 2012
    Publication date: September 26, 2013
    Applicant: Novira Therapeutics, INC.
    Inventors: George D. HARTMAN, Osvaldo A. FLORES
  • Publication number: 20130244995
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedsø, Lars Kristian Albert Blæhr
  • Publication number: 20130237542
    Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.
    Type: Application
    Filed: October 17, 2011
    Publication date: September 12, 2013
    Applicants: DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Kyeong Lee, Mi Sun Won, Hwan Mook Kim, Song Kyu Park, Kiho Lee, Ki Hoon Lee, Chang Woo Lee, Jung Joon Lee, Kyung Sook Chung, Bo Kyung Kim, Yinglan Jin, Seung-hee Lee
  • Publication number: 20130231323
    Abstract: Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
    Type: Application
    Filed: September 6, 2011
    Publication date: September 5, 2013
    Applicant: DUKE UNIVERSITY
    Inventors: Pei Zhou, Eric J. Toone
  • Patent number: 8513461
    Abstract: The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrien, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: August 20, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Jochen Heinicke
  • Publication number: 20130203733
    Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
    Type: Application
    Filed: December 20, 2012
    Publication date: August 8, 2013
    Applicants: Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: The General Hospital Corporation, Massachusetts Institute of Technology
  • Patent number: 8470831
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: June 25, 2013
    Assignee: Cogenia SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Publication number: 20130158261
    Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: TaiMed Biologics, Inc.
    Inventor: TaiMed Biologics, Inc.
  • Patent number: 8466201
    Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs wherein: Ar1 and Ar2=aryl or heteroaryl; a=0 to 5; R1=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R1 is the same or different; b=0 to 5; R2=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and where b is >1, each R2 is the same or different; V=(CR3aR3b)pSO2N(R3b)X and (CR3aR3b)pN(R3b)SO2(X); W=NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X=hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with ?1 NR8R9 groups wherein R8 and R9+nitrogen atom form a saturated or partially unsaturated heterocyclic group
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: June 18, 2013
    Assignee: Ramot at Tel-Aviv University ltd.
    Inventors: Simon David Edwards, Meriel Ruth Kimberly, Kanesalingam Suthaharan, Nawaz Mohammed Khan, Geoff Lawton
  • Patent number: 8461134
    Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: June 11, 2013
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Vincent S. Hernandez, Xianfeng Li, Suoming Zhang, Tsutomu Akama, Yanchen Zhang, Yang Liu, Jacob J. Plattner, Michael Richard Kevin Alley, Yasheen Zhou, James A. Nieman
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Patent number: 8425890
    Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: April 23, 2013
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: RE44874
    Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: April 29, 2014
    Assignee: Glaxo Group Limited
    Inventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Panayiotis Alexandrou Procopiou