The Other Ring Is A Benzene Ring Patents (Class 548/304.4)
  • Publication number: 20130095322
    Abstract: Disclosed are: a yellow pigment composition which contains at least one kind of yellow pigment microparticle having excellent transmission characteristics; and a method for producing the yellow pigment microparticle. Specifically disclosed are: a yellow pigment composition which contains at least one kind of yellow pigment microparticle that are characterized in that the difference between the maximum transmittance (Tmax) and the minimum transmittance (Tmin), namely (Tmax?Tmin) is 80% or more in the transmission spectrum at 350-800 nm; and a method for producing the yellow pigment microparticle.
    Type: Application
    Filed: May 20, 2011
    Publication date: April 18, 2013
    Applicant: M. TECHNIQUE CO., LTD.
    Inventors: Masaki Maekawa, Daisuke Honda, Masakazu Enomura
  • Patent number: 8420828
    Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: April 16, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
  • Patent number: 8410283
    Abstract: An electrolyte additive is selected from N-alkyl benzimidazole derivatives and is applicable to dye-sensitized solar cells. Accordingly, the electrolyte additive can be added to electrolyte at low concentration, and loss of function due to crystallization after long-term use can be prevented; in addition, short circuit photocurrent density and solar energy-to-electricity conversion efficiency of solar cells incorporating the electrolyte additive can be increased.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: April 2, 2013
    Assignee: National Taipei University of Technology
    Inventors: Sheng-Tung Huang, Chung-Kuang Yang
  • Patent number: 8410284
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 12, 2009
    Date of Patent: April 2, 2013
    Assignees: Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.
    Inventors: Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka, Brett C. Bookser
  • Patent number: 8389558
    Abstract: The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: March 5, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegroz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8383663
    Abstract: The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: February 26, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegorz Pietrzynski, Patel Kishore, Thomasz Popek
  • Publication number: 20130046095
    Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Inventors: Laurent DUBOIS, Yannick EVANNO, Andre MALANDA
  • Publication number: 20130040389
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 14, 2013
    Applicant: Intrexon Coporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Publication number: 20130035487
    Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 7, 2013
    Applicant: Intrexon Corporation
    Inventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
  • Patent number: 8362056
    Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: January 29, 2013
    Assignee: Array BioPharma Inc.
    Inventor: George A. Doherty
  • Publication number: 20130004509
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: February 22, 2011
    Publication date: January 3, 2013
    Inventor: Levi Garraway
  • Patent number: 8344010
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: January 1, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: V. S. Prasadarao Lingam, Abraham Thomas, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20120316197
    Abstract: This invention relates to a compound with EP4 antagonistic activity, or a pharmaceutically acceptable salt with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof with EP4 receptor antagonistic activities, which is useful in the treatment of immune disease or allergy. This invention also relates to a pharmaceutical composition for the treatment of immune disease or allergy which comprises a therapeutically effective amount of a compound of formula (I), (II), (III), (IV), (Va) or (Vb), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 22, 2011
    Publication date: December 13, 2012
    Applicant: RAQUALIA PHARMA INC.
    Inventors: Kiyoshi Kanazawa, Kazuhiko Nonomura, Takako Okumura, Shinichi Koizumi
  • Patent number: 8323805
    Abstract: Disclosed herein are compounds represented by a formula: R1—O-A-C?C-D, where R1, A, and D are defined as described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: December 4, 2012
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae
  • Patent number: 8314135
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: November 20, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Lu Ying, Xiaowen Peng, Yat Sun Or
  • Patent number: 8314134
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: November 20, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Jun Jiang, Hao Li, David James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhiqiang Xia
  • Publication number: 20120253049
    Abstract: The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.
    Type: Application
    Filed: May 3, 2012
    Publication date: October 4, 2012
    Inventors: John DeMattei, Tsung-Hsun Chuang, Christopher John Squire, Ronald John Roberts, Gorkhn Sharma-Singh, Mohammed Pervez, James Gair Ford, Richard Anthony Storey, Paul Alfred Dickinson
  • Patent number: 8278459
    Abstract: The present invention provides novel diol compounds, novel cosmetic or dermatological sunscreen compositions containing these compounds and the use of the novel compounds as UV-filters. The compounds are particularly advantageous, because they adhere to the skin and therefore provide sunscreen protection for a prolonged period of time.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: October 2, 2012
    Assignee: DSM IP Assets B.V.
    Inventors: Jürgen H. Vollhardt, Yevgen Blyumin, Alexander Poschalko
  • Patent number: 8278460
    Abstract: This invention relates to novel substituted benzimidazoles and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound that modulates the GABAA receptor. This invention also provides novel intermediates for the preparation of the compounds of the invention, and salts thereof.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: October 2, 2012
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Scott L. Harbeson
  • Publication number: 20120244208
    Abstract: This invention relates to a topical cosmetic skin care method and composition. The method and composition is for treating facial skin to cause contraction and tightening of the facial skin, by effecting contraction of the collagen of the skin using an active agent/s that induces fibroblast contraction of the extra cellular matrix of the skin. A preferred active agent is a beta-2-adrenergic receptor (beta2AR) inhibitor.
    Type: Application
    Filed: September 6, 2010
    Publication date: September 27, 2012
    Inventor: Hugo Barrie Nel
  • Publication number: 20120238611
    Abstract: The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2?, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
    Type: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Patent number: 8269019
    Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: September 18, 2012
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
  • Publication number: 20120213806
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Patent number: 8236841
    Abstract: A fused heterocycle derivative represented by the general formula (I): (wherein R1 represents optionally substituted lower alkyl, or the like; R2 represents an optionally substituted aliphatic heterocyclic group, or the like; R3 represents —C(?Z)NR5R6 (wherein R5 and R6 represent optionally substituted lower alkyl, or the like, and Z represents an oxygen atom or the like), or the like; n represents an integer of 1 to 3; and W represents C—R5 (wherein R5 represents a hydrogen atom or the like)) or a pharmaceutically acceptable salt thereof, and the like are provided.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: August 7, 2012
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Takashi Sawada, Naoto Osakada, Satoshi Kaneko, Atsuko Mizutani, Noriaki Uesaka, Keishi Katayama
  • Patent number: 8232410
    Abstract: The present invention relates to novel benzimidazole derivatives and pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating a patient infected by Mycobacterium tuberculosis or Francisella tulerensis by administering to the patient a benzimidazole derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2008
    Date of Patent: July 31, 2012
    Assignee: The Research Foundation of State University of New York
    Inventors: Iwao Ojima, Seung-yub Lee
  • Patent number: 8232312
    Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20120184556
    Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.
    Type: Application
    Filed: July 23, 2010
    Publication date: July 19, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
  • Patent number: 8222519
    Abstract: A merocyanine dye is provided. The merocyanine dye is represented by formula (1). In the formula (1), A1 represents a divalent atomic group, n represents an integer of 1 to 3, A2 and A3 each independently represent an aromatic hydrocarbon ring or a heterocyclic ring having 3 to 18 carbon atoms, and R11 and R12 each independently represent a hydrogen atom, an alkyl group having 1 to 18 carbon atoms, an aryl group having 6 to 18 carbon atoms, or a heterocyclic group having 3 to 18 carbon atoms.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: July 17, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Kimiatsu Nomura, Rui Shen, Hideyuki Suzuki
  • Patent number: 8212052
    Abstract: The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2?, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 8, 2008
    Date of Patent: July 3, 2012
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Patent number: 8211923
    Abstract: The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: July 3, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20120165305
    Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 28, 2012
    Inventors: Wenqing YAO, Colin ZHANG, Meizhong XU, Jincong ZHUO, Chunhong HE
  • Publication number: 20120142921
    Abstract: The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R have the same meanings as given in the Description. The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
    Type: Application
    Filed: August 9, 2010
    Publication date: June 7, 2012
    Applicant: SHENYANG J & HEALTH PHARMACEUTICAL CO., LTD.
    Inventor: Xiulan Shi
  • Patent number: 8188282
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: May 29, 2012
    Assignee: Sanofi-Aventis
    Inventors: Jorge Alonso, Andreas Lindenschmidt, Marc Nazare, Nis Halland, Omar Rkyek, Matthias Urmann
  • Patent number: 8183385
    Abstract: Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X1, X2, X5, R1, R2 and R4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: May 22, 2012
    Assignees: Array BioPharma Inc., AstraZeneca AB
    Inventors: John DeMattei, Sagar Shakya, Paul J. Nichols, Bradley R. Barnett, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, John Leonard
  • Publication number: 20120122137
    Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonie, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
    Type: Application
    Filed: July 29, 2010
    Publication date: May 17, 2012
    Applicant: bioMérieux S.A.
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Patent number: 8178693
    Abstract: Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 15, 2012
    Assignee: Array Biopharma Inc.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • Publication number: 20120111796
    Abstract: Boron selective ionic liquids and polymeric ionic liquids, methods of making and methods of using the same are disclosed.
    Type: Application
    Filed: August 10, 2009
    Publication date: May 10, 2012
    Applicant: UNIVERSITY OF TOLEDO
    Inventor: Jared L. Anderson
  • Patent number: 8168668
    Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: May 1, 2012
    Assignee: AstraZeneca AB
    Inventors: Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
  • Patent number: 8158628
    Abstract: Sulfonylated tetrahydroazolopyrazine compounds corresponding to the formula I wherein R1, R2a, R2b, R3a, R3b, R4, R8, R9a, R9b, R10, R11, A, B, W1, W2 and W3 have the meanings defined herein, pharmaceutical compositions containing such compounds, a method for the preparation of such compounds, and the use of such compounds for treating or inhibiting various types of pain and/or other conditions mediated at least in part by the bradykinin 1 receptor (B1R).
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: April 17, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Stefan Oberboersch, Melanie Reich, Stefan Schunk, Ruth Jostock, Sabine Hees, Michael Engels, Tieno Germann, Edward Bijsterveld
  • Patent number: 8147987
    Abstract: An organic electroluminescent element comprises: a pair of electrodes; and one or more organic compound layers at least one of which is a light-emitting layer, the one or more organic compound layers being provided between the pair of electrodes, wherein at least one of the one or more organic compound layers comprises a compound represented by general formula (Z): wherein R31 and R32 each represents a hydrogen atom or a substituent, R3A represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom, X31 to X38 each represents a substituted or unsubstituted carbon atom or a nitrogen atom, and Y31 to Y33 each represents a nitrogen atom or C—R3B (wherein R3B represents a substituent other than an aromatic hetero ring connected through a nitrogen atom, or a hydrogen atom).
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: April 3, 2012
    Assignee: Fujifilm Corporation
    Inventors: Itaru Osaka, Tatsuya Igarashi, Toshihiko Ise, Eiji Fukuzaki, Satoshi Sano
  • Publication number: 20120071447
    Abstract: Methods, compounds, and pharmaceutical compositions for treating an arenavirus infections are disclosed. Methods for preparing the compounds and pharmaceutical compositions are also disclosed. The novel compounds and compositions are used for treatment of an arenavirus infections, which include but are not limited to the following viruses: Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV.
    Type: Application
    Filed: November 10, 2011
    Publication date: March 22, 2012
    Applicant: Siga Technologies Inc.
    Inventors: Dongcheng Dai, Sean M. Amberg, Tove Bolken, Dennis E. Hruby
  • Patent number: 8138177
    Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: March 20, 2012
    Assignee: Pfizer Inc.
    Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
  • Patent number: 8119675
    Abstract: Novel compounds of the formula I (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R, Q, W, X and Z have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: February 21, 2012
    Assignee: Merck Patent GmbH
    Inventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
  • Publication number: 20120041207
    Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.
    Type: Application
    Filed: August 10, 2011
    Publication date: February 16, 2012
    Applicant: Sterix Limited
    Inventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
  • Publication number: 20120035139
    Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.
    Type: Application
    Filed: April 16, 2010
    Publication date: February 9, 2012
    Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
  • Publication number: 20120035217
    Abstract: There is provided compounds of formula I, wherein Y, ring A, D1, D2a, D2b, D3, L1, Y1, L2 and Y2 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.
    Type: Application
    Filed: March 12, 2010
    Publication date: February 9, 2012
    Applicant: BIOLIPOX AB
    Inventors: Peter Nilsson, Benjamin Pelcman, Martins Katkevics, Edgars Suna, Ilya Popovs
  • Publication number: 20120028969
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 2, 2012
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Liansheng SU
  • Patent number: 8106090
    Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: January 31, 2012
    Assignee: Eli Lilly and Company
    Inventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Michael Robert Wiley
  • Publication number: 20120020915
    Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
    Type: Application
    Filed: January 13, 2011
    Publication date: January 26, 2012
    Applicants: QUEENS UNIVERSITY AT KINGSTON, THE SIR MORTIMER B. DAVIS JEWISH GENERAL HOSPITAL, OSTA BIOTECHNOLOGIES, INC.
    Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
  • Patent number: 8097349
    Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.
    Type: Grant
    Filed: April 7, 2010
    Date of Patent: January 17, 2012
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura