The Other Ring Is A Benzene Ring Patents (Class 548/304.4)
  • Patent number: 8703300
    Abstract: Disclosed is a long-life organic electroluminescent element which can be driven at low voltage. Also disclosed are a display and illuminator using the same. Specifically disclosed is an organic electroluminescent element comprising on a substrate, an anode, a cathode and an organic compound layer arranged between the anode and the cathode and including at least one light emission layer. This organic electroluminescent element is characterized in that the organic compound layer includes an electron transport material-containing layer which contains an electron transport material represented by Formula (a) and at least one substance selected from the group consisting of metals, salts of the metals and electron-donating compounds. Formula (a) Ar1-(Ar2)n [In the formula, Ar1 represents a group derived from an aromatic hydrocarbon ring or a group derived from an aromatic heterocycle; Ar2 represents a group derived from an aromatic heterocycle; and n represents an integer of 2 or more.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: April 22, 2014
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Yoshiyuki Suzuri, Akira Kawakami, Hiroshi Kita
  • Patent number: 8703964
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 22, 2014
    Assignee: Supratek Pharma Inc.
    Inventors: Tomasz Popek, Kishore Patel, Valery Alakhov, Grzegorz Pietrzynski
  • Patent number: 8703811
    Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.
    Type: Grant
    Filed: May 7, 2009
    Date of Patent: April 22, 2014
    Assignees: Genzyme Corporation, Massachusetts Institute of Technology, President and Fellows of Harvard College
    Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
  • Publication number: 20140107120
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8697885
    Abstract: An object is to provide a novel carbazole compound that can be used for a transport layer, a host material, or a light-emitting material in a light-emitting element. A carbazole compound where nitrogen of a carbazole group, the carbazole skeleton of which whose 3-position is bonded to the 4-position of a dibenzofuran skeleton or a dibenzothiophene skeleton, is bonded to a benzimidazole skeleton through a phenylene group, is provided. The carbazole compound has a high carrier-transport property, and can be suitably used for a material for a light-emitting element or for an organic semiconductor material.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: April 15, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Sachiko Kawakami, Nobuharu Ohsawa
  • Patent number: 8697255
    Abstract: The present invention relates to an organic light-emitting diode comprising an anode and a cathode Ka and a light-emitting layer E and if appropriate at least one further layer, where the light-emitting layer E and/or the at least one further layer comprises at least one compound selected from disilylcarbazoles, disilyldibenzofurans, disilyldibenzothiophenes, disilyldibenzophospholes, disilyldibenzothiophene S-oxides and disilyldibenzothiophene S,S-dioxides, to a light-emitting layer comprising at least one of the aforementioned compounds, to the use of the aforementioned compounds as matrix material, hole/exciton blocker material, electron/exciton blocker material, hole injection material, electron injection material, hole conductor material and/or electron conductor material, and to a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: April 15, 2014
    Assignee: BASF SE
    Inventors: Nicolle Langer, Klaus Kahle, Christian Lennartz, Oliver Molt, Evelyn Fuchs, Jens Rudolph, Christian Schildknecht, Soichi Watanabe, Gerhard Wagenblast
  • Patent number: 8691998
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 8, 2014
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam S. Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Patent number: 8685541
    Abstract: Disclosed are electroluminescent materials comprising a homopolymer based on recurring structural units of the formula (I) wherein R9, R9? R9?, R11, R13 R14, R11?, R13?, R14? independently are H or an organic substituent, where at least one of R9, R9? R9?, R11, R13 R14, R11?, R13?, R14? comprises a group R10 of the formula —(Sp)x10-[PG?]< wherein Sp is a divalent organic spacer, PG? is a group derived from a polymerizable group, and x10 is 0 or 1, with substituents and spacer as defined in claim 1. Further disclosed are some novel polymers of this class as well as monomers for their preparation. The homopolymers are advantageously used as a host material in devices further comprising a luminescent component, which is usually selected from phosphorescent metal complexes and fluorescent dopants.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: April 1, 2014
    Assignee: BASF SE
    Inventors: Natalia Chebotareva, Roger Pretot, Paul Adriaan Van Der Schaaf, Annemarie Wolleb, Heinz Wolleb
  • Patent number: 8679645
    Abstract: The present invention relates to novel materials which can be used in organic electronic devices, in particular electroluminescent devices, and are certain derivatives of fused aromatic systems.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: March 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Holger Heil, Arne Buesing, Philipp Stoessel, Horst Vestweber
  • Patent number: 8673459
    Abstract: An object is to provide a light-emitting element with high emission efficiency which includes a novel carbazole derivative that has a wide energy gap and can be used for a transport layer or a host material in a light-emitting element. A carbazole derivative in which the 4-position of dibenzothiophene or dibenzofuran is bonded to the 2- or 3-position of carbazole has been able to be provided by use of the carbazole derivative. Further, a light-emitting element having high emission efficiency has been able to be provided by use of the carbazole derivative.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: March 18, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Satoshi Seo, Harue Osaka, Sachiko Kawakami, Nobuharu Ohsawa, Tsunenori Suzuki, Hiromi Nowatari, Hiroki Suzuki, Kyoko Takeda
  • Patent number: 8669114
    Abstract: The subject of the invention at hand are novel, a little basic, fluorinated pentafluorophenyl imide anions, which can be used as anions in ionic liquids. Methods for producing ionic liquids are described, which contain these novel pentafluorophenyl imide ions as anions, as well as quaternary organic ammonium ions, guanidinium ions, N-organo-pyridinium ions, imidazolium, imidazolidinium or benzimidazolidinium ions, alkyl-alkylidene phosphoranes or aryl-alkylidene phosphoranes as cations. Alternative methods according to the present invention provide ionic liquids through reaction of ketene N,N-diacetals or alkyl or aryl-alkylidene phosphoranes with acids. The ionic liquids according to the present invention are suitable, for example, as solvents for syntheses, as mobile and/or stationary phase in chromatography, as electrolyte systems for batteries, galvanic elements, fuel cells and rechargeable battery packs.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: March 11, 2014
    Assignee: Philipps-Universitaet Marburg
    Inventors: Jorg Sundermeyer, Thomas Linder
  • Patent number: 8658207
    Abstract: The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Wolfram Eisenreich, Thomas Friedl, Florian Sommer, Nantharat Pearnchob, Karl G. Wagner
  • Patent number: 8658635
    Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Patent number: 8652653
    Abstract: Novel materials are provided, having a single phenyl or a chain of phenyls where there is a nitrogen atom on each end of the single phenyl or chain of phenyls. The nitrogen atom may be further substituted with particular thiophene, benzothiophene, and triphenylene groups. Organic light-emitting devices are also provided, where the novel materials are used as a hole transport material in the device. Combinations of the hole transport material with specific host materials are also provided.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: February 18, 2014
    Assignee: Universal Display Corporation
    Inventors: Chun Lin, Bin Ma, Chuanjun Xia, Yonggang Wu, Raymond Kwong
  • Patent number: 8637676
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: January 28, 2014
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8633235
    Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: January 21, 2014
    Assignee: Neomed Institute
    Inventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
  • Patent number: 8628864
    Abstract: There is provided an indolo[3,2,1-jk]carbazole compound having an excellent membrane property, a high T1 energy, and a deep HOMO level. There is also provided an organic light-emitting device that contains the indolo[3,2,1-jk]carbazole compound. There is provided an indolo[3,2,1-jk]carbazole compound having a high T1 energy and a deep HOMO level.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: January 14, 2014
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shigemoto Abe, Jun Kamatani, Kengo Kishino
  • Patent number: 8629170
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel 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, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 14, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dennis E. Hruby, Tove Bolken, Sean M. Amberg, Dongcheng Dai
  • Patent number: 8629285
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: January 14, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
  • Publication number: 20140005221
    Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 2, 2014
    Applicant: SATO PHARMACEUTICAL CO., LTD.
    Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130317027
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
  • Patent number: 8586205
    Abstract: Disclosed herein are compounds represented by a formula: Wherein Ar1, Cb, Ph1, Het1, and A are described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, David T. Sisk, Brett T. Harding, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae, Sazzadur Rahman Khan, Liping Ma, Rebecca Bottger
  • Publication number: 20130302248
    Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
    Type: Application
    Filed: June 25, 2013
    Publication date: November 14, 2013
    Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharla, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
  • Publication number: 20130292601
    Abstract: The present invention relates to the use of at least one tertiary amine-N-oxide of formula I as additive in dye-sensitized solar cells and to special electrolyte formulations and a dye-sensitized solar cell comprising at least one compound of formula I.
    Type: Application
    Filed: May 24, 2013
    Publication date: November 7, 2013
    Inventors: Hiroki YOSHIZAKI, Kentaro KAWATA, Tomohisa GOTO, Hiromi SHINOHARA, Peter KIRSCH
  • Publication number: 20130296346
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 7, 2013
    Applicant: Faes Farma, S.A.
    Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
  • Publication number: 20130281392
    Abstract: The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Publication number: 20130267711
    Abstract: The invention provides a method of activating PPAR ? and a method of treating or preventing a disease associated with PPAR ? by administering a tricyclic compound having a PPAR ? agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
    Type: Application
    Filed: June 3, 2013
    Publication date: October 10, 2013
    Inventors: Arata YANAGISAWA, Keiji UEHARA, Masahiro MATSUBARA, Kimihisa UENO, Michihiko SUZUKI, Takeshi KUBOYAMA, Keisuke YAMAMOTO, Tomohiro TAMURA
  • Patent number: 8551988
    Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: October 8, 2013
    Assignee: Mei Pharma, Inc.
    Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
  • Patent number: 8545886
    Abstract: The invention is directed to a Pharmaceutical extended release system, particularly for oral administration, of a pH-dependent water-soluble active substance, comprising or essentially consisting of a) flibanserin or a pharmaceutically acceptable derivative thereof as active substance; b) one or more pharmaceutically acceptable pH-dependent polymers; c) one or more pharmaceutically acceptable pH-independent polymers; d) one or more pharmaceutically acceptable acids; and e) optionally one or more additives. The present invention provides a release profile of flibanserin which is independent on the pH in the gastrointestinal tract when administered orally resulting in a significantly improved bioavailability.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Wolfram Eisenreich, Thomas Friedl
  • Patent number: 8541596
    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: April 21, 2011
    Date of Patent: September 24, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
  • Publication number: 20130245279
    Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.
    Type: Application
    Filed: September 13, 2012
    Publication date: September 19, 2013
    Inventors: John Demattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
  • Patent number: 8530670
    Abstract: Novel heterocyclic derivatives of formula (I): or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein Ra, n, R1 and R2 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).
    Type: Grant
    Filed: March 16, 2012
    Date of Patent: September 10, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck
  • Patent number: 8519074
    Abstract: Polymers including pendent hydrophobic groups and pendent proton transfer groups are shown to form nanostructured films exhibiting greatly increased proton conductivity compared with films prepared from corresponding polymers lacking hydrophobic groups. The polymers can include repeating units each of which has both a hydrophobic group and a proton transfer group. Alternatively, the polymers can be the product of copolymerizing a first monomer with at least one hydrophobic group and a second monomer with at least one proton transfer group. The polymers are useful for the preparation of fuel cell proton exchange membranes.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 27, 2013
    Assignee: The University of Massachusettes
    Inventors: Sankaran Thayumanavan, Mark Tuominen, Ryan Hayward
  • Patent number: 8513432
    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: May 30, 2012
    Date of Patent: August 20, 2013
    Assignee: Theravance, Inc.
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Patent number: 8501887
    Abstract: A radical polymerizable composition includes a radical polymerizable compound and an organoborane-azole complex. The organoborane-azole complex includes an azole having at least two nitrogen atoms wherein at least one nitrogen atom is an sp3 nitrogen atom and is substituted. A method of forming the composition includes the step of combining the radical polymerizable compound and the organoborane-azole complex to form the composition. The method also includes the step of polymerizing the composition. A composite article which includes a substrate and a cured composition disposed on the substrate is also provided. The cured composition is formed from polymerization of the composition.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: August 6, 2013
    Assignee: Dow Corning Corporation
    Inventors: Dongchan Ahn, Gang Lu
  • Patent number: 8501956
    Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: August 6, 2013
    Assignees: Array BioPharma Inc., AstraZeneca SB
    Inventors: John Demattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
  • Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20130172389
    Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.
    Type: Application
    Filed: December 27, 2012
    Publication date: July 4, 2013
    Applicant: Allegan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130158047
    Abstract: Provided are heterocyclic compounds, having effects of treating and preventing inflammatory diseases and treating skin wounds, and particularly, exhibiting effects of recovering disrupted skin barriers, mitigating inflammation, and pruritus. Also, a composition containing the compound as an effective component can be used to mitigate various inflammatory diseases and protease activated receptor-2 (PAR-2)-overexpressed diseases, and can be particularly used as a composition having an anti-inflammatory function in inflammatory skin diseases including atopic dermatitis and the like, by inhibiting PAR-2 activity.
    Type: Application
    Filed: August 25, 2011
    Publication date: June 20, 2013
    Applicant: NEOPHARM CO., LTD.
    Inventors: Hyung Sub Gwak, Yong Zu Kim, Uk Il Kim, Byeong Deog Park, Tae Kyo Park, Sung Ho Woo, Joung Yul Yun, Dae Yon Lee, Hyang Sook Lee, Jeong Eun Jeon, Se Kyoo Jeong, Hyung Mook Choi
  • Patent number: 8461351
    Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: June 11, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20130143910
    Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.
    Type: Application
    Filed: November 14, 2012
    Publication date: June 6, 2013
    Inventor: Zhang Weihua
  • Patent number: 8455661
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 4, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam Steven Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Patent number: 8455662
    Abstract: Formulations are provided, comprising: a compound of Formula I, a pharmaceutically acceptable salt thereof, or a mixture of any two or more thereof; and an ingredient selected from a hydrophilic solvent, a lipophilic solvent, an emulsifier, or a mixture of any two or more thereof; wherein the compound of Formula I is: In some embodiments, the formulations are liquids. In other embodiments, the formulations are solids. Also provided are methods of preparing such formulations.
    Type: Grant
    Filed: July 20, 2007
    Date of Patent: June 4, 2013
    Assignee: Novartis AG
    Inventors: Ahmad Hashash, Sean Ritchie, Kangwen Lin, Peng Shen, Augustus Okhamafe, Rampurna Gullapalli
  • Patent number: 8455640
    Abstract: Novel process for statins and its pharmaceutically acceptable salts thereof represented by general formula (I).
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: June 4, 2013
    Assignee: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Srinivasan Thirumalai Rajan, Maramreddy Sahadeva Reddy
  • Patent number: 8450354
    Abstract: The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 28, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Mohan Rao, Raju Bore Gowda, Robert Carl Andrews, Rongyuan Xie, Soumya P. Sahoo, Tan Ren, William Kenneth Banner
  • Patent number: 8436032
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Tomasz Popek, Kishore Patel, Valery Alakhov, Grzegorz Pietrzynski
  • Patent number: 8436031
    Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: May 7, 2013
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventor: Oak K. Kim
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.