Patents Issued in July 31, 2012
  • Patent number: 8232233
    Abstract: The present invention provides a refrigerating machine oil, a compressor oil composition, a hydraulic oil composition, a metalworking oil composition, a heat treating oil composition, a lubricating oil composition for machine tools and a lubricating oil composition which comprise a lubricating oil base oil having % CA of not more than 2, % CP/% CN of not less than 6 and an iodine value of not more than 2.5.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: July 31, 2012
    Assignee: Nippon Oil Corporation
    Inventors: Kazuo Tagawa, Yuji Shimomura, Ken Sawada, Katsuya Takigawa, Toshio Yoshida, Shinichi Mitsumoto, Eiji Akiyama, Junichi Shibata, Satoshi Suda, Hideo Yokota, Masahiro Hata, Hiroyuki Hoshino, Hajime Nakao, Shozaburo Konishi
  • Patent number: 8232234
    Abstract: Polymer-derived nanocomposite lubricants reduce friction and wear in applications involving elevated temperatures, such as within an internal combustion engine.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: July 31, 2012
    Assignee: PDC-Scientific, LLC
    Inventors: Rishi Raj, Sandeep R. Shah
  • Patent number: 8232235
    Abstract: Compositions are provided that include blends that consist essentially of 1,1,1,2,2,3,4,5,5,5-decafluoro-3-methoxy-4-(trifluoromethyl)pentane, trans-1,2-dichloroethylene, and a third component. The third component is selected from methanol, ethanol, isopropanol, t-butanol, and 1-propanol. The blends form ternary azeotropes. Provided compositions can be useful for cleaning electronic parts, as coating solvent components, as heat transfer fluids, and as lubricants.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: July 31, 2012
    Assignee: 3M Innovative Properties Company
    Inventor: John G. Owens
  • Patent number: 8232236
    Abstract: The claims encompass hard surface cleaner and hard surface treatment compositions containing particular ampholytic polymers which impart not only good residual cleaning properties but in particular give fast drying properties to the cleaning compositions. The polymers are for example terpolymers formed from diallydialkyammonium chloride, anionic monomers and N,N di-C1-C8 alkyl(meth)acrylamides.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: July 31, 2012
    Assignee: BASF SE
    Inventors: Bingham S. Jaynes, Ashish Taneja, Xian-Zhi Zhou, Joseph A. Lupia
  • Patent number: 8232237
    Abstract: A cleaning article comprises a substrate in the form of a wipe loaded with a cleaning agent and loaded with a heat generating agent which generates heat when the wipe is exposed to water.
    Type: Grant
    Filed: September 13, 2004
    Date of Patent: July 31, 2012
    Assignee: Reckitt Benckiser (UK) Limited
    Inventor: Malcolm Tom McKechnie
  • Patent number: 8232238
    Abstract: A water soluble strip that includes a carrier film that include water soluble polymer, one or more actives and one or more agents such as heat forming agent and/or degrading accelerator. The water soluble strip can optionally include other additives. The actives includes antimicrobial agent, cleaning agent and/or surfactant. The water soluble strip can include other materials. The heat forming agent and/or degrading accelerator, when used, are designed facilitate in degrading or dissolving the water soluble strip and/or increase the activity of the one or more actives. The water soluble film can be used for a variety of applications such as a hard surface cleaning strip, dishwashing strip, laundry cleaning strip, stop removing strip, drain unclogging strip, toilet bowl cleaning strip and the like. The water soluble strip eliminates the need to purchase and store numerous containers and/or heavy containers of cleaner that take up large amounts of shelf space.
    Type: Grant
    Filed: June 3, 2010
    Date of Patent: July 31, 2012
    Assignee: The Clorox Company
    Inventors: Maria Ochomogo, Nancy Falk, Aram Garabedian, Jessica Diaz, Kaj Johnson
  • Patent number: 8232239
    Abstract: Disclosed are concentrated liquid rinse cycle fabric softener compositions comprising a quaternary ammonium cation and benzylated alcohol solvent having between 50% to 90% weight active ingredients. Benzyl alcohol is disclosed as a preferred solvent to produce a clear liquid solution formulation rather than emulsion. The concentrated liquid rinse cycle fabric softener compositions of the present invention possess desirable stability, sustainability and fabric-softening properties. Methods of use are further described.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: July 31, 2012
    Assignee: Ecolab USA Inc.
    Inventors: Jessica Carlson, Stephen Christensen, Robert D. P. Hei
  • Patent number: 8232240
    Abstract: The present invention relates to treatment of infection by enveloped viruses through the use of papain-like cysteine protease inhibitors and kits thereof. Specifically, methods for treatment of filoviruses as well as other enveloped viruses such as Nipah, in particular using cathepsin inhibitors are described.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: July 31, 2012
    Assignee: The Brigham and Women's Hospital, Inc.
    Inventors: James Cunningham, Kartik Chandran
  • Patent number: 8232241
    Abstract: This document provides methods and materials related to treating liver conditions. For example, the methods and materials relating to the use of cAMP inhibitors to treat liver conditions are provided.
    Type: Grant
    Filed: May 1, 2006
    Date of Patent: July 31, 2012
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Nicholas F. Larusso, Tetyana V. Masyuk, Melissa Muff-Luett
  • Patent number: 8232242
    Abstract: The present invention relates to treatment of inflammatory bowel diseases with mammal beta defensins.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 31, 2012
    Assignee: Novozymes Adenium Biotech A/S
    Inventors: Tanja Maria Rosenkilde Kjaer, Thomas Kruse, Per Holse Mygind, Karoline Sidelmann Brinch, Soeren Kjaerulff, Birgitte Andersen
  • Patent number: 8232243
    Abstract: The invention relates to the use of tryptophan-containing, in particular tryptophan- and tyrosine-containing, peptides as antioxidants. The compounds can be used for the therapy or prophylaxis of syndromes and disorders associated with unwanted oxidative processes in the extracellular space.
    Type: Grant
    Filed: December 4, 2000
    Date of Patent: July 31, 2012
    Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.
    Inventors: Bernd Moosmann, Christian Behl
  • Patent number: 8232244
    Abstract: The present invention discloses methods and materials for delivering a cargo compound into a cancer cell. Delivery of the cargo compound is accomplished by the use of protein transduction domains derived from cupredoxins. The cargo compound may be a nucleic acid and specifically a DNA, RNA or anti-sense. The invention further discloses methods for treating cancer and diagnosing cancer.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: July 31, 2012
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Tapas Das Gupta, Ananda Chakrabarty, Craig Beattie, Tohru Yamada
  • Patent number: 8232245
    Abstract: The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable salt of caspofungin as active ingredient being useful for the prevention and/or treatment of fungal infections. The compositions additionally comprise specific bulking agents and small amounts or no amounts of an additional pH modifier and may be in a liquid or solid form, e.g. may be lyophilized compositions. The compositions show good stability and reduced amounts of sub-visible particulate matter formed in solutions which are reconstituted from the lyophilized product.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: July 31, 2012
    Assignee: Sandoz AG
    Inventors: Christian Welz, Gottfried Stubauer, Andreas Schmarda, Herwig Jennewein, Ingolf Macher, Johannes Ludescher
  • Patent number: 8232246
    Abstract: Compounds capable of inhibiting replication of the hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Abbott Laboratories
    Inventors: Keith F. McDaniel, Dale J. Kempf
  • Patent number: 8232247
    Abstract: The present invention relates to Angiopoietin-3 (Ang-3) and Angiopoietin-4 (Ang-4). The present invention also relates to methods of modulating an activity of Ang-3 or Ang-4. The present invention further relates to methods of treating cancer, diabetes, and arthritis.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: July 31, 2012
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Yin Xu, Qin Yu
  • Patent number: 8232248
    Abstract: The present invention relates to treatment of rheumatoid arthritis with mammal beta defensins.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 31, 2012
    Assignee: Novozymes Adenium Biotech A/S
    Inventors: Tanja Maria Rosenkilde Kjaer, Thomas Kruse, Per Holse Mygind, Karoline Sidelmann Brinch, Soeren Kjaerulff, Birgitte Andersen
  • Patent number: 8232249
    Abstract: The invention relates to the manufacture of a unit dose of a medicament for relieving the symptoms and/or restoring and/or protecting the neurons of patients suffering from Parkinson's disease. According to the invention, bee's venom is used in an amount of between 33 and 330 micrograms inclusive, for the manufacture of a unit dose for subcutaneous injection, every one to six weeks, of a medicament for relieving the symptoms and/or restoring and/or protecting the neurons of patients suffering from Parkinson's disease. The invention finds use in particular in the field of pharmacy.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: July 31, 2012
    Assignee: Assistance Publique Hopitaux de Paris
    Inventors: Andréas Hartmann, Anne-Marie Bonnet, Michael Schüpbach
  • Patent number: 8232250
    Abstract: A method of alleviating a symptom of relapsing-remitting multiple sclerosis in a human patient suffering from relapsing-remitting multiple sclerosis or a patient who has experienced a first clinical episode and is determined to be at high risk of developing clinically definite multiple sclerosis comprising administering to the human patient three subcutaneous injections of a therapeutically effective dose of glatiramer acetate over a period of seven days with at least one day between every subcutaneous injection so as to thereby alleviate the symptom of the patient.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: July 31, 2012
    Assignee: Yeda Research & Development Co., Ltd.
    Inventor: Ety Klinger
  • Patent number: 8232251
    Abstract: The invention features compounds of the general formula: B-L-M where B is a binding agent capable of selectively binding to a nerve cell surface receptor and mediating absorption of the compound by the nerve cell; M is a moiety which performs a useful non-cytotoxic function when absorbed by a nerve cell, and can be a therapeutic moiety or an imaging moiety; and L is a linker coupling B to M. The invention also features methods of use of the compounds in, for example, treating conditions such as viral infections and pain, as well as in labeling nerve cells.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: July 31, 2012
    Assignee: Manzanita Pharmaceuticals, Inc.
    Inventors: G. Craig Hill, Stephen B. Kahl, Robert R. Webb, Constance A. McKee
  • Patent number: 8232252
    Abstract: A novel P-selectin ligand glycoprotein is disclosed, comprising the amino acid sequence set forth in SEQ ID NO:2 or by the amino acid sequence set forth in SEQ ID NO:4. DNA sequences encoding the P-selectin ligand protein are also disclosed, along with vectors, host cells, and methods of making the P-selectin ligand protein. Pharmaceutical compositions containing the P-selectin ligand protein and methods of treating inflammatory disease states characterized by P-selectin- and E-selectin-mediated intercellular adhesion are also disclosed.
    Type: Grant
    Filed: July 3, 2008
    Date of Patent: July 31, 2012
    Assignee: Genetics Institute, LLC
    Inventors: Glenn R. Larsen, Dianne S. Sako, Xiao-Jia Chang, Geertruida M. Veldman, Dale Cumming, Ravindra Kumar, Gray Shaw
  • Patent number: 8232253
    Abstract: Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: July 31, 2012
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Yoel Kloog, Adi Zundelevich, Roni Haklai
  • Patent number: 8232254
    Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.
    Type: Grant
    Filed: October 8, 2007
    Date of Patent: July 31, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Jon S. Thorson, Ahmed Aqeel
  • Patent number: 8232255
    Abstract: The invention pertains to methods for protecting against malaria infection by vaccination. The method of the invention involves priming an anti-malaria immune response with a DNA-based vaccine and boosting that response with a protein-based a vaccine. The method of the invention also relates to broadening the resulting immune response by boosting with a protein-based vaccine.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: July 31, 2012
    Assignees: GlaxoSmithKline Biologicals S.A., The United States of America as represented by the Secretary of the Navy
    Inventors: Stephen L. Hoffman, Ruobing Wang, Judith E. Epstein, Joseph D. Cohen
  • Patent number: 8232256
    Abstract: The present invention is related to a nucleic acid molecule and uses thereof. The nucleic acid molecule comprises a double-stranded structure, whereby the double-stranded structure comprises a first strand and a second strand, whereby the first strand comprises a first stretch of contiguous nucleotides and said first stretch is at least partially complementary to a target nucleic acid, and whereby the second strand comprises a second stretch of contiguous nucleotides and said second stretch is at least partially complementary to the first stretch, whereby the first stretch comprises a nucleic acid sequence which is at least partially complementary to a nucleotide core sequence of the nucleic acid sequence according to SEQ ID NO:1 (NM_013355).
    Type: Grant
    Filed: July 20, 2007
    Date of Patent: July 31, 2012
    Assignee: Silence Therapeutics AG
    Inventors: Jorg Kaufmann, Oliver Keil, Ansgar Santel
  • Patent number: 8232257
    Abstract: Embodiments of the present invention provide methods for targeted inactivation of viral genomes. In one embodiment, zinc-finger proteins in which DNA binding sites are altered such that they recognize and bind different, desired DNA sequences contained in hepatitis B virus (HBV) and that include nuclease domains are used for inactivation. Other embodiments for targeted inactivation of viral genomes use small nucleic acid molecules, such as short micro-RNA molecules or short hairpin RNA molecules capable of mediating RNA interference (RNAi) against the hepatitis B virus.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: July 31, 2012
    Assignee: University of Iowa Research Foundation
    Inventors: Anton P. McCaffrey, Thomas J. Cradick
  • Patent number: 8232258
    Abstract: The present invention relates to variants of the NK1 fragment of the polypeptide growth factor HGF/SF which act as agonists of the MET receptor and their use. The agonists comprise at least one substitution at positions equivalent to 132, 134, 170 and 181 of full length HGF/SF and these substitutions provide a variant which shows scatter factor activity and induces DNA synthesis. In vivo the variants provide protection from liver damage in a model of acute liver failure.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: July 31, 2012
    Assignees: Cambridge Enterprise Limited, Medical Research Council
    Inventors: Ermanno Gherardi, Daniel Lietha, Thomas Leon Blundell, Dimitry Yurievich Chirgadze
  • Patent number: 8232259
    Abstract: Compositions including multiple oligodeoxynucleotides with a CpG motif are disclosed herein. The compositions can include either D or K type oligodeoxynucleotides. These compositions are of use in inducing an immune response in a large percentage of the individuals in a population.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: July 31, 2012
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Dennis Klinman, Ken Ishii, Daniela Verthelyi
  • Patent number: 8232260
    Abstract: The invention provides engineered RNA precursors that when expressed in a cell are processed by the cell to produce targeted small interfering RNAs (siRNAs) that selectively silence targeted genes (by cleaving specific mRNAs) using the cell's own RNA interference (RNAi) pathway. By introducing nucleic acid molecules that encode these engineered RNA precursors into cells in vitro with appropriate regulatory sequences, expression of the engineered RNA precursors can be selectively controlled both temporally and spatially, i.e., at particular times and/or in particular tissues, organs, or cells.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: July 31, 2012
    Assignee: University of Massachusetts
    Inventors: Phillip D. Zamore, Juanita McLachlan, Gyorgy Hutvagner, Alla Grishok, Craig C. Mello
  • Patent number: 8232261
    Abstract: The present invention provides a method of reducing phytotoxicity or plant injury at a crop plant locus caused by a herbicide application at the locus which method includes applying to the crop plant locus a chloronicotinyl insecticide before the herbicide application.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: July 31, 2012
    Assignee: Bayer CropScience LP
    Inventor: Michael R. Schwarz
  • Patent number: 8232262
    Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyperproliferative disorders, also are disclosed.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: July 31, 2012
    Assignee: DEKK-TEC, Inc.
    Inventor: Lee Roy Morgan
  • Patent number: 8232263
    Abstract: This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1?,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: July 31, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8232264
    Abstract: The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: July 31, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Eugene H. Gans, Mitchell S. Wortzman
  • Patent number: 8232265
    Abstract: Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: July 31, 2012
    Assignee: Board of Trustees of the University of Alabama
    Inventors: Robin D. Rogers, Daniel T. Daly, Richard P. Swatloski, Whitney L. Hough, James Hilliard Davis, Jr., Marcin Smiglak, Juliusz Pernak, Scott K. Spear
  • Patent number: 8232266
    Abstract: Manzamine compounds have been discovered to decrease cell dissociation and cell migration associated with the metastatic potential of cancer cells and a restoration of cancer cell susceptibility to agents, such as TRAIL, which can induce apoptosis. Specifically, Manzamine A has a formerly unrecognized utility in both blocking tumor cell invasion and tumor metastasis as well in restoring cancer cell susceptibility to standard chemotherapeutic agents which induce apoptosis and, therefore, has utility in treating cancer.
    Type: Grant
    Filed: February 20, 2007
    Date of Patent: July 31, 2012
    Assignee: Florida Atlantic University Board of Trustees
    Inventors: Esther A. Guzman, Jacob D. Johnson, Amy E. Wright
  • Patent number: 8232267
    Abstract: This invention provides a novel class of substituted macrocyclic porphyrin compounds. The compounds are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof are also described.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: July 31, 2012
    Assignee: The Trustees of Princeton University
    Inventor: John T. Groves
  • Patent number: 8232268
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: July 31, 2012
    Assignee: FOB Synthesis, Inc.
    Inventors: Woo-Baeg Choi, Ewa Kowalik
  • Patent number: 8232269
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substitu
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: July 31, 2012
    Assignee: Pfizer Inc.
    Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Patent number: 8232270
    Abstract: The present invention belongs to pharmaceutical field. It relates to a novel family of bivalent (?)-meptazinol compounds and/or their salts, as well as the preparation and utilization of the compounds in the treatment of neurodegenerative disorders and dementias such as Alzheimer's Disease (AD). In the present invention, bivalent (?)-meptazinol compounds were synthesized, from the starting material (?)-meptazinol, successively by N-demethylation forming (?)-nor-meptazinol and then by acylation with ?,?-alkanediacyl dihalides or alkylation with ?,?-dihaloalkanes. Results from in vitro cholinesterase inhibiting test and AChE-induced A? aggregation test demonstrated that the bivalent (?)-meptazinol compounds and/or their salts were novel bivalent inhibitors of both AChE and A? aggregation. The most potent compound inhibited both AChE and BChE at nM level, which was 10000 and 1500 times more potent than (?)-MEP hydrochloride, respectively.
    Type: Grant
    Filed: July 24, 2007
    Date of Patent: July 31, 2012
    Inventors: Zhuibai Qiu, Qiong Xie, Hongzhuan Chen, Hao Wang, Zheng Xia, Meiyan Lu, Xinghai Wang
  • Patent number: 8232271
    Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
  • Patent number: 8232272
    Abstract: The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.
    Type: Grant
    Filed: October 13, 2008
    Date of Patent: July 31, 2012
    Assignee: Merck Patent Gesellschaft mit beschränkter Haftung
    Inventors: Gerard Botton, Caroline Leriche, Annick Arbellot de Vacqueur, Annick Audet, Johannes Gleitz
  • Patent number: 8232273
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 31, 2012
    Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Institute of Medical Research
    Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
  • Patent number: 8232274
    Abstract: Disclosed is a set of compounds useful as glucan synthase inhibitors having the generic structure of Formula I: wherein the various moieties A, D, R6, etc., are as defined in the specification. These compounds are useful in treating or preventing fungal infections in a patient.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: July 31, 2012
    Assignees: Albany Molecular Research, Inc., Merck Sharp & Dohme Corp.
    Inventors: Pauline C. Ting, Robert G. Aslanian, Jianhua Cao, David Won-Shik Kim, Rongze Kuang, Gang Zhou, Robert Jason Herr, Andrew John Zych, Jinhai Yang, Heping Wu, Nicolas Zorn
  • Patent number: 8232275
    Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: July 31, 2012
    Assignees: Wayne State University, The Regents of the University of Michigan
    Inventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
  • Patent number: 8232276
    Abstract: The present invention provides anhydrous compositions for topical delivery of a medicament comprising (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol, or any combination of any of the foregoing; and (C) an anhydrous vehicle. In an alternate embodiment, the present invention provides anhydrous compositions for topical delivery of a medicament which comprise (A) a penetration enhancer/solvent selected from the group consisting of alcohol, propylene glycol, or a combination thereof; (B) a humectant/solvent selected from the group consisting of polyethylene glycol, glycerin, sorbitol, xylitol or any combination of any of the foregoing; (C) an anhydrous vehicle; and (D) a medicament.
    Type: Grant
    Filed: November 26, 2003
    Date of Patent: July 31, 2012
    Assignee: Johnson & Johnson Comsumer Companies, Inc.
    Inventors: Katherine M. Burnett, Ellen S. Kurtz
  • Patent number: 8232277
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: July 31, 2012
    Assignee: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
  • Patent number: 8232278
    Abstract: Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: July 31, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven Cesar Alfons De Jonghe, Piet André Maurits Maria Herdewijn, William A. Lee, William John Watkins
  • Patent number: 8232279
    Abstract: The present invention relates to a novel medicinal use of pyrazolopyrimidine compounds having superior effect as serotonin 5-HT2C receptor ligand thus being useful for the prevention and treatment of central nervous system (CNS) diseases. Accordingly, the pharmaceutical composition comprising pyrazolopyrimidine compounds and their pharmaceutically acceptable salts as active ingredients are useful for the prevention and treatment of serotonin 5-HT2C-related central nervous system diseases such as obesity, depression, anxiety and withdrawal symptoms due to drug abuse.
    Type: Grant
    Filed: October 7, 2009
    Date of Patent: July 31, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Ae Nim Pae, Hyunah Choo, Yong Seo Cho, Ahmed Asif, Woo-Kyu Park
  • Patent number: 8232280
    Abstract: Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: July 31, 2012
    Assignee: Pharmacyclics, Inc.
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 8232281
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Patent number: 8232282
    Abstract: The present invention relates to a bicyclic pyrimidine compound of the following formula (I) or a salt thereof. wherein R1 is lower alkyl, cyclic lower alkyl. etc.; R2 is H, lower alkyl, lower alkenyl, etc.; R3 is H, lower alkyl, lower alkenyl, etc.; X is O, S or —N(R4)—; R4 is H or lower alkyl; or R2 and R4 may combine each other to form cyclic amino; Y is amido, keto, sulfonyl, etc.; R5 is H or lower alkyl; Z is O or S; m and n are 1 or 2. Said compound (I) or a salt thereof have MGAT inhibitory activity, and are useful as an agent for treatment or prophylaxis of adiposity, metabolic syndromes, hyperlipidemia, hyper neutral lipemia, hyper VLDL-mia, hyper fatty acidemia, diabetes mellitus, arteriosclerosis.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: July 31, 2012
    Assignees: Dainippon Sumitomo Pharma Co., Ltd., Sumitomo Chemical Company, Limited
    Inventors: Keiji Nakamura, Hiroyuki Nakagawa, Yoko Kan