Patents Issued in May 14, 2013
  • Utilization of hypertension/hypercardia-preventing effect of D-allose
    Patent number: 8440619
    Abstract: The object is to provide a novel application of D-allose (e.g., use for prevention of hypertension or hypercardia). Thus, disclosed is a composition for preventing the increase in blood pressure which comprises D-allose as an active ingredient; or a composition containing D-allose and/or a derivative thereof, preferably in an amount of 0.1 to 50% by weight. Preferably, the composition is in a form selected from the group consisting of a food additive, a food material, a beverage/food, a health beverage/food, a pharmaceutical and a feeding stuff which can be used for the prevention and treatment of a cardiovascular system disorder (e.g., hypertension, hypercardia). The increase in blood pressure may be caused by salt-sensitive hypertension. Also disclosed is use of D-allose for preventing the increase in blood pressure (excluding medical practices).
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: May 14, 2013
    Assignees: National University Corporation Kagawa University, Matsutani Chemical Industry Co., Ltd.
    Inventors: Masaaki Tokuda, Shoji Kimura, Ken Izumori
  • Methods, compositions and articles of manufacture for contributing to the treatment of cancers
    Patent number: 8440620
    Abstract: Methods, compositions and articles of manufacture for contributing to the treatment of cancers, including solid tumors, are disclosed. The methods, compositions and articles of manufacture can utilize an endothelin B agonist (ETB) to enhance the delivery and resulting efficacy of a chemotherapeutic agent.
    Type: Grant
    Filed: August 29, 2011
    Date of Patent: May 14, 2013
    Assignee: Spectrum Pharmaceuticals, Inc.
    Inventors: Anil Gulati, Guru Reddy, Luigi Lenaz
  • Analogs of ShK toxin and their uses in selective inhibition of Kv1.3 potassium channels
    Patent number: 8440621
    Abstract: Analogs of ShK toxin and methods for using such ShK analogs. The ShK analogs generally comprise ShK toxin attached to a chemical entity (e.g. an atom, molecule, group, residue, compound, moiety, etc.) that has an anionic charge. The ShK analogs may be administered to human or non-human animal subjects to cause inhibition of potassium channels or to otherwise treat diseases or disorders. In some embodiments, the chemical entity to which the ShK toxin is attached may be chosen to provide selective inhibition of certain potassium channels (e.g., Kv1.3 channels) over other potassium channels (e.g., Kv1.1 channels). In come embodiments, the chemical entity to which the ShK toxin is attached may include a fluorophore and such fluorophore-tagged ShK analogs may be used in flow cytometry alone, or in conjunction with class II tetramers that can detect autoreactive cells.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: May 14, 2013
    Assignees: The Regents of the University of California, Bachem Biosciences, Inc.
    Inventors: George K. Chandy, Christine Beeton, Michael William Pennington
  • Use of gelsolin to treat multiple sclerosis and to diagnose neurologic disease (stossel)
    Patent number: 8440622
    Abstract: The invention relates to the use of gelsolin to treat neurologic diseases (e.g., multiple sclerosis) and to the use of gelsolin to diagnose, monitor, and evaluate therapies of neurologic diseases.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: May 14, 2013
    Assignees: The Brigham and Women's Hospital, Inc., BloodCenter Research Foundation, Inc.
    Inventors: Thomas P. Stossel, Po-Shun Lee, Bonnie Dittel, Katarzyna Maresz
  • Polymer stabilized neuropeptides
    Patent number: 8440623
    Abstract: A substantially hydrophilic conjugate is provided having a peptide that is capable of passing the blood-brain barrier covalently linked to a water-soluble nonpeptidic polymer such as polyethylene glycol. The conjugate exhibits improved solubility and in vivo stability and is capable of passing the blood-brain barrier of an animal.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: May 14, 2013
    Assignee: Nektar Therapeutics
    Inventors: Michael David Bentley, Michael James Roberts
  • Peptide whitening agents and cosmetic compositions comprising the same
    Patent number: 8440624
    Abstract: The present invention relates to novel peptide compounds having the following formula [R1R2N—CH(Ra)—CO]a-(AA1)m-(AA2)b-X1—X2—X3—Y1—Y2—Y3—X4-(AA3)n-[NH—CH(Rb)—COOR3]c. It also pertains to cosmetic and dermatological compositions comprising one or more of these peptide compounds and to their uses in the cosmetic whitening of human skin and for the manufacture of a dermatological preparation intended to depigment human skin.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: May 14, 2013
    Assignee: Chanel Parfums Beaute
    Inventors: Stefan Honing, Gaelle Saintigny
  • Secreted protein acidic and rich in cysteine (SPARC) as chemotherapeutic sensitizers
    Patent number: 8440625
    Abstract: The present invention relates to compositions and methods of use thereof for cancer therapy sensitization. Such compositions comprise functional fragments of the nucleotide and/or polypeptide sequences of a Secreted Protein Acidic and Rich in Cysteine (SPARC). The compositions can be used in combination with existing chemotherapeutic agents for treatment of cancers.
    Type: Grant
    Filed: June 26, 2007
    Date of Patent: May 14, 2013
    Assignee: University of British Columbia
    Inventor: Isabella T. Tai
  • Antineoplastic peptides
    Patent number: 8440626
    Abstract: The present invention provides antineoplastic peptides of formula I, I R1R2N-CHX-CO-A-B-D-E-(G)S-K wherein R1, R2, X, A, B, D, E, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: May 14, 2013
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilhelm Amberg, Teresa Barlozzari, Harald Bernard, Ernst Buschmann, Andreas Haupt, Hans-Guenther Hege, Bernd Janssen, Andreas Kling, Helmut Lietz, Kurt Ritter, Martina Ullrich, Jurgen Weymann, Thomas Zierke
  • G protein coupled receptor agonists and antagonists and methods of use
    Patent number: 8440627
    Abstract: The invention relates generally to G protein coupled receptors (GPCRs) and in particular to GPCR agonists and antagonists, use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with GPCRs, such as in treating conditions in which chemokine receptors play a role, e.g., sepsis, arthritis, inflammation and autoimmune diseases.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: May 14, 2013
    Assignee: Tufts Medical Center, Inc.
    Inventors: Athan Kuliopulos, Lidija Covic, Nicole Kaneider
  • Medical compositions containing ghrelin
    Patent number: 8440628
    Abstract: It is provided a pharmaceutical composition stably containing ghrelin or its derivative, which is an endogenous growth hormone secretagogue (GHS) to a growth hormone secretagogue-receptor (GHS-R), comprising a aqueous solution containing the ghrelins having pH range of 2 to 7, wherein the aqueous solution having pH range of 2 to 7 is a buffer solution, especially, glycine hydrochloride buffer, acetate buffer, citrate buffer, lactate buffer, phosphate buffer, citric acid-phosphate buffer, phosphate-acetate-borate buffer or phthalate buffer, and the concentration of the ghrelins in the solution is from 0.03 nmol/mL to 6 ?mol/mL.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: May 14, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Yoshiharu Minamitake, Masaru Matsumoto
  • Cyclic receptor-associated protein (RAP) peptides
    Patent number: 8440629
    Abstract: The present invention relates generally to receptor-selective variants of the low-density lipoprotein receptor-associated protein (RAP) and compositions thereof, methods of generating such variants and methods of using such receptor-selective RAP variant compositions for therapeutic purposes.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: May 14, 2013
    Assignee: Raptor Pharmaceuticals Inc.
    Inventors: Christopher M. Starr, Todd C. Zankel
  • Akt activity specifically inhibiting polypeptide
    Patent number: 8440630
    Abstract: The present invention is to provide a polypeptide specifically inhibiting the activity of Akt (Protein Kinase B), the DNA thereof, the antibody thereof, an inhibitor of Akt activity or an antitumor agent, and the like. The polypeptide comprises polypeptides (SEQ ID NO: 1, 3, 5, 7, and 9 of the sequence listing) that contain an amino acid sequence corresponding to any of the position of amino acid residue 10-24 of human TCL1, amino acid residue 8-22 of human TCL1B, amino acid residue 5-19 of human MTCP1, and amino acid residue 9-24 of mouse or rat TCL1; and the derivatives. Further, the present invention includes DNA encording the polypeptide (SEQ ID NO: 2, 4, 6, 8 or 10 of the sequence listing), and the antibodies specifically binding to the polypeptides. The polypeptide of the present invention can be used for an inhibitor of Akt activity, an antitumor agent, or the like.
    Type: Grant
    Filed: December 14, 2004
    Date of Patent: May 14, 2013
    Assignee: Japan Science and Technology Agency
    Inventors: Masayuki Noguchi, Futoshi Okada, Makoto Hiromura
  • Compositions for drug administration
    Patent number: 8440631
    Abstract: The present invention provides compositions and methods and for increasing the bioavailability of therapeutic agents in a subject, as well as compositions and methods for providing migraine pain relief. The compositions include at least one alkyl glycoside and at least one therapeutic agent, such as a 5-HT receptor agonist, wherein the alkylglycoside has an alkyl chain length from about 10 to about 16 carbon atoms.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: May 14, 2013
    Assignee: Aegis Therapeutics, LLC
    Inventor: Edward T. Maggio
  • Protopanaxadiol-type ginsenoside compositions and uses thereof
    Patent number: 8440632
    Abstract: Provided herein are ginsenoside compositions comprising at least 10% (w/w) of a protopanaxadiol type of ginsenoside suitable for administration to a subject. Also provided are methods using the ginsenoside compositions for reducing acetaldehyde concentrations, preventing or ameliorating a symptom of elevated acetaldehyde concentration, or reducing the risk of diseases or disorders caused by the intake of ethyl alcohol.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: May 14, 2013
    Assignee: Raptor Therapeutics Inc.
    Inventors: Thomas E. Daley, Michael Tempesta
  • Anthelmintic combination
    Patent number: 8440633
    Abstract: A composition comprising 2-desoxoparaherquamide and abamectin for the treatment of a parasitic infestation in mammals.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: May 14, 2013
    Assignee: AH USA 42 LLC
    Inventors: Timothy G. Geary, Peter Rolfe
  • Bicyclic derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics
    Patent number: 8440634
    Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, and n are as defined in the disclosure, and addition salts solvates and hydrates thereof. The disclosure also relates to the preparation method of said compounds and to the use of the same in therapeutics.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: May 14, 2013
    Assignee: Sanofi
    Inventors: Alain Dlubala, Claire Trecant, Isabelle Ripoche
  • Oligonucleotide conjugates
    Patent number: 8440635
    Abstract: Oligonucleotide conjugates, where an oligonucleotide is covalently attached to an aromatic system, are provided. In particular embodiments the oligonucleotide is complementary to the RNA component of human telomerase and is covalently attached to a nucleobase via an optional linker. The conjugates inhibit telomerase enzyme activity.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: May 14, 2013
    Assignee: Geron Corporation
    Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Richard L. Tolman, Gregg B. Morin
  • Micro-RNA family that modulates fibrosis and uses thereof
    Patent number: 8440636
    Abstract: The present invention relates to the identification of a microRNA family, designated miR-29a-c, that is a key regulator of fibrosis in cardiac tissue. The inventors show that members of the miR-29 family are down-regulated in the heart tissue in response to stress, and are up-regulated in heart tissue of mice that are resistant to both stress and fibrosis. Also provided are methods of modulating expression and activity of the miR-29 family of miRNAs as a treatment for fibrotic disease, including cardiac hypertrophy, skeletal muscle fibrosis other fibrosis related diseases and collagen loss-related disease.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: May 14, 2013
    Assignee: The Board of Regents, The University of Texas System
    Inventors: Eric Olson, Eva van Rooij
  • Combination treatment for the treatment of hepatitis C virus infection
    Patent number: 8440637
    Abstract: The present invention relate to the use of a combination of an inhibitor of miR-122 and an inhibitor of VLDL assembly, for the treatment of HCV, hyperlipidemia and hypercholesterolemia.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: May 14, 2013
    Assignee: Santaris Pharma A/S
    Inventor: Joacim Elmén
  • Compositions and methods for modulating calcium flux, glucose homeostasis and apoptosis
    Patent number: 8440638
    Abstract: Compositions and methods are disclosed which are effective for modulating glucose homeostasis, calcium ion flux and cell death in target cells.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: May 14, 2013
    Assignees: Wisconsin Alumni Research Foundation, University of Washington
    Inventors: John M. Denu, Andrew M. Scharenberg
  • Combination compositions for reducing intraocular pressure
    Patent number: 8440639
    Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of dorzolamide marketed under the brand Trusopt™ and Compound A.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: May 14, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Methods and compositions for treating obesity and related disorders
    Patent number: 8440640
    Abstract: The invention provides methods for, and compositions effective for, treating obesity, inhibiting weight gain, treating diabetes mellitus, inhibiting atherosclerosis and treating related disorders and conditions comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to a patient. The compound capable of inhibiting AC5 may be administered singly or in combination with another agent. In some embodiments, the AC5 inhibiting compound is 9-?-D-arabinofuranosyladenine (AraAde). The compounds may be administered in an amount of about 1 to about 200 mg/kg/day, about 1 to about 100 mg/kg/day, about 10 to about 80 mg/kg/day, about 12 to about 40 mg/kg/day or about 15 to about 25 mg/kg/day. In some embodiments, the compound is administered orally.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: May 14, 2013
    Assignee: University of Medicine and Dentistry of New Jersey
    Inventor: Stephen F. Vatner
  • Phthalocyanine salt formulations
    Patent number: 8440641
    Abstract: Pharmaceutical compositions of phthalocyanine compounds with a structure according to Formula (I) are described. Phthalocyanines are photosensitizer compounds having a phthalocyanine ring system that can be used for photodynamic therapy. Different phthalocyanines and phthalocyanine salts are shown to have useful characteristics such as water solubility, oil solubility, or tunable photostability. Formulations of phthalocyanines and phthalocyanine salts that can be used for topical and systemic administration are described.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: May 14, 2013
    Assignee: Case Western Reserve University
    Inventors: Ming Guo, Yun Liu, Malcolm E. Kenney
  • Boron-containing small molecules
    Patent number: 8440642
    Abstract: This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: May 14, 2013
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. Baker, Tsutomu Akama, Carolyn Bellinger-Kawahara, Vincent S. Hernandez, Karin M. Hold, James J. Leyden, Kirk Maples, Jacob J. Plattner, Virginia Sanders, Yong-Kang Zhang
  • Inhibitors of beta-lactamase
    Patent number: 8440643
    Abstract: This invention provides novel ?-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ?-lactamases and synergize the antibacterial effects of ?-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ?-lactam antibiotics as a result of the presence of the ?-lactamases.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: May 14, 2013
    Assignee: MethylGene Inc.
    Inventors: Frank Dininno, Milton L. Hammond, Kevin Dykstra, Seongkon Kim, Qiang Tan, Katherine Young, Jeffrey Donald Hermes, Helen Chen, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Arkadii Vaisburg, Jubrail Rahil, Nafsika Georgopapadakou, Nancy Z. Zhou
  • Compounds as receptor modulators with therapeutic utility
    Patent number: 8440644
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: May 14, 2013
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Todd M. Heidelbaugh
  • Ceramide production promoter
    Patent number: 8440645
    Abstract: Provided are a drug, a cosmetic, etc. for promoting production of ceramide. Provided is a ceramide production promoter including a compound represented by the formula (1) or salts thereof as an active ingredient (in the formula, R1 represents a phosphono group or a hydrogen atom, R2 represents an alkyl group having 8 to 24 carbon atoms or an acyl group having 8 to 24 carbon atoms, and R3 represents an alkyl group having 1 to 24 carbon atoms when R1 represents a phosphono group or represents a phosphono group when R1 represents a hydrogen atom, or a salt thereof as an active ingredient.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: May 14, 2013
    Assignee: Kao Corporation
    Inventors: Yoshiya Sugai, Hiroshi Hashimoto, Shinya Amano, Shotaro Ito, Yoshie Shimotoyodome, Yoriko Nakagiri
  • Substituted tetracycline compounds for treatment of infections
    Patent number: 8440646
    Abstract: Methods and compositions for the treatment of Bacillus anthracis infections are described.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 14, 2013
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Michael N. Alekshun, S. Ken Tanaka
  • 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin Dand their uses
    Patent number: 8440647
    Abstract: This invention discloses 2?-methyl and 2?-methyl analogs of 19,26,27-trinor-(20S)-1?-hydroxyvitamin D3 and pharmaceutical uses therefor. These compounds exhibit 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. These compounds also have little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. These compounds may also be used for the treatment or prevention of obesity.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: May 14, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Pawel K. Grzywacz, Margaret Clagett-Dame
  • Methods and compositions for treatment of intraepithelial neoplasia
    Patent number: 8440648
    Abstract: The present invention provides for compositions, kits and methods for treatment of intraepithelial neoplasia, where the compositions include catecholic butanes, which include NDGA derivatives.
    Type: Grant
    Filed: July 19, 2005
    Date of Patent: May 14, 2013
    Assignees: Erimos Pharmaceuticals LLC, University of Maryland, Baltimore, Johns Hopkins University
    Inventors: Neil Frazer, Jonathan Heller, Rocio Lopez, Melissa Rhodes, Ru Chih C. Huang, Richard Dalby, Niharika Khanna
  • Phenanthroindolizidine analogues
    Patent number: 8440649
    Abstract: Treatment of coronavirus infection with phenanthroindolizidine analogues.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: May 14, 2013
    Assignee: National Health Research Institutes
    Inventors: Shiow-Ju Lee, Cheng-Wei Yang, Yue-Zhi Lee
  • Pyrido[3,2-d]pyrimidine PI3K delta inhibitor compounds and methods of use
    Patent number: 8440651
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 14, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
  • MST1 kinase inhibitors and methods of their use
    Patent number: 8440652
    Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: May 14, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
  • 3-substituted-1,4-diazepan-2-one melanocortin-5 receptor antagonists
    Patent number: 8440653
    Abstract: The present invention provides compounds of Formula (I) that are useful for modulating the biological activity of the melanocortin-5 receptor (MC5R). Compounds of this invention can be used to treat diseases and/or conditions in which downregulation of MC5R is beneficial. Such diseases and/or conditions include, but are not limited to, acne, seborrhea, seborrheic dermatitis, cancer, and inflammatory diseases.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 14, 2013
    Assignee: Mimetica Pty Ltd
    Inventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
  • Thieno- and furo-pyrimidine modulators of the histamine H4 receptor
    Patent number: 8440654
    Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: May 14, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
  • Combination therapy for the treatment of diabetes
    Patent number: 8440655
    Abstract: The present invention provides methods of treating, reducing, preventing, or inhibiting symptoms of diabetes and/or lowering plasma levels of HbA1c by co-administration of therapeutic or subtherapeutic doses of telenzepine and sertraline to a subject in need thereof.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: May 14, 2013
    Assignee: Theracos, Inc.
    Inventors: Brian Seed, Jordan Mechanic
  • Methods of treating pulmonary diseases and disorders by modulating calcium/calmodulin dependent protein kinase II activity
    Patent number: 8440656
    Abstract: Disclosed are methods of treating or preventing a pulmonary disease or disorder in a subject, the methods comprising administering an effective amount of an compound that inhibits Calmodulin Kinase II (CaMKII) activity, either directly or indirectly, thereby treating or preventing the pulmonary disease or disorder in the subject.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: May 14, 2013
    Assignee: University of Iowa Research Foundation
    Inventors: Mark E. Anderson, Isabella M. Grumbach, Joel N. Kline
  • Substituted piperidines
    Patent number: 8440657
    Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular diseases and tumour diseases.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 14, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
  • Cyclic urea inhibitors of 11?-hydroxysteroid dehydrogenase 1
    Patent number: 8440658
    Abstract: Disclosed is a compound represented by Formula (I): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (I) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (I) are defined herein.
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: May 14, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Yuanjie Ye, Wei He, Suresh B. Singh, Zhenrong Xu, Salvacion Cacatian, Wei Zhao
  • Termite-proofing agent and its application method
    Patent number: 8440659
    Abstract: The present invention is a composition comprising a neonicotinoid-based compound having a high degree of insecticide activity, an organic solvent and a surfactant. The present invention is also a method that allows the obtaining of lumber that does not require termite-proofing treatment following production of lumber by injecting this composition into a tree trunk and allowing the chemical to circulate and disperse within the tree trunk.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: May 14, 2013
    Assignee: LANXESS Deutschland GmbH
    Inventors: Kunitoshi Watanabe, Toshio Suzuki, Suguru Shinya
  • Method for treating a disease related to the glucocorticoid receptor
    Patent number: 8440660
    Abstract: A method for treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-hydroquinoline compound.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: May 14, 2013
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Mamoru Matsuda, Masato Nagatsuka, Toshiyuki Mori, Sachiko Kobayashi, Masatomo Kato, Miwa Takai
  • Methods of modulating inflammatory cell recruitment and gene expression using haloaryl substituted aminopurines
    Patent number: 8440661
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: May 13, 2010
    Date of Patent: May 14, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Kate Northcote, Brian Edwin Cathers
  • Substituted quinazoline and pyrido-pyrimidine derivatives
    Patent number: 8440662
    Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: May 14, 2013
    Assignee: Endo Pharmaceuticals, Inc.
    Inventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
  • 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as JAK-2 modulators and methods of use
    Patent number: 8440663
    Abstract: This invention relates to certain pyrimidine derivative inhibitors of JAK-2, having Formula (I): wherein D, E, L, Z, R1, R2, R25, and n1 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: January 30, 2007
    Date of Patent: May 14, 2013
    Assignee: Exelixis, Inc.
    Inventors: Grace Mann, Naing Aay, Arlyn Arcalas, S. David Brown, Wai Ki Vicky Chan, Jeff Chen, Hongwang Du, Sergey Epshteyn, Timothy Patrick Forsyth, Adam A. Galan, Tai Phat Huynh, Mohamed Abdulkader Ibrahim, Henry William Beecroft Johnson, Brian Kane, Patrick Kearney, Byung Gyu Kim, Elena S. Koltun, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Lisa E. Meyr, Robin Tammie Noguchi, Michael Pack, Brian Hugh Ridgway, Xian Shi, John Woolfrey, Peiwen Zhou
  • Heteroaryls and uses thereof
    Patent number: 8440664
    Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: May 14, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: David P. Cardin, Jeffrey Gaulin, Paul Greenspan, Christelle C. Renou, Stepan Vyskocil, Tianlin Xu
  • Apoptosis signal-regulating kinase inhibitors
    Patent number: 8440665
    Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: May 14, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Gregory Notte, Jeff Zablocki
  • Pyridazinone compounds and P2X7 receptor inhibitors
    Patent number: 8440666
    Abstract: Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: May 14, 2013
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Yutaka Hirokawa, Hiroshi Nagai, Kei Nagae, Tsuneo Watanabe, Megumi Io, Yusuke Shintani, Junji Kamon, Masato Horikawa, Kazuya Takeuchi
  • Imidazopyrazine Syk inhibitors
    Patent number: 8440667
    Abstract: Certain imidazopyrazines of Formula (I): and pharmaceutical compositions thereof are provided herein. Methods of treating patients responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity of Formula (I) effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 14, 2013
    Assignee: Gilead Connecticut, Inc.
    Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
  • Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment of type 2 diabetes
    Patent number: 8440668
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: May 14, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Scott D. Edmondson, Michael Fisher, Dooseop Kim, Malcolm MacCoss, Emma R. Parmee, Ann E. Weber, Jinyou Xu
  • Pharmaceutical composition for prevention and treatment of diabetes or obesity comprising a compound that inhibits activity of dipeptidyl peptidase-IV, and other antidiabetic or antiobesity agents as active ingredients
    Patent number: 8440669
    Abstract: The present invention relates to a pharmaceutical composition for the prevention and treatment of diabetes or obesity comprising as active ingredients a compound which inhibits the activity of dipeptidyl peptidase-IV (DPP-IV), a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof, and one or more other antidiabetic or antiobesity agents. The pharmaceutical composition exhibits excellent glucose tolerance and may be useful in the prevention and treatment of diabetes, obesity, and the like by effectively inhibiting blood glucose levels and reducing fat mass.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: May 14, 2013
    Assignee: Dong-A Pharmaceutical Co. Ltd.
    Inventors: Chang Yell Shin, Song-Hyen Choi, Yu Na Chae, Eun Kyoung Yang, Gook Jun Ahn, Moon-Ho Son, Heung Jae Kim, Woo Young Kwak, Jong Pil Min, Tae Hyun Yoon, Soon Hoe Kim, Moohi Yoo