Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai Patents (Class 514/183)
  • Patent number: 8557798
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
  • Patent number: 8551979
    Abstract: The present invention relates to nonaqueous preparation for percutaneous absorption prepared by laminating an adhesive layer comprising a nonsteroidal anti-inflammatory analgesic in an alkali metal salt form, and an inorganic acid which is strongly acidic compared with the nonsteroidal anti-inflammatory analgesic in a free form, together with a nonaqueous base, on a support. According to the present invention, drug-releasing characteristics and skin penetration in a nonaqueous preparation for percutaneous absorption can be improved because the addition of an inorganic acid in a nonaqueous base containing a drug in an alkali metal salt form leads to an improvement in the solubility of the drug in the base, and a good partitioning of the drug to skin surface. In addition, as the inorganic acid has no alcoholic hydroxy group in the structure, the inorganic acid does not react with the drug, therefore it causes no lowering in the stability of the drug by esterification.
    Type: Grant
    Filed: November 5, 2004
    Date of Patent: October 8, 2013
    Assignee: Lead Chemical Co., Ltd.
    Inventors: Seijirou Yama, Naoki Murai
  • Patent number: 8551983
    Abstract: Nicotine receptor agonists or analogs or derivatives thereof for treating inflammatory pulmonary diseases, and pharmaceutical compositions including nicotine receptor agonists or analogs or derivatives thereof. Compounds of formula wherein R1, R2, Xa and Ya are as defined herein are also provided.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: October 8, 2013
    Assignee: Universite Laval
    Inventors: Yvon Cormier, Evelyne Israel-Assayag, Marie-Renee Blanchet, Rene C. Gaudreault, Philippe Labrie
  • Patent number: 8551980
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: October 8, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Benjamin Bader, Philip Lienau, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner
  • Patent number: 8551972
    Abstract: The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A2A adenosine receptors (ARs).
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: October 8, 2013
    Assignee: Adenosine Therapeutics, LLC
    Inventors: Onno Kranenburg, Jarmila van der Bilt, Inne Borel Rinkes, Jayson M. Rieger
  • Patent number: 8552005
    Abstract: The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation. In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: October 8, 2013
    Assignee: Avincuro Pharmaceuticals, Inc.
    Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Nikolay Filippovich Savchuk
  • Publication number: 20130261099
    Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.
    Type: Application
    Filed: May 24, 2013
    Publication date: October 3, 2013
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventor: Bruce BRANCHAUD
  • Patent number: 8546370
    Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS, or combinations thereof.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: October 1, 2013
    Assignee: IRM LLC
    Inventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
  • Patent number: 8546368
    Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: October 1, 2013
    Assignee: AbbVie Inc.
    Inventors: Thomas D. Penning, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda
  • Patent number: 8546369
    Abstract: The present invention relates to stable salts of creatine imino sugar amides and an inorganic or organic acid endowed with enhanced nutritional and/or therapeutical efficacy in respect to their individual effects and to solid compositions containing such salts, particularly suited to oral and parenteral administration. Methods of preparation and use of these compositions are also provided.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: October 1, 2013
    Assignee: Northern Innovations Holding Corp.
    Inventors: Marvin Heuer, Michele Molino, Joseph MacDougall
  • Patent number: 8546372
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: October 1, 2013
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventors: Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
  • Patent number: 8546430
    Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: October 1, 2013
    Assignee: P2D, Inc.
    Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
  • Patent number: 8546305
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: October 1, 2013
    Assignee: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8546371
    Abstract: A composition for stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells includes a glycolipid antigen and a nanoparticle conjugated with the glycolipid antigen. The glycolipid antigen and the nanoparticle are not antigenic in mouse and human being. The composition can further include covalent or non-covalent connection between the glycolipid antigen and the nanoparticle. The glycolipid antigen is alpha-galactosylceramide or an analog of that. The nanoparticle can be a polymer. A production method of the composition includes preparing a nanoparticle and a glycolipid antigen and loading the glycolipid antigen to the nanoparticle. The glycolipid antigen can be coated onto the surface of the nanoparticle or encapsulated within the nanoparticle. A method of stimulating NKT cells to produce anti-cancer and anti-viral cytokines without causing anergy of NKT cells is also provided.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: October 1, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Dapeng Zhou, Chun Li
  • Publication number: 20130252932
    Abstract: Pharmaceutical preparations, compositions, systems, and devices including medical devices and diagnostic or therapeutic agents, and methods to treat disease by modification of local tissue environment to modulate the therapeutic index of locally or systemically delivered therapeutic or diagnostic agents. Improved ability to reduce sympathetic nerve activity in the adventitia and perivascular tissues around arteries and veins in the body. Modulation of the local tissue environment around an artery to enable more effective denervation with or without a therapeutic agent. Modulation may include adjustment of the pH of the tissue.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 26, 2013
    Applicant: MERCATOR MEDSYSTEMS, INC.
    Inventor: Kirk P. SEWARD
  • Patent number: 8541466
    Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: September 24, 2013
    Assignee: Duke University
    Inventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
  • Patent number: 8541401
    Abstract: Compositions are provided which contain immobilized flavorants for flavor delivery. In particular, smoking compositions are provided which contain flavorant ester salts of polycarboxylic acids.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: September 24, 2013
    Assignee: Philip Morris USA Inc.
    Inventors: Munmaya K. Mishra, Shengsheng Liu, Diane S. Kellogg
  • Publication number: 20130244992
    Abstract: Disclosed herein are compounds useful in inhibiting the action of AB-type bacterial toxins such as cholera, traveler's diarrhea, enterohemorrhagic diarrhea caused by E. coli O157:H7 and pertussis or whooping cough. Also included in the invention is the use of these compounds in treatment of diseases associated with those toxins.
    Type: Application
    Filed: January 3, 2013
    Publication date: September 19, 2013
    Applicant: Univerity of Central Florida Research Foundation, Inc.
    Inventors: Kenneth Robert Teter, Michael Prentice Taylor
  • Publication number: 20130243698
    Abstract: The present invention provides a variety of radicals, which are useful as polarizing compounds. Exemplary radicals are represented by compounds of Structural Formulae (I), (II), (III) and (IV) as described herein.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 19, 2013
    Applicant: Massachusetts Institute of Technology
    Inventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
  • Patent number: 8536133
    Abstract: This invention provides polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each binds different regions on the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: September 17, 2013
    Assignees: Lawrence Livermore National Security, LLC., The Regents of the University of California
    Inventors: Sally DeNardo, Gerald DeNardo, Rodney Balhorn
  • Patent number: 8536161
    Abstract: Combinations of PI3K inhibitor compounds having Formula I and chemotherapeutic agents, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for treating hematopoietic malignancies. Methods of using such combinations 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: March 11, 2010
    Date of Patent: September 17, 2013
    Assignee: Genentech, Inc.
    Inventors: Allen J. Ebens, Jr., Lori Friedman
  • Patent number: 8536163
    Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.
    Type: Grant
    Filed: February 18, 2013
    Date of Patent: September 17, 2013
    Assignee: LEO Laboratories Limited
    Inventors: Marc Barry Brown, Michael Crothers, Tahir Nazir
  • Patent number: 8536162
    Abstract: Conjugates of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes with a variety of conjugating members are used in the formation of dinuclear metal complexes which bind to phosphate esters. By virtue of their conjugated forms, the complexes are incorporated into chromatographic media, affinity binding reagents, and dyes, which make the complexes useful in a wide range of assays, separations, and purifications. In addition, dinuclear metal complexes of 1,3-bis(1,4,7-triazacyclonon-1-yl)-2-hydroxypropanes that are not so conjugated are used in the detection of phosphate esters of biological species by either MALDI-TOF mass spectrometry or by dye displacement.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: September 17, 2013
    Assignee: Bio-Rad Laboratories, Inc.
    Inventors: Thomas R. Berkelman, Lisandra Martin, Rhiannon Jones, John Walker, II
  • Patent number: 8529928
    Abstract: Biodegradable polymers incorporating biomolecules and methods of their use are provided. Certain aspects provide biomolecules crosslinked with diglycidyl esters. The disclosed compositions have numerous applications including cellular regeneration, wound healing, and cellular differentiation.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: September 10, 2013
    Assignee: Georgia Tech Research Corporation
    Inventors: Yadong Wang, Blaine Zern, Christiane Gumera
  • Patent number: 8530456
    Abstract: The present invention relates to macrocyclic small molecule inhibitors of the Sonic Hedgehog signaling pathway, syntheses thereof, and intermediates thereto. Such small molecule modulators of the Sonic Hedgehog signaling pathway are useful in the treatment of proliferative diseases (e.g., basal cell carcinoma, Gorlin syndrome, medulloblastoma, or pancreatic cancer), pulmonary diseases (e.g., interstitial pnuemonitis or interstitial pulmonary fibrosis), and developmental disorders (e.g., phocomelia or cyclopia). Novel non-natural macrocycles are provided that inhibit Sonic Hedgehog induced-protein transcription.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: September 10, 2013
    Assignees: President and Fellows of Harvard College, Massachusetts Institute of Technology, The General Hospital Corporation
    Inventors: Lee F. Peng, Julia Lamenzo, Nicole Maloof, Kazuo Nakai, Benjamin Stanton, Sara Jean Buhrlage, Lawrence MacPherson, Michel Weiwer, Stuart L. Schreiber
  • Patent number: 8530457
    Abstract: Treatment of lymphangioleiomyomatosis with the MEK1/2 inhibitor CI-1040 delayed the development of primary tumors and blocked the estrogen-induced lung metastases in treated animals. Such treatment also reduced the number of circulating ELT3 cells and decreased their lung colonization after intravenous injection.
    Type: Grant
    Filed: May 20, 2009
    Date of Patent: September 10, 2013
    Assignee: Fox Chase Cancer Center
    Inventors: Elizabeth Petri Henske, Jane Yu
  • Patent number: 8529917
    Abstract: The invention provides active agents, such as paclitaxel, rapamycin, or 17-DMAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) (“PEG-b-PLA”) micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-DMAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailability without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: September 10, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Glen S. Kwon
  • Patent number: 8524214
    Abstract: Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: September 3, 2013
    Assignee: Mersana Therapeutics, Inc.
    Inventors: Aleksandr Yurkovetskiy, Mao Yin, Gui Liu, Laura C. Akullian, John J. Kane, Cheri A. Stevenson, Charles E. Hammond, Russell C. Petter, John H. Van Duzer, Timothy B. Lowinger
  • Patent number: 8524696
    Abstract: Water-soluble compositions comprising a lipophilic compound and a solubilizing agent of the general formula: {X—OOC—[(CH2)n—COO]m}p—Y??(I) wherein: X is a residue of a hydrophobic moiety, Y is a residue of a hydrophilic moiety, p is 1 or 2, m is 0 or 1, and n is an integer greater than or equal to 0 are disclosed. The lipophilic compound is preferably selected from the group consisting of water-insoluble ubiquinones, ubiquinols, vitamins, provitamins, polyene macrolide antibiotics, and mixtures thereof. The hydrophobic moiety is preferably a sterol or a tocopherol and the hydrophilic moiety is preferably a polyalkylene glycol. In some embodiments, the sterol is cholesterol or sitosterol, the tocopherol is ?-(+)-tocopherol, the polyalkylene glycol is a polyethylene glycol or its methyl monoether having an average molecular weight between 400 and 1000, p is equal to 1 or 2, m is equal to 0 or 1 and n is an integer between 2 and 18.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: September 3, 2013
    Assignee: National Research Council of Canada
    Inventors: Henryk Borowy-Borowski, Marianna Sikorska-Walker, P. Roy Walker
  • Patent number: 8524695
    Abstract: Modified release pharmaceutical compositions (controlled release, sustained release, and/or extended release) of the R-(+) enantiomer of pramipexole (RPPX) and methods of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: September 3, 2013
    Assignee: Knopp Neurosciences, Inc.
    Inventors: Michael E. Bozik, Thomas Petzinger, Jr., Valentin Gribkoff
  • Patent number: 8524698
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: September 3, 2013
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventors: Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
  • Patent number: 8524697
    Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: September 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John C. Anthes, Kevin D. McCormick, John A. Hey, Robert G. Aslanian, Purakkattle J. Biju, Michael Y. Berlin, Hongwu Yang, Yeon-Hee Lim, Yoon Joo Lee, Rema Danielle Bitar, Phillippa H. Solomon
  • Patent number: 8518927
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Grant
    Filed: February 10, 2010
    Date of Patent: August 27, 2013
    Assignee: The Scripps Research Institute
    Inventor: Carlos F. Barbas, III
  • Patent number: 8518928
    Abstract: The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and - - - have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: August 27, 2013
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
  • Patent number: 8518926
    Abstract: Pharmaceutical compositions of (R)-pramipexole and methods and kits of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: August 27, 2013
    Assignee: Knopp Neurosciences, Inc.
    Inventors: Michael E. Bozik, Thomas Petzinger, Jr., Valentin Gribkoff
  • Patent number: 8518925
    Abstract: The present invention relates to an opioid controlled release oral dosage form comprising at least one opioid for the manufacture of a medicament to treat patients with Chronic Obstructive Pulmonary Disease (COPD).
    Type: Grant
    Filed: June 8, 2005
    Date of Patent: August 27, 2013
    Assignee: Euro-Celtique S.A.
    Inventors: Wolfgang Fleischer, Karen Reimer, Petra Leyendecker
  • Patent number: 8518929
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of blood lipid therapy comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Grant
    Filed: February 25, 2013
    Date of Patent: August 27, 2013
    Assignee: Amarin Pharmaceuticals Ireland Limited
    Inventors: Mehar Manku, Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni
  • Patent number: 8518930
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: August 27, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Marina Ciomei, Aurelio Marsiglio, Valter Domenico Croci, Enrico Pesenti
  • Patent number: 8518371
    Abstract: The invention features a class of 2-nitroimidazole compounds with a secondary basic nitrogen atom and a linker bearing one or more therapeutic agents, cytotoxic agents, detectable labels, or chelating groups. In particular, the invention provides 2-nitroimidazole compounds containing a cluster of boron atoms for use in boron neutron capture therapy (BNCT). The 2-nitroimidazole compounds can be used to treat hypoxic conditions, including, e.g., cancer, inflammation, and ischemia. The weakly basic 2-nitroimidazole compounds target to hypoxic tissue and provide increased tissue concentration overall.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: August 27, 2013
    Assignee: Natural Pharmacia International, Inc.
    Inventors: David Y-W Lee, Xiao-Shen Ji, James A. Raleigh
  • Publication number: 20130216531
    Abstract: Inhibition of CXCR4 can inhibit tumor growth and metastasis during certain therapeutic windows. Disclosed are novel methods for treating and preventing cancer in a subject related to administration of CXCR4 inhibitors during a therapeutic window following treatment with another anti-tumor therapy.
    Type: Application
    Filed: June 28, 2011
    Publication date: August 22, 2013
    Inventors: Rakesh K. Jain, Dan G. Duda, Sergey V. Kozin, Dai Fukumura
  • Patent number: 8513433
    Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
  • Patent number: 8513188
    Abstract: This invention relates to the use of a cyclic compound of formula (I) wherein A, B independently in each occurrence is alkane-i,j-diyl having k carbon atoms, i and independently j being less than or equal k and k being selected from 1 to 10, wherein said alkane-i,j-diyl (i) may comprise one or more double bonds; (ii) is optionally substituted; and/or (iii) comprises a cycle, wherein the total number of cycles being cyclic sugars in said compound is selected from 0 to 4 and is less than p·(n+m); X,Y independently in each occurrence is a biocompatible functional group comprising at least one oxygen atom or two sulphur atoms; n, m independently of each other are selected from 0 to 20; p is selected from 1 to 10; n+m is equal or greater than 1; and p·(n+m) is selected from 3 to 30; wherein said compound is capable of forming a complex with a protonated primary and/or protonated secondary amino group and/or a protonated guanidinium group for the manufacture of a pharmaceutical or diagnostic composition.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: August 20, 2013
    Inventor: Paolo Botti
  • Patent number: 8513300
    Abstract: An oral dosage form comprises cromolyn sodium (sodium or disodium cromoglycate), and an acylated amino acid delivery agent.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: August 20, 2013
    Assignee: Emisphere Technologies, Inc.
    Inventors: Richat Abbas, Ehud Arbit, Michael Goldberg, Vivien Wong, Donald J. Sarubbi
  • Patent number: 8513161
    Abstract: Treatment with N-(2-phenylethyl)succinamic acid or its salts protects against inhibition of growth by a neonicotinoid compound applied as a seed treatment or applied directly on or near the root zone of the seedling.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: August 20, 2013
    Assignees: Valent Biosciences Corporation, Valent U.S.A. Corporation
    Inventors: Franklin Paul Silverman, Dale O. Wilson, Jr., Jennifer C. Kochan, Nicole Higgs, Peter D. Petracek, Prem Warrior, Karen S. Arthur
  • Publication number: 20130210771
    Abstract: This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.
    Type: Application
    Filed: February 13, 2013
    Publication date: August 15, 2013
    Applicant: IRM LLC
    Inventor: Novartis AG
  • Patent number: 8507468
    Abstract: Contemplated pharmaceutical compositions comprise a benzodiazepine anti-convulsive compound for intranasal administration in a single phase, multi-component solvent system with water content of at least 15 vol % and a benzodiazepine concentration of at least 30 mg/ml. It is noted that contrary to common expectation, the concentration of the anti-convulsive compound was increased by increasing water content in the multi-component solvent. Moreover, the anti-convulsive compound remained chemically stable and substantially completely dissolved over large periods of time. Thus, stable and highly concentrated spray formulations for intranasal administration could be prepared having sufficiently high concentrations of the anti-convulsive compounds that now allow single spray administration to achieve clinically relevant dosages.
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: August 13, 2013
    Inventor: Robert Orr
  • Patent number: 8506993
    Abstract: According to some embodiments, the present invention provides compositions and methods for making and using multifunctional polymerized liposomes finding relevant application in medical sciences, particularly in bioimaging, diagnostics, drug delivery, and drug formulation. The compositions and methods involve lipids that are both polymerizable and have a “clickable” group that provides the ability to functionalize via a click reaction with various functional moieties useful for the above-listed applications.
    Type: Grant
    Filed: August 14, 2008
    Date of Patent: August 13, 2013
    Assignee: University of Houston
    Inventors: Chengzhi Cai, Guoting Qin, Amit Kumar
  • Patent number: 8507509
    Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: August 13, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Fiona Murphy Kessabi, Hans-Georg Brunner, Renaud Beaudegnies, Laura Quaranta, Fredrik Cederbaum, Jayant Umarye
  • Publication number: 20130203738
    Abstract: The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g.
    Type: Application
    Filed: February 9, 2011
    Publication date: August 8, 2013
    Applicants: NAGOYA CITY UNIVERSITY, NAGASAKI UNIVERSITY
    Inventors: Yoshifumi Nishimura, Aritaka Nagadoi, Yuuka Hirao, Yoshio Goshima, Naoya Yamashita, Naoki Miyata, Takayoshi Suzuki, Ryuta Hiraishi, Hiroshi Ueda
  • Publication number: 20130203724
    Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 8, 2013
    Applicant: Infinity Discovery, Inc.
    Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright