Patents Examined by Elli Peselev
  • 10a-Azalide compound
    Patent number: 8097708
    Abstract: [Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against Hemophilus influenzae, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: January 17, 2012
    Assignees: Taisho Pharmaceutical Co., Ltd., Meiji Seika Kaisha, Ltd.
    Inventors: Tomohiro Sugimoto, Kanako Yamamoto, Akira Manaka, Haruhisa Ogita, Jun Kurosaka, Madoka Kawamura, Masato Kashimura, Naoki Sasamoto, Tomoaki Miura, Kenichi Kanemoto, Tomohiro Ozawa, Ken Chikauchi, Eiki Shitara, Dai Kubota
  • Lipid A and other carbohydrate ligand analogs
    Patent number: 8097593
    Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: January 17, 2012
    Assignee: Oncothyreon Inc.
    Inventors: Zi-Hua Jiang, R. Rao Koganty, Wladyslaw Budzynski
  • Macrolides and ketolides having antimicrobial activity
    Patent number: 8097594
    Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: January 17, 2012
    Assignee: Wockhardt Ltd.
    Inventors: Milind Dattatraya Sindkhedkar, Vijaya Narayan Desai, Rajesh Maganlal Loriya, Mahesh Vithalbhai Patel, Bharat Kalidas Trivedi, Rajesh Onkardas Bora, Santosh Devidas Diwakar, Ganesh Rajaram Jadhav, Shivaji Sampatrao Pawar
  • Cocrystal of C-glycoside derivative and L-proline
    Patent number: 8097592
    Abstract: A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: January 17, 2012
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co. Ltd.
    Inventors: Masakazu Imamura, Keita Nakanishi, Ryota Shiraki, Kenichi Onda, Daisuke Sasuga, Masamichi Yuda
  • Compositions and processes for preparing 13-deoxy-anthracyclines
    Patent number: 8097707
    Abstract: 13-benzenesulfonylhydrazone anthracyclines useful in producing improved yields in the synthesis 13-deoxyanthracyclines, and an improved method of reducing 13-benzene-sulfonylhydrazone anthracyclines to 13-deoxyanthracyclines wherein the reduction reaction is maintained at temperatures of about 55° C. to 64° C. without stirring or agitation. The reaction is completed with the addition of aqueous bicarbonate which forms the 13-deoxyanthracycline and precipitates. The precipitates are filtered and the precipitate and filtrate are extracted separately with organic solvents. The crude 13-deoxy anthracycline can be converted to 5-imino-13-deoxy anthracycline by reaction with methanolic ammonia. The reaction can also be performed with an acidic pyridinium salt instead of a strong acid so that neutralization of the reaction or extraction of the product is not necessary, thereby facilitating purification.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: January 17, 2012
    Assignee: Gem Pharmaceuticals, LLC
    Inventors: Gerald M. Walsh, Richard D. Olson
  • Topical application of ivermectin for the treatment of dermatological conditions/afflictions
    Patent number: 8093219
    Abstract: Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: January 10, 2012
    Assignee: Galderma S.A.
    Inventors: Vincent Manetta, Gary R. Watkins
  • Forms of CDDO methyl ester
    Patent number: 8088824
    Abstract: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.
    Type: Grant
    Filed: August 13, 2008
    Date of Patent: January 3, 2012
    Assignee: Reata Pharmaceuticals Inc.
    Inventors: John Walling, Stephan D. Parent, David T. Jonaitis, Robert M. Kral, Jr.
  • Cystitis treatment with high dose chondroitin sulfate
    Patent number: 8084441
    Abstract: Interstitial cystitis and related GAG-deficient conditions of the bladder and urinary tract are treated by instillation of high dose chondroitin sulfate, such as 400 mg/20 mL. The higher dose of chondroitin is effective for the rapid reduction of symptoms, particularly in patients with severe and otherwise recalcitrant cystitis.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: December 27, 2011
    Assignee: Stellar Pharmaceuticals, Inc.
    Inventors: Peter R. Riehl, Sungtack Samuel Hahn
  • Topical application of ivermectin for the treatment of dermatological conditions/afflictions
    Patent number: 8080530
    Abstract: Dermatological conditions/afflictions such as rosacea, common acne, seborrheic dermatitis, perioral dermatitis, acneform rashes, transient acantholytic dermatosis, and acne necrotica miliaris, most notably rosacea, are treated by topically applying onto the affected skin area of an individual in need of such treatment, a topical pharmaceutical composition which comprises a thus effective amount of ivermectin.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: December 20, 2011
    Assignee: Galderma S.A.
    Inventors: Vincent Manetta, Gary R. Watkins
  • Compositions and methods for treatment of cachexia
    Patent number: 8080528
    Abstract: Compositions and methods for preventing and treating wasting disorders, such as cachexia and anorexia, are provided. In one aspect, the present invention provides a method for preventing and treating a wasting disorder in a mammal. In one embodiment, the method of the invention comprises administering to such mammal a macrolide and a ?2-adrenergic agonist in combination such that the macrolide and said ?2-agonist are administered in amounts effective to prevent or at least alleviate said wasting disorder.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: December 20, 2011
    Assignee: The Releef Initiative
    Inventors: Richard Kenley, Jonas Ekblom, Mikhail Denissenko
  • Macrolides with anti-inflammatory activity
    Patent number: 8080529
    Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: December 20, 2011
    Assignee: Glaxo Group Limited
    Inventors: Sulejman Alihodzic, Martina Bosnar, Ognjen Culic, Vesna Erakovic Haber, Antun Hutinec, Dubravko Jelic, Goran Kragol, Nikola Marjanovic, Zorica Marusic-Istuk, Marija Ribic, Vanja Vela
  • Steroid compounds and formulations
    Patent number: 8076316
    Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: December 13, 2011
    Assignee: Harbor BioSciences, Inc.
    Inventor: James M. Frincke
  • 10-substituted macrolide antibiotics
    Patent number: 8076301
    Abstract: Disclosed herein are 10-desmethyl, 10 substituted-macrolides, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. The 10-desmethyl macrolides are particularly useful as antibiotics.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: December 13, 2011
    Assignee: C10 Pharma AS
    Inventors: Kjell Undheim, Solvi Gunnes
  • Guanidinium derivatives for improved cellular transport
    Patent number: 8071535
    Abstract: Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: December 6, 2011
    Assignee: The Regents of the University of California
    Inventors: Yitzhak Tor, Nathan Luedtke
  • Orlistat compositions
    Patent number: 8071571
    Abstract: A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: December 6, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Pierre Barbier, Paul Hadvary, Hans Lengsfeld
  • Substrates for beta-lactamase and uses thereof
    Patent number: 8071761
    Abstract: Substrates for ?-lactamase of the general formula I in which one of X and Y is a fluorescent donor moiety and the other is a quencher (which may or may not re-emit); R? is selected from the group consisting of H, lower (i.e., alkyl of 1 to about 5 carbon atoms) and (CH2)nOH, in which n is 0 or an integer from 1 to 5; R? is selected from the group consisting of H, physiologically acceptable metal and ammonium cations, —CHR2OCO(CH2)nCH3, —CHR2OCOC (CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, delta-butyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, acyloxyalkyl, dialkylaminocarbonyloxymethyl and aliphatic, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z? and Z? are linkers for the fluorescent donor and quencher moieties.
    Type: Grant
    Filed: November 29, 2006
    Date of Patent: December 6, 2011
    Assignee: The Regents of the University of California
    Inventors: Roger Y. Tsien, Gregor Zlokarnik
  • Ketolide anti-infective compounds
    Patent number: 8063021
    Abstract: Compounds according to formula I wherein m is 0 or 1; X is and R1, R2, R3 R4, and R5 are as defined herein, are useful as anti-infective agents.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: November 22, 2011
    Assignee: Kosan Biosciences Incorporated
    Inventors: Yong Li, Yandong Li, Yan Zhu, Chaitan Khosla, David C. Myles
  • Anti-penicillin resistant pneumococci agent and novel 16-membered macrolide derivative
    Patent number: 8053418
    Abstract: A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd?N—.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: November 8, 2011
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Toshiaki Miyake, Yoshiaki Takahashi
  • Mono- and disaccharide derivatives
    Patent number: 8052981
    Abstract: The present invention includes a formulation comprising a physiological salt solution, or an oil-in-water emulsion, or a water immiscible solid phase, and an adjuvant comprising one or more disaccharide derivatives derived from cellobiose, gentiobiose, lactose, lactulose, maltose, melibiose, sucrose or turanose, wherein at least four of the free hydroxyl groups of the disaccharide molecule have been modified such that the disaccharide derivative has: (i) at least 3, but not more than N-1, fatty acid ester groups, wherein each of the fatty acid ester groups is represented by a general formula of —O—C(?O)—(CH2)xCH3 wherein x is between 6 and 14, and (ii) at least one, but no more than N-1 anionic groups, wherein N is the number of hydroxyl groups of the disaccharide from which the derivative is derived and wherein the combined number of fatty acid esters and anionic groups does not exceed N.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: November 8, 2011
    Assignee: Protherics Medicines Development Limited
    Inventors: Lucas Alfonsus T. Hilgers, Anneke Georgine Blom
  • Pesticidal formulations
    Patent number: 8048861
    Abstract: The present invention relates to an active composition for controlling or eradicating Phthiraptera, Siphonaptera and Acarina Pests, typically in domestic animals, comprising a synergistic combination of at least one A83543 compound and at least one macrocyclic lactone. The invention also relates to the use of the active composition in pesticidal formulations, the formulations themselves and to the various applications of those formulations as pesticides, specifically in controlling all species of Phthiraptera, Siphonaptera and Acarina pests, typically in domestic animals. Such applications include the control of such external Phthiraptera, Siphonaptera and Acarina pests in domestic animals including but not limited to sheep, cattle, poultry, pigs, goats, camelids, horses, dogs and cats.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: November 1, 2011
    Assignee: Eli Lilly and Company
    Inventors: Lionel Barry Lowe, James Terence Rothwell