Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/469)
Chalcogen or nitrogen bonded directly to the hetero ring (Class 514/470)
  • TREATMENT OF SUICIDAL IDEATION OR BEHAVIOR USING INHIBITORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20120269906
    Abstract: The invention concerns methods of treating suicidal ideation or behavior in a subject in need thereof, comprising decreasing endogenous nicotinic acetylcholine receptor (nAChR) activity in the subject; therapeutic packages for treating suicidal ideation or behavior; and methods for determining the efficacy of a treatment for suicidal ideation or behavior. In some embodiments, the treatment methods comprise administering to the subject an effective amount of an inhibitor of a nAChR, such as a lithium compound, mecamylamine, clozapine, or asenapine.
    Type: Application
    Filed: October 15, 2010
    Publication date: October 25, 2012
    Applicant: University of South Florida
    Inventors: David Vincent Sheehan, Roland Douglas Shytle
  • OXABICYCLOHEPTANES AND OXABICYCLOHEPTENES, THEIR PREPARATION AND USE
    Publication number: 20120270736
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: June 30, 2011
    Publication date: October 25, 2012
    Applicant: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • Angiotensin II receptor antagonists
    Patent number: 8293777
    Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is Y is selected from the group consisting of R1 is selected from the group consisting of —O—C1-6 alkyl, —O-aryl, —O-heteroaryl, —O—C3-8 cycloalkyl, —C1-6 alkyl, -aryl, -heteroaryl, and —C3-8 cycloalkyl; R2 and R3 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: October 23, 2012
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Michael Man-Chu Lo, Amjad Ali, Ravi P. Nargund
  • Methods And Compositions For The Treatment Of Anxiety Disorders, Including Post Traumatic Stress Disorder (PTSD) And Related Central Nervous System (CNS) Disorders.
    Publication number: 20120264703
    Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 18, 2012
    Inventors: Arifulla Khan, John Frederick Reinhard, JR.
  • NOVEL BENZOFURAN TYPE DERIVATIVES, A COMPOSITION COMPRISING THE SAME FOR TREATING OR PREVENTING COGNITIVE DYSFUNCTION AND THE USE THEREOF
    Publication number: 20120259006
    Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.
    Type: Application
    Filed: June 5, 2012
    Publication date: October 11, 2012
    Applicants: DAEWOONG PHARMACEUTICAL CO., LTD, MEDIFRON DBT CO., LTD.
    Inventors: Dong Wook KANG, Jee Woo LEE, Young Ho KIM, Hee KIM, Hee Jin HA, Eun Joo NAM, Chan Mi JOUNG
  • Tubulin polymerisation inhibitors
    Patent number: 8278290
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: October 2, 2012
    Assignee: Biononics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • NOVEL BENZOFURAN TYPE DERIVATIVES, A COMPOSITION COMPRISING THE SAME FOR TREATING OR PREVENTING COGNITIVE DYSFUNCTION AND THE USE THEREOF
    Publication number: 20120245225
    Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.
    Type: Application
    Filed: June 5, 2012
    Publication date: September 27, 2012
    Applicants: DAEWOONG PHARMACEUTICAL CO., LTD, MEDIFRON DBT CO., LTD.
    Inventors: Dong Wook KANG, Jee Woo LEE, Young Ho KIM, Hee KIM, Hee Jin HA, Eun Joo NAM, Chan Mi JOUNG
  • HETEROCYCLIC SULFONAMIDE DERIVATIVES
    Publication number: 20120245209
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation).
    Type: Application
    Filed: December 7, 2010
    Publication date: September 27, 2012
    Applicant: NOVARTIS AG
    Inventors: Dinesh Chikkanna, Mark Gary Bock, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramulu Poddutorri
  • Compositions and Methods for Treatment of Eye Disorders
    Publication number: 20120232019
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: February 16, 2012
    Publication date: September 13, 2012
    Applicant: SARcode Bioscience Inc.
    Inventors: Thomas Gadek, John Burnier, Johan Oslob, Wang Shen, Kenneth Barr, Min Zhong
  • Benzofuran type derivatives, a composition comprising the same for treating or preventing cognitive dysfunction and the use thereof
    Patent number: 8263649
    Abstract: The present invention relates to the novel benzofuran derivatives, the preparation thereof and the composition comprising the same. The benzofuran derivatives of the present invention showed potent inhibiting activity of beta-amyloid aggregation and cell cytotoxicity resulting in stimulating the proliferation of neuronal cells as well as recovering activity of memory learning injury caused by neuronal cell injury using transformed animal model with beta-amyloid precursor gene, therefore the compounds can be useful in treating or preventing cognitive function disorder.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: September 11, 2012
    Assignee: Medifron DBT Co., Ltd.
    Inventors: Dong Wook Kang, Jee Woo Lee, Young Ho Kim, Hee Kim, Hee Jin Ha, Eun Joo Nam, Chan Mi Joung
  • Escitalopram and solid pharmaceutical composition comprising the same
    Patent number: 8252336
    Abstract: The present invention relates to Escitalopram having a small median particle size and a solid pharmaceutical composition comprising the same.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: August 28, 2012
    Assignee: Ratiopharm GmbH
    Inventors: Parshwakumar V. Kalyankar, Ganesh V. Gat, Jawed Hussain
  • SUBSTITUTED BENZOFURANS, BENZOTHIOPHENES, BENZOSELENOPHENES AND INDOLES AND THEIR USE AS TUBULIN POLYMERISATION INHIBITORS
    Publication number: 20120214770
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.
    Type: Application
    Filed: May 1, 2012
    Publication date: August 23, 2012
    Applicant: BIONOMICS LIMITED
    Inventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
  • Novel Antagonists of the Glucagon Receptor
    Publication number: 20120214769
    Abstract: The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: April 8, 2011
    Publication date: August 23, 2012
    Applicant: METABASIS THERAPEUTICS, INC.
    Inventors: Jorge E. Gomez-Galeno, K. Raja Reddy, Paul D. van Poelje, Robert Huerta Lemus, Thanh Huu Nguyen, Matthew P. Grote, Qun Dang, Scott J. Hecker, Venkat Reddy Mali, Mingwei Chen, Zhili Sun, Serge Henri Boyer, Haiqing Li, William Craigo
  • Methods and Compositions for Treating Viral Hemorrhagic Fever
    Publication number: 20120207730
    Abstract: Disclosed herein are methods and compositions for treating viral hemorrhagic fever in a subject by use of at least one inhibitor or suppressor of oxidase, inducible nitric oxide synthase (iNOS) and apoptosis pathway.
    Type: Application
    Filed: April 30, 2012
    Publication date: August 16, 2012
    Applicant: NATIONAL TAIWAN UNIVERSITY
    Inventors: Betty A. Wu-Hsieh, Yu-Ting Yen
  • SUBSTITUTED ALKYNYL PHENOXY COMPOUNDS AS NEW SYNERGISTS IN PESTICIDAL COMPOSITIONS
    Publication number: 20120208874
    Abstract: A composition comprising an alkynyl phenoxy compound of Formula (I) as a synergist and a pesticidal active ingredient is described, wherein R1 and R2, similar or different, are (C1-C4)alkyl or R1O— and R2O— together represent a group —O—CH2—O—, —O—CH(CH3)—O, —O—CH2—CH2—O—, —O—CH2—CH2—, R3 is (C1-C6)alkyl, (C3-C6)alkenyl or —B—(CH2-CH2—O)z-R6 where B is —CH2—O— or —O—, z is 0, 1 or 2 and R6 is (C1-C4)alkyl; R4 is hydrogen or methyl; R5 is hydrogen or methyl; x is an integer from 1 to 2; y is 0, 1 or 2; with the proviso that when R3 is —B—(CH2CH2—O)z-R6, y is 1 and 5-(propargyloxy)-benzo[1,3]dioxole is excluded.
    Type: Application
    Filed: August 18, 2010
    Publication date: August 16, 2012
    Inventors: Valerio Borzatta, Elisa Capparella, Leni Moroni, Graham Moores, Despina Philippou
  • Use of phthalide derivatives for the treatment of type 2 diabetes mellitus
    Patent number: 8242168
    Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: August 14, 2012
    Assignee: DSM IP Assets B.V.
    Inventors: Daniel D'Orazio, Antoine De Saizieu, Goede Schueler, Daniel Raederstorff, Sandra Renata Teixeira, Ying Wang Schmidt, Peter Weber, Swen Wolfram
  • 1,3-dihydro-5-isobenzofurancarbonitrile derivatives and pharmaceutical composition thereof for the treatment of premature ejaculation
    Patent number: 8242159
    Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: August 14, 2012
    Assignee: Dong-A Pharmaceutical. Co., Ltd
    Inventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
  • USE OF DRONEDARONE FOR THE PREPARATION OF A DRUG FOR USE IN THE MANAGEMENT OF THE RISK OF LIVER INJURY
    Publication number: 20120190740
    Abstract: The present disclosure concerns methods of managing the risk of liver injury in patients receiving treatment with dronedarone or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 12, 2011
    Publication date: July 26, 2012
    Applicant: SANOFI
    Inventor: Laurent AUCLERT
  • EP2 AND EP4 AGONISTS AS AGENTS FOR THE TREATMENT OF INFLUENZA A VIRAL INFECTION
    Publication number: 20120190739
    Abstract: The present invention is directed to the use of EP2 and/or EP4 agonists as therapeutics for the treatment of diseases associated with influenza A viruses, such as for example H5N1 and mutations thereof.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 26, 2012
    Applicant: GEMMUS PHARMA INC.
    Inventors: Daryl Faulds, William J. Guilford, Wolfgang Seifert
  • COMPOUNDS AND METHODS FOR ENHANCING HAIR GROWTH
    Publication number: 20120190733
    Abstract: The present invention provides a method for stimulating hair growth in a mammalian species or converting vellus hair or intermediate hair to terminal hair or stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles or increasing one or more of: length, thickness, number, and density, of eyelash hair or eyebrow hair comprising applying to the skin of a patient a composition comprising an effective amount of an EP3 agonist or an EP4 agonist prodrug or a mixture thereof. Such compositions which are used in treating the skin or scalp of a human or non-human animal may comprise an effective amount of 3, 7 or 3 and 7 thia prostanoic acid. A mixture of 3,7-dithia PGE1 and 3,7-dithiaPGE1-isopropyl ester is preferred for this treatment.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 26, 2012
    Inventors: Jenny W. Wang, David F. Woodward
  • Oxabicycloheptanes and oxabicycloheptenes, their preparation and use
    Patent number: 8227473
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 24, 2012
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S. Kovach, Francis Johnson
  • PHYTOCHEMICAL COMPOSITIONS INCLUDING SESAMIN FOR ANTI-INFLAMMATORY, ANTI-CYTOKINE STORM, AND OTHER USES
    Publication number: 20120178712
    Abstract: A composition (e.g., phytochemical composition) including sesamin, the composition exhibiting anti-inflammatory, anti-cytokine storm, connective tissue preservation, anti-viral, and/or other properties in biological tissue. The phytochemical composition therapeutically affects a pro-inflammatory cytokine condition, for instance facilitating or effectuating decrease in a quantity of a pro-inflammatory cytokine, for example, interleukin-1 and tumor necrosis-alpha. The phytochemical composition facilitates or effectuates an increase in quantity of an anti-inflammatory cytokines. The phytochemical composition can additionally facilitate a connective tissue extracellular matrix (ECM) preservation effect. The phytochemical composition can also inhibit an action of a viral neuraminidase, for example, the influenza A virus neuraminidase.
    Type: Application
    Filed: September 14, 2009
    Publication date: July 12, 2012
    Applicants: Center of Excellence For Innovation n Chemistry, Commission on Higher Education, Thailand Excellence Center of Tissue Engineering
    Inventor: Prachya Kongtawelert
  • Compositions for Reducing the Incidence of Drug Induced Arrhythmia
    Publication number: 20120178724
    Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 12, 2012
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
  • NOVEL MONASCUSPURPURONES, PREPARATION PROCESS THEREOF, AND USES OF THE MONASCUSPURPURONES
    Publication number: 20120164120
    Abstract: The present invention relates to a novel monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.
    Type: Application
    Filed: December 23, 2011
    Publication date: June 28, 2012
    Applicant: FOOD INDUSTRY RESEARCH AND DEVELOPMENT INSTITUTE
    Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
  • Hydroxamic acid derivatives of aniline useful as therapeutic agents for treating anthrax poisoning
    Publication number: 20120157462
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Application
    Filed: January 30, 2008
    Publication date: June 21, 2012
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • TREATMENT OF MACULAR DEGENERATION
    Publication number: 20120157521
    Abstract: The present invention relates generally to methods for treating macular degeneration, and in particular age-related macular degeneration, involving the use of specific benzofuran based compounds.
    Type: Application
    Filed: August 27, 2010
    Publication date: June 21, 2012
    Applicant: Bonomics Limited
    Inventor: Gabriel Kremmidiotis
  • COMBINATION THERAPY FOR TREATING PROLIFERATIVE DISEASES
    Publication number: 20120149665
    Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.
    Type: Application
    Filed: August 25, 2010
    Publication date: June 14, 2012
    Applicant: Bionomics Limited
    Inventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
  • FORMULATIONS INCLUDING AMIODARONE AND SALTS THEREOF AND METHODS OF THEIR MANUFACTURE AND USE
    Publication number: 20120142768
    Abstract: The invention encompasses ready to administer liquid formulations including amiodarone and a substituted cyclodextrin. The invention also encompasses methods of making the liquid formulations to provide acceptable concentrations of amiodarone suitable for parenteral administration. The liquid formulations of the invention are formulations included, for example, in a ready to use intravenous bag, bottle or syringe.
    Type: Application
    Filed: June 8, 2011
    Publication date: June 7, 2012
    Applicants: BAXTER INTERNATIONAL INC.
    Inventors: Gerold L. Mosher, Stephen Machatha, Daniel Cushing, Bushra Agha
  • COMPOUNDS AND METHODS FOR SKIN REPAIR
    Publication number: 20120142684
    Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.
    Type: Application
    Filed: November 29, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Robert M. Burk, Wha Bin Im, Scott M. Whitcup
  • Histone Deacetylase Inhibitors Sensitize Cancer Cells To Epidermal Growth Factor Inhibitors
    Publication number: 20120141479
    Abstract: Disclosed is the use of a combination of histone deacetylase inhibitors and kinase inhibitors with anti-EGFR activity.
    Type: Application
    Filed: July 23, 2008
    Publication date: June 7, 2012
    Inventors: Samir E. Witta, Paul A. Bunn, Harry A. Drabkin, Robert M. Gemmill, Daniel Chan
  • COMPOUNDS AND METHODS FOR SKIN REPAIR
    Publication number: 20120136011
    Abstract: The disclosure provides compositions and methods for treating a skin blemish. The compositions comprise a therapeutically effective amount of a compound useful for treating skin blemishes such as wounds, scars and wrinkles.
    Type: Application
    Filed: July 29, 2011
    Publication date: May 31, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Guang L. Jiang, Wha-Bin Im, Frederick C. Beddingfield, Larry A. Wheeler, Scott M. Whitcup, Robert M. Burk
  • USE OF A MELATONIN AGONIST FOR THE TREATMENT OF SLEEP DISORDERS INCLUDING PRIMARY INSOMNIA
    Publication number: 20120136050
    Abstract: Embodiments of the invention include the treatment of a sleep disorder comprising the administration of N-[[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cycloproply]methyl]propanamide or a salt, stereoisomer, solvate, or hydrate thereof, in amorphous or crystalline form.
    Type: Application
    Filed: July 16, 2010
    Publication date: May 31, 2012
    Applicant: VANDA PHARMACEUTICALS INC.
    Inventors: Mihael H. Polymeropoulos, Gunther Birznieks, Deepak Phadke
  • S1P1 RECEPTOR AGONISTS AND USE THEREOF
    Publication number: 20120129828
    Abstract: The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
    Type: Application
    Filed: June 18, 2009
    Publication date: May 24, 2012
    Inventors: Victor J. Cee, Jian Lin, Xiang Y. Yu, Zhaoda Zhang
  • SYSTEMS AND METHODS FOR TREATING HUMAN INFLAMMATORY AND PROLIFERATIVE DISEASES AND WOUNDS, WITH FATTY ACID METABOLISM INHIBITORS AND/OR GLYCOLYTIC INHIBITORS
    Publication number: 20120128724
    Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and/or an antibody against UCP and/or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.
    Type: Application
    Filed: November 22, 2011
    Publication date: May 24, 2012
    Applicant: The Regents of the University of Colorado, a body corporate
    Inventors: M. Karen Newell, Evan Newell, Elizabeth Villalobos-Menuey
  • NEW PROCESS FOR PREPARING HYDROXYLAMINES AND MEDICAMENTS
    Publication number: 20120122971
    Abstract: There is provided a process for the preparation of a compound of formula II, wherein R1, R2, R3 and R4 are as described in the description. Such compounds may, for example, be useful intermediates in the synthesis of drugs such as Dronedarone.
    Type: Application
    Filed: April 6, 2010
    Publication date: May 17, 2012
    Applicant: CAMBREX KARLSKOGA AB
    Inventors: Lars O. Hansson, Anders Bergh, Lars Eklund
  • NOVEL CALCIUM SENSING RECEPTOR MODULATING COMPOUNDS AND PHARMACEUTICAL USE THEREOF
    Publication number: 20120122784
    Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: May 17, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
  • Pharmacological Treatment for Sleep Apnea
    Publication number: 20120108570
    Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Miodrag Radulovacki, David W. Carley
  • Synthesis of thieno[3,4-b]thiophene, thieno[3,4-b]furan, related compounds and their derivatives and use thereof
    Patent number: 8168671
    Abstract: Inexpensive and facile methods of preparing fused heterocycles such as thieno[3,4-b]thiophene, thieno[3,4-b]furan, related compounds, and their derivatives are disclosed. Also disclosed are regioregular polymers prepared from the fused heterocycles.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: May 1, 2012
    Assignee: The University of Connecticut
    Inventor: Gregory A. Sotzing
  • ANTIFUNGAL COMPOUNDS
    Publication number: 20120095093
    Abstract: Antifungal compounds having a benzofuran structure. Antifungals exhibit much less toxicity to human cells than amiodarone. These compounds are useful alone or in combination with other compounds having antifungal activity. Compounds of this invention exhibit synergistic antifungal activity in combination with antifungal amiodarone compounds. The invention provides pharmaceutical compositions useful for treating fungal infections, methods for treating fungal infections and compounds useful in such compositions for treating fungal infections. Compounds of this invention are further useful as antifungal agents for the prevention and or treatment of fungal infections in plants. The invention includes agriculturally useful compositions comprising one or more compounds of this invention which exhibit fungistatic or fungicidal function against one or more plant pathogen is a fungus.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 19, 2012
    Inventors: William E. Courchesne, Elzbieta Hejchman, Dorota Maciejewska, Jerzy Kossakowski, Kinga Ostrowska
  • ALLOSTERIC BINDING COMPOUNDS
    Publication number: 20120095048
    Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.
    Type: Application
    Filed: February 19, 2010
    Publication date: April 19, 2012
    Applicants: REGION MIDT JYLLAND, AARHUS UNIVERSITET
    Inventors: Henrik Amtoft Neubauer, Ove Kjaer Wiborg, Henrik Helligsø Jensen
  • POORLY SOLUBLE DRUG CONTAINING MICROSPHERE WITH IMPROVED BIOAVAILABILTY AND METHOD OF PREPARING THE SAME
    Publication number: 20120076838
    Abstract: A poorly soluble drug containing microsphere with improved bioavailability, an oral formulation comprising the same, and a method of preparing the same are provided, wherein the poorly soluble drug containing microsphere is a solid dispersion wherein the poorly soluble drug is dispersed in the water-soluble polymer carrier in a noncrystalline form by spray drying, thus increasing bioavailability of the poorly soluble drug.
    Type: Application
    Filed: May 27, 2010
    Publication date: March 29, 2012
    Applicant: SAMYANG BIOPHARMACEUTICALS CORPORATION
    Inventors: Kyung-Hee Kim, Hyun-Ki Lee, Jun- Seok Hwang, Su-long Hwang, Chaul-Min Pai
  • BENZOFURAN-4,5-DIONES AS SELECTIVE PEPTIDE DEFORMYLASE INHIBITORS
    Publication number: 20120071523
    Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.
    Type: Application
    Filed: May 5, 2010
    Publication date: March 22, 2012
    Applicant: Sloan-Kettering Institute for Cancer Research
    Inventors: Hakim Djaballah, Christophe Antczak
  • COMPOUNDS FROM SOFT CORAL, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF
    Publication number: 20120071547
    Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.
    Type: Application
    Filed: March 15, 2011
    Publication date: March 22, 2012
    Applicants: NATIONAL MUSEUM OF MARINE BIOLOGY & AQUARIUM, NATIONAL SUN YAT-SEN UNIVERSITY
    Inventors: JYH-HORNG SHEU, WEI-HSIEN WANG, ZHI-HONG WEN, BO-WEI CHEN, PING-JYUN SUNG
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20120071516
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: September 22, 2011
    Publication date: March 22, 2012
    Applicant: CalciMedica, Inc.
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Yazhong Pei, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Novel phenoxyisobutyric acid compounds and methods for synthesis
    Publication number: 20120071502
    Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
    Type: Application
    Filed: September 13, 2011
    Publication date: March 22, 2012
    Applicant: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Multi-Functional Biocompatible Coatings for Intravascular Devices
    Publication number: 20120070483
    Abstract: A polymeric coating is adapted to substantially eliminate thrombus formation when in contact with blood. The polymeric coating includes a first polymeric layer and a second polymeric layer. Interposed between the first and second polymeric layers is a polymeric matrix layer doped with at least one of a nitric oxide donor and a nitric oxide generator. The nitric oxide donor and/or the nitric oxide generator are capable of releasing or generating NO. A bioactive agent is either immobilized to the surface of the second polymeric layer or is incorporated into the polymeric matrix layer.
    Type: Application
    Filed: April 25, 2011
    Publication date: March 22, 2012
    Inventors: Zhengrong Zhou, Mark E. Meyerhoff, Melissa M. Reynolds
  • Isotopically-labeled benzofuran compounds as imaging agents for amyloidogenic proteins
    Patent number: 8138360
    Abstract: Benzofuran compounds which contain at least one detectable label selected from the group consisting of 131I, 123I, 124I, 125I, 76Br, 75Br, 18F, 19F, 11C, 13C, 14C and 3H are provided as amyloid imaging agents for detecting brain amyloid deposits as well as other amyloidogenic peptides associated with systemic or localized amyloidosis. Additionally, the compounds are useful for determining if patients, presenting with clinically confusing cases of dementia or presenting with mild cognitive impairment, have Alzheimer's disease. The compounds are additionally useful as surrogate markers for monitoring the efficacy of anti-amyloidosis therapies.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: March 20, 2012
    Assignee: University of Pittsburgh—of the Commonwealth System of Higher Education
    Inventors: William E. Klunk, Chester A. Mathis, Jr.
  • NOVEL HYDROXAMATES AS THERAPEUTIC AGENTS
    Publication number: 20120064032
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: August 12, 2011
    Publication date: March 15, 2012
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Method of treating amblyopia
    Patent number: 8133906
    Abstract: The present invention relates to a method of treating or alleviating the symptoms of amblyopia. It is based on the discovery that repeated administration of a specific drug, which is known to be clinically active to treat depression in humans, results in improved vision of the amblyopic eye.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: March 13, 2012
    Assignee: Hermo Pharma Oy
    Inventors: Eero Castrén, Lamberto Maffei, Jose Maya Vetencourt
  • METHOD OF PREDICTING A PREDISPOSITION TO QT PROLONGATION
    Publication number: 20120058201
    Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.
    Type: Application
    Filed: April 5, 2010
    Publication date: March 8, 2012
    Applicant: VANDA PHARMACEUTICALS, INC.
    Inventors: Christian Lavedan, Simona Volpi, Louis Licamele