Acridines (including Hydrogenated) Patents (Class 514/297)
  • Patent number: 10195190
    Abstract: Local delivery formulations of the antineoplastic and microbicide agent acriflavine, and methods of making and using thereof are significantly more efficacious at increasing the median survival of subjects with proliferative disease than systemic administrations of acriflavine. The local delivery formulations of acriflavine show a dose-dependent increase in the median survival of subjects. The local delivery forms provide the increased efficacy without the toxicity associated with systemic administration of the agent.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: February 5, 2019
    Assignee: The Johns Hopkins University
    Inventors: Henry Brem, Antonella Mangraviti, Alessandro Olivi, Betty M. Tyler, Tula Raghavan
  • Patent number: 10125129
    Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like mu opioid receptor agonists. Compounds of the present technology demonstrate remarkable potency and selectivity for the mu opioid receptor over the kappa opioid receptor, while also exhibiting a significant reduction (or, essentially, absence) of the negative side effects of many morphine-derived compounds.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: November 13, 2018
    Assignee: UNIVERSITY OF KANSAS
    Inventors: Thomas E. Prisinzano, Andrew P. Riley, Chad E. Groer
  • Patent number: 9840500
    Abstract: It relates to the use of compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I?), wherein R2? is an alcoxy group, a hydrocarbon chain or a ring system, and R1, R3, and R4 are as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I?), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R2? is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I).
    Type: Grant
    Filed: March 30, 2015
    Date of Patent: December 12, 2017
    Assignee: FUNDACIÓN PARA LA INVESTIGACIÓN MÉDICA APLICADA
    Inventors: Xabier Aguirre Ena, Julen Oyarzabal Santamarina, Felipe Prósper Cardoso, Maria Obdulia Rabal Gracia, Juan Roberto Rodríguez Madoz, Edurne San José Enériz
  • Patent number: 9708304
    Abstract: The present invention relates to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine salts and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine salts; especially to novel crystal forms of 4-(6-ethoxy-1-methoxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride and 4-(6-ethoxy-1-hydroxy-thioxanthene-9-ylidene)-1-methyl piperidine hydrochloride as well as to the use of these salts for preventing or treating migraine or pulmonary hypertension.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: July 18, 2017
    Assignee: Biofrontera Bioscience GmbH
    Inventors: Beate Schmitz, Hermann Luebbert
  • Patent number: 9695279
    Abstract: Provided are a fluoreneol-based monomer, a polymer for preparing a resist underlayer film obtained therefrom, a resist underlayer film composition containing the polymer, and a method for forming a resist underlayer film using the resist underlayer film composition, wherein the fluoreneol-based monomer is represented by Chemical Formula 2 below:
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: July 4, 2017
    Assignees: SK Innovation Co., Ltd., SK Global Chemical Co., Ltd.
    Inventors: Kwang Kuk Lee, Jin Su Ham, Sun Joo Kim, Hye Ryoung Lee, Min Ho Jung
  • Patent number: 9642830
    Abstract: The invention includes methods of treating a subject having hepatitis B viral (HBV) infection. In certain embodiments, the method of the invention comprises stimulating the innate cytokine response in macrophages, dendritic cells and/or liver non-parenchymal cells with small molecular STING agonists, thus suppressing HBV replication in hepatocytes. In other embodiments, the method of the invention can be used to treat chronic HBV infections. The invention further provides methods of identifying compounds useful in treating HBV infection in a subject.
    Type: Grant
    Filed: October 21, 2014
    Date of Patent: May 9, 2017
    Assignee: Drexel University
    Inventors: Jinhong Chang, Fang Guo, Timothy M. Block, Ju-Tao Guo
  • Patent number: 9567634
    Abstract: The present invention relates to methods and compositions for characterization of global cellular changes in response to introduction of viral vector compositions into target cells. It more particularly refers to a method for assessing the quality of a viral vector composition for a transgene transfer into target cells comprising measuring the expression level of at least one biomarker selected in the group consisting of CXCL2 and EREG and/or of at least one biomarker selected in the group consisting of ASPM, AURKB, CENPA, CENPF, CKS1B, E2F8, ERCC6L, FAM83D, KIFC1, MKI67, NEK2, NUSAP1, OIP5, PRC1, RRM2, SGOL1, SPC25, TOP2A and TTK.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: February 14, 2017
    Assignee: VECTALYS
    Inventors: Pascale Bouillé, Régis Gayon, Alexandra Iché
  • Patent number: 9498473
    Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: November 22, 2016
    Assignee: Heptiva LLC
    Inventor: Vincent I. Teow
  • Patent number: 9408841
    Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.
    Type: Grant
    Filed: November 29, 2013
    Date of Patent: August 9, 2016
    Assignee: Heptiva LLC
    Inventor: Vincent I. Teow
  • Patent number: 9221760
    Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
    Type: Grant
    Filed: May 9, 2012
    Date of Patent: December 29, 2015
    Assignees: VAN ANDEL RESEARCH INSTITUTE, TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
    Inventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
  • Patent number: 9211289
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 15, 2015
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
  • Patent number: 9044472
    Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.
    Type: Grant
    Filed: May 29, 2014
    Date of Patent: June 2, 2015
    Assignee: Chase Pharmaceuticals Corporation
    Inventors: Thomas N. Chase, Kathleen E. Clarence-Smith
  • Patent number: 9040553
    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: Grant
    Filed: July 11, 2013
    Date of Patent: May 26, 2015
    Assignee: CELL VIABLE CORPORATION
    Inventors: Iraj Lalezari, Jill Fabricant
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Patent number: 8987296
    Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: March 24, 2015
    Assignees: Oregon Health & Science University, The United States of America DBA The Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
  • Publication number: 20150072973
    Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 12, 2015
    Inventors: Roman Lopez, Frederic Colland
  • Patent number: 8975274
    Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: March 10, 2015
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Justin M. Lopchuk
  • Publication number: 20150023950
    Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
  • Publication number: 20150025044
    Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.
    Type: Application
    Filed: June 30, 2014
    Publication date: January 22, 2015
    Inventors: Jon R. Lorsch, Julie Ellen Takacs, Timothy Brian Neary
  • Publication number: 20150011522
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Applicants: IRM LLC, Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
  • Publication number: 20150005328
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20140371260
    Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
    Type: Application
    Filed: May 16, 2014
    Publication date: December 18, 2014
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventor: Hans-Joerg Moebius
  • Publication number: 20140363479
    Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Julius BORODY, Soledad CARSULA
  • Publication number: 20140349976
    Abstract: As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.
    Type: Application
    Filed: May 28, 2014
    Publication date: November 27, 2014
    Applicant: Acadia Pharmaceuticals Inc.
    Inventors: Uli HACKSELL, Krista MCFARLAND
  • Publication number: 20140348768
    Abstract: The present invention relates to a compound of general formula (I) in which: —R1 and R2 are simultaneously or independently H, OH, OCH3 or a C1-C5 alkyl radical, —R3 and R4 are simultaneously CH3, —or R3 is H and R4 is CH3, CH2CH3 or an isopropyl radical or a phenyl radical, —R5 is a C4-C24 alkyl radical or a 3-phenylpropanyl or 2,2-diphenylethanyl radical.
    Type: Application
    Filed: December 21, 2012
    Publication date: November 27, 2014
    Inventors: Stéphane Poigny, Françoise Belaubre
  • Publication number: 20140350045
    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: July 11, 2013
    Publication date: November 27, 2014
    Inventors: IRAJ LALEZARI, JILL FABRICANT
  • Publication number: 20140323423
    Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.
    Type: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Publication number: 20140323420
    Abstract: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subject
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Stephen Dewhurst, David Easterhoff, Brad Nilsson, John Dimaio, Alan Smrcka, Jerry Yang, Christina Capule
  • Patent number: 8871754
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: October 28, 2014
    Assignees: IRM LLC, Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan K S Yeung, Bin Zou, Venkatataiah Bollu
  • Publication number: 20140309244
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, A, X, D1, D2 and Y3 are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: September 23, 2011
    Publication date: October 16, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato, Clara Massol
  • Publication number: 20140301999
    Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
  • Patent number: 8841453
    Abstract: The invention relates to novel hybrid cholinesterase inhibitors containing the melatonin or its oxidation products unit and tetrahydroacridine unit linked via a carbamate bond. Due to the high selectivity of action, which is expressed with high ratio of IC50 for acetylcholinesterase inhibition to IC50 for butyrylcholinesterase inhibition ([IC50(AChE)]/[IC50(BChE)]), the novel compounds may be used in relief and/or treatment of the neurodegenerative diseases, among them the Alzheimer's disease.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: September 23, 2014
    Assignees: Uniwersytet Warszawski, Centrum Medyczne Ksztalcenia Podyplomowego
    Inventors: Anna Zawadzka, Zbigniew Czarnocki, Iwona Lozinska, Zuzanna Moleda, Miroslawa Panasiewicz
  • Patent number: 8828976
    Abstract: A screening method for identifying compounds that alter the fidelity with which the initiation codon in mRNAs is recognized by the translational apparatus in eukaryotes is disclosed. This screening method was used to identify compounds having such activity. Methods of altering the fidelity of initiation codon selection are also disclosed. Methods of treating disorders characterized by single nucleotide mutations in initiation codons using compounds identified by the screening method, as well as methods of treating fungal and parasitic infections and hyperproliferative disorders using compounds identified by the screening method are also disclosed.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: September 9, 2014
    Assignee: The Johns Hopkins University
    Inventors: Jon R. Lorsch, Julie Ellen Takacs, Timothy Brian Neary
  • Publication number: 20140235631
    Abstract: The present invention relates to efflux inhibitor compositions and methods of using these agents for treating conditions where the activity of efflux transporter proteins (e.g., Breast Cancer Resistance Protein (BCRP) and P-Glycoprotein (P-GP)) inhibit effective delivery of a therapeutic agent to a target tissue (e.g., brain, spinal cord, nerves, cerebrospinal fluid, testis, eyeballs, retina, inner ear, placenta, mammary gland, liver, biliary tract, kidney, intestines, lung, adrenal cortex, endometrium, hematopoietic cells, and/or stem cells).
    Type: Application
    Filed: July 26, 2013
    Publication date: August 21, 2014
    Inventors: Antonius Martinus Gustave Bunt, Olaf van Tellingen
  • Publication number: 20140228392
    Abstract: The present invention is bis-acridine or bis-quinoline intercalators having a modified bis(4-aminophenyl)ether tether to improve activity, selectivity, solubility and bioavailability of the antitumor compound.
    Type: Application
    Filed: September 18, 2012
    Publication date: August 14, 2014
    Inventors: Gordon W. Gribble, Justin M. Lopchuk
  • Publication number: 20140228333
    Abstract: In one aspect, the invention relates to methods for treating muscle atrophy by providing to an animal in need thereof an effective amount of a compound. The compound can modulate the expression levels of multiple mRNA of a muscle atrophy signature. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 6, 2012
    Publication date: August 14, 2014
    Applicants: UNIVERSITY OF IOWA RESEARCH FOUNDATION, The United States of America as Represented by the Department of Veterans Affairs
    Inventors: Christopher M. Adams, Steven D. Kunkel, Michael Welsh
  • Patent number: 8765781
    Abstract: The present invention is a DNA intercalating agent represented by the structure Y—Z—Y, wherein Y is an antitumor bis-carbazole and Z is a linear arrangement of multiple aromatic rings, containing at least two aromatic rings, or at least two alicyclic rings, said rings being linked in a 1,4 or 1,3 manner. Methods of inhibiting cancer cells and treating subjects having cancer with these agents are also provided.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: July 1, 2014
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Dmity A. Androsov
  • Publication number: 20140178354
    Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: The Regents of the University of California
    Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Publication number: 20140162980
    Abstract: The present invention provides compounds of formula (I) wherein G1, G2, G3, G4, G5, G6, Y1, Y2, Y3, Y4, Y5 and Y6 and p and q are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: July 28, 2011
    Publication date: June 12, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Daniel Stierli, Kurt Nebel, Werner Zambach, Andrea Bortolato
  • Publication number: 20140155367
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Application
    Filed: November 18, 2013
    Publication date: June 5, 2014
    Applicants: Novartis AG, IRM LLC
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
  • Publication number: 20140148451
    Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 29, 2014
    Applicants: Translational Genomics Research Institute, Van Andel Research Institute
    Inventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
  • Patent number: 8722701
    Abstract: Disclosed are 1,2,3,4,5,6,7,8-octohydro-9-phenylacetamidoacridine and the salt thereof, as well as the preparation method and medical use thereof. The compound can be useful for the preparation of medicaments for treating cardiovascular diseases, especially arrhythmia.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: May 13, 2014
    Assignees: Changchun Huayang High Technology, Inc., Jiangsu Shen ER Yang High Technology Co., Ltd.
    Inventor: Tonghui Wang
  • Publication number: 20140128423
    Abstract: A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.
    Type: Application
    Filed: October 29, 2013
    Publication date: May 8, 2014
    Applicants: Government of the United States of America dba The Department of Veterans Affairs, Oregon Health & Science University
    Inventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
  • Publication number: 20140113930
    Abstract: This invention relates to a synergistic pharmaceutical combination of glucose lowering drugs and autophagy inhibitors, kits containing such combinations, and methods of using such combinations to treat subjects suffering from cancers carrying a specific KRAS mutation. This invention also relates to a theranostic method for cancer treatment.
    Type: Application
    Filed: June 11, 2012
    Publication date: April 24, 2014
    Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
    Inventor: Stephen T. Gately
  • Publication number: 20140105824
    Abstract: Provided herein are diagnostic methods for identifying subjects susceptible to treatment with a hypoxia-activated agent, and related methods. Also provided herein are methods of monitoring treatments with anti-hyaluronan agents, and related methods.
    Type: Application
    Filed: October 16, 2013
    Publication date: April 17, 2014
    Inventors: H. Michael Shepard, Xiaoming Li, Curtis Thompson
  • Publication number: 20140100218
    Abstract: The present invention relates to methods of treatment using [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl amine (“COMPOUND I”) or a pharmaceutically acceptable salt thereof. In various embodiments, the methods of treatment include treatment of mild-to-moderate dementia of Alzheimer's type, diabetes, insomnia, and other indications. The present invention also relates to pharmaceutical compositions comprising COMPOUND I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 22, 2013
    Publication date: April 10, 2014
    Applicant: TransTech Pharma, LLC
    Inventors: Cesare Orlandi, David J. Clark, Imogene M. Grimes, Maria Carmen Valcarce Lopez, Matthew J. Kostura
  • Publication number: 20140088136
    Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Applicant: Heptiva LLC
    Inventor: Vincent I. Teow
  • Publication number: 20140088137
    Abstract: Compositions of hepatic therapeutic actives from one or more acridone compounds, one or more xanthone compounds, one or more thioxanthone compounds, one or more tocotrienol compounds, and one or more oleanolic triterpenoid compounds. Also, methods for treating various liver diseases or certain cancers with such hepatic therapeutic actives, as well as providing liver health maintenance.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Applicant: Heptiva LLC
    Inventor: Vincent I. Teow
  • Publication number: 20140086910
    Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of Alzheimer's diseases.
    Type: Application
    Filed: August 29, 2013
    Publication date: March 27, 2014
    Applicant: DARA BIOSCIENCES, INC.
    Inventor: Mary Katherine Delmedico