Acridines (including Hydrogenated) Patents (Class 514/297)
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Publication number: 20140128423Abstract: 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: ApplicationFiled: October 29, 2013Publication date: May 8, 2014Applicants: Government of the United States of America dba The Department of Veterans Affairs, Oregon Health & Science UniversityInventors: Michael K. Riscoe, Rolf W. Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
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Publication number: 20140113930Abstract: 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: ApplicationFiled: June 11, 2012Publication date: April 24, 2014Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: Stephen T. Gately
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Publication number: 20140105824Abstract: 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: ApplicationFiled: October 16, 2013Publication date: April 17, 2014Inventors: H. Michael Shepard, Xiaoming Li, Curtis Thompson
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Publication number: 20140100218Abstract: 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: ApplicationFiled: October 22, 2013Publication date: April 10, 2014Applicant: TransTech Pharma, LLCInventors: Cesare Orlandi, David J. Clark, Imogene M. Grimes, Maria Carmen Valcarce Lopez, Matthew J. Kostura
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Publication number: 20140088137Abstract: 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: ApplicationFiled: November 29, 2013Publication date: March 27, 2014Applicant: Heptiva LLCInventor: Vincent I. Teow
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Publication number: 20140086910Abstract: The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of Alzheimer's diseases.Type: ApplicationFiled: August 29, 2013Publication date: March 27, 2014Applicant: DARA BIOSCIENCES, INC.Inventor: Mary Katherine Delmedico
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Publication number: 20140088136Abstract: 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: ApplicationFiled: November 29, 2013Publication date: March 27, 2014Applicant: Heptiva LLCInventor: Vincent I. Teow
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Publication number: 20140080811Abstract: NSC antagonists are disclosed as useful in the treatment of dementia, in delaying the onset of dementia, and in the prevention of dementia. Dementia so treated may be, for example, Alzheimer's Disease (AD). NSC antagonists for treating dementia such as AD may be administered alone, a) in combination with other drugs used for treating dementia, b) in combination with drugs that stabilize or increase blood plasma glucose levels, or with both a) and b). Pharmaceutical compositions, dosage forms, and methods for using the same are disclosed, which include NSC antagonists, NSC antagonists combined with dementia drugs, NSC antagonists combined with glucose-level stabilizing or enhancing drugs, or combinations of these. Dosage forms may be designed to provide stable plasma levels for extended periods of time.Type: ApplicationFiled: February 27, 2013Publication date: March 20, 2014Applicant: Remedy Pharmaceuticals, Inc.Inventor: Remedy Pharmaceuticals, Inc.
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Publication number: 20140080860Abstract: 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: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicants: CENTRUM MEDYCZNE KSZTALCENIA PODYPLOMOWEGO, UNIWERSYTET WARSZAWSKIInventors: Anna Zawadzka, Zbigniew Czarnocki, Iwona Lozinska, Zuzanna Moleda, Miroslawa Panasiewicz
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Publication number: 20140066421Abstract: 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: ApplicationFiled: May 17, 2012Publication date: March 6, 2014Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
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Patent number: 8630703Abstract: Hydrophobic weak base compounds such as hydrophobic weak base chemotherapeutic agents (which are not an anthracycline) for use in the treatment of medical conditions such as proliferative disease or disorder in a subject, in combination with illumination of a region in a body of the subject which is characterized by the presence of proliferating cells, are disclosed. The hydrophobic weak base compound and a wavelength of illumination are selected such that the hydrophobic weak base compound acts as a therapeutically effective photosensitizer when exposed to the illumination.Type: GrantFiled: March 8, 2012Date of Patent: January 14, 2014Assignee: Technion Research & Development Foundation LimitedInventors: Yehuda G. Assaraf, Yamit Adar Turgeman, Andrzej M. Skladanowski, Arjan W. Griffioen, Henk Verheul, Kristy Gotink, Hubert Van Den Bergh, Patrycja Nowak-Sliwinska
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Patent number: 8618125Abstract: 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: GrantFiled: January 14, 2011Date of Patent: December 31, 2013Assignee: Heptiva LLCInventor: Vincent I. Teow
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Publication number: 20130344079Abstract: A method of diagnosing Phenylketonuria (PKU) in a subject in need thereof is disclosed. The method comprises detecting phenylalanine fibrils in a tissue of the subject, wherein a presence or level above a predetermined threshold of said phenylalanine fibrils in said tissue, is indicative of PKU in the subject. Antibodies capable of detecting phenylalanine fibrils are also disclosed as well as additional uses.Type: ApplicationFiled: March 8, 2012Publication date: December 26, 2013Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Lihi Adler-Abramovich, Ohad Carny, Ehud Gazit
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Publication number: 20130317018Abstract: The present invention provides methods and compositions for inducing expression of Ube3a in a cell by contacting the cell with a topoisomerase inhibitor. Particular embodiments include a method of treating a genomic imprinting disorder, such as Angelman syndrome, in a subject by administering to the subject an effective amount of a topoisomerase inhibitor.Type: ApplicationFiled: November 9, 2011Publication date: November 28, 2013Inventors: Benjamin David Philpot, Mark John Zylka, Bryan Leo Roth, John Arthur Allen, Hsien-Sung Huang
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Patent number: 8592447Abstract: 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: GrantFiled: November 13, 2007Date of Patent: November 26, 2013Assignees: Oregon Health & Science University, The United States of America, as represented by the Department of Veterans AffairsInventors: Michael K. Riscoe, Rolf Winter, Jane X. Kelly, David J. Hinrichs, Martin J. Smilkstein
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Publication number: 20130296324Abstract: The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject.Type: ApplicationFiled: February 25, 2013Publication date: November 7, 2013Applicant: VIVUS, Inc.Inventor: Jerry M. Held
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Publication number: 20130243886Abstract: The present invention relates to the use of one or more compounds selected from the following classes of biologically active agents: an a-adrenergic antagonist, an anthelmintic agent, an antifungal agent, an antimalarial agent, an antineoplastic agent, an antipsychotic agent, an antioxidant, a vasodilator and/or a vitamin, or a pharmaceutically acceptable derivative thereof, for use in the treatment of a microbial infection and in particular for killing multiplying, non-multiplying and/or clinically latent microorganisms associated with such an infection.Type: ApplicationFiled: September 9, 2011Publication date: September 19, 2013Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Yanmin Hu, Anthony RM Coates
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Patent number: 8530496Abstract: 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: GrantFiled: September 20, 2011Date of Patent: September 10, 2013Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Justin M. Lopchuk
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Publication number: 20130225560Abstract: A method for improving cognition comprising administering to a patient certain alpha-7 receptor agonists and an acetylcholinesterase inhibitor is described together with related compositions.Type: ApplicationFiled: July 25, 2011Publication date: August 29, 2013Applicant: ENVIVO PHARMACEUTICALS, INC.Inventors: Gerhard Koenig, Dana Hilt
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Publication number: 20130225531Abstract: A composition and method of treating Alzheimer's disease or a dementia of vascular origin are disclosed. The composition and method utilize an endothelin antagonist as the active agent to treat Alzheimer's disease or a dementia of vascular origin in mammals, including humans.Type: ApplicationFiled: December 19, 2012Publication date: August 29, 2013Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventor: The Board Of Trustees Of The University of Illinois
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Publication number: 20130225517Abstract: The invention provides compounds of formula I: or salts thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I and therapeutic methods for treating cancer.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: University of Iowa Research FoundationInventor: University of Iowa Research Foundation
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Patent number: 8518965Abstract: The present invention embraces bis-acridine and bis-quinoline intercalators having a bis(4-aminophenyl)ether tether, and diglycolate salts thereof, for selectively decreasing colon cancer and glial cell proliferation and preventing or treating colon cancers and gliomas.Type: GrantFiled: July 13, 2010Date of Patent: August 27, 2013Assignee: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmitry A. Androsov
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Publication number: 20130217673Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.Type: ApplicationFiled: February 22, 2012Publication date: August 22, 2013Applicant: Warsaw Orthopedic, IncInventor: Jared T. Wilsey
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Publication number: 20130178494Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.Type: ApplicationFiled: June 29, 2012Publication date: July 11, 2013Applicant: Academia SinicaInventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
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Publication number: 20130158065Abstract: 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: ApplicationFiled: September 2, 2011Publication date: June 20, 2013Applicants: JIANGSU SHEN ER YANG HIGH TECHNOLOGY CO., LTD, CHANGCHUN HUAYANG HIGH TECHNOLOGY CO., LTDInventor: Tonghui Wang
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Publication number: 20130137694Abstract: There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions.Type: ApplicationFiled: May 31, 2011Publication date: May 30, 2013Inventors: Gerald Batist, Jian Hui Wu
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Publication number: 20130102627Abstract: The present disclosure is directed to compounds of Formula I: which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity.Type: ApplicationFiled: April 8, 2011Publication date: April 25, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Jonathan Higgins, Gregory D. Cuny, Marcie Glicksman, Debasis Patnaik, Maxime Robin, Ross L. Stein, Jun Xian
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Publication number: 20130090307Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.Type: ApplicationFiled: December 6, 2012Publication date: April 11, 2013Applicant: PHARNEXTInventor: PHARNEXT
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20130053333Abstract: This invention relates to novel aminoquinoline derivatives of Formula (I) or Ia, or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an aminoquinoline derivative, such as a derivative of primaquine.Type: ApplicationFiled: January 19, 2011Publication date: February 28, 2013Inventor: Roger D. Tung
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Publication number: 20130035351Abstract: 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: ApplicationFiled: August 3, 2011Publication date: February 7, 2013Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Publication number: 20130023521Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: January 17, 2011Publication date: January 24, 2013Applicant: HYBRIGENICS SAInventors: Roman Lopez, Frederic Colland
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Publication number: 20130005666Abstract: The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Applicant: CORNELL UNIVERSITYInventors: Rajiv RATAN, Irina GAZARYAN, Natalya A. SMIRNOVA
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Publication number: 20130005650Abstract: Methods and compositions are provided comprising acriflavine for inhibiting and treating diseases and disorders associated with pathogenic proteins causing neurodegenerative diseases and amyloid diseases, such as protease resistant prion proteins (PrPSc) and those associated with transmissible spongiform encephalopathies (TSEs), Alzheimer's disease, amyloidosis, and the like.Type: ApplicationFiled: July 2, 2012Publication date: January 3, 2013Inventor: Peter K. Chiang
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Publication number: 20130005720Abstract: This invention relates to a pharmaceutical composition for treating cancer, comprising an effective amount of a compound represented by formula (I): wherein R is —CCOCCOCC— or —CCOCCOCCOCC—; and a pharmaceutical acceptable carrier. This invention also relates to a method for treating cancer, comprising administering a therapeutically effective amount of said compound to a subject; and a method for stabilizing G4 structure of telomere by using this compound.Type: ApplicationFiled: June 30, 2011Publication date: January 3, 2013Applicant: Academia SinicaInventors: Ta-Chau CHANG, Zi-Fu Wang, Chih-Chien Cho, Wei-Chun Huang, Jen-Fei Chu
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Patent number: 8337835Abstract: Compositions comprising the peroxisome proliferator-activated receptor alpha (PPAR?)-ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC) are disclosed. These compositions may be used for the prophylaxis and treatment of PPAR?-related liver disorders including, but not necessarily limited to, fatty liver disease, to lower lipid and triglyceride levels, and to increase high density lipoprotein levels in animals. Foods modified with 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1GPC) may be used to improve the metabolism of animals.Type: GrantFiled: April 12, 2010Date of Patent: December 25, 2012Assignee: Washington UniversityInventors: Clay F. Semenkovich, Manu V. Chakravarthy, John W. Turk
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Publication number: 20120321696Abstract: A novel function for the p53 gene related to resolution of deep venous thrombosis is disclosed herein. Lack of the p53 gene results in impaired thrombus resolution in a clinically relevant in vivo model of deep venous thrombus resolution. It is further shown that augmentation of p53 activity with quinacrine accelerates thrombus resolution in vivo, and that this beneficial effect is completely dependent on p53. p53-based therapy is therefore provided to accelerate thrombus resolution in patients, and to prevent or ameliorate the debilitating long-tem complications of deep venous thrombosis such as post-thrombotic syndrome.Type: ApplicationFiled: October 1, 2010Publication date: December 20, 2012Inventor: Rajabrata Sarkar
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Publication number: 20120316111Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of one or more of the following compounds prazosin, quinacrine, emetine, apomorphine, and debrisoquine, whereby endogenous BMP-2 up-regulation is stimulated in said subject. The endogenous BMP-2 up-regulation may enhance bone formation and/or cartilage formation.Type: ApplicationFiled: June 8, 2011Publication date: December 13, 2012Applicant: SOUTHWEST RESEARCH INSTITUTEInventor: Jorge G. ROSSINI
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Publication number: 20120277178Abstract: Compositions and methods of treatment or prophylaxis of fragile-X associated disorders are provided, as well as methods of screening compounds and kits to screen a library of compounds.Type: ApplicationFiled: April 27, 2012Publication date: November 1, 2012Applicant: EMORY UNIVERSITYInventors: Peng JIN, Abrar QURASHI
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Patent number: 8299062Abstract: The present invention provides compositions and methods for preventing, treating or reversing neuronal dysfunction in a mammal resulting from exposure to organophosphate nerve agents, organophosphate insecticides and incapacitating agents of the central nervous system (CNS); CNS injury, including traumatic brain injury, neurologic complications of cardiac surgery, perinatal asphyxia, and stroke, spinal cord injury, and peripheral nerve injury; and neuronal disorders associated with the loss of motor function including post-polio syndrome, amyotrophic lateral sclerosis, myasthenia gravis, Parkinson's disease and Rett syndrome; neurodegenerative disorders including Alzheimer's disease, mild cognitive impairment and schizophrenia; and cognitive impairment associated with aging.Type: GrantFiled: September 17, 2004Date of Patent: October 30, 2012Inventor: Franklin Volvovitz
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Publication number: 20120269738Abstract: The present invention relates to methods of detecting and monitoring aggregation of beta-amyloid peptides which are associated with neurodegenerative diseases as well as treating and/or preventing the neurodegenerative diseases by using carbazole-based fluorophores. In particular, the present invention provides methods for labeling and imaging the beta-amyloid (A?) peptides, oligomers, and fibrils in vitro and/or in vivo, as well as treating and/or preventing Alzheimer's disease by using the carbazole-based fluorophores of the present invention.Type: ApplicationFiled: April 13, 2012Publication date: October 25, 2012Applicant: Hong Kong Baptist UniversityInventors: Wanggui YANG, Yi WONG, Olivia T. W. NG, Hung Wing LI, Ken K. L. YUNG, Daniel W. J. KWONG, Ricky M. S. WONG
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Publication number: 20120258176Abstract: The invention discloses particulate complexes composed of chitosan, poly-glutamic acid, and at least one bioactive agent, wherein equal moles of the positively charged chitosan and the negatively charged poly-glutamic acid substrate form an electrostatic network enabling improved loading the bioactive agent.Type: ApplicationFiled: May 7, 2012Publication date: October 11, 2012Inventors: Hsing-Wen Sung, Zi-Xian Liao, Shu-Fen Peng, Hosheng Tu
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Publication number: 20120251491Abstract: The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: May 12, 2010Publication date: October 4, 2012Inventors: Stuart B. Rosenblum, Kevin X. Chen, Joseph A. Kozlowski, F. George Njoroge, Craig A. Coburn
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Publication number: 20120230972Abstract: 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: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
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Publication number: 20120225931Abstract: The present invention relates, inter alia, to methods and compositions for regulating the host response to biomaterials, including inhibiting inflammation from and rejection of biomaterials using salicylate compounds and/or TLR7/TLR9 antagonists as described herein.Type: ApplicationFiled: September 28, 2010Publication date: September 6, 2012Applicant: Yale UniversityInventors: Wajahat Z. Mehal, Themis Kyriakides
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Publication number: 20120220537Abstract: N-substituted 9-aminoacridine and bis-acridino derivatives containing electron-withdrawing groups (EWG) or electron-donating groups (EDG), including amino acid residues, and one-pot methods for their synthesis are disclosed. The derivatives are potential candidates for cancer treatment.Type: ApplicationFiled: November 1, 2010Publication date: August 30, 2012Applicant: ARIEL-UNIVERSITY RESEARCH AND DEVELOPMENT COMPANY LTD.Inventor: Gary Gellerman
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Publication number: 20120213758Abstract: 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: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Publication number: 20120190648Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH—C(?NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a —CO—(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.Type: ApplicationFiled: July 23, 2010Publication date: July 26, 2012Inventors: Philippe Jubault, Jean-Charles Quirion, Gerald Lemonnier, Cedric Lion
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Publication number: 20120183522Abstract: 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: ApplicationFiled: March 26, 2012Publication date: July 19, 2012Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
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Publication number: 20120184578Abstract: 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: ApplicationFiled: January 14, 2011Publication date: July 19, 2012Applicant: Heptiva LLCInventor: Vincent I. Teow