Acridines (including Hydrogenated) Patents (Class 514/297)
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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
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Patent number: 8222255Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: GrantFiled: September 25, 2008Date of Patent: July 17, 2012Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20120172292Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.Type: ApplicationFiled: September 10, 2010Publication date: July 5, 2012Applicant: NEW YORK UNIVERSITYInventors: Evgeny A. Nudler, Ivan Gusarov
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Publication number: 20120165365Abstract: 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: ApplicationFiled: July 13, 2010Publication date: June 28, 2012Applicant: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Dmitry A. Androsov
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Publication number: 20120129816Abstract: The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.Type: ApplicationFiled: March 3, 2009Publication date: May 24, 2012Applicant: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti
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Publication number: 20120129837Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.Type: ApplicationFiled: January 30, 2012Publication date: May 24, 2012Inventors: Wieslaw M. Cholody, Yi Zang, Norman E. Ohler, Sheela Chellappan, Janak Padia, Karina Zuck, Jeffrey W.H. Watthey, Zoe Ohler, Jeffrey Strovel
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Publication number: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Publication number: 20120107269Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Applicant: Tianjin Hemay Biotech Co., LtdInventors: Hesheng Zhang, Guanghuai Zeng, Yifei Gao
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Publication number: 20120071502Abstract: 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: ApplicationFiled: September 13, 2011Publication date: March 22, 2012Applicant: CELL VIABLE CORPORATIONInventors: Iraj Lalezari, Jill Fabricant
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Publication number: 20120058992Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate angiogenesis for treating said disease.Type: ApplicationFiled: October 29, 2010Publication date: March 8, 2012Applicant: PHARNEXTInventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Esther Graudens
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Patent number: 8129532Abstract: Amino(oligo)thiophene dyes useful for studying the electrophysiology of organelles, cells, and tissues are described. Compared to previously known dyes, the amino(oligo)thiophene dyes exhibit improved (faster) response to membrane potential changes, as well as the ability to be excited by 1064 nanometer femtosecond pulses. Methods of preparing the amino( oligo )thiophene dyes are also described.Type: GrantFiled: July 30, 2008Date of Patent: March 6, 2012Assignee: The University of ConnecticutInventors: Leslie M. Loew, Ping Yan
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Publication number: 20120040962Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.Type: ApplicationFiled: March 25, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8110562Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.Type: GrantFiled: July 19, 2007Date of Patent: February 7, 2012Assignees: University of Tennessee Research Foundation, The Ohio State University Research FoundationInventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20120022097Abstract: 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: ApplicationFiled: September 20, 2011Publication date: January 26, 2012Applicant: Trustees of Dartmouth CollegeInventors: Gordon W. Gribble, Justin M. Lopchuk
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Publication number: 20120009253Abstract: Use of an anti-inflammatory agent such as povidone iodine for the preparation of a pharmaceutical composition for the treatment of diseases of the lower respiratory tract which are susceptible to the administration of such agents.Type: ApplicationFiled: September 22, 2011Publication date: January 12, 2012Inventors: Wolfgang Fleischer, Karen Reimer
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Publication number: 20110319387Abstract: The invention relates to a compound of the following formula (I), or to a pharmaceutically acceptable salt thereof or to a stereoisomer or mixture of stereoisomers at any proportions, where: X1 is a CH2 or C?O group; X2 is a linear saturated or unsaturated carbohydrate chain with 8 to 24 carbon atoms; R1 is a hydrogen atom or an OH or (C1-C6)alkoxy group such as methoxy; and R2 is a CH3 or CH2OR3 group, with R3 being a hydrogen atom or a (C1-C6)alkyl, CO—(C1-C6)alkyl or NH—(C1-C6)alkyl group. The invention also relates to the use of said compound as a drug, in particular for treating neurodegenerative diseases, and to a method for preparing same.Type: ApplicationFiled: March 2, 2010Publication date: December 29, 2011Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)Inventors: Fanny Schmidt, Bruno Figadere, Rita Raisman-Vozari, Pierre Champy
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Publication number: 20110319386Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: June 10, 2011Publication date: December 29, 2011Applicant: BrainCells Inc.Inventors: Carrolee Barlow, Todd A. Carter, Kai Treuner, Michael Lee
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Publication number: 20110312938Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula (I) wherein R1, R2, R3, and RN are as defined herein. Compounds of Formula (I) are useful in the prevention and/or treatment of neurological and psychiatric disorder, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the disclosure and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: June 30, 2009Publication date: December 22, 2011Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Regina Graul, John Jeffrey Talley, Ara Mermerian
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Publication number: 20110301154Abstract: The present invention involves new and original sigma receptors Ligands: (Mono-or dialkylaminoalkyl)-?-butyro-lactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)ben-zyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or di-astereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Astemizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, an-timetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotectve and cytoregenerative activity against the cytodegenerative diseases.Type: ApplicationFiled: February 17, 2010Publication date: December 8, 2011Inventor: Alexandre Vamvakides
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Publication number: 20110293640Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.Type: ApplicationFiled: May 27, 2011Publication date: December 1, 2011Inventors: Kevin J. Tracey, Valentin A. Pavlov
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Publication number: 20110286927Abstract: In one aspect, the invention relates to a method for identifying a drug candidate with activity as a neuroprotective agent. The method includes determining whether a compound reduces ATF4 activity; and identifying the compound that reduces ATF4 activity as a drug candidate.Type: ApplicationFiled: August 4, 2008Publication date: November 24, 2011Applicant: CORNELL UNIVERSITYInventor: Rajiv R. Ratan
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Patent number: 8063062Abstract: Embodiments of this invention relate to compounds having a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB1 antagonism and cholinesterase inhibition is a compound of formula (1) wherein the symbols have the meanings given in the specification.Type: GrantFiled: December 17, 2007Date of Patent: November 22, 2011Assignee: Solvay Pharmaceuticals B.V.Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Belal Shadid
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Publication number: 20110280808Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, 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. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 18, 2011Publication date: November 17, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Publication number: 20110281907Abstract: Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met obtained by virtual screening, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.Type: ApplicationFiled: March 31, 2009Publication date: November 17, 2011Applicant: The Government of the United States of America, as represented by the Secretary, Dept.of Health and.Inventors: Donald P. Bottaro, Megan Peach, Marc Nicklaus, Nelly Tan
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Publication number: 20110256064Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, 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. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 15, 2011Publication date: October 20, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Publication number: 20110250129Abstract: A bioluminescence imaging-based high-throughput assay for inhibitors of ABCG2 is described. Compositions of inhibitors of ABCG2 and methods of using ABCG2 inhibitors are also described.Type: ApplicationFiled: November 12, 2009Publication date: October 13, 2011Applicant: The Johns Hopkins UniversityInventors: Martin Gilbert Pomper, Yimao Zhang, John Laterra
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Publication number: 20110230451Abstract: 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: ApplicationFiled: March 18, 2011Publication date: September 22, 2011Applicant: The Johns Hopkins UniversityInventors: Jon R. Lorsch, Julie Ellen Takacs, Timothy Brian Neary
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Publication number: 20110212928Abstract: The invention relates to methods and compositions for improving cognitive function by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an acetylcholinesterase inhibitor (AChEI) or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In particular, it relates to the use of a combination of an SV2A inhibitor and an AChEI in treating a central nervous system disorder with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, amyotrophic lateral sclerosis (ALS), and cancer-therapy-related cognitive impairment.Type: ApplicationFiled: February 9, 2011Publication date: September 1, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Michela Gallagher, Rebecca Haberman, Ming Teng Koh
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Patent number: 8003632Abstract: A method of treating a subject with a cytokine-mediated inflammatory disorder comprising administering to the subject an effective amount of a pharmaceutically acceptable cholinesterase inhibitor, provided that the inhibitor is not galantamine.Type: GrantFiled: August 14, 2007Date of Patent: August 23, 2011Assignee: The Feinstein Institute for Medical ResearchInventors: Kevin J. Tracey, Valentin A. Pavlov
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Publication number: 20110201576Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: ApplicationFiled: February 4, 2011Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida, University of Central FloridaInventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
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Patent number: 7993670Abstract: A germicidal absorptive material for use in surgical packings, wound bandages, sanitary tampons and bed sore prevention and/or treatment uses is provided by a foam-like matrix of hydrophilic polyurethane polymer to which application-specific loads of a germicidal disinfectant dye have been made. Polyurethane polymer of various densities and thicknesses exhibits an exceptional ability to absorb different levels of a number of disinfectant dyes, both basic and acidic, such as gentian violet and methylene blue, respectively. The relationship between dye-load and application-specific uses permits a totally-bound gentian violet pad to be used as a conventional bandage or pad on a surface wound with the capability of preventing the incursion of external pathogens from entering the wound through the pad, where the pathogens are killed by the bound-dye. The wound exudate is absorbed safely by the pad, where wound-originating pathogens are also killed.Type: GrantFiled: August 20, 2003Date of Patent: August 9, 2011Assignee: General Wound Kare, Inc.Inventors: Richard M. Simonson, Theodore McAllister, Richard R. Suchanec, Daniel A. White
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Patent number: 7994189Abstract: The present invention relates to dihydropyridine derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, phenyl, (1-5C)heteroaryl R2, R3 are independently (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkoxy, (24C)alkenyloxy, (2-4C)alkynyloxy, halogen X is SO2, CH2, C(O) or X is absent R4 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (3-6C)cycloalkenyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl, (2-6C)heterocycloalkyl(14C)alkyl, (6-1 OC)aryl, (6-10C)aryl(1-4C)alkyl, (1-9C)heteroaryl or (1-9C)heteroaryl(14C)alkyl. The compounds are useful for the treatment of fertility disorders.Type: GrantFiled: May 4, 2005Date of Patent: August 9, 2011Assignee: N.V. OrganonInventors: Nicole Corine Renee Van Straten, Gerritdina Geziena Gerritsma, Lars Anders Van Der Veen
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Publication number: 20110190285Abstract: The present invention provides methods of treating a botulinum toxin related condition in a subject. In certain embodiments, the methods involve administering a compound of the following formulas: (I), (II), (III), (IV), (V).Type: ApplicationFiled: August 26, 2009Publication date: August 4, 2011Applicant: ABSOLUTE SCIENCE, INC.Inventors: Alan Jacobson, Scott Moe
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Publication number: 20110183942Abstract: A method is disclosed for inhibiting the build-up of amyloid plaques in the brain of a patient with at least one risk factor for, or a diagnosis of, Alzheimer's Disease by administering to the patient an amount of one or more compounds effective to inhibit the phosphorylative activity of eEF2K, thereby inhibiting amyloid plaque deposition.Type: ApplicationFiled: July 15, 2009Publication date: July 28, 2011Applicants: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY, JOHNS HOPKINS UNIVERSITYInventors: Paul Worley, Sungjin Park, Alexey G. Ryazanov
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Publication number: 20110177061Abstract: The disclosure relates to methods of treating or preventing neurological disorders using docosahexaenoic acid.Type: ApplicationFiled: July 9, 2010Publication date: July 21, 2011Applicant: MARTEK BIOSCIENCES CORPORATIONInventors: Paul S. AISEN, Joseph F. Quinn, Karin Yurko-Mauro
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Publication number: 20110177105Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.Type: ApplicationFiled: August 13, 2010Publication date: July 21, 2011Inventors: Roman Lopez, Frédéric Colland
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Patent number: 7973030Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.Type: GrantFiled: February 25, 2005Date of Patent: July 5, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri, Ken-Ichi Kasahara
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Publication number: 20110152219Abstract: The use of enhancers with possibly riboflavin, as well as the corresponding compositions for the treatment of keratoconus or other ectasic corneal disorders by the method of corneal cross-linking.Type: ApplicationFiled: February 28, 2011Publication date: June 23, 2011Applicant: SOOFT ITALIA SPAInventors: Marcello STAGNI, Edoardo STAGNI, Massimo FILIPPELLO, Giovanni CAVALLO, Eugenio SODO
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Patent number: 7964611Abstract: An alkaline earth metal borated sulfonate prepared by a process comprising reacting a mixture of the following materials (A) (1) at least one of an oil soluble sulfonic acid or alkaline earth sulfonate salt or mixtures thereof (2) at least one source of an alkaline earth metal; and (3) at least one source of boron, in the presence of a mixture of comprising (4) at least one hydrocarbon solvent; and (5) at least one low molecular weight alcohol; and (6) from 0 to less than 10 mole percent, relative to the source of boron, of an overbasing acid, other than the source of boron; and (B) heating the reaction product of (A) to a temperature above the distillation temperatures of (4) and (5) to distill (4), (5) and water of reaction, wherein no additional water is added in the process.Type: GrantFiled: December 15, 2008Date of Patent: June 21, 2011Assignee: Chevron Oronite Company LLCInventors: Jean-Louis Le Coent, Pierre Tequi, John McDonald
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Publication number: 20110144148Abstract: The invention provides compounds of formula: which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the ?-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer's disease.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Applicant: NOSCIRA, S.A.Inventors: Ana Martinez Gil, Isabel Dorronsoro Diaz, Laura Rubio Arrieta, Diana Alonso Gordillo, Ana Fuertes Huerta, Susana Morales-Alcelay, Maria Del Monte Millan, Esther Garcia Palomero, Paola Usan Egea, Celia De Austria, Miguel Medina Padilla, Pilar Munoz Ruiz
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Patent number: 7956066Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.Type: GrantFiled: February 8, 2007Date of Patent: June 7, 2011Assignee: Janssen Pharmaceutica NVInventors: Daniel J. Buzard, James P. Edwards, David E. Kindrachuk, Jennifer D. Venable
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Patent number: 7951796Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers as well as their pharmaceutically compatible salts, and to the use thereof for producing a medicament suited for treating diseases associated with misfolded proteins.Type: GrantFiled: February 28, 2006Date of Patent: May 31, 2011Inventors: Carsten Korth, Ralf Klingenstein, Stefan Löber, Peter Gmeiner
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Publication number: 20110124631Abstract: A method for improving cognition comprising administering to a patient (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide or a pharmaceutically acceptable salt thereof and an acetylcholinesterase inhibitor is described together with related compositions.Type: ApplicationFiled: December 27, 2010Publication date: May 26, 2011Inventors: Gerhard Koenig, Dana Hilt
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Publication number: 20110117202Abstract: Methods and systems for producing a change in a medium. A first method and system (1) place in a vicinity of the medium at least one upconverter including a gas for plasma ignition, with the upconverter being configured, upon exposure to initiation energy, to generate light for emission into the medium, and (2) apply the initiation energy from an energy source including the first wavelength ?1 to the medium, wherein the emitted light directly or indirectly produces the change in the medium. A second method and system (1) place in a vicinity of the medium an agent receptive to microwave radiation or radiofrequency radiation, and (2) apply as an initiation energy the microwave radiation or radiofrequency radiation by which the agent directly or indirectly generates emitted light in the infrared, visible, or ultraviolet range to produce at least one of physical and biological changes in the medium.Type: ApplicationFiled: November 10, 2010Publication date: May 19, 2011Applicants: Immunolight, LLC, Duke UniversityInventors: Frederic A. Bourke, JR., Zakaryae Fathi, Ian Nicholas Stanton, Michael J. Therien, Paul Rath Stauffer, Paolo MacCarini, Katherine Sarah Hansen, Diane Renee Fels, Cory Robert Wyatt, Mark Wesley Dewhirst
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Publication number: 20110105554Abstract: The present invention provides a method of designing a modulator of a myosin, the method comprising molecular modeling of a compound such that the modeled compound interacts with at least three amino acid residues of said myosin, said residues being selected from (a) ranges K265-V268, V411-L441, N588-Q593, D614-T629, and V630-E646 of SEQ ID NO: 2, said myosin comprising or consisting of (i) the sequence of SEQ ID NO: 2; (ii) the sequence encoded by the sequence of SEQ ID NO: 1; (iii) a sequence being at least 40% identical to the sequence of SEQ ID NO: 2 or to the sequence encoded by the sequence of SEQ ID NO: 1; or (iv) a sequence encoded by a sequence being at least 40% identical to the sequence of SEQ ID NO: 1; wherein said sequence of (iii) or (iv) comprises said three amino acid residues, and wherein said residues comprise K265; or (b) ranges of any one of SEQ ID NOs: 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 36, 38, 40, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, 64, 66, 68, 70, 72, 7Type: ApplicationFiled: November 21, 2008Publication date: May 5, 2011Applicant: KINARIS BIOMEDICALS GMBHInventors: Dietmar Manstein, Roman Fedorov, Georgios Tsiavaliaris, Hans-Joachim Knölker, René Martin, Juliane Kirst, Herwig Gutzeit, Markus Böhl
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Publication number: 20110092464Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The invention includes compositions and methods based on modulating angiotensin activity to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Applicant: BrainCells Inc.Inventors: Carolee BARLOW, Todd A. Carter, Kai Treuner, Kym I. Lorrain
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Publication number: 20110077221Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.Type: ApplicationFiled: July 19, 2007Publication date: March 31, 2011Inventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20110064804Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.Type: ApplicationFiled: April 9, 2010Publication date: March 17, 2011Applicant: Adamas Pharmaceuticals, Inc.Inventors: Gregory T. Went, Timothy J. Fultz
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Publication number: 20110065674Abstract: The invention relates to methods and compositions for improving cognitive function by using a combination of valproic acid and analogs and derivatives thereof (“valproate”) and an acetylcholinesterase inhibitor (AChEI). In particular, it relates to the use of a combination of a valproate and an AChEI in treating age-related cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for Mild Cognitive Impairment (MCI), Age-Associated Memory Impairment (AAMI) or Age-Related Cognitive Decline (ARCD).Type: ApplicationFiled: May 14, 2009Publication date: March 17, 2011Inventors: Michela Gallagher, Ming Teng Koh
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Patent number: RE42802Abstract: Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e.Type: GrantFiled: April 25, 2007Date of Patent: October 4, 2011Assignee: H. Lundbeck A/SInventors: Hâkan Vilheim Wikström, Durk Dijkstra, Bastiaan Johan Venhuis