Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
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Publication number: 20130183278Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD as opposed to another neurodegenerative disease. The method of the invention comprises measuring the concentration of ?-synuclein (?-syn) and the concentration of unphosphorylated tau (tau) and/or phosphorylated tau (p-tau) in a cerebrospinal fluid sample taken from an individual. The method also comprises calculating the ratio of the concentration of tau and/or p-tau to the concentration of ?-syn, and thereby determining whether or not the individual has PD.Type: ApplicationFiled: July 6, 2011Publication date: July 18, 2013Applicant: United Arab Emirates UniversityInventors: Omar El-Agnaf, Lucilla Parnetti, Paolo Calabresi
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Publication number: 20130165493Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: ApplicationFiled: February 22, 2012Publication date: June 27, 2013Applicant: Siga Technologies, Inc,Inventors: Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Dongcheng Dai
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Publication number: 20130157990Abstract: A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state.Type: ApplicationFiled: February 20, 2013Publication date: June 20, 2013Applicant: EAGLE ADVANCEMENT INSTITUTE LLCInventor: EAGLE ADVANCEMENT INSTITUTE LLC
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Publication number: 20130150346Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.Type: ApplicationFiled: January 7, 2011Publication date: June 13, 2013Applicants: Ironwood Pharmaceutical, Inc.Inventors: James Philip Pearson, Todd G. Milne, Thomas Henry Johnston, Jonathan Michael Brotchie
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Publication number: 20130150326Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: Amira Pharmaceuticals, Inc.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, Nicholas Simon Stock, Deborah Volkots, John Howard Hutchinson
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Patent number: 8455252Abstract: Disclosed herein are materials and methods for sensitizing multidrug resistant cancer cells that express ABCG2 and related proteins members of a family of ATP-binding transporter superfamily that mediate drug efflux found in some types of multidrug resistant cancer cells. A series of compounds, including (N-(4-chlorophenyl)-2-[(6-{[4,6-di(4-morpholinyl)-1,3,5-tri-azin-2-yl]amino}-1,3-benzothiazol-2-yl)sulfanyl]acetamide), specifically inhibits ABCG2 and can be used to boost the bio-avail-ability of one or more effective cancer killing drugs, making it possible to use certain widely used chemotherapeutic reagent to treat multidrug resistance cancers. Using these compounds in combination with chemotherapeutic drugs that are substrates for ABCG2 and related proteins may also find utility in treating cancer cells that are not currently identified as multi-drug resistant. Additionally, these compounds appear to accelerate the intercellular degradation of ABCG2 and related proteins.Type: GrantFiled: October 24, 2009Date of Patent: June 4, 2013Assignee: Indiana University Research and Technology Corp.Inventors: Jian-Ting Zhang, Jing Qi, Hui Peng, Zizheng Dong
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Publication number: 20130131061Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R5 and R6 are as defined in the specification.Type: ApplicationFiled: January 11, 2013Publication date: May 23, 2013Applicant: KARO BIO ABInventors: Patrik Rhonnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstal, Aiping Cheng
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Publication number: 20130131114Abstract: The present invention provides compounds of formula (I), as well as pharmaceutically acceptable salt thereof, wherein R1 to R7 have the significance given herein. The compounds are useful in the treatment of prophylaxis of diseases that are related to AMPK regulation.Type: ApplicationFiled: January 18, 2013Publication date: May 23, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130115309Abstract: In one aspect, the invention provides a method for inhibiting the growth and/or proliferation of a myc-driven tumor cell comprising the step of contacting the tumor cells with a CSNK1? inhibitor. In another aspect, the invention provides a method of treating a subject suffering from a tumor comprising myc-driven tumor cells, comprising administering to the subject an amount of a composition comprising a CSNK1? inhibitor effective to inhibit the growth and/or proliferation of the tumor cells.Type: ApplicationFiled: April 6, 2011Publication date: May 9, 2013Applicant: FRED HUTCHINSON CANCER RESEARCH CENTERInventors: Carla Grandori, Masafumi Toyoshima
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Publication number: 20130109672Abstract: Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).Type: ApplicationFiled: April 26, 2011Publication date: May 2, 2013Applicant: The United States of America,as represented by the Secretary, Department of Health and Human ServiceInventors: Matthew B. Boxer, Min Shen, Douglas S. Auld, Craig J. Thomas, Martin J. Walsh
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Publication number: 20130095095Abstract: A method for treating thrombotic disorders using a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid. Also disclosed is a method of improving the efficacy of a blood thinning medication by co-administering a composition containing quercetin, together with one or more of vitamin B3, vitamin C, and folic acid to a subject being treated with a blood thinning medication.Type: ApplicationFiled: October 13, 2011Publication date: April 18, 2013Inventor: Thomas Christian Lines
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Patent number: 8399481Abstract: A compound of formula (I) Or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II): X is selected from a group consisting of CH2, C(?O), CH(R5), C(R5)(R6) or C(R5)(R6)CH2; R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein; and n=1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.Type: GrantFiled: June 4, 2010Date of Patent: March 19, 2013Assignee: Xention LtdInventors: Richard John Hamlyn, David Madge, Mushtaq Mulla, Basil Hartzoulakis, Simon Mark Jones, Derek Edward John, Oliver Gareth Dugdale
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Patent number: 8394843Abstract: Compounds are provided which have the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture which contain such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to activate glucokinase.Type: GrantFiled: July 18, 2011Date of Patent: March 12, 2013Assignee: Takeda California, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Robert J. Skene, Mingnam Tang, Sheldon X. Cao, David J. Hossfield, Jeffrey A. Stafford
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Publication number: 20130059852Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).Type: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
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Publication number: 20130053368Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.Type: ApplicationFiled: August 24, 2012Publication date: February 28, 2013Applicant: Newron Pharmaceuticals S.P.AInventors: Fariello Ruggero, Carlo CATTANEO, Patricia SALVATI, Luca BENATTI
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Publication number: 20130045241Abstract: An aqueous dispersion having a mixture of a hydrolysis-sensitive biocide, an iodo-derived hydrophobic biocide and an inert carrier dispersed in water. The iodo-derived hydrophobic biocide forms a complex with the inert carrier and the hydrolysis-sensitive biocide that is dispersible in water. The hydrophobic coating includes an inert carrier and the hydrolysis-sensitive biocide may be trihalogenomethylthio phthalimide or an analogue thereof and the iodo-derived hydrophobic biocide may be iodopropynyl butylcarbamate. The aqueous dispersion may also include a water-repelling layer coating the complex.Type: ApplicationFiled: December 7, 2010Publication date: February 21, 2013Applicant: ISP Investments Inc.Inventors: Raman Premachandran, Daniel H. Brown, Blanca Gomez, Karen Winkowski
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Patent number: 8377663Abstract: The present invention relates to cosmetic compositions comprising an association of hydroxymethionine and 3-aminopropanesulfonic acid, and a cosmetic method for the skin. These compositions are intended to prevent and/or treat the signs of the cutaneous ageing such as the sagging of the cutaneous and subcutaneous tissue, the loss of cutaneous elasticity and atony of the texture of the skin, the loss of firmness and tonicity, dermal atrophy and loss of density, wrinkle, little wrinkle, crack.Type: GrantFiled: September 11, 2008Date of Patent: February 19, 2013Assignee: Sederma, S.A.S.Inventors: Karl Lintner, Claire Mas Chamberlin
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Publication number: 20130035364Abstract: Compounds of general formula I: wherein R1a, R1b, R2, R3a, R3b and X are as defined herein are tyrosine kinase inhibitors and are useful for the treatment of various diseases and conditions, for example cancer.Type: ApplicationFiled: August 1, 2012Publication date: February 7, 2013Inventors: Mei Lin GO, Han Kiat HO, Xiao CHEN
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3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, preparation thereof and therapeutic use thereof
Patent number: 8362067Abstract: The present invention relates to novel 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives, to their preparation and to their therapeutic application. The compounds of the present invention correspond to the formula (I): in which the variables are as set forth in the specification. These compounds exhibit a strong affinity and a high selectivity for human arginine-vasopressin (AVP) V1a receptors and some compounds additionally exhibit a strong affinity for AVP V1b receptors.Type: GrantFiled: August 18, 2010Date of Patent: January 29, 2013Assignee: SanofiInventors: Loïc Foulon, Laurent Goullieux, Brigitte Pouzet, Claudine Serradeil-Le Gal, Gerard Valette -
Publication number: 20130022609Abstract: The present invention is directed to a method treating prostate cancer. The method comprises administering to a patient in need thereof at least one compound selected from N-methyl-?3,3?-dihydroindole-2,2? diketone; N-1-(?-D-O-triacetyl-xylopranosyl)-?3,3?-dihydroindole-2,2? diketone; and N-1-(?-D-O-triacetyl-xylopranosyl)-N?-methyl-?3,3?-dihydroindole-2,2? diketone. Preferably the compound is in an amount sufficient to inhibit growth, invasion, and/or metastasis of prostate cancer cells.Type: ApplicationFiled: September 20, 2012Publication date: January 24, 2013Applicant: NATROGEN THERAPEUTICS INTERNATIONAL, INC.Inventor: Natrogen Therapeutics International, Inc.
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Publication number: 20130018040Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.Type: ApplicationFiled: July 30, 2012Publication date: January 17, 2013Applicant: University of Washington through its Center for CommercializationInventors: Wesley C. VAN VOORHIS, Wilhelmus G.J. HOL, Eric T. LARSON, Dustin James MALY, Ethan MERRITT, Kayode K. OJO
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Patent number: 8354440Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: GrantFiled: September 15, 2011Date of Patent: January 15, 2013Assignee: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Bertal Huseyin Aktas, Yun-Hua Fan, Han Chen
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Publication number: 20130004481Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.Type: ApplicationFiled: January 5, 2012Publication date: January 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
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Publication number: 20130004577Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: NIPPON SHINYAKUInventors: Hironobu KATO, Hirokazu SAKAMOTO
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Patent number: 8344018Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: GrantFiled: July 14, 2009Date of Patent: January 1, 2013Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani
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Patent number: 8343986Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).Type: GrantFiled: September 1, 2009Date of Patent: January 1, 2013Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Publication number: 20120322770Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 21, 2012Publication date: December 20, 2012Inventor: Robert P. RICCIARDI
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Publication number: 20120308608Abstract: Provided herein are Compounds that induce interferon production and methods for identifying such Compounds. Also provided herein are compositions comprising such Compounds and methods of using such Compounds to treat interferon-sensitive diseases such as viral infections, cancer, and multiple sclerosis.Type: ApplicationFiled: January 31, 2011Publication date: December 6, 2012Inventors: Megan Shaw, Mila Ortigoza, Adolfo Garcia-Sastre, Peter Palese
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Publication number: 20120302581Abstract: The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by Candida albicans, and proliferative disorders such as glioblastoma.Type: ApplicationFiled: August 12, 2011Publication date: November 29, 2012Inventors: Nancy Ratner, Yolanda Sanchez, Gunnar Johansson, William Seibel
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Patent number: 8318699Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.Type: GrantFiled: January 31, 2006Date of Patent: November 27, 2012Assignees: The Trustees Of The University Of Pennsylvania, Cephalon, Inc.Inventors: Mark I Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiao
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Patent number: 8318793Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: March 29, 2010Date of Patent: November 27, 2012Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Wilfried Hornberger, Falko Ernst Wolter
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Patent number: 8309608Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.Type: GrantFiled: November 2, 2004Date of Patent: November 13, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Zeiher, Stefanie Dimmeler, Christopher Heeschen, Hartmut Ruetten
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Patent number: 8309595Abstract: Hydrazone compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.Type: GrantFiled: July 14, 2008Date of Patent: November 13, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Mohamed Naguib Attala, Philippe Diaz
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Patent number: 8303986Abstract: An oral dosage form comprising a pharmaceutical tablet of one or more layers, one of which carries a biologically active substance; the formulation of said tablet includes different percentages of hydrophilic and lipophilic polymeric materials, and adjuvant substances. The tablets of the present invention show a release rate which is independent from the amounts of active substance present in the tablet.Type: GrantFiled: June 5, 2009Date of Patent: November 6, 2012Assignee: Jagotec AGInventors: Guy Vergnault, Pascal Grenier, Lauretta Maggi, Ubaldo Conte
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Publication number: 20120276121Abstract: The present invention relates to the use of inhibitors of scavenger receptor class proteins, in particular ScarB1 for the production of a medicament for treatment of and/or prophylaxis against infections, involving liver cells and/or hematopoietic cells, in particular malaria.Type: ApplicationFiled: July 13, 2012Publication date: November 1, 2012Applicants: INSTITUTO DE MEDICINA MOLECULAR, FACULDADE DE MEDICINA DA UNIVERSIDADE DE LISBOA, CENIX BIOSCIENCE GMBHInventors: MICHAEL HANNUS, CECILIE MARTIN, MARIA M. MOTA, MIGUEL PRUDENCIO, CHRISTINA DIAS RODRIGUES
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Publication number: 20120264771Abstract: Provided is a method of inhibiting growth of androgen receptor positive cancer cells. The method entails administering to an individual diagnosed with or suspected of having an androgen receptor positive cancer and administering to the individual a composition containing a compound that can inhibit the growth of the androgen receptor positive cancer.Type: ApplicationFiled: October 25, 2010Publication date: October 18, 2012Applicants: PANACELA LABS, INC., HEALTH RESEARCH INC.Inventors: Katerina Gurova, Natalya Narizhneva
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Patent number: 8278342Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula XVII which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula XVII can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: GrantFiled: August 6, 2009Date of Patent: October 2, 2012Assignee: The Trustees of the University of PennsylvaniaInventor: Robert P. Ricciardi
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Publication number: 20120245147Abstract: Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.Type: ApplicationFiled: April 19, 2012Publication date: September 27, 2012Inventors: John C. REED, In-Ki Kim
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Patent number: 8273749Abstract: A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: GrantFiled: September 30, 2008Date of Patent: September 25, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London
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Patent number: 8268879Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: GrantFiled: June 9, 2010Date of Patent: September 18, 2012Assignee: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
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Publication number: 20120232031Abstract: Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.Type: ApplicationFiled: October 19, 2010Publication date: September 13, 2012Applicant: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Petpiboon Peppi Prasit, Isabelle Marguerite Dearmond
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Publication number: 20120232063Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: September 13, 2012Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M.J. Bourque
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Patent number: 8258173Abstract: The present subject matter relates generally to antioxidant compounds having the formula (I): wherein each of R1, R2, R3, and R4 are as defined below. These compounds are potentially useful as, for example, antioxidants.Type: GrantFiled: November 19, 2007Date of Patent: September 4, 2012Assignee: University of SunderlandInventors: Rosaleen Joy Anderson, Paul William Groundwater, David Antony Philip Small, Yu Gong
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Publication number: 20120214860Abstract: The present invention relates to a method of regulating the expression level of survival of motor neuron 1 (SMN1) comprising administering to a subject in need thereof a therapeutically effective amount of ubiquitin carboxyl-terminal hydrolase L1 (UCHL1) regulator and a pharmaceutically acceptable carrier. The present invention also relates to a method of detecting enzyme activity of ubiquitin carboxyl-terminal hydrolase L1 (UCHL1) in human fibroblasts comprising detecting protein expression level of survival of motor neuron 1 (SMN1).Type: ApplicationFiled: February 23, 2011Publication date: August 23, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSISTYInventors: Yuh-Jyh Jong, Shih-Hsien Hsu, Jan-Gowth Chang
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Publication number: 20120190700Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Publication number: 20120190723Abstract: A viral modulator and process thereof. A method may include contacting one or more viral modulators to one or more biological systems. A biological system may be configured to be infected by one or more virus. A virus may include an HIV virus, a VEEV virus and/or the like. A viral modulator may include a viral inhibitor and/or a viral activator.Type: ApplicationFiled: December 14, 2011Publication date: July 26, 2012Inventors: Fatah Kashanchi, Kylene Kehn-Hall, Olaf Kutsch
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Publication number: 20120190708Abstract: The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.Type: ApplicationFiled: July 12, 2010Publication date: July 26, 2012Applicants: UNIVERSITY OF MARYLAND, BALTIMORE, The Board of Regents of the University of the University of Texas System, SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTEInventors: Alexander Mackerell, JR., Hong Zhang, Andrei Osterman, Rohit Kolhatkar
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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: 20120190652Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD in the pre-symptomatic phase of the disease or to distinguishing PD from another neurological disorder. The method of the invention comprises measuring the amount of soluble ?-synuclein oligomers in a cerebrospinal fluid sample taken from an individual. The method optionally also comprises measuring the total amount of ?-synuclein in the CSF sample, calculating the ratio of the amount of ?-synuclein oligomers to the total amount of ?-synuclein, and thereby determining whether or not the individual has PD. The method of the invention can be used in clinical trials to measure the effect of drugs in both PD animal models and human PD patients.Type: ApplicationFiled: September 13, 2010Publication date: July 26, 2012Applicant: United Arab Emirates UniversityInventor: Omar El-Agnaf
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Patent number: 8227502Abstract: There are described Compounds of formula (I) in which R3 to R8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, osteoarthritis, mental disorders, or for inducing central nerve regeneration.Type: GrantFiled: November 9, 2007Date of Patent: July 24, 2012Assignee: Anamar ABInventors: Torbjorn Lundstedt, Elisabeth Seifert, Per Lek, Arne Boman