C-c(=x)-x-c Containing (x Is Chalcogen And At Least One X Is Other Than Oxygen) Patents (Class 514/513)
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Patent number: 7388028Abstract: The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients.Type: GrantFiled: February 14, 2007Date of Patent: June 17, 2008Assignee: Eastern Virginia Medical SchoolInventors: Karl A. Schellenberg, Frank A. Lattanzio, James Shaefer
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Publication number: 20080131503Abstract: A pharmaceutical composition for oral administration comprising a fixed dose combination of a first solid pharmaceutical composition containing fenofibrate as the active substance and second solid pharmaceutical composition containing an HMG-CoA reductase inhibitor such as a statin as the active substance, wherein the first and the second pharmaceutical compositions are present in separate entities in a single solid dosage form. For example a multilayer tablet, a two-layer tablet, or capsules or sachets containing the active ingredients in separate granulates or beads, either granulate or bead optionally being coated with a protective coating or an entero-coating.Type: ApplicationFiled: February 10, 2006Publication date: June 5, 2008Inventors: Per Holm, Tomas Norling
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Patent number: 7381749Abstract: Disclosed herein are carbonyl compounds of having the structural formula: or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof, Methods and compositions are disclosed for treating disease states including, but not limited to cancers, autoimmune diseases, tissue damage, central nervous system disorders, neurodegenerative disorders, fibrosis, bone disorders, polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, cardiovascular conditions, and disorders in which angiogenesis play a role in pathogenesis, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 9, 2005Date of Patent: June 3, 2008Assignee: Kalypsys, Inc.Inventors: James William Malecha, Stewart Alwyn Noble, Christian Andreus Hassig, Paul L. Wash, Brandon M. Wiley, Charles Maxwell Lawrence, Timothy Z. Hoffman
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Patent number: 7378442Abstract: The invention relates to methods of treatment and pharmaceutical compositions of new chemical compounds that inhibit the various enzymes in the arachidonic acid pathway implicated in inflammatory disease conditions.Type: GrantFiled: October 12, 2007Date of Patent: May 27, 2008Assignee: Sami Labs LimitedInventors: Muhammed Majeed, Kalyanam Nagabushnam, Rajendran Ramanujam, Subbalakshmi Prakash
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Patent number: 7365096Abstract: Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.Type: GrantFiled: December 9, 2003Date of Patent: April 29, 2008Assignee: Board of Regents, The University of Texas SystemInventors: Robert A. Kirken, Barry D. Kahan, Stanislaw M. Stepkowski, Waldemar Priebe, Izabela Fokt, Szymon Kosinski
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Publication number: 20080058412Abstract: The invention relates to substituted 1,3-diphenylprop-2-en-1-one derivative compounds, pharmaceutical and/or cosmetic compositions containing same, and the applications thereof in therapeutics and cosmetics. The invention also relates to a method for preparing said derivatives.Type: ApplicationFiled: January 7, 2005Publication date: March 6, 2008Applicant: GENFITInventors: Karine Caumont-Bertrand, Jean-Francois Delhomel
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Patent number: 7335683Abstract: Compositions and methods for therapy of cystic fibrosis and other conditions are provided. The compositions comprise one or more compounds such as flavones and/or isoflavones capable of stimulating chloride transport in epithelial tissues. Therapeutic methods involve the administration (e.g., orally or via inhalation) of such compositions to a patient afflicted with cystic fibrosis and/or another condition responsive to stimulation of chloride transport.Type: GrantFiled: October 17, 2001Date of Patent: February 26, 2008Assignee: Children's Hospital & Research Center at OaklandInventors: Horst Fischer, Beate Illek
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Patent number: 7288262Abstract: Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R? groups, —CO—NHR? groups, NH—COR? groups and —S—COR? groups, wherein R?, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least onType: GrantFiled: September 20, 2000Date of Patent: October 30, 2007Assignee: L'Oreal S.A.Inventor: Aude Livoreil
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Patent number: 7276536Abstract: The invention is directed to a method of increasing the bioavailability of the active form of S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate by administration of a therapeutically effective amount of the drug with food. The invention also provides a kit comprising a pharmaceutical composition comprising a therapeutically effective amount of S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate and a pharmaceutically acceptable carrier, prescribing information, and a container, wherein the prescribing information includes advice to a patient regarding administration of the drug with food to improve bioavailability.Type: GrantFiled: March 17, 2004Date of Patent: October 2, 2007Assignee: Japan Tobacco Inc.Inventors: Yasuo Urata, Tomohiro Ishikawa
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Patent number: 7253296Abstract: The invention relates to novel acylated aminopropanediols and the nitrogen and sulfur analogues thereof, pharmaceutical compositions comprising same, therapeutic uses thereof, in particular for the treatment of cerebral ischemia. The invention also provides a method of preparing said derivatives.Type: GrantFiled: February 12, 2004Date of Patent: August 7, 2007Assignee: GenfitInventors: Raphaël Darteil, Karine Caumont-Bertrand, Jamila Najib
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Patent number: 7223793Abstract: The present invention relates to phenolic acid derivatives of the formula I and compositions for the preventing and the treating blood lipid level-related diseases comprising the phenolic acid derivatives. The compounds have excellent effects of reducing blood lipid level, inhibiting cholesterol metabolism-related enzymes and preventing and treating blood lipid level-related diseases.Type: GrantFiled: December 4, 2002Date of Patent: May 29, 2007Assignee: Bionutrigen Co., Ltd.Inventors: Songhae Bok, Sangku Lee, Taesook Jeong, Euneai Kim, Surksik Moon, Myungsook Choi, Byunghwa Hyun, Chulho Lee, Yangkyu Choi, Gootaeg Oh
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Patent number: 7166744Abstract: The present invention relates to a novel retinoid derivative compound represented by the formula I: wherein X, R1, R2 and R3 are as defined herein or pharmaceutically acceptalbe salts thereof. Also, the present invention relates to processes for producing the compound of the formula I and to an anti-cancer composition comprising the compound of the formula I. The compound of the formula I according to the present invention exerts high anti-cancer effects while not causing undesirable side effects.Type: GrantFiled: May 29, 2002Date of Patent: January 23, 2007Assignee: Chebigen Co., Ltd.Inventors: Hong-Sig Sin, Soo-Jong Um, Young-Soy Rho, Si-Ho Park, Youn-Ja Kwon, Myoung-Soon Park, Hye-Sook Han, So-Mi Kim, Dong-Myoung Kim, Deok-Kun Oh, Jong-Sup Park, Tae-Sung Bae
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Patent number: 7141609Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 21, 2005Date of Patent: November 28, 2006Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 7112612Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.Type: GrantFiled: November 14, 2001Date of Patent: September 26, 2006Assignee: UCB S.A.Inventors: Benoit Kenda, Philippe Michel, Luc Quere
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Patent number: 7091231Abstract: Compounds comprising are disclosed, wherein Y, A, X, R, D, and n are as described. A compound comprising a prostaglandin EP2 selective agonist wherein the ?-chain comprises a substituted phenyl, wherein at least one substituent consists of hydrocarbyl or non-linear hydroxyhydrocarbyl is also disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: December 10, 2004Date of Patent: August 15, 2006Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Patent number: 7078402Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: May 31, 2001Date of Patent: July 18, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
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Patent number: 7078435Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.Type: GrantFiled: October 10, 2003Date of Patent: July 18, 2006Assignee: Montana State UniversityInventor: Tom Livinghouse
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Patent number: 7045547Abstract: Compounds of formula I wherein A is R3, OR3, SR3, and NR3R4; and R1, R2, R3 and R4 are as defined. The compounds of the invention are reversible inhibitors of acyl-CoA dehydrogenase, and are useful in treating disorders such as diabetes, heart diseases (including angina and congestive heart failure), and peripheral vascular disease in patients suffering from these diseases or conditions resulting thereof.Type: GrantFiled: August 20, 2002Date of Patent: May 16, 2006Assignee: University of DelawareInventors: Colin Thorpe, Wenzhong Wang
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Patent number: 7034057Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.Type: GrantFiled: November 19, 2003Date of Patent: April 25, 2006Assignee: Schering CorporationInventors: Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
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Patent number: 7019031Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.Type: GrantFiled: October 23, 2001Date of Patent: March 28, 2006Assignee: The Arizona Disease Control Research CommissionInventors: Seth D. Rose, Scott R. Lefler, Steven R. Ottersberg, Ann Y. Kim, Karl J. Okolotowicz, Rosemarie F. Hartman
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Patent number: 6913761Abstract: A pharmaceutical and/or veterinary formulation comprising about 2-30% (w/w) (on an active basis) of at least one active agent, about 0.5-20.0% (w/w) of a pore-foaming agent and the balance stearin. Such formulations provided release of the at least one active agent in humans and other animals for periods of 7 days up to about 2 years.Type: GrantFiled: July 20, 1999Date of Patent: July 5, 2005Assignee: Peptech LimitedInventors: Timothy Elliot Trigg, John Desmond Walsh, Deborah Ann Rathjen
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Patent number: 6864383Abstract: This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: GrantFiled: January 25, 2002Date of Patent: March 8, 2005Assignee: Merck & Co., Inc.Inventors: Maria L. Garcia, Gregory J. Kaczorowski, Ying-Duo Gao
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Publication number: 20040254225Abstract: Novel compounds and compositions including those compounds, as well as methods of using and making the compounds are herein described. The compounds are useful in therapeutic applications, including modulation of disease or disease symptoms in a subject (e.g., mammal, human, dog, cat, horse). The compounds are useful as modulators of the mu opioid receptor (MOR) through their binding affinity with that receptor.Type: ApplicationFiled: October 10, 2003Publication date: December 16, 2004Inventors: Bryce A. Harrison, Tiffany M. Gierasch, Gregory L. Verdine, Zhangjie Shi
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Publication number: 20040242683Abstract: The invention is directed to a method of increasing the bioavailability of the active form of S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate by administration of a therapeutically effective amount of the drug with food. The invention also provides a kit comprising a pharmaceutical composition comprising a therapeutically effective amount of S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate and a pharmaceutically acceptable carrier, prescribing information, and a container, wherein the prescribing information includes advice to a patient regarding administration of the drug with food to improve bioavailability.Type: ApplicationFiled: March 17, 2004Publication date: December 2, 2004Applicant: Japan Tobacco Inc.Inventors: Yasuo Urata, Tomohiro Ishikawa
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Patent number: 6806261Abstract: The present invention relates to methods for regulating the release of TGF-&bgr; from living cells in vitro or in vivo, comprising bringing the cells into contact with an effective amount of a NAALADase inhibitor. Such methods are believed to be useful for affecting neuroregeneration, cell proliferation, cell differentiation, extracellular matrix formation, myelination, inflammation, immune function, liver function, pancreatic function, angiogenesis, or wound healing; and/or for preventing or treating diabetes.Type: GrantFiled: August 1, 2002Date of Patent: October 19, 2004Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Xi-Chun May Lu, Krystyna Wozniak
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Publication number: 20040198727Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.Type: ApplicationFiled: June 6, 2003Publication date: October 7, 2004Inventors: Takumi Kawabe, Hidetaka Kobayashi
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Publication number: 20040192770Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.Type: ApplicationFiled: December 11, 2003Publication date: September 30, 2004Inventors: Alan P. Kozikowski, Lixin Qiao, Garth Powis
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Publication number: 20040192656Abstract: Methods and compositions for altering the viability of cells, particularly cancers in animals and humans are disclosed. The compositions of the present invention are formed from a set of components comprising one or more of the following: a dithiocarbonyl, preferably dithiocarbamate, compound; a divalent metal ion; a modulator of cellular glutathione levels; and an inhibitor of the phosphorylation of choline. The compositions described herein induce a relatively selective and rapid effect on the viability of cancer cells by inducing a mixture of apoptotic and necrotic cell death, with the dominant pathway being apoptosis. Particularly preferred active compositions comprise all four components, although combinations of fewer components can be fully effective in certain tumors.Type: ApplicationFiled: April 6, 2004Publication date: September 30, 2004Applicant: Zoltan Laboratories, LLCInventor: Zoltan Kiss
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Patent number: 6797504Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1. The invention provides recombinant serine protease domains and methods of using peptides comprising a recombinant serine protease domain to screen for compounds that inhibit serine protease activity of matriptase or MTSP1.Type: GrantFiled: September 8, 2000Date of Patent: September 28, 2004Assignee: Dendreon San Diego LLCInventors: Edwin L. Madison, Joseph Edward Semple, Gary Samuel Coombs, John Eugene Reiner, Edgar O. Ong, Gian Luca Araldi
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Patent number: 6794414Abstract: Diseases Mediated by transglutaminase, such as Huntington's Disease, spinobulbar atrophy, spinocerebellar ataxia, and dentatorubralpallidoluysian atrophy, as well as inflammatory diseases of the central nervous system, including mautiple sclerosis, rheumatoid arthritis, and insulin dependent diabetes mellitus, can be treated by administering a transglutaminase inhibitor such as monadansyl cadaverine, monoamines and diamines such as cystamine, putrescine, GABA. (gamma-amino benzoic acid), N-benzyloxy carbonyl, 5-deazp-4-oxonorvaline p-nitrophenylester, glycine methyl ester, CuSO4, and the oral anti-hyperglycemic agent tolbutamide.Type: GrantFiled: September 6, 2001Date of Patent: September 21, 2004Assignee: Yeda Research and Development Co. Ltd.Inventor: Lawrence Steinman
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Publication number: 20040176444Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: November 26, 2003Publication date: September 9, 2004Inventors: Jonas Fagerhad, Lanna Li, Lindstedt Alstermark Eva-Lotte
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Patent number: 6756404Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.Type: GrantFiled: March 13, 2002Date of Patent: June 29, 2004Assignee: The Research & Development Institute, Inc.Inventor: Tom Livinghouse
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Publication number: 20040116517Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: 1Type: ApplicationFiled: December 5, 2002Publication date: June 17, 2004Inventors: Gary David Lopaschuk, John Christopher Vederas, Jason Roland Dyck
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Publication number: 20040116408Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolving, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: ApplicationFiled: August 12, 2003Publication date: June 17, 2004Inventor: Charles N. Serhan
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Publication number: 20040102418Abstract: This invention relates to compounds of the Formula (I): 1Type: ApplicationFiled: November 19, 2003Publication date: May 27, 2004Inventors: Zhoaning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
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Patent number: 6734211Abstract: Neurite outgrowth and nerve regeneration are promoted by disruption of the steroid receptor complex and stimulation of MAP kinase/kinase activity. This disruption can take the form of disruption of the physical assembly or function of the steroid receptor complex, such as the mature complex or a precursor of the mature complex that is required for assembly of the mature complex. Geldanamycin and its analogs, bastadin and members of the bastadin family, and radicicol and its analogs, as well as FKBP-52 antibody, are shown to disrupt the complex and promote nerve growth. Assays for finding neurotrophic compounds, as well as compounds found by these assays, pharmaceutical compositions into which they are incorporated, and methods of treating subjects having neuronal dysfunction caused by injury or disease are disclosed.Type: GrantFiled: April 29, 2002Date of Patent: May 11, 2004Assignee: Oregon Health & Sciences UniversityInventor: Bruce G. Gold
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Publication number: 20040072907Abstract: A magnetic circuit component having a plurality of claws arranged in a plurality of rows, with the base of each claw connected to a common yoke. A plurality of non-interlaced coils constituting a multi-phase winding are included, with the coils being wound around the bases of corresponding claws, and being distributed uniformly in the direction of motion.Type: ApplicationFiled: July 30, 2003Publication date: April 15, 2004Inventors: Dragovich S. Peter, Prins J. Thomas, Zhou Ru
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Publication number: 20040072899Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent.Type: ApplicationFiled: June 10, 2003Publication date: April 15, 2004Inventors: L. Gordon Letts, David S. Garvey
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Publication number: 20040063781Abstract: 1Type: ApplicationFiled: October 14, 2003Publication date: April 1, 2004Inventors: Benjamin Pelcman, Annika Gustafsson, Philip R Kym
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Patent number: 6713506Abstract: Disclosed herein are ester-bond containing tea polyphenols that has a susceptibility to nucleophilic attack, their analogs and pharmaceutically acceptable salts, method for inhibiting proteasomal chymotrypsin-like activity in vivo and in vitro, methods for cancer treatment with tea-derived polyphenols, such as EGCG, ECG, GCG, or CG, as well as pharmaceutical compositions comprising the same.Type: GrantFiled: October 11, 2001Date of Patent: March 30, 2004Assignee: University of South FloridaInventors: Q. Ping Dou, Sangkil Nam, David M. Smith
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Publication number: 20040058976Abstract: This invention relates a formulation comprising potent potassium channel blockers or pharmaceutically acceptable salts thereof in combination with peanut oil for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.Type: ApplicationFiled: July 16, 2003Publication date: March 25, 2004Inventor: Christine Stelmach
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Publication number: 20040058991Abstract: The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.Type: ApplicationFiled: September 29, 2003Publication date: March 25, 2004Inventors: Benoit Kenda, Philippe Michel, Luc Quere
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Publication number: 20040048808Abstract: Methods for inhibiting angiogensis are disclosed the comprise administering oleouropein and/or the products of its hydrolysis in therapeutically effective amounts. The methods and compositions of the present invention are particularly effective in inhibiting the vascularization of endothelial cells, and may be utilized to treat a wide variety of cancers, ocular diseases, and inflammatory conditions.Type: ApplicationFiled: September 8, 2003Publication date: March 11, 2004Inventors: Hamdi K. Hamdi, Jeffrey H. Tavis, Raquel Castellon
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Publication number: 20040044050Abstract: The present invention is directed to compounds that are analogues of lipid mediators derived from a fish oil-derived fatty acid, eicosapentaenoic acid [C20:5 &ohgr;-3; EPA], but with a longer tissue half-life and enhanced bioactivity. These analogues may be used to treat inflammatory, angioproliferative, cardiovascular, thrombophlebotic, vascular, ocular, dermatologic, neurodegenerative, pulmonary, endocrine, reproductive, rheumatologic and gastrointestinal diseases.Type: ApplicationFiled: June 13, 2003Publication date: March 4, 2004Inventors: Daniel W. Goodman, Michael R. Hanley, Stuart L. Bursten
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Publication number: 20040044034Abstract: Compounds are described which modulate the tzrosine kinase activity of p56lck and signal transduction pathways in which this enzyme is involved. The invention also relates to compounds which have immunomodulatory activity, e.g., which have immunosuppressant or immunostimulatory activity, and/or which have an antineoplastic effect. The invention further relates to compositions comprising these compounds, and methods of using them.Type: ApplicationFiled: January 22, 2003Publication date: March 4, 2004Inventors: Jun Hayashi, Alexander D. Mackerell
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Publication number: 20040039032Abstract: Compounds of formula I 1Type: ApplicationFiled: August 20, 2002Publication date: February 26, 2004Inventors: Colin Thorpe, Wenzhong Wang
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Publication number: 20040029903Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 12, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Publication number: 20040029839Abstract: Cosmetic or pharmaceutical compositions comprising compounds of formula (I) and the corresponding salts thereof: 1Type: ApplicationFiled: February 3, 2003Publication date: February 12, 2004Inventors: Christophe Boulle, Maria Dalko, Jean-Luc Leveque, Lucie Simonetti
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Publication number: 20040024024Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: ApplicationFiled: November 12, 2002Publication date: February 5, 2004Inventors: John N. Freskos, Y vette M. Fobian, Alok K. Awasthi, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Nizal S. Chandrakumar, Gary A. DeCrescenzo, Bipin N. Desai, Marcia I. Heron, Susan L. Hockerman, Sara M. Jull, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Patrick B. Mullins, Monica B. Norton, Joseph G. Rico, John J. Talley, Mahima Trivedi, Clara I. Villamil, Lijuan Jane Wang