The Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/472)
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Publication number: 20120122877Abstract: The present invention is antibiotic compositions having the ability to disrupt a MazEF complex in S. aureus. The compositions also have the ability to inhibit growth of S. aureus and as such are useful as antibiotic compounds.Type: ApplicationFiled: July 1, 2010Publication date: May 17, 2012Applicant: TRUSTEES OF DARTMOUTH COLLEGEInventors: Ambrose Cheung, Zhibiao Fu
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Patent number: 8163796Abstract: A novel treatment regimen is described for the control and elimination of cancer cell populations including cancer stem cells. The disclosed protocol consists of a pretreatment step followed by a treatment step. The pretreatment step sensitizes cancer cells to apoptosis by altering their intracellular oxidation-reduction state via reduced glutathione depletion. The treatment step involves the sequential administration of a cancerostatic dicarbonyl compound to induce apoptosis. The use of nanoparticle delivery systems further enhances both the pharmacokinetic and pharmacodynamic properties of the pretreatment compounds and the cancerostatic dicarbonyls. Since the pretreatment and treatment compounds are carefully selected and delivered, normal cells are not affected and side effects are kept to a minimum.Type: GrantFiled: July 20, 2010Date of Patent: April 24, 2012Assignee: BioChemical Solutions, LLCInventors: Morris A. Johnson, Michael M. Smits
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Publication number: 20120071430Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.Type: ApplicationFiled: November 1, 2011Publication date: March 22, 2012Applicant: Los Alamos National LaboratoryInventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
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Patent number: 8124653Abstract: Disclosed is a composition that includes a tetrahydrobiopterin in a controlled-release pharmaceutical preparation. Also disclosed is a method of treating a patient with phenylketonuria that includes administering, to the patient, a composition that contains tetrahydrobiopterin in a controlled-release pharmaceutical preparation. Also disclosed is a method of treating a patient with ADHD that includes administering a tetrahydropterin to the patient. Compositions for the treatment of ADHD are also described.Type: GrantFiled: June 25, 2005Date of Patent: February 28, 2012Assignee: The Board of Regents of The University of Texas SystemInventors: Reuben Matalon, Ofer Matalon
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Publication number: 20120022116Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.Type: ApplicationFiled: July 13, 2011Publication date: January 26, 2012Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
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Publication number: 20120022100Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 28, 2011Publication date: January 26, 2012Inventors: Juergen Klaus Maibaum, Daniel K. Baeschlin, Holger Sellner
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Publication number: 20110319455Abstract: A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.Type: ApplicationFiled: April 19, 2011Publication date: December 29, 2011Inventors: Bruce Steven Klein, Brad Mark Tebbets
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Patent number: 8053435Abstract: The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.Type: GrantFiled: November 1, 2007Date of Patent: November 8, 2011Assignees: Korea Research Institute of Chemical Technology, Crystalgenomics, Inc.Inventors: Cheol Hae Lee, Hee Jung Jung, Jae Hak Kim, Won Jang Jeong, Joong Myung Cho, Seong Gu Ro, Young Lan Hyun, Cheol Soon Lee, Dongkyu Shin
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Publication number: 20110245204Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: ApplicationFiled: July 12, 2010Publication date: October 6, 2011Inventors: Kevin R. Lynch, Timothy L. MacDonald
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Publication number: 20110245262Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 20, 2007Publication date: October 6, 2011Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
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Publication number: 20110178108Abstract: A group of amino substituted benzoyl derivatives, their preparation and their use. The screening and research on an antiviral drug with hA3G/Vif as a target point proves that the 3-amino benzoyl derivatives not only have the combined activity for the hA3G/Vif, but also have a function of inhibiting replication of viruses. The present invention provides the possible breakthrough progress for the problem of HIV drug resistance, thereby providing a novel clinical antiviral drug which has higher efficiency.Type: ApplicationFiled: September 28, 2009Publication date: July 21, 2011Applicant: Institute of Medicinal Biotechnology Academy of Medical ScienceInventors: Jian-Dong Jiang, Liyan Yu, Shan Cen, Zhourong Li, Yanping Li, Jlan Xu
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Publication number: 20110144043Abstract: The present invention is directed to methods, kits and compositions for modulating the activity of Stat molecules (e.g., Stat1, Stat3 and Stat5). The compounds of the invention are useful for treating and/or preventing disorders characterized by Stat dysregulation, such as hyperproliferative disorders. Further, the compounds of the present invention are also useful in culturing stem cells and treating ischemic disorders.Type: ApplicationFiled: December 11, 2009Publication date: June 16, 2011Applicant: Dana-Farber Cancer InstituteInventor: David A. Frank
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Patent number: 7960588Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: GrantFiled: March 29, 2010Date of Patent: June 14, 2011Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald
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Publication number: 20110105533Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.Type: ApplicationFiled: June 25, 2010Publication date: May 5, 2011Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
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Publication number: 20110092564Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).Type: ApplicationFiled: February 26, 2009Publication date: April 21, 2011Inventors: Ernest Puil, Bernard A. Macleod, Richard Wall
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Patent number: 7910622Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: GrantFiled: March 19, 2008Date of Patent: March 22, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. O'Neill
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Publication number: 20110053890Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.Type: ApplicationFiled: September 1, 2009Publication date: March 3, 2011Applicant: Los Alamos National Security, LLC.Inventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
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Publication number: 20110046142Abstract: Methods for identifying prodrug antibiotic compounds and direct inhibitory antibiotic compounds utilizing various screens are provided. Also provided are methods for treating infections using these compounds.Type: ApplicationFiled: June 11, 2008Publication date: February 24, 2011Applicant: Northeastern UniversityInventors: Kim Lewis, Gabriele Casadei
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Publication number: 20110027356Abstract: Oral pharmaceutical dosage form containing at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another, at least one of the medicaments being selected from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, clopidogrel.Type: ApplicationFiled: January 26, 2009Publication date: February 3, 2011Inventors: Anne-Emmanuelle Lugrin, Claude Griscelli, Mehdi El Glaoui, Guillaume El Glaoui, Jean Hoffelt
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Publication number: 20100305182Abstract: The present invention provides compositions and methods for modulating the communication and virulence of quorum sensing bacteria. In various exemplary embodiments, the invention provides a combinatorial library of quorum sensing compounds including synthetic analogs of naturally occurring and non-naturally occurring acyl-homoserine lactone (AHL) analogs, and methods of synthesizing and using these compounds.Type: ApplicationFiled: December 17, 2009Publication date: December 2, 2010Inventors: Helen E. BLACKWELL, Grant D. Geske, Rachel Wezeman
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Publication number: 20100292261Abstract: In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.Type: ApplicationFiled: May 3, 2007Publication date: November 18, 2010Applicant: SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATIONInventors: Je-Yong Yoon, Cheol-Jin Kim, Jae-Eun Kim, Hyung-Yeon Park
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Publication number: 20100292321Abstract: Compositions and methods suitable for killing bacteria and controlling biofilms comprising one or more microorganisms are provided wherein molecules capable of emulating cell-to-cell signal molecules of the microorganisms are utilized.Type: ApplicationFiled: June 29, 2007Publication date: November 18, 2010Applicant: ALBEMARLE CORPORATIONInventors: Joe D. Sauer, Christopher J. Nalepa, William S. Pickrell, Richmond M. Starrett, Hassan Y. Elnagar, George W. Cook, Robert M. Moore, Jennifer Moore
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Publication number: 20100286261Abstract: The substituted N-acyl homoserine lactones have the formula (I) wherein R is a saturated or unsaturated straight chain or branched chain aliphatic hydrocarbyl group containing from 5 to 14 carbon atoms; R2 is H or a 1-4C alkyl group; R3 is H or F; and any enantiomer thereof. These compounds exhibit immunosuppressant activity while exhibiting reduced biosensor (autoinducer) activity compared to known N-acyl homoserine lactones.Type: ApplicationFiled: May 22, 2007Publication date: November 11, 2010Inventors: David Idris Pritchard, Siri Ram Chhabra
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Publication number: 20100160371Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: November 17, 2009Publication date: June 24, 2010Inventors: Gerald RANGES, William Scott, Michael Bombara, Deborah Rauner, Aniko Redman, Roger Smith, Holger Paulsen, David Gunn, Jinshan Chen, Joel Renick
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Publication number: 20100160423Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.Type: ApplicationFiled: December 21, 2009Publication date: June 24, 2010Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
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Publication number: 20100137401Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: February 2, 2010Publication date: June 3, 2010Applicant: Incyte CorporationInventors: Wenqing Yao, Colin Zhang, Jincong Zhuo, Meizhong Xu, Konstantinos Agrios, Brian Metcalf
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Publication number: 20100069484Abstract: The present invention involves new and original sigma receptors ligands : (Mono- or di-alkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl)phenyl(s) alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or -alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular bio-chemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action.Type: ApplicationFiled: January 14, 2008Publication date: March 18, 2010Inventor: Alexandre Vamvakides
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Publication number: 20100063088Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Publication number: 20100048545Abstract: The invention relates to 4-hydroxyisoleucine, isomers, analogs, lactones, salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. More particularly, the invention relates to the use of those compounds in the prevention and treatment of disorders of fat metabolism and related syndromes. The invention further relates to the use of those compounds in the prevention and treatment of obesity and related syndromes including, but not limited to, the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight, and more particularly loss of body fat.Type: ApplicationFiled: March 22, 2007Publication date: February 25, 2010Applicant: INNODIA INC.Inventors: Lucie Jette, Patricia Mcnicol, Manjinder Gill, André Marette
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Patent number: 7655681Abstract: A method of treating or preventing Obstructive Sleep Apnea (OSA) comprises the administration of a pharmacologically effective amount of zonisamide to a patient in need thereof, with the proviso that OSA caused by external mechanical obstruction of the airways, such as by mucus, is excluded. Also disclosed is the use of zonisamide for the manufacture of a medicament useful in the treatment; a protective patch comprising zonisamide and a pharmaceutically acceptable carrier for transdermal or transmucosal administration to a person suffering from OSA; and the use of zonisamide for the manufacture of a diagnostic device, kit or composition for the diagnosis of sleep disordered breathing.Type: GrantFiled: February 15, 2005Date of Patent: February 2, 2010Inventors: Ludger Grote, Kaj Stenlof, Jan Hedner
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Publication number: 20100016424Abstract: The present invention provides analogues of autoinducer molecules that are derivatized to allow their attachment to other molecules and surfaces. Libraries of the autoinducer analogues are also contemplated. Also provided are methods for using the compounds of the invention to produce compositions, such as immunoconjugates, antibodies and vaccines, which are useful for treating and preventing disease states in a subject. The compositions of the invention are also useful in various assays, including assessing the autoinducer load in a subject.Type: ApplicationFiled: July 13, 2009Publication date: January 21, 2010Applicant: Ensisheim Partners LLCInventor: Steven C. Quay
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Publication number: 20090221643Abstract: Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl and thienyl optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.Type: ApplicationFiled: February 6, 2007Publication date: September 3, 2009Inventors: Kevin Michael Thewlis, Simon Edward Ward
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Publication number: 20090203641Abstract: Moenomycin inhibits bacterial growth by clocking the transglycosylase activity of class A penicillin-binding proteins (PBPs), which are key enzymes in bacterial cell wall synthesis. The binding affinities of moenomycin A with various truncated PBPs were compared showing that the transmembrane domain is important for moenomycin binding. Full-length class-A PBPs from 16 bacterial species were produced, and their binding activities showed a correlation with the antimicrobial activity of moenomycin against Enterococcus faecalis and Staphylococcus aureus. Moreover, a fluorescence anisotropy-based high-throughput assay was developed and used successfully for identification of transglycosylase inhibitors.Type: ApplicationFiled: January 15, 2009Publication date: August 13, 2009Inventors: Chi-Huey Wong, Ting-Jen Cheng, Che Alex Ma, Wei-Chieh Cheng
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Publication number: 20090176836Abstract: The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: July 28, 2006Publication date: July 9, 2009Inventors: Philippe G. Nantermet, Joseph P. Vacca
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Publication number: 20090170902Abstract: Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl, furanyl and thienyl, each optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.Type: ApplicationFiled: February 6, 2007Publication date: July 2, 2009Inventors: Daniele Andreotti, Simon Edward Ward
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Publication number: 20090156652Abstract: A therapeutic agent for impaired gastric accommodation which contains as an active ingredient a compound represented by the general formula (1): (wherein R1 represents a hydrogen atom, a hydroxyl group or a halogen atom; A represents a furyl group, a thienyl group, a thiazolyl group or an oxazolyl group; R2 and R3 each represents an alkyl group with 1 to 5 carbon atoms; and n represents an integer of 2 to 4), or an acid addition salt thereof. Use of a therapeutic agent of the present invention greatly alleviates symptoms caused by said disorders, such as early satiety and bloating, because it improves relaxation of gastric fundus and impaired gastric accommodation.Type: ApplicationFiled: February 17, 2009Publication date: June 18, 2009Applicant: ZERIA PHARMACEUTICAL CO., LTD.Inventors: Yugo Matsunaga, Shigeru Ueki, Hiroki Kato, Shiro Kobayashi
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Patent number: 7541379Abstract: The present invention relates to di(amido-substituted)-heteroarene compounds and their use as osteoblastogenesis agents. The invention provides a method for inducing osteogenesis in a precursor cell capable of undergoing osteogenesis.Type: GrantFiled: October 10, 2006Date of Patent: June 2, 2009Assignee: The University of Hong KongInventors: Chi Ming Che, Annie Wai-Chee Kung
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Publication number: 20090076062Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: September 13, 2007Publication date: March 19, 2009Inventors: Juergen Klaus Maibaum, Daniel Kaspar Baeschlin, Holger Sellner
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Publication number: 20080312319Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.Type: ApplicationFiled: March 19, 2008Publication date: December 18, 2008Inventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. O'Neill
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Publication number: 20080261952Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
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Publication number: 20080146445Abstract: The present invention concerns nematicidal compounds, their formulation as nematicidal composition and their use for controlling nematodes, preferably plant parasitic nematodes.Type: ApplicationFiled: December 16, 2005Publication date: June 19, 2008Applicant: Devgen NVInventors: Jan Octaaf De Kerpel, Dirk Leysen
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Patent number: 7371779Abstract: A composition having immunosuppressant activity comprises at least one compound of the formula (I) in which R is an acyl group of the formula (II) wherein one of R1 and R2 is H and the other is selected from OR4, SR4 and NHR4, wherein R4 is H or 1-6C alkyl, or R1 and R2 together with the carbon atom to which they are joined form a keto group, and R3 is a straight or branched chain, saturated or unsaturated aliphatic hydrocarbyl group containing from 8 to 11 carbon atoms and is optionally substituted by one or more substituent groups selected from halo, 1-6C alkoxy, carboxy, 1-6C alkoxycarbonyl and NR5R6 wherein each of R5 and R6 is selected from H and 1-6C alkyl or R5 and R6 together with the N atom form a morpholino or piperazino group, or any enantiomer thereof; and at least one compound of the formula (III): wherein R7 is a straight or branched chain, saturated or ethylenically-unsaturated aliphatic hydrocarbyl group containing from 1 to 18 carbon atoms which may optionally be substituted by one or more suType: GrantFiled: July 3, 2002Date of Patent: May 13, 2008Assignee: The Secretary of State for Defense Science and TechnologyInventor: David Idris Pritchard
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Patent number: 7202274Abstract: A compound represented by the following formula (I) wherein R1 is a lower alkyl group, R2 is a hydrogen, a halogen, a cyano group, a lower alkyl group or a lower alkoxy group, and n is 0 or 1, which has a calpain inhibitory activity, is provided.Type: GrantFiled: March 14, 2003Date of Patent: April 10, 2007Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Masayuki Nakamura, Jun Inoue
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Patent number: 7176201Abstract: Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH2, O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R1 and R2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R1 and R2 is absent, and that if Z is N, optionally R1 and R2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which theyType: GrantFiled: October 7, 2003Date of Patent: February 13, 2007Assignees: The Regents of the University of California, Universita Degli Studi di Parma, Universita Degli Studi di UrbinoInventors: Daniele Piomelli, Andrea Duranti, Andrea Tontini, Marco Mor, Giorgio Tarzia
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Patent number: 7132448Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative or a chloronicotinyl insecticide and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: August 3, 2004Date of Patent: November 7, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Albert Ahn, Richard Fisher, Christine M. Monro, Pierre R. Joseph
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 7049338Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumor growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.Type: GrantFiled: March 9, 2005Date of Patent: May 23, 2006Inventors: Washington Odur Ayuko, Michael John Tisdale, Eric Lattmann
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6984662Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: November 3, 2003Date of Patent: January 10, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Christine M. Monro, Pierre R. Joseph, Albert Ahn, Richard Fisher