Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Publication number: 20140336200Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: July 23, 2014Publication date: November 13, 2014Applicant: ADAMED SP. Z O.O.Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
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Patent number: 8883795Abstract: Provided for in the instant application are two additional polymorphic forms of rifaximin; namely substantially pure APO-I and APO-II. Also provided are processes for preparing substantially pure APO-I and APO-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by Escherichia coli bacteria, as well as in the treatment of irritable bowel syndrome, diverticular disease, hepatic encephalopathy, pyogenic skin infections and as an antibacterial prophylactic prior to colon surgery.Type: GrantFiled: June 16, 2011Date of Patent: November 11, 2014Assignee: Apotex Pharmachem Inc.Inventors: Kiran Kumar Kothakonda, Allan W. Rey
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Publication number: 20140323467Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: May 23, 2014Publication date: October 30, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
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Publication number: 20140323412Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: October 30, 2014Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
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Publication number: 20140309213Abstract: This invention relates to compounds of Formula I-VI having the following general structure: Z1—Y1—(CH2)n1—R—(CH2)n2—Y2—Z2 wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with —(CH2)n1— and —(CH2)n2—, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: October 16, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Reynalda K. DeJesus, Haifeng Tang, Barbara Pio, Aurash Shahripour, Kevin M. Belyk, Harry R. Chobanian, Yan Guo, Jessica L. Frie, Zhi-Cai Shi, Helen Chen, Timothy A. Blizzard, Brian Cato
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Publication number: 20140303155Abstract: The invention relates to pharmacology and medicine, more particularly to novel pharmaceutical compositions and pharmaceutical kits for treating bacterial infections, and to novel method for treating diseases caused by bacterial infections including tuberculosis. The pharmaceutical composition is disclosed comprising Rifamycin and interferon inducer in pharmacologically effective doses, and also pharmaceutical kit for treating diseases caused by bacterial and healthcare acquired infections, comprising pharmacologically effective doses of Rifamycin in the form of a tablet, a capsule or an injection, interferon inducer in the form of a tablet, a capsule or an injection, and instruction for administration of the components of this pharmaceutical kit.Type: ApplicationFiled: October 25, 2012Publication date: October 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Publication number: 20140296232Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicants: Massachusetts General Hospital, The Broad Institute, Inc.Inventors: Deborah Hung, Sarah Stanley, Tomohiko Kawate, Noriakie Iwase, Motohisa Shimizu
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Publication number: 20140296225Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: ApplicationFiled: October 22, 2012Publication date: October 2, 2014Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
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Publication number: 20140296249Abstract: Dopamine D3 receptor antagonists and partial agonists are known to modulate the reinforcing and drug-seeking effects induced by cocaine and other abused substances. By introducing functionality into the butylamide linking chain of the 4-phenylpiperazine class of ligands, improved D3 receptor affinity and selectivity, as well as water solubility, is achieved. A series of linking-chain derivatives are disclosed wherein functionality such as OH, OAc, and cis or trans-cyclopropyl groups have been introduced into the linking chain. In general, these modifications are well tolerated at D3 receptors and achieve high selectivity over D2 and D4 receptors.Type: ApplicationFiled: April 30, 2014Publication date: October 2, 2014Applicants: The United States of America, as Represented by the Secretary, Department of Health and Human Serv, THE UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE AT FORT WORTHInventors: Amy Hauck Newman, Peter Grundt, George C. Cyriac, Robert Luedtke, Jianjing Cao
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Publication number: 20140296134Abstract: Embodiments include methods for generating a metabolite profile of a stool sample and methods of assessing the status of a subject using the metabolic profile derived from a stool sample.Type: ApplicationFiled: November 8, 2012Publication date: October 2, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Tor Savidge, Sara Dann
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Publication number: 20140288088Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: ApplicationFiled: October 22, 2012Publication date: September 25, 2014Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
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Publication number: 20140271897Abstract: This invention provide novel compositions, methods and devices for sustained drug delivery. The microencapsulated sustained drug delivery compositions are deposited using oscillating needle apparatus oscillating at 10-12000 minutes per minutes. The injected compositions may undergo variety of physical chemical changes upon deposition. The physical and chemical changes enables improved drug encapsulation and sustained drug release. Also described are new methods to form polymer microparticles or polymer films/implants in situ inside the tissue. The invention also describes colored biodegradable microparticle based compositions wherein the compositions comprise drug encapsulated microparticles and coloring agent encapsulated microparticles mixed in any proportion. Medical applications of the compositions and methods described in this invention are also described.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Pathak Holding, LLCInventor: Chandrashekhar P. Pathak
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Publication number: 20140271822Abstract: The present invention provides compositions for the treatment of cancer. The compositions include liposomes containing a phosphatidylcholine lipid, a sterol, a PEG-lipid, and a taxane. The PEG-lipid constitutes from about 2 to about 8 mol % of the lipids in the liposome. The taxane is docetaxel esterified at the 2?-O position with a heterocyclyl-(C2-5alkanoic acid). Methods for preparation of liposomal taxanes and treatment of cancer with liposomal taxanes are also disclosed.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Mallinckrodt LLCInventors: William McGhee, James Blackledge, Margaret Grapperhaus
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Publication number: 20140256741Abstract: The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.Type: ApplicationFiled: August 6, 2012Publication date: September 11, 2014Applicant: Cardero Therapeutics, Inc.Inventors: Cyrus K. Becker, George F. Schreiner, Sundeep Dugar, Dinesh Mahajan
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Publication number: 20140256664Abstract: The present application discloses rapid Mycobacterium tuberculosis drug susceptibility utilizing real-time PCR of mycobacteriophage D29 DNA. One protocol involves culturing Tb isolates for 48 hours with and without drugs at critical concentrations, followed by incubation with 103 pfu/ml of D29 mycobacteriophage for 24 hours and then real-time PCR. Many drugs can be incubated instantly with Tb and phage. The change in phage DNA real-time PCR cycle threshold (Ct) between control Tb and Tb treated with drugs was calculated and correlated with conventional agar proportion drug susceptibility results. Specifically, 9 susceptible clinical isolates, 22 MDR, and 1 XDR Tb strains were used and Ct control?Ct drug cutoffs of between +0.3 and ?6.0 yielded 422/429 (98%) accurate results for the drugs tested. The Ct values correlated with isolate minimal inhibitory concentration (MIC) for most agents. This D29 qPCR assay offers a rapid, accurate, 1-3 day phenotypic drug susceptibility test.Type: ApplicationFiled: May 11, 2012Publication date: September 11, 2014Applicant: University of Virginia Patent FoundationInventors: Eric R. Houpt, Kimberly A. Kelly, Suporn Pholwat
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Publication number: 20140256616Abstract: Modified green tea polyphenols and methods of their use are provided. One aspect provides compounds and compositions containing green tea polyphenols with one on more ester-linked fatty acids.Type: ApplicationFiled: May 19, 2014Publication date: September 11, 2014Applicant: Georgia Regents Research Institute, Inc.Inventor: Stephen D. Hsu
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Publication number: 20140249150Abstract: The invention described herein features methods, compositions, and kits that utilize activators of pyruvate kinase M2 (PKM2) for the treatment or amelioration of disorders related to PKM2 function and characterized by abnormally low levels of serine.Type: ApplicationFiled: October 12, 2012Publication date: September 4, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Charles Kung
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Publication number: 20140249155Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: ApplicationFiled: March 23, 2014Publication date: September 4, 2014Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140243352Abstract: A pharmaceutical composition that includes a carbamoyloxy arylalkanoyl arylpiperazine compound and effectively prevents or treats diabetic nephropathy, diabetic neuropathy, diabetic vascular complications, hyperlipidemia, coronary artery disease, or inflammation.Type: ApplicationFiled: January 24, 2014Publication date: August 28, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Hong Sik MOON, Han Ju YI, Eun Hee CHAE, Sang Mi CHAE, Hye Won SHIN
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Publication number: 20140242097Abstract: A method for promoting entry of an agent (introduced agent) into a cell, the method comprising the step of complexing the introduced agent in the presence of an entry-promoting agent and then exposing to cells, wherein the entry-promoting agent comprises a linear and/or branched or cyclic polymonoguanide/polyguanidine, polybiguanide, analogue or derivative thereof according to the following Formula 1a & b. The method also provides a means for formation of nanoparticles formed between the entry promoting agent and the introduced agent.Type: ApplicationFiled: October 11, 2012Publication date: August 28, 2014Applicant: THE ROYAL VETERINARY COLLEGEInventors: Liam Good, Kantaraja Chindera, Valentina Gburcik
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Patent number: 8815852Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: GrantFiled: April 30, 2008Date of Patent: August 26, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Ki Ho Lee, Han Ju Yi, Hyeon Cho, Dae Joong Im, Eun Hee Chae, Yeon Jung Choi
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Publication number: 20140234410Abstract: A pharmaceutical formulation comprises a plurality of seamless minicapsules having a diameter from 0.5 mm to 5 mm, at least some of the minicapsules containing a methyxanthine as one active ingredient, and at least some of the minicapsules containing a corticosteroid as another active ingredient.Type: ApplicationFiled: April 23, 2014Publication date: August 21, 2014Applicant: SIGMOID PHARMA LTD.Inventors: Joey Moodley, Ivan Coulter
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Publication number: 20140235649Abstract: A method of treating a mammalian subject afflicted with a disease characterized by a loss of protein function caused by a genetic abnormality associated with the disease comprising administering to the subject a therapeutically effective amount of a protein phosphatase 2A inhibitor or a histone deacetylase inhibitor.Type: ApplicationFiled: May 24, 2012Publication date: August 21, 2014Applicant: LIXTE BIOTECHNOLOGY, INC.Inventors: John S. Kovach, Zhengping Zhuang, Jie Lu, Chunzhang Yang, Russell Lonser
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Publication number: 20140228312Abstract: The present invention relates to a composition comprising: an antibiotic selected from the group consisting of an aminoglycoside antibiotic, a beta-lactam antibiotic, an ansamycin antibiotic, a macrolide antibiotic, a sulfonamide antibiotic, a quinolone antibiotic, an oxazolidinone antibiotic, a glycopeptide antibiotic, and a mixture thereof; and a fatty acid represented by formula (I), a stereoisomer, a salt or an ester thereof, wherein R1 is a substituted or unsubstituted aliphatic group.Type: ApplicationFiled: October 1, 2012Publication date: August 14, 2014Inventors: Lianhui Zhang, Yinyue Deng
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Publication number: 20140220109Abstract: A process for producing a small-sized, lipid-based cochleates. Cochleates are derived from liposomes which are suspended in an aqueous two-phase polymer solution, enabling the differential partitioning of polar molecule based-structures by phase separation. The liposome-containing two-phase polymer solution, treated with positively charged molecules such as Ca2+ or Zn2+, forms a cochleate precipitate of a particle size less than one micron. The process may be used to produce cochleates containing biologically relevant molecules.Type: ApplicationFiled: December 31, 2013Publication date: August 7, 2014Applicant: Rutgers, The State University of New JerseyInventors: Leila Zarif, Tuo Jin, Ignacio Segarra, Raphael J. Mannino
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Publication number: 20140221349Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Publication number: 20140220098Abstract: In some embodiments, a device (102) may include a mesh having at least one bioresorbable polymer coating. The coating may comprise at least one active agent which is eluted over time. The device (102) may at least partially cover at least a portion of an implanted transdermal medical device (100).Type: ApplicationFiled: July 20, 2012Publication date: August 7, 2014Applicant: TYRX, INC.Inventors: Daniel Jeremy Lerner, William McJames, Randy Mansfield, Robert S. White
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Patent number: 8790691Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: GrantFiled: May 26, 2009Date of Patent: July 29, 2014Assignee: The University of British ColumbiaInventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20140187554Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: ApplicationFiled: May 16, 2012Publication date: July 3, 2014Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Publication number: 20140179694Abstract: Described herein are methods for using compounds that activate pyruvate kinase.Type: ApplicationFiled: May 3, 2012Publication date: June 26, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20140171442Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.Type: ApplicationFiled: July 31, 2012Publication date: June 19, 2014Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
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Publication number: 20140171445Abstract: The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.Type: ApplicationFiled: August 2, 2012Publication date: June 19, 2014Applicant: The USA, as represented by the Secretary, Department of Health and Human ServicesInventors: Katrin Mayer-Barber, Bruno de Bezerril Andrade, Alan Sher, Daniel Leo Barber
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Publication number: 20140155261Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 4, 2012Publication date: June 5, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140155369Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.Type: ApplicationFiled: January 16, 2014Publication date: June 5, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Izumi KAMO, Tadatoshi HASHIMOTO
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Publication number: 20140155411Abstract: The present application includes biomarkers, methods, devices, reagents, systems, and kits for the detection, treatment and diagnosis of tuberculosis (TB). In one aspect, the present application includes the identification of biomarkers that can be used alone or in various combinations for the detection of TB, including those set forth in Tables 1, 2, 4, 5, and 8 to 12. In another aspect, the application provides biomarkers that can be used alone or in various combinations to diagnose or prognose TB or follow treatment response. In another aspect, methods are provided for diagnosing TB in an individual, where the methods include detecting, in a biological sample from an individual, at least one biomarker value corresponding to at least one biomarker selected from the group of biomarkers provided in Tables 1, 2, 4, 5, and 8 to 12, wherein the individual is classified as having TB, or the likelihood of the individual having TB is determined, based on the at least one biomarker value.Type: ApplicationFiled: April 12, 2013Publication date: June 5, 2014Applicant: SomaLogic, Inc.Inventor: SomaLogic, Inc.
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Patent number: 8741904Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: July 25, 2013Date of Patent: June 3, 2014Assignee: Alfa Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
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Publication number: 20140148444Abstract: Described herein are compounds that activate pyruvate kinase, for use in a method for increasing lifetime of the red blood cells, for regulating 2,3-diphosphoglycerate levels in blood and for treating sickle cell anemia.Type: ApplicationFiled: May 3, 2012Publication date: May 29, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventor: Shin-San M. Su
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Patent number: 8735391Abstract: A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.Type: GrantFiled: September 25, 2009Date of Patent: May 27, 2014Assignee: University of KansasInventors: Jeffrey Aube, Bryan L. Roth, Partha Ghosh, Kevin J. Frankowski
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Publication number: 20140142115Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: January 24, 2014Publication date: May 22, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Yuping Zhu, Aurash Shahripour, Haifeng Tang, Lihu Yang, Shawn P. Walsh, Nardos H. Teumelsan
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Publication number: 20140142114Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Applicant: Merial LimitedInventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
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Patent number: 8729060Abstract: The invention provides compounds of formula (I) wherein A, B, R1, F, G, n, n? and the dotted line have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.Type: GrantFiled: August 1, 2008Date of Patent: May 20, 2014Assignee: Rutgers, the State University of New JerseyInventors: Edmond J. LaVoie, Joseph E. Rice, Satyanarayana Mavurapu
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Patent number: 8722683Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 10, 2012Date of Patent: May 13, 2014Assignee: Hoffmann LA-Roche Inc.Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20140127294Abstract: Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not contact directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin.Type: ApplicationFiled: April 10, 2012Publication date: May 8, 2014Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Maojian Gu, Qilan Zheng, Chao Xu, Ning Li, Guixian Chen, Lan Zheng, Min Wang, Lintao Jiang
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Publication number: 20140120038Abstract: Compositions of nanoparticles and targeting moieties for imaging and treating Chlamydial infection are provided, including nanoparticles conjugated to folic acid and comprising at least one antibiotic effective against Chlamydia.Type: ApplicationFiled: January 2, 2014Publication date: May 1, 2014Applicant: Wayne State UniversityInventors: Jayanth Panyam, Judith A. Whittum-Hudson, Alan P. Hudson
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Publication number: 20140120191Abstract: Disclosed herein are methods and compositions for treating a disorder associated with sequestered bacteria in a mammalian subject comprising the step of administering to the subject a combination therapy comprising streptolysin O and antibiotic therapy in an amount effective to treat the disorder.Type: ApplicationFiled: January 26, 2012Publication date: May 1, 2014Applicant: BEECH TREE LABS INC.Inventor: John McMichael
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Patent number: 8685978Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.Type: GrantFiled: July 26, 2010Date of Patent: April 1, 2014Assignee: University of Tennessee Research FoundationInventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, Vnr Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
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Publication number: 20140088078Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: May 7, 2012Publication date: March 27, 2014Applicant: ZAFGEN, Inc.Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Publication number: 20140088095Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: September 16, 2013Publication date: March 27, 2014Applicant: SK Biopharmaceuticals Co., Ltd.Inventors: Byong Sung KWAK, Hong Sik MOON, Han-Ju YI, Young Soon KANG, Dae Joong IM, Eun Hee CHAE, Sang Mi CHAE, Ki Ho LEE
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Publication number: 20140079760Abstract: The present invention relates to polymers modified to increase their resorbability. In particular, the polymers of the invention have phenyl ester side chains which are good leaving groups and which thereby increase the resorption rate of the polymer relative to the same polymer, for example, bearing a comparable amount of an alkyl ester side chain. Such polymers are generally water insoluble, but when modified are able to solubilize drugs and upon degradation and resorption, release those in a physiological environment in a controlled and/or sustained manner.Type: ApplicationFiled: November 26, 2013Publication date: March 20, 2014Applicant: TYRX Pharma, Inc.Inventors: Arthur Schwartz, Satish Pulapura, Sarita Nethula