Plural Carbocyclic Rings Bonded Directly To The Same Acyclic Carbon Atom Which Is Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/255.04)
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Publication number: 20120156259Abstract: The present invention relates to biodegradable polyethylene glycol based water-insoluble hydrogels comprising backbone moieties which are interconnected by hydrolytically degradable bonds, the backbone moieties further comprising reactive functional groups, wherein the water-insoluble hydrogel is further characterized in that the ratio between the time period for the complete degradation of the hydrogel by hydrolysis of the degradable bonds into water-soluble degradation products comprising one or more backbone moieties and the time period for the release of the first 10 mol-% of water-soluble degradation products comprising one or more backbone moieties based on the total amount of backbone moieties in the hydrogel is greater than 1 and equal to or less than 2. The invention further relates to conjugates of such hydrogels with ligands or ligating groups, prodrugs and pharmaceutical compositions as well as their use in a medicament.Type: ApplicationFiled: July 30, 2010Publication date: June 21, 2012Applicant: ASCENDIS PHARMA A/SInventors: Harald Rau, Ulrich Hersel, Mathias Krusch, Dirk Vetter, Tobias Voigt
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Publication number: 20120157474Abstract: The present invention is based on the discovery of a cell-based system to identify novel modulators of splicing or splicing dependent processes. The cell-based system of the present invention utilizes a fast and highly sensitive reporter, that responds to defects in the splicing machinery itself and is sensitive to changes in the signals that regulate splicing dependent processes such as those that modulate the EJC, splicing-dependent export, localization or translation efficiency. The present invention further uses the cell-based screen to identify several small molecules that modulate both constitutive and alternative splicing. Accordingly, the present invention includes general or alternative splicing inhibitors identified using the assay described herein. The present invention also provides methods of treating a subject having a condition associated with aberrant target RNA expression.Type: ApplicationFiled: May 21, 2010Publication date: June 21, 2012Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIAInventors: Gideon Dreyfuss, Ihab Younis, Lili Wan
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Publication number: 20120157475Abstract: The use of cinnarizine and dimenhydrinate or their physiologically compatible salts in combination is described for the treatment of vertigo of any genesis.Type: ApplicationFiled: February 27, 2012Publication date: June 21, 2012Applicant: HENNIG ARZNEIMITTEL GMBH & CO. KGInventor: Helga Schleenhain
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Publication number: 20120149717Abstract: Compounds of general formula: as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain, depression and anxiety.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Inventors: William Brown, Andrew Griffin, Thomas Hudzik, Carla Maciag, Gennady Smagin, Christopher Walpole
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Publication number: 20120142704Abstract: A pharmaceutical solution comprising cetirizine hydrochloride, an alcohol compound with less than 3 carbon atoms, a preservative and urea is disclosed. The cetirizine hydrochloride is in racemic form or in levo form.Type: ApplicationFiled: August 11, 2010Publication date: June 7, 2012Applicant: LUN BETTER PHARMACEUTICAL CO., LTDInventor: Zhiquan Zhao
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Publication number: 20120136007Abstract: Model systems have shown that shifting a cell's reliance from oxidative phosphorylation (OXPHOS) to glycolysis can protect against cell death. Exploiting the therapeutic potential of this strategy, however, has been limited by the lack of clinically safe agents that remodel energy metabolism. The present invention identifies non-toxic small molecules (e.g., drug-like compounds) that are capable of modulating oxidative metabolism. One identified compound comprises meclizine. As described herein, meclizine, and its enantiomer S-meclizine, redirects OXPHOS to glycolysis. Such compounds could be protective or therapeutic in degenerative disorders such as diabetes, Huntington's, Parkinson's, and Alzheimer's disease and/or ischemic disorders including, but not limited to, stroke, heart attack, or reperfusion injuries.Type: ApplicationFiled: May 14, 2010Publication date: May 31, 2012Applicant: The General Hospital CorporationInventors: Vamsi K. Mootha, Vishal Gohil, Sunil Sheth, Yuhua Ji
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Patent number: 8183244Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: May 12, 2009Date of Patent: May 22, 2012Assignee: Amgen Inc.Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Publication number: 20120108608Abstract: Methods of treating or preventing a vertigo, nausea, or vomiting condition comprising injecting a subject with a pharmaceutically acceptable formulation consisting essentially of an effective amount of meclizine or a pharmaceutically acceptable salt thereof, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 are disclosed. An injectable pharmaceutical formulation for treating or preventing a vertigo, nausea, or vomiting condition consisting essentially of an effective amount of meclizine, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 is also disclosed.Type: ApplicationFiled: January 12, 2012Publication date: May 3, 2012Inventors: WALKER ANDERSON LONG, EDWIN CURRAN MURPHY, III
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Patent number: 8163734Abstract: The invention concerns the use of a mast cell activation- or degranulation-blocking agent in the manufacture of a medicament for preventing and treating cerebral complications caused by thrombolytic treatment. The invention also relates to treatment of patients suffering from cerebral complications associated with thrombolysis. Further, the invention provides thrombolytic compositions comprising a mast cell degranulation-blocking and/or mast cell activation-blocking agent present in a therapeutically effective amount to prevent or reduce any cerebral complications caused by the active thrombolytic component.Type: GrantFiled: February 13, 2004Date of Patent: April 24, 2012Inventors: Perttu J. Lindsberg, Marja-Liisa Karjalainen-Lindsberg, Turgut Tatlisumak, Daniel Strbian, Petri Kovanen
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Patent number: 8138192Abstract: Methods of treating or preventing a vertigo, nausea, or vomiting condition comprising injecting a subject with a pharmaceutically acceptable formulation consisting essentially of an effective amount of meclizine or a pharmaceutically acceptable salt thereof, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 are disclosed. An injectable pharmaceutical formulation for treating or preventing a vertigo, nausea, or vomiting condition consisting essentially of an effective amount of meclizine, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 is also disclosed.Type: GrantFiled: October 31, 2007Date of Patent: March 20, 2012Assignee: Genebiology, Inc.Inventors: Walker Anderson Long, Edwin Curran Murphy, III
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Publication number: 20120058962Abstract: A buccal and/or sublingual formulation comprising one or more active compounds; and a buccal matrix which releases the active compounds at a predetermined rate for transport across the buccal and/or sublingual membranes, wherein the rate of release of the active compounds is either (A) the same or substantially the same rate at which the active compounds are transported across the buccal and/or sublingual membranes; or (B) a rate which releases the active compounds over an extended period as required by the therapeutic affect or treatment window for those active compounds.Type: ApplicationFiled: May 20, 2010Publication date: March 8, 2012Applicant: Lingual Conseqna Pty Ltd.Inventors: Alistair Cumming, Lance Sparrow, David Kannar
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Patent number: 8129393Abstract: Compounds of general formula: as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain, depression and anxiety.Type: GrantFiled: December 22, 2009Date of Patent: March 6, 2012Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Thomas Hudzik, Carla Maciag, Gennady Smagin, Christopher Walpole
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Publication number: 20120028993Abstract: The present invention describes a Composition, comprising one or more compounds selected from the group consisting of a) compound (I) which is ethacrynic acid bezafibrate, fenofibrate, and/or griseofulvin, b) compound (II), which is ciclopirox ciclopirox olamine, octopirox, and/or cinnarizine, c) mixtures of compound (I) and compound (II), or pharmaceutically acceptable derivatives thereof for the treatment of cancer. The present invention is further directed to the use of said compounds or a mixture of compounds for the manufacture of a medicament for the treatment of cancer and to the use of said compound in a method for treating cancers in animals and humans.Type: ApplicationFiled: January 13, 2009Publication date: February 2, 2012Inventor: Ingo Schmidt-Wolf
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Publication number: 20120027879Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: August 3, 2011Publication date: February 2, 2012Inventor: Harry A. DUGGER, III
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Publication number: 20120028992Abstract: Disclosed are pharmaceutical compositions for and methods of preventing or treating acute and/or chronic cardiac arrhythmias in a mammal, including terminating acute episodes of cardiac arrhythmia, restoring normal sinus rhythm, preventing recurrence of cardiac arrhythmia and/or maintaining normal sinus rhythm, which contain a combination of 1-[2-[(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.Type: ApplicationFiled: August 2, 2010Publication date: February 2, 2012Inventor: Arthur M. Brown
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Publication number: 20120024743Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.Type: ApplicationFiled: February 5, 2010Publication date: February 2, 2012Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Endre Mikulasik, Patrik Fazekas
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Publication number: 20120022079Abstract: The invention relates to a process for producing formulations of sparingly water-soluble substances, said sparingly soluble substances being present in amorphous embedded form in a copolymer, and said copolymer being obtained by free-radically initiated polymerization of a mixture of i) 30 to 80% by weight of N-vinyllactam, ii) 10 to 50% by weight of vinyl acetate, and iii) 10 to 50% by weight of a polyether, with the proviso that the sum of components i), ii) and iii) equals 100% by weight, which comprises embedding the sparingly soluble substance into the copolymer at temperatures above the melting point of the sparingly soluble substances.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: BASF SEInventors: Kathrin Meyer-Böehm, Rainer Dobrawa, Stefan Fischer, Karl Kolter
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Publication number: 20120010216Abstract: Disclosed embodiments are related to compositions of vanoxerine (GBR 12909), including compositions of vanoxerine and one or more diluents, disintegrants, binders and lubricants, and the processes for their preparation thereof.Type: ApplicationFiled: July 6, 2010Publication date: January 12, 2012Inventor: Arthur M. Brown
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Publication number: 20120010218Abstract: The present invention relates to pharmaceutical compositions for oral administration of active compounds.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Inventors: Domenico Fanara, Monique Berwaer, Anthony Guichaux, Michel Deleers
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Publication number: 20120010217Abstract: Described herein are injectable compositions containing non-sedating or second and third generation antihistamines such as cetirizine/levocetirizine and methods of use thereof. Specifically, methods of treating acute urticaria or angioedema associated with an acute allergic reaction are disclosed. In certain embodiments, the injectable compositions are bioequivalent to currently marketed oral dosage forms with the same number of mg of cetirizine.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Inventor: Jie Du
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Publication number: 20120004242Abstract: The invention relates to (among other things) oligomer-diarylpiperazine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated diarylpiperazine compounds.Type: ApplicationFiled: January 22, 2009Publication date: January 5, 2012Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Jennifer Riggs-Sauthier
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Publication number: 20110318321Abstract: The present invention relates to a controlled release pharmaceutical or food formulation comprising at least one active pharmaceutical or food ingredient dispersed in a mixture of a glycogen with a polysaccharide, and the process for its preparation. The invention also relates to a slow release system represented by a mixture of a glycogen with a polysaccharide, and its use for the preparation of slow release pharmaceutical or food formulations.Type: ApplicationFiled: January 8, 2010Publication date: December 29, 2011Applicant: AZIENDE CHIM.RIUN.ANG.FRANC.A.C.R.A.F. S.p.A.Inventors: Stefano Selva, Leonardo Marchitto, Giovanni Battista Ciottoli, Lorella Ragni, Vincenzo Russo, Elisa Liberati
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Publication number: 20110306603Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: August 23, 2011Publication date: December 15, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110293750Abstract: The present invention is directed to a method of determining the prospects for survival of a melanoma patient. This method involves providing a biological sample from a patient diagnosed with melanoma, determining the level of an indicator of Wnt/?-catenin activation in the sample, comparing the level of the indicator of Wnt/?-catenin activation in the sample against a standard level of the indicator of Wnt/?-catenin activation correlated to survival of melanoma, and determining a patient's prospects for survival of melanoma based on the comparison. The present invention also relates to a method of improving survival of melanoma patients, decreasing metastases in melanoma patients, decreasing proliferation of cancer cells in melanoma patients, decreasing melanoma recurrence in melanoma patients, and/or decreasing tumor size in melanoma patients. This involves selecting melanoma patients and subsequently determining and monitoring therapy based on their level of Wnt/?-catenin activation.Type: ApplicationFiled: November 10, 2009Publication date: December 1, 2011Applicants: YALE UNIVERSITY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Andy J. Chien, David L. Rimm
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Publication number: 20110280939Abstract: The present invention relates to an oral particle including pseudoephedrine hydrochloride and cetirizine dihydrochloride, which primarily includes a nucleus having a diameter ranging 25˜40 mesh, a pseudoephedrine-hydrochloride layer coated outside the nucleus with a coating solution composed of pseudoephedrine hydrochloride, a binder, a lubricant and pure water/alcohol, a release-control layer coated outside the pseudoephedrine-hydrochloride layer, and a cetirizine-dihydrochloride layer coated outside the release-control layer with a coating solution composed of cetirizine dihydrochloride, a binder, a lubricant and pure water/alcohol. Accordingly, by distributing pseudoephedrine hydrochloride and cetirizine dihydrochloride into hundreds of the particles and controlling the dissolution rate with the release-control layer, the particles can perform good absorption efficiency, and quick, stable and long-term edicinal effect.Type: ApplicationFiled: July 5, 2011Publication date: November 17, 2011Applicant: EVEREST PHARM. INDUSTRIAL CO., LTD.Inventor: TA-PING LIAO
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Publication number: 20110281892Abstract: Methods and dosage formulations for the safe treatment of cold, cough, flu, and sinus symptoms in children and adolescents by age and nature of symptoms, and adults and the elderly by age, nature of symptoms, and concomitant patient medical conditions. The method of the present invention comprises the formulation of a cold medication which consists essentially of combinations of a nonsedating or minimally sedating antihistamines with pain relievers and the expectorant, guaifenesin.Type: ApplicationFiled: May 16, 2011Publication date: November 17, 2011Inventor: Bernard Silverman
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Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110256218Abstract: The present invention provides pharmaceutically acceptable compositions for once-daily dosing comprising a piperazine derivative of H1-receptor antagonists, or its salt, and/or solvate and methods of making and using the compositions in the treatment of treating vertigo and other diseases. The present invention also provides once-a-day dosage forms as orally disintegrating tablets comprising compositions of the present invention.Type: ApplicationFiled: January 4, 2011Publication date: October 20, 2011Applicant: EURAND, INC.Inventors: Gopi M. VENKATESH, Troy M. HARMON
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Publication number: 20110251144Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject at least one compound selected from the group consisting of those set forth in Table 1, Table 2, Table 3, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: September 16, 2009Publication date: October 13, 2011Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20110250197Abstract: This invention relates to a combination product or medicament comprising at least one novel substituted pyrrole derivative and one or more dyslipidemic agents, antiobesity agents, antihyperglycaemic agents, anti-inflammatory agents or mixture thereof.Type: ApplicationFiled: June 1, 2011Publication date: October 13, 2011Applicant: RANBAXY LABORATORIESInventors: Jitendra A. SATTIGERI, Vinay S. BANSAL
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Publication number: 20110245244Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.Type: ApplicationFiled: April 4, 2011Publication date: October 6, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
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Publication number: 20110237604Abstract: Disclosed are methods of preventing or treating cardiac arrhythmia comprising administering to a mammal in need thereof, such as a human, an effective amount of vanoxerine (GBR 12909) or a pharmaceutically acceptable salt, derivative or metabolite thereof.Type: ApplicationFiled: June 13, 2011Publication date: September 29, 2011Inventors: Arthur M. Brown, Naresh Chand
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Publication number: 20110237563Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.Type: ApplicationFiled: March 23, 2010Publication date: September 29, 2011Inventor: Dominique Costantini
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Publication number: 20110230496Abstract: A process for preparing pure levocetirizine and salts thereof, e.g., the levocetirizine dihydrochloride, and a pharmaceutical composition comprising levocetirizine dihydrochloride produced by the process are disclosed.Type: ApplicationFiled: August 4, 2008Publication date: September 22, 2011Applicant: CHEMAGIS LTD.Inventors: Lior Zelikovitch, Hila Shaked
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Publication number: 20110217289Abstract: Formulations of sparingly water-soluble active ingredientscomprising carrier particles provided with active ingredient-containing coatings, the sparingly soluble active ingredients being embedded in coatings composed of amphiphilic copolymers, and the coatings being applied in the form of a solvent-free melt.Type: ApplicationFiled: March 4, 2011Publication date: September 8, 2011Applicant: BASF SEInventors: Karl Kolter, Dejan Djuric
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Publication number: 20110207745Abstract: Solid forms comprising salts of 4-{(R)-(3-aminophenyl)[4-(4-fluorobenzyl)piperazin-1-yl]methyl}-N,N-diethylbenzamide, compositions comprising the solid forms, methods of making the solid forms, and methods of their use for the treatment of various diseases and/or disorders are provided herein.Type: ApplicationFiled: November 23, 2010Publication date: August 25, 2011Applicant: ASTRAZENECA ABInventors: Louis Diorazio, Andrew Hornby Dobson, Alison Norton, Anne O'Kearney-McMullan, Dedong Wu
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Publication number: 20110200686Abstract: The present invention is directed to a composition comprising a modulator of the Wnt/?-catenin pathway or a pharmaceutically acceptable salt thereof and an N-cinnamyl-N?-benzhydryl piperazine or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method of treating a neoplastic condition in a subject by administering the modulator of the Wnt/?catenin pathway or a pharmaceutically acceptable salt thereof and an N-cinnamyl-N?-benzhydryl piperazine or a pharmaceutically acceptable salt thereof to the subject under conditions effective to treat a neoplastic disorder.Type: ApplicationFiled: April 7, 2009Publication date: August 18, 2011Applicants: UNIVERSITY OG WASHINGTON, MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass, Andy J. Chien
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Publication number: 20110160186Abstract: The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.Type: ApplicationFiled: June 9, 2009Publication date: June 30, 2011Applicant: Nektar TherapeuticsInventors: Michael A. Eldon, C. Simone Jude-Fishburn, Hema Gursahani, Myong Gyong Lee
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Publication number: 20110144107Abstract: The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.Type: ApplicationFiled: June 11, 2009Publication date: June 16, 2011Applicants: IRM LLC, DANA-FARBER CANCER INSTITUTE INC.Inventors: Arnab K. Chatterjee, Advait Nagle, Tao Wu, Nathanael S. Gray
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Patent number: 7960389Abstract: Compounds of general formula: wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: July 9, 2007Date of Patent: June 14, 2011Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Paul Jones, Daniel Page, Niklas Plobeck, Christopher Walpole
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Publication number: 20110086023Abstract: The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) a mucosal adjuvant, (3) an antihistamine drug and (4) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.Type: ApplicationFiled: December 20, 2010Publication date: April 14, 2011Applicant: Fairfield Clinical Trials LLCInventor: Edward M. Lane
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Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Publication number: 20110071124Abstract: The present invention relates to compounds with activity as inhibitors of sAPP? and A? production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds.Type: ApplicationFiled: August 18, 2010Publication date: March 24, 2011Applicant: The Trustees of Columbia University in the City of New YorkInventors: Tae-wan Kim, Donald W. Landry, Jeremy C. Hwang, Shi Xian Deng, Gangli Gong, Yuli Xie, Yidong Liu, Alison Rinderspacher
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Publication number: 20110070287Abstract: A compressed chewing gum tablet includes at least one compressed chewing gum module, the at least one compressed chewing gum module including a compressed particulate chewing gum composition, which compressed particulate chewing gum composition includes compressed chewing gum particles containing gum base. The content of gum base is at least 5% by weight of the tablet, the chewing gum tablet is provided with a film coating, and the film coating includes liquid flavoring.Type: ApplicationFiled: November 24, 2010Publication date: March 24, 2011Inventors: Bruno Provstgaard Nielsen, Jan Dalhoff, Gitte Lorenzen
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Publication number: 20110034480Abstract: There is described a pharmaceutical composition comprising a therapeutically effective amount of cetirizine, or a pharmaceutically acceptable derivative thereof, and a therapeutically effective amount of one or more compounds selected from the group consisting of a non beta-2-adrenoreceptor agonist; a beta-2-adrenoreceptor agonist and an anti-inflammatory agent; in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.Type: ApplicationFiled: October 3, 2008Publication date: February 10, 2011Inventors: Malcolm Philip Young, Roy Drucker
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Publication number: 20110034446Abstract: The invention features derivatives of R(?)-2-methoxy-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.Type: ApplicationFiled: July 10, 2008Publication date: February 10, 2011Applicant: THE MCLEAN HOSPITAL CORPORATIONInventors: John L. Neumeyer, Yu-Gui Si
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Publication number: 20110027397Abstract: Disclosed are compositions that inhibit brain blood vessel leakage, compositions for treating autism spectrum disorders, methods of treating autism spectrum disorders, and methods of screening for an autism spectrum disorder.Type: ApplicationFiled: August 3, 2009Publication date: February 3, 2011Inventor: Theoharis C. THEOHARIDES
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel