Plural Hetero Atoms In The Tricyclo Ring System Patents (Class 514/291)
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Patent number: 8258299Abstract: The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779. Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.Type: GrantFiled: March 29, 2010Date of Patent: September 4, 2012Assignee: Chungwa Chemical Synthesis & Biotech Co., Ltd.Inventors: Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee
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Publication number: 20120219522Abstract: The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: February 21, 2012Publication date: August 30, 2012Inventor: Ning XI
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Publication number: 20120220619Abstract: A method for treating polycystic kidney disease, comprising administering to a subject in need thereof a therapeutical effective amount of an inosine-5?-monophosphate dehydrogenase inhibitor or a rapamycin derivative.Type: ApplicationFiled: May 3, 2012Publication date: August 30, 2012Inventors: Lothar FÄRBER, Harald GSCHAIDMEIER
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Publication number: 20120214774Abstract: Rapamycin derivatives have interesting effects in the treatment of solid tumours, optionally in combination with a chemotherapeutic agent.Type: ApplicationFiled: February 23, 2012Publication date: August 23, 2012Inventors: Heidi Lane, Terence O'Reilly, Jeanette Marjorie Wood
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Publication number: 20120214836Abstract: A target therapy sensitizer including rapamycin and substituted quinoline is disclosed. In addition, a pharmaceutical composition containing the sensitizer, a target therapy sensitization kit containing the two aforementioned compounds, and a use of a combination of the two aforementioned compounds as a target therapy sensitizer are also disclosed. The application of the target therapy sensitizer, pharmaceutical composition, kit and use is advantageous for improving the treatment effect of target therapies.Type: ApplicationFiled: September 21, 2011Publication date: August 23, 2012Inventor: Pei-Ru Liao
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Publication number: 20120214835Abstract: A cancer therapy sensitizer is disclosed. The cancer therapy sensitizer includes rapamycin and substituted quinoline. The present invention discloses a cancer therapy sensitization kit containing the two aforementioned compounds and a use of a combination of the two aforementioned compounds as a cancer therapy sensitizer as well. The application of the cancer therapy sensitizer, the kit and the use of the present invention is advantageous for improving the treatment effect of cancer therapies.Type: ApplicationFiled: September 21, 2011Publication date: August 23, 2012Inventor: Pei-Ru LIAO
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Publication number: 20120214837Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicants: ExonHit Therapeutics SA, ALLERGAN, INC.Inventors: Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
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Publication number: 20120214834Abstract: An immune enhancement composition is disclosed. The immune enhancement composition includes rapamycin, substituted quinoline and a pharmaceutically acceptable carrier, diluent, excipient or a combination thereof. An immune enhancement kit containing the two aforementioned compounds and a use of a combination containing the two aforementioned compounds as an immune enhancement composition are also disclosed. The application of the composition, kit and use is advantageous for promoting the activity of the immune system.Type: ApplicationFiled: September 21, 2011Publication date: August 23, 2012Inventor: Pei-Ru LIAO
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Publication number: 20120207817Abstract: The invention found that overexpression and activation of ?9-nAChR are associated with tumorigenesis of breast cancer and create a number of small interfering RNAs to inhibit the expression of ?9-nAChR so as to inhibit breast cancer. Therefore, the invention provides small interfering RNAs (siRNAs) for inhibiting expression of ?9-nAChR so as to inhibit breast cancer, methods to prevent/inhibit/treat malignant progression of nicotine-derived-compound-induced breast cancer and method of determining malignant level of such breast cancer.Type: ApplicationFiled: February 14, 2011Publication date: August 16, 2012Applicant: TAIPEI MEDICAL UNIVERSITYInventors: Chia-Hwa Lee, Ching-Shui Huang, Ching-Shyang Chen, Shih-Hsin Tu, Ying-Jan Wang, Yu-Jia Chang, Ka-Wai Tam, Po-Li Wei, Tzu-Chun Cheng, Jan-Show Chu, Li-Ching Chen, Chih-Hsiung Wu, Yuan-Soon Ho
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Publication number: 20120207751Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.Type: ApplicationFiled: April 23, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
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Publication number: 20120208836Abstract: Provided herein are compositions and methods for the treatment of obesity and related disorders, including, but not limited to insulin resistance, diabetes, and hepatic steatosis. For example, in some embodiments, pharmaceutically acceptable compositions and methods are provided employing amlexanox, a derivative thereof, or a pharmaceutically acceptable salt thereof, alone or in combination with other agents and/or medical interventions, for the treatment, prevention, and management of such diseases and conditions.Type: ApplicationFiled: February 14, 2012Publication date: August 16, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Alan R. Saltiel, Stuart Decker
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Publication number: 20120202841Abstract: The present invention relates to a composition for topical administration comprising an ascomycin and a carrier vehicle comprising means to retain water in the outer skin layer and means to hinder water evaporating from the skin.Type: ApplicationFiled: August 5, 2011Publication date: August 9, 2012Applicant: MEDA Pharma SARLInventors: Katrin Kriwet, Dorothea Ledergerber, Jutta Riedl
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Publication number: 20120202842Abstract: The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.Type: ApplicationFiled: November 4, 2011Publication date: August 9, 2012Applicant: Bayer Schering Pharma AGInventors: Martin Hendrix, Frank-Gerhard Böß, Christina Erb, Timo Fleßner, Marja van Kampen, Joachim Luithle, Christoph Methfessel, Welf-Burkhard Wiese
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Patent number: 8236329Abstract: The invention provides active agents, such as paclitaxel, rapamycin, or 17-AAG, encapsulated by safe poly(ethylene glycol)-block-poly(lactic acid) (“PEG-b-PLA”) micelles. The compositions provide effective solubilization of drug combinations, such as paclitaxel, rapamycin, and 17-AAG, as well as others described herein. A significant advantage of PEG-b-PLA as a carrier is that it is less toxic than Cremophor® EL or DMSO, which are used in currently known compositions. Additionally, PEG-b-PLA micelles are easier to handle than DMSO and they do not possess a foul odor, which is a problem with formulations currently in clinical trials. Accordingly, the invention provides stable and biocompatible drug formulations that improve bioavailabilty without causing toxicity. It was also found that larger doses of individual drugs in micelle formulations can be administered compared to non-micelle formulations.Type: GrantFiled: September 24, 2010Date of Patent: August 7, 2012Assignee: Wisconsin Alumni Research FoundationInventor: Glen S. Kwon
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Publication number: 20120196870Abstract: The disclosure relates to methods of treating tuberous sclerosis in a subject, comprising administering a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor to a subject that is diagnosed with, suspected of, or exhibiting symptoms of cancer. In some embodiments, the cancer is tuberous sclerosis. In some embodiments, the mTOR inhibitor is sirolimus and the tyrosine kinase inhibitor is imatinib. In some embodiments, the disclosure relates to a composition comprising an mTOR inhibitor and a tyrosine kinase inhibitor. In some embodiments, the disclosure relates to a composition comprising sirolimus and imatinib.Type: ApplicationFiled: January 25, 2012Publication date: August 2, 2012Applicant: EMORY UNIVERSITYInventor: Jack L. Arbiser
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Publication number: 20120190620Abstract: The present invention discloses methods to identify targets, pathways and molecules regulating purinosomes and their uses for treating pathophysiological disorders associated with purinosomes. Disclosed are methods related to both label-free cellular assays and fluorescence imaging to confirm the regulatory roles of various targets and molecules in purinosome dynamics. Disclosed are methods to classify molecules and the uses of these molecules for different indications. Specifically, the purinosome-disrupting molecules can be used for improved prevention and treatment of cancer development.Type: ApplicationFiled: July 18, 2011Publication date: July 26, 2012Inventors: Stephen Benkovic, Ye Fang, Songon An, Florence Verrier
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Publication number: 20120190705Abstract: The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular tissues. The treatment, inhibition, and/or prevention of choroidal neovasculature (CNV) is provided, along with an animal model for CNV and imaging techniques that permit the screening of potential agents as anti-angiogenesis and anti-CNV agents.Type: ApplicationFiled: March 29, 2012Publication date: July 26, 2012Inventors: Rong Wen, Zhijun Luo, Alan M. Laties
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Publication number: 20120184511Abstract: The invention provides novel pharmaceutical compositions of macrolide immunosuppressants. The compositions comprise a hydrophilic component, a lipophilic component, and an amphiphilic component. Preferably, the compositions are formulated as liquid microemulsion. Furthermore, the invention provides uses of such compositions, such as for the topical treatment of inflammatory and autoimmune diseases. Methods for preparing the compositions are also provided.Type: ApplicationFiled: October 7, 2010Publication date: July 19, 2012Applicant: Novaliq GmbHInventor: Alexandra Sabine Baerbel Goebel
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Publication number: 20120184531Abstract: The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.Type: ApplicationFiled: January 18, 2012Publication date: July 19, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Alan J. HENDERSON, Matthew ISHERWOOD, Chong Yew LEE, Animesh GHOSH, He ZHAO
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Patent number: 8221783Abstract: Described herein are implantable medical devices comprising a biocompatible polymer comprising a triggerable bioadhesive property that allows the device to adhere to body tissue. The triggerable bioadhesive property of the polymer can be triggered or activated by exposure to a stimulus. Also, the present invention pertains to methods of making an implantable medical device comprising a biocompatible polymer comprising a triggerable bioadhesive property that allows the device to adhere to body tissue.Type: GrantFiled: September 10, 2008Date of Patent: July 17, 2012Assignee: Boston Scientific Scimed, Inc.Inventors: Michael N. Helmus, Yixin Xu, Barron W. Tenney, Paul L. Valint, Shrirang V. Ranade
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Patent number: 8222271Abstract: Described herein are formulations and methods for treating, inhibiting, preventing, delaying onset, or causing regression of a disease or condition relating to vascular permeability.Type: GrantFiled: March 23, 2007Date of Patent: July 17, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: David M. Kleinman, Thierry Nivaggioli, Mary E. Gerritsen, David A. Weber
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Patent number: 8222277Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: GrantFiled: December 28, 2010Date of Patent: July 17, 2012Assignee: NiCox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20120177692Abstract: A delivery system for water-insoluble pharmaceutical active ingredients is provided. The delivery system includes water-insoluble pharmaceutical active ingredient(s), organic solvent(s) and amphiphilic co-solvent(s), and a mixture of hydrophilic and hydrophobic non-ionic surfactants. Upon dilution in an aqueous medium, this formulation forms spontaneously dispersion of non-ionic surfactant nanoparticles.Type: ApplicationFiled: August 11, 2008Publication date: July 12, 2012Applicant: EMS S/AInventors: Flavia Giuliana Tinti, Marcia Cristina Breitreitz, Vladimir Matha, Carlo Oliani
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Publication number: 20120178775Abstract: Methods for rescuing learning, memory and/or motor function deficits associated with frontotemporal lobar degeneration with ubiquitinated inclusions (FTLD-U) are disclosed. The method comprises: a) administering to an animal having FTLD-U a therapeutically effective amount of an autophagy inducer; b) causing a decrease in the amount of ubiquitinated TDP-43 aggregation forms in the brain of the animal; and c) causing an improvement of the learning, memory capacities and/or motor function of the animal.Type: ApplicationFiled: January 4, 2012Publication date: July 12, 2012Applicant: Academia SinicaInventors: Che-Kun James SHEN, Kuen-Jer Tsai
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Publication number: 20120177742Abstract: Devices, coatings, and methods therefore comprise a medical device for delivering nanoparticles of an active agent to a treatment site. A coating on the medical device comprises active agent nanoparticles, which delivers coating to the treatment site and releases active agent nanoparticles into the treatment site over at least one day. A coating may comprise a polymer, a surfactant, and the nanoparticles. The coating may be prepared by forming a nanoemulsion. A coating may comprise encapsulated active agent nanoparticles which comprise active agent nanoparticles encapsulated in a polymer. The coating may have a positive surface charge. The coating may deliver active agent nanoparticles into the treatment site over at least about one day. The coating may be formed of a surfactant and nanoparticles mixture. The active agent nanoparticles may be deposited on the medical device using electrostatic capture.Type: ApplicationFiled: December 29, 2011Publication date: July 12, 2012Applicant: MICELL TECHNOLOGIES, INC.Inventors: James B. McCLAIN, Charles Douglas Taylor, Brett G. Zani, Timothy Charles Kiorpes
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Publication number: 20120178769Abstract: The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.Type: ApplicationFiled: July 15, 2010Publication date: July 12, 2012Applicant: The University of Medicine and DentistryInventor: Alexey G. Ryazanov
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Publication number: 20120177626Abstract: The present invention provides an HDL comprising an agent selected from the group consisting of antiproteases, antixoxidants, antimitotics, anti-apoptotic agents and agents involved in the iron metabolism for use as a medicament.Type: ApplicationFiled: January 13, 2012Publication date: July 12, 2012Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventor: Olivier Meilhac
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Publication number: 20120172389Abstract: A method for treating liver-associated fibrosing disorders or lupus, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula optionally in conjunction with a co-agent.Type: ApplicationFiled: March 14, 2012Publication date: July 5, 2012Inventor: Ruey-Shiuan TSAI
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Publication number: 20120165364Abstract: This invention relates to novel crystalline forms of tiotropium bromide, processes for preparing them, and their use in pharmaceutical formulations.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Applicant: SICOR INC.Inventors: Nicola Diulgheroff, Francesca Scarpitta, Alessandro Pontiroli, Adrienne Kovacsne-Mezei, Judith Aronhime, Alexandr Jegorov
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Publication number: 20120149665Abstract: A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.Type: ApplicationFiled: August 25, 2010Publication date: June 14, 2012Applicant: Bionomics LimitedInventors: Gabriel Kremmidiotis, David Bibby, Annabell Leske
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Publication number: 20120149725Abstract: Novel Anhydrate The present invention relates to a novel form of anhydrous tiotropium bromide, processes for the preparation of anhydrous tiotropium bromide, pharmaceutical compositions comprising anhydrous tiotropium bromide and uses of the compositions.Type: ApplicationFiled: August 6, 2010Publication date: June 14, 2012Inventors: Vinayak Govind Gore, Bindu Manojkumar, Dattatraya Shinde, Dattatrey Kokane
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Publication number: 20120148595Abstract: The present invention relates to GABA-linked anthracycline-lipid conjugates and to methods of using the conjugates to treat cancer. Methods for making the GABA-linked anthracycline lipid conjugates are also provided.Type: ApplicationFiled: March 11, 2010Publication date: June 14, 2012Applicant: Luitpold Pharmaceuticals, Inc.Inventors: Charles S. Swindell, Glenn G. Fegley, Hema M. Sundar, Richard Lawrence
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Publication number: 20120141531Abstract: A composition comprises a water-soluble polymer matrix in which are dispersed droplets of oil, the composition comprising an active principle. The invention includes embodiments in which the active principle is included in at least some of the oil droplets as well as embodiments in which the oil droplets are free of active principle. The oil droplets are released as the matrix containing them dissolves in an aqueous medium. In one embodiment, the oil droplets are substantially immobilized in or by the matrix and the immobilizing feature is lost as the matrix dissolves in aqueous media. In certain embodiments, the oil drops may collectively be referred to as the oil phase of the composition of the invention. The product may be in the form of mini-beads. The oil phase and/or the polymer matrix may each include a surfactant.Type: ApplicationFiled: May 18, 2010Publication date: June 7, 2012Inventors: Ivan Coulter, Bernard Francis McDonald, Vincenzo Aversa
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Publication number: 20120141513Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.Type: ApplicationFiled: December 5, 2011Publication date: June 7, 2012Inventors: Julie F. Liu, Rose A. Persichetti
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Publication number: 20120141605Abstract: Provided herein are pyrazoloanthrones or functional derivatives or analogues thereof to activate MIS receptor-mediated downstream effects in a cell. In particular, methods are provided to prevent and treat cancer that expresses MIS receptor type II (MISRII) by administering to a subject at least one pyrazoloanthrone or a functional derivative or analogue thereof. Also provided herein are methods to lower plasma androgen levels in a subject, and/or for the treatment of a subject with a disease characterized by excess androgen, whereby the subject is administered at least one pyrazoloanthrone or a functional derivative or analogue thereof. Also provided are methods to decrease the dose of a chemotherapeutic agent by administering the chemotherapeutic agent with a pyrazoloanthrone or a functional derivative or analogue thereof that lowers the effective dose of the chemotherapeutic agent.Type: ApplicationFiled: December 16, 2011Publication date: June 7, 2012Applicant: The General Hospital CorporationInventors: Jose Teixeira, Patricia K. Donahoe
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Patent number: 8193212Abstract: Methods and compositions containing huperzine are used to prevent and alleviate neuropathic pain. The invention is also directed to methods and compositions for using huperzine for the prevention and/or treatment of neuropathic pain and orthostatic hypotension.Type: GrantFiled: May 23, 2006Date of Patent: June 5, 2012Assignee: President and Fellows of Harvard CollegeInventor: Steven C. Schachter
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Publication number: 20120136046Abstract: The present invention relates to the use of fujimycin for the treatment of a disorder related to the chronological and/or replicative life-span of a cell, and to methods for increasing the replicative life span of a cell, said method comprising disrupting the function of a polynucleotide or gene encoding a polypeptide comprising SEQ ID No: 1, 3 or 5.Type: ApplicationFiled: July 8, 2010Publication date: May 31, 2012Applicant: Chronos Therapeutics LimitedInventors: Elizabeth Jane Mellor, Michael Youdell, Jonathan Ayling, Alexandre Akoulitchev
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Publication number: 20120132204Abstract: An inhaler includes a first body member and a second body member fit closely together to form an inhaler body, and an outlet. The first body member has a medicament chamber containing a unit dose of powdered medicament. A seal such as a foil strip seals the medicament chamber and extends outwardly of the inhaler body. In use, one end of the seal can be grasped by a user and withdrawn, fully or partially, from the inhaler body, to release the powdered medicament from the medicament chamber. The second body member includes a medicament collection well in which the medicament is collected upon its release from the medicament chamber. The medicament collection well forms part of an airway connecting into the outlet. In use, air can be drawn by inhalation at the outlet to entrain the powder medicament in the collection well for inhalation by a user.Type: ApplicationFiled: February 9, 2012Publication date: May 31, 2012Applicant: INNOVATA BIOMED LIMITEDInventors: Samuel W. Lucking, Glen P. Martyn
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Publication number: 20120136023Abstract: The present invention relates to novel 2,3,4-substituted 5,6,7,8-tetrahydro[1]benzothieno[2,3-b]pyridine compounds and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HIV replication.Type: ApplicationFiled: November 14, 2011Publication date: May 31, 2012Inventors: Andrew Simon Bell, Iain Brian Gardner, Karl Richard Gibson, David Cameron Pryde, Florian Michel Wakenhut
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Patent number: 8187620Abstract: The invention relates generally to a medical device, such as an intravascular stent, for delivering a therapeutic agent to the body tissue of a patient, and a method for making such a medical device. More particularly, the invention pertains to a medical device having a metal oxide or metal material with a plurality of pores therein disposed on the surface of the medical device and a polymer disposed on the metal oxide or metal material. The invention also relates to medical devices having a surface and an outer region comprising a metal oxide or metal material having a plurality of pores therein and a polymer disposed on the metal oxide or metal material.Type: GrantFiled: March 27, 2006Date of Patent: May 29, 2012Assignee: Boston Scientific Scimed, Inc.Inventors: Chandru Chandrasekaran, Rajesh Radhakrishnan
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Patent number: 8188279Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: June 1, 2011Date of Patent: May 29, 2012Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael Garst
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Publication number: 20120129810Abstract: The present invention is directed to methods of using a sirolimus drug and chloroquine or a quinoline derivative in combination. Methods of use are also described.Type: ApplicationFiled: May 4, 2010Publication date: May 24, 2012Applicant: The Trustees of the University of PennsylvaniaInventors: Ravi Kumar Amaravadi, Craig B. Thompson
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Publication number: 20120125325Abstract: An agent, which is amlexanox, is useful in the therapy of a disease associated with neutrophilia.Type: ApplicationFiled: May 28, 2010Publication date: May 24, 2012Inventors: Robin Mark Bannister, John Brew
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Publication number: 20120128665Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an agent to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.Type: ApplicationFiled: November 18, 2011Publication date: May 24, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Vojo Vukovic
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Publication number: 20120122913Abstract: Methods, uses, compositions, combinations and kits relating to the decrease of Tau protein levels, and prevention and/or treatment of diseases or disorders associated with Tau protein (Tauophathies), such as Alzheimer's disease, using a curcuminoid and a mammalian target rapamycin (mTOR) inhibitor, are described.Type: ApplicationFiled: July 14, 2010Publication date: May 17, 2012Inventors: Michel Charbonneau, Guylaine Lassonde
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Publication number: 20120121684Abstract: Implantable medical devices are disclosed. The devices comprise a coating comprising an interpenetrating network or semi-interpenetrating network. The interpenetrating network or semi-interpenetrating network comprises poly(ethylene glycol) and an aliphatic polyester copolymer. A method of using the implantable device is also provided.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: Abbott Cardiovascular Systems Inc.Inventors: Mikael Trollsas, Florencia Lim, Syed F.A. Hossainy
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Publication number: 20120115897Abstract: The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children.Type: ApplicationFiled: December 24, 2009Publication date: May 10, 2012Applicants: WUXI HONGRUI BIO-PHARMA-TECH CO., LTD .Inventors: Luhong Tang, Ajuan Dai, Ze Wang, Yang Sun, Xinning Liu, Lingyan Xu, Xin Fang, Shuang Qiu, Yaqing Cao, Xiaomin Xu, Ruixia Jiang, Chao Wu
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Publication number: 20120115896Abstract: Isogenic human cell lines comprising at least one mutated cancer allele under the control of the cell line endogenous promoter, which corresponds to the wild-type cancer allele promoter are disclosed, as well as an in vitro process for determining sensitivity/resistance of a patient suffering from a tumor to a pharmacological agent comprising the following steps: a) identifying at least one mutated cancer allele in a tissue affected by a tumor of said patient; b) providing an isogenic human cell line representative of the tissue, wherein the cell line comprises at least the identified mutated cancer allele, which is under the control of the cell line endogenous promoter corresponding to the wild-type cancer allele promoter; c) putting in contact said cell line with the pharmacological agent; d) determining a variation of proliferation, apoptosis or cytotoxicity of the cell line in presence of the pharmacological agent; wherein the variation of proliferation, apoptosis car cytotoxicity indicative of the sensitType: ApplicationFiled: December 3, 2008Publication date: May 10, 2012Inventors: Alberto Bardelli, Federica Di Nicolantonio, Sabrina Arena
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Publication number: 20120115778Abstract: Methods for treating eating disorders associated with excessive weight gain, suppressing appetite, reducing body weight, or treating obesity in an animal by administering one or more antagonists of the serotonin Htr1a or Htr2b receptor, or a Tph2 inhibitor are provided, or combinations thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 10, 2012Applicant: The Trustees of Columbia University in the City of New YorkInventors: Gerard Karsenty, Vijay Yadav, Franck Oury
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Publication number: 20120114637Abstract: Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are ophthalmic formulations that deliver a variety of therapeutic agents, including but not limited to rapamycin (sirolimus), analogs thereof (rapalogs) or other mTOR inhibitors, to a subject for an extended period of time. The ophthalmic formulations may be placed in an aqueous medium of a subject, including but not limited to intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer a therapeutic agent to treat or prevent age-related macular degeneration, macular edema, diabetic retinopathy, uveitis, dry eye, or a hyperpermeability disease in a subject.Type: ApplicationFiled: May 4, 2010Publication date: May 10, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Thierry Nivaggioli, David A. Weber, Philippe JM Dor, Philip Reilly