Plural Hetero Atoms In The Tricyclo Ring System Patents (Class 514/291)
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Publication number: 20130184305Abstract: The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.Type: ApplicationFiled: August 2, 2011Publication date: July 18, 2013Inventors: Dhananjay Sharad Rane, Rajnikant Gandalal Vyas, Pramod Kumar Minocha
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Publication number: 20130184214Abstract: Pharmaceutical compositions and kits including a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor are provided. Also provided are methods of treating cancer in a subject, comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof. Also provided are methods of reducing cell proliferation in a subject comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof.Type: ApplicationFiled: February 10, 2012Publication date: July 18, 2013Inventor: Steven Hoffman
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Patent number: 8486960Abstract: 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: June 21, 2012Date of Patent: July 16, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: David M. Kleinman, Thierry Nivaggioli, Mary E. Gerritsen, David A. Weber
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Patent number: 8486482Abstract: Methods are disclosed to improved adhesion of polymer coatings over polymer surfaces of stents which include plasma treatment, applying an adhesion promoting layer, surface treatments with solvents, and mechanical roughening techniques.Type: GrantFiled: July 1, 2011Date of Patent: July 16, 2013Assignee: Abbott Cardiovascular Systems Inc.Inventors: Yunbing Wang, Daniel A. Castro, Stephen D. Pacetti
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Publication number: 20130178494Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.Type: ApplicationFiled: June 29, 2012Publication date: July 11, 2013Applicant: Academia SinicaInventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
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Publication number: 20130177598Abstract: A pharmaceutical composition comprising protein micro and/or nanoparticles are provided. The particles have a predetermined geometric shape and a broadest dimension less than about 10 micrometers. The particles may further comprise active agents.Type: ApplicationFiled: February 27, 2008Publication date: July 11, 2013Applicant: The University of North Carolina at Chapel HillInventors: Joseph M. Desimone, Stephanie Gratton, Ji Guo, Jennifer Yvonne Kelly, Andrew James Murphy, Mary E Napier
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Publication number: 20130178459Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.Type: ApplicationFiled: March 29, 2011Publication date: July 11, 2013Applicant: Oncotherapy Science, Inc.Inventors: Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
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Patent number: 8481561Abstract: The present invention relates to novel GABAA/BzR ligands of the general formulas (I), (II) and (III) wherein R1 is selected from the group consisting of hydrogen, halogen, haloalkyl having 1-2 carbon atoms, alkoxy having 1 to 3 carbon atoms in the alkyl chain, alkyl having 1 to 3 carbon atoms, and nitro, and R2 is selected from the group consisting of hydrogen, halogen and alkyl having 1 to 2 carbon atoms, as well as the use of these compounds for treating anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals including pharmaceutical compositions comprising the same.Type: GrantFiled: April 2, 2009Date of Patent: July 9, 2013Assignee: Innovationspatent Sverige ABInventors: Mogens Peter Cherly Nielsen, Tommy Liljefors, Jakob Alexander Nilsson, Olov A Sterner
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Publication number: 20130172336Abstract: Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives and their uses in the manufacture of pharmaceutical compositions and in the treatment of cancers.Type: ApplicationFiled: December 30, 2011Publication date: July 4, 2013Applicant: Kaohsiung Medical UniversityInventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Yu-Wen Chen, Pei-Jung Lu
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Publication number: 20130171207Abstract: The invention provides active agents, such as paclitaxel, rapamycin, or 17-DMAG, 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-DMAG, 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 bioavailability 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: ApplicationFiled: February 26, 2013Publication date: July 4, 2013Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventor: Wisconsin Alumni Research Foundation
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Publication number: 20130172383Abstract: 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: February 22, 2013Publication date: July 4, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130165471Abstract: Disclosed herein are 2-substituted-thienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R3, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a 2-substituted-thienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a 2-substituted-thienoquinolone to an animal suffering from a microbial infection.Type: ApplicationFiled: December 21, 2012Publication date: June 27, 2013Applicant: Achillion Pharmaceuticals Inc.Inventors: Avinash Phadke, Jason Allan Wiles
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Publication number: 20130164344Abstract: The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X? represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, ?-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation.Type: ApplicationFiled: December 6, 2012Publication date: June 27, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Michael TRUNK, Claudius WEILER, Werner PIEROTH
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Publication number: 20130158035Abstract: Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor.Type: ApplicationFiled: August 23, 2011Publication date: June 20, 2013Applicant: Brigham Young UniversityInventor: Marc Hansen
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Publication number: 20130150397Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible rapamycin composition comprising a specific mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers. In other aspects, the present invention is directed to a method of making the composition.Type: ApplicationFiled: December 13, 2011Publication date: June 13, 2013Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
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Publication number: 20130150332Abstract: 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: EMORY UNIVERSITYInventor: Emory University
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Patent number: 8455510Abstract: Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.Type: GrantFiled: September 17, 2009Date of Patent: June 4, 2013Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jian Ding, Jianping Zuo, Linqian Yu, Linghua Meng, Yangming Zhang, Na Yang, Min Gu
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Patent number: 8450339Abstract: New stable compositions comprising the combination of a topically active vasoconstrictor and a topically active anticholinergic drug are disclosed. Preferably, the composition comprises ipratropium or a salt thereof in combination with xylometazoline hydrochloride and a salt thereof. Upon topically administering such compositions to a nasal mucosa in individuals suffering from the common cold the symptoms of rhinorrhea are significantly reduced.Type: GrantFiled: December 11, 2009Date of Patent: May 28, 2013Assignee: Takeda Pharma A/SInventors: Hanne Anette Moesgaard, Karin Lowenstein Christensen
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Publication number: 20130131070Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.Type: ApplicationFiled: October 30, 2012Publication date: May 23, 2013Inventor: John K. Buolamwini
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Publication number: 20130129814Abstract: The present invention relates to the regional delivery of therapeutic agents for the treatment of vascular diseases wherein regional delivery refers to delivery of a therapeutically effective amount of the therapeutic agent to an area of the vessel that includes not only afflicted tissue but non-afflicted tissue at the periphery of the afflicted tissue as well.Type: ApplicationFiled: December 21, 2012Publication date: May 23, 2013Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventor: ABBOTT CARDIOVASCULAR SYSTEMS INC.
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Publication number: 20130129817Abstract: This invention is directed to methods of treating solid tumor cancers, particularly refractory cancers by administration of a drug capable of inhibiting mTOR and/or inhibiting an efflux pump and/or inhibiting HIF-1? and VEGF, the drug in particular being selected from the group consisting of sirolimus, everolimus, zotarolimus, tacrolimus, iolimus A9, deforolimus, AP23572, tacrolimus, temsirolimus, pimecrolimus, novolimus, 40-O-(3-hydroxypropyl), 40-O-[2-(2-hydroxy)ethoxy]ethyl-rapamycin and 40-O-tetrazolylrapamycin, the drug being administered along with a chemotherapeutic agent and/or radiation therapy.Type: ApplicationFiled: January 24, 2013Publication date: May 23, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventor: Abbott Cardiovascular Systems Inc.
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Publication number: 20130129794Abstract: Implantable medical devices including a coating having a bioactive agent and a poly(ester amide) polymer. Methods of forming these coatings are also described.Type: ApplicationFiled: December 31, 2012Publication date: May 23, 2013Applicant: ABBOTT CARDIOVASCULAR SYSTEMS INC.Inventor: ABBOTT CARDIOVASCULAR SYSTEMS INC.
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Patent number: 8445435Abstract: The present invention is directed to methods of treating or preventing the development of obesity by administering compounds that stabilize mast cells. In addition, it includes pharmaceutical compositions which have both a mast cell stabilizer and instructions regarding the use of the stabilizer in treating or preventing obesity.Type: GrantFiled: September 24, 2008Date of Patent: May 21, 2013Assignee: The Brigham and Women's Hospital, Inc.Inventor: Guo-Ping Shi
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Publication number: 20130123235Abstract: 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: July 21, 2011Publication date: May 16, 2013Inventors: David Clark, Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
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Publication number: 20130123328Abstract: We describe a method of determining whether a cancer cell is likely to be resistant to treatment by an mTOR inhibitor. The method may comprise detecting PPP2R2B (GenBank Accession Number: NM_18167) in or of the cell. It may, alter-natively, or in addition, comprise detecting PDK1 (GenBank Accession Number: NM_002613), in or of the cell. The method may comprise detecting methylation of the PPP2R2B promoter in or of the cell. It may comprise detecting the expression and/or activity of PPP2R2B in or of the cell. It may comprise detecting PDK1 mediated Myc phosphorylation activity.Type: ApplicationFiled: January 10, 2011Publication date: May 16, 2013Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Qiang Yu, Jing Tan
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Publication number: 20130123286Abstract: Certain novel fused quinazoline derivatives of formula (I) as c-Met inhibitors, their synthesis and their uses for treating a c-Met mediated disorder. Methods for treating a c-Met-mediated disorder are also disclosed in the invention.Type: ApplicationFiled: July 14, 2011Publication date: May 16, 2013Inventors: Shaojing Hu, Fei Wang, Wei Long, Xiaoyan Shen, Fenlai Tan, Yinxiang Wang
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Publication number: 20130123263Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 10, 2013Publication date: May 16, 2013Applicants: F. HOFFMANN - LA ROCHE AG, GENENTECH, INC.Inventors: GENENTECH, INC., F. HOFFMANN - LA ROCHE AG
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Publication number: 20130116271Abstract: The purpose is to provide a tacrolimus-containing pharmaceutical composition which is a creamy preparation for external application having good feeling upon use and has high stability of a main ingredient contained therein (high main ingredient residual ratio), and allows easy control of skin concentration of the main ingredient. The present invention relates to an oil-in-water type creamy composition comprising (A) tacrolimus, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, (B) an oil prepared by mixing (a) a medium-chain fatty acid triglyceride with (b) ethylene glycol salicylate and/or diisopropyl sebacate, (C) an emulsifying agent having a HLB value of 12 or more, and (D) a hydrophilic polymer, and having a pH value of 4 to 7.Type: ApplicationFiled: July 22, 2011Publication date: May 9, 2013Applicant: MARUHO CO., LTD.Inventors: Mikito Ihara, Yoshinori Ueda
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Publication number: 20130115165Abstract: Polymeric nanoparticles with a hydrophobic core and a hydrophilic shell are formed from: 1) N-isopropylacrylamide (NIPAAM), at a molar ratio of about 50% to about 90%, and preferably 60% for specific delivery routes such as oral or parenteral; either water-soluble vinyl derivatives like vinylpryolidone (VP) or vinyl acetate (VA), or water insoluble vinyl derivaties like methyl methacrylate (MMA) or styrene (ST), at a molar ratio of about 10% to about 30%; and acrylic acid (AA), at a molar ration of about 10% to about 30%.Type: ApplicationFiled: October 12, 2012Publication date: May 9, 2013Inventors: Anirban Maitra, Georg Feldmann, Savita Bisht
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Patent number: 8436010Abstract: Rapamycin derivatives have interesting effects in the treatment of solid tumors, optionally in combination with a chemotherapeutic agent.Type: GrantFiled: February 23, 2012Date of Patent: May 7, 2013Assignee: Novartis Pharmaceuticals CorporationInventors: Heidi Lane, Terence O'Reilly, Jeanette Marjorie Wood
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Patent number: 8435544Abstract: The embodiments disclosed herein relate to ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors, and more particularly to methods for treating an ocular disease and/or condition using the disclosed compositions. According to aspects illustrated herein, there is provided a pharmaceutical composition that includes a calcineurin inhibitor or an mTOR inhibitor; a first surfactant with an HLB index greater than about 10; and a second surfactant with an HLB index of greater than about 13, wherein an absolute difference between the HLB index of the first surfactant and the HLB index of the second surfactant is greater than about 3, and wherein the composition forms mixed micelles.Type: GrantFiled: October 8, 2008Date of Patent: May 7, 2013Assignee: Lux Biosciences, Inc.Inventors: Ashim K. Mitra, Poonam R. Velagaleti, Subramanian Natesan
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Publication number: 20130109630Abstract: This document features method related to variants in the Inverted Formin 2 (INF2) gene that are susceptibility to focal segmental glomerulosclerosis (FSGS). For example, methods of using such variants for risk assessment and for diagnosing and optimizing treatment of FSGS are provided.Type: ApplicationFiled: December 7, 2010Publication date: May 2, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Martin Pollak, Elizabeth J. Brown, Johannes Schlondorff
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Publication number: 20130109713Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.Type: ApplicationFiled: June 24, 2011Publication date: May 2, 2013Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
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Publication number: 20130109674Abstract: The present invention relates to, among other things, methods for treating trigeminal cephalgias such as migraine and migraine like headaches and other cerebrovascular conditions associated with pain and or inflammation. When non-steroidal anti inflammatory drugs (NSAIDs), such as ketoprofen, are applied locally using specific topical formulations immediate relief of pain is obtained. Intense pain is typically reduced to mild pain or no pain within 30 minutes of application of the topical formulation. The NSAID may be given in combination with other pharmacological agents, such as vasoconstrictors, opioids, decongestants and/or non-opioid migraine drugs, such as triptans and ergots and agents that affect serotonin receptors as agonists, antagonists or partial agonists.Type: ApplicationFiled: December 17, 2010Publication date: May 2, 2013Applicant: Achelios Therapeutics LLCInventors: Harry J. Leighton, Matthew J. Buderer, Crist J. Frangakis
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Publication number: 20130104881Abstract: Pharmaceutical pressurized metered dose inhalers are disclosed having improved temperature and moisture stability comprising CFC-free, ethanol-free compositions that include lactose of particle diameter larger than 1 ?m as a means of minimizing sticking to the walls and other destabilization mechanisms activated by moisture ingress from the environment.Type: ApplicationFiled: October 31, 2011Publication date: May 2, 2013Applicant: Laboratorio Pablo Cassara S.R.L.Inventors: Fernando Toneguzzo, Julio Cesar Vega
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Publication number: 20130101615Abstract: This invention is a method for immunizing, preventing or treating a Mycobacterium avium subspecies paratuberculosis-associated disease or condition by screening subjects for markers indicative of predisposition or susceptibility to a Mycobacterium avium subspecies paratuberculosis-associated disease or condition and administering a Mycobacterium avium subspecies paratuberculosis vaccine or prophylactic or therapeutic agent.Type: ApplicationFiled: December 14, 2012Publication date: April 25, 2013Inventor: Robert J. Greenstein
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Publication number: 20130102553Abstract: The invention relates to therapeutic agents for use in the prevention or treatment of Alzheimer's disease. In particular the invention relates to use of inhibitors of cell cycle reentry and progression to the G1/S transition or inhibitors of progression of the cell cycle through the G1/S transition point in the prevention or treatment of Alzheimer's disease.Type: ApplicationFiled: November 30, 2012Publication date: April 25, 2013Applicant: ISIS INNOVATION LTD.Inventor: ISIS INNOVATION LTD.
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Publication number: 20130101572Abstract: Compositions and methods are disclosed for treating vitiligo and promoting the formation of collagen.Type: ApplicationFiled: December 4, 2012Publication date: April 25, 2013Inventor: Sarah Bacus
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Publication number: 20130102569Abstract: The invention provides methods for treating or preventing an age-related disease, condition, or disorder comprising administering a therapeutically effective amount of an inhibitor of TOR to a patient in need thereof. The invention also provides pharmaceutical compositions and topical formulations for treating or preventing an age-related disease, condition, or disorder comprising an inhibitor of TOR and a pharmaceutically acceptable carrier. In particular, the invention provides methods, pharmaceutical compositions, and topical formulations comprising rapamycin or an analog of rapamycin.Type: ApplicationFiled: December 10, 2012Publication date: April 25, 2013Applicant: Tartis-Aging, LLCInventor: Tartis-Aging, LLC
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Publication number: 20130102572Abstract: The present application relates to methods of preventing or treating skin disorders exhibiting telangiectasia, for example, rosacea exhibiting an erythematotelangiectatic subtype. Exemplary methods comprise administering to a patient a formulation comprising a therapeutically effective amount of an mTOR inhibitor, such as rapamycin, wherein the mTOR inhibitor is the only active agent in the formulation. Suitably, the formulations are topical formulations administered to the face.Type: ApplicationFiled: April 11, 2012Publication date: April 25, 2013Applicant: Dow Pharmaceutical SciencesInventor: Jeffrey SUGARMAN
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Patent number: 8426398Abstract: The present invention is directed to compounds which are conjugates of two non-toxic natural products, noscapine (and various noscapine analogs) and folic acid (and various folic acid analogs), where the folic acid is conjugated to noscapine or the noscapine analog at the 9-position on the isoquinoline ring on the noscapine framework. Pharmaceutical compositions including the compounds, and methods of treating various tumors using the compounds and compositions, are also disclosed. The conjugates are particularly useful for treating cancers which overexpress the Folate Receptor ? (FRa) receptor.Type: GrantFiled: January 8, 2010Date of Patent: April 23, 2013Assignee: Emory UniversityInventors: Harish C. Joshi, Surya N. Vangapandu, Ritu Aneja
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Patent number: 8426438Abstract: The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: September 20, 2010Date of Patent: April 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk
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Patent number: 8426457Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.Type: GrantFiled: March 12, 2004Date of Patent: April 23, 2013Assignee: Medicis Pharmaceutical CorporationInventors: Richard L. Miller, James H. Lee, Mary L. Owens
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Publication number: 20130095144Abstract: The present invention discloses a stable solid pharmaceutical matrix composition comprising sirolimus or pharmaceutically acceptable salts thereof along with one or more sugars.Type: ApplicationFiled: April 25, 2011Publication date: April 18, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Sunilendu Bhushan Roy, Sushrut Krishnaji Kulkarni, Kiritkumar Maulik Panchal, Shubhashchandra Shailendra Mandge
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Publication number: 20130096069Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.Type: ApplicationFiled: September 10, 2012Publication date: April 18, 2013Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V.S. Sista, Thorsten A. Kirschberg
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Publication number: 20130096150Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.Type: ApplicationFiled: December 6, 2012Publication date: April 18, 2013Applicant: TRANSTECH PHARMA, INC.Inventor: TransTech Pharma, Inc
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Patent number: 8420660Abstract: A derivative of ?-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-?-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug.Type: GrantFiled: February 25, 2011Date of Patent: April 16, 2013Inventors: Sabra Begum, Syed Nawazish Ali, Bina Shaheen Siddiqui
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Publication number: 20130089577Abstract: Described herein are compositions (e.g., a pharmaceutical composition) and methods for controlling the delivery of a therapeutic agent, and their use in the treatment and/or prevention of diseases and disorders.Type: ApplicationFiled: March 11, 2011Publication date: April 11, 2013Inventors: Joseph P. St. Laurent, Scott A. Goodrich, Gerald S. Jones, JR.
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Publication number: 20130090367Abstract: This application relates to the modulation of host cell factors required for influenza virus replication. The application relates to compounds, including nucleic acid compounds (such as, e.g., small interfering RNAs (siRNAs)) and small molecules, that target human host cell factors involved in influenza virus replication, and the use of such compounds for modulating influenza virus replication and as antiviral agents. The application also relates to methods of treating an influenza virus infection and methods of treating or preventing a symptom or disease associated with influenza virus infection, comprising administering to a subject a composition comprising a compound, such as a nucleic acid compound (e.g., an siRNA) or small molecule, that targets a human host cell factor involved in influenza virus replication.Type: ApplicationFiled: December 10, 2010Publication date: April 11, 2013Inventors: Megan Shaw, Peter Palese, Adolfo Garcia-Sastre, Silke Stertz, John Young, Renate König, Sumit Chanda