The Hetero Ring Has At Least Seven Members Patents (Class 514/450)
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Patent number: 8486993Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.Type: GrantFiled: July 7, 2011Date of Patent: July 16, 2013Assignee: Veloxis Pharmaceuticals A/SInventor: Per Holm
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Patent number: 8486980Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:Type: GrantFiled: August 6, 2009Date of Patent: July 16, 2013Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
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Publication number: 20130178434Abstract: A method of treating otitis externa is disclosed. The method includes topically applying an otic composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier into the external auditory canal and the auricle of an affected ear of an individual suffering from otitis externa.Type: ApplicationFiled: October 14, 2011Publication date: July 11, 2013Applicant: GALDERMA S.A.Inventors: L. Dean Parks, Jeffrey D. Parks
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Publication number: 20130178433Abstract: A method of treating hemorrhoids is disclosed. The method includes locally administering a composition including an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds, milbemycin compounds, or mixture thereof and a pharmaceutically acceptable carrier to the affected anorectal region of an individual suffering from hemorrhoid.Type: ApplicationFiled: October 14, 2011Publication date: July 11, 2013Applicant: GALDERMA S.A.Inventors: L. Dean Parks, Jeffrey D. Parks
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Patent number: 8481757Abstract: Provided herein compounds, compositions and methods useful for the treatment of malaria for a subject in need thereof, including compounds of Formula (I), Formula (II), Formula (III), Formula (IV), and Formula (V).Type: GrantFiled: February 4, 2011Date of Patent: July 9, 2013Assignees: Georgua Tech Research Corporation, The Regents of the University of CaliforniaInventors: Julia M. Kubanek, Mark E. Hay, Karine G. Le Roch, E. Paige Stout, Amy L. Lane, An-Shen Lin
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Publication number: 20130172282Abstract: A method of treating herpes simplex virus infection or varicella zoster virus infection is disclosed. The method includes topically applying a composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to the affected area of an individual suffering from herpes simplex virus infection or varicella zoster virus infection.Type: ApplicationFiled: October 14, 2011Publication date: July 4, 2013Applicant: GALDERMA S.A.Inventors: L. Dean Parks, Jeffrey D. Parks
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Patent number: 8476192Abstract: An aqueous seed treatment insecticidal and/or nematicidal composition in the form of a suspension comprising (A) at least one insecticide and/or nematicide in an amount of at least 3 weight %, based on the total weight of the composition, and (B) at least two surface active compounds, wherein (i) at least one is an anionic phosphate type compound, and (ii) at least one is a non-ionic alkoxylated phenol. Such compositions demonstrate improved dust-off performance when applied to plant propagation material, such as seeds.Type: GrantFiled: March 15, 2005Date of Patent: July 2, 2013Assignee: Syngenta Crop Protection LLCInventors: Lear Michael Haulsee, Humberto B. Lopez
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Publication number: 20130165453Abstract: The invention provides for the use of protein kinase activators or boosters of nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF) or other neurotrophic factors to treat stroke. Specifically, the present invention provides methods of treating stroke comprising the steps of identifying a subject having suffered a stroke and administering to said subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of stroke.Type: ApplicationFiled: July 19, 2012Publication date: June 27, 2013Inventors: Miao-Kun Sun, Daniel L. Alkon
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Publication number: 20130165375Abstract: The invention provides for the use of carbonic anhydrase activators; protein kinase C activators and FGF-18 to treat depressive disorders. The invention also relates to improved animal models and methods for screening and identifying compounds to treat depressive disorders.Type: ApplicationFiled: November 5, 2012Publication date: June 27, 2013Applicant: Blanchette Rockefeller Neuroscience InstituteInventor: Blanchette Rockefeller Neuroscience Institute
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Publication number: 20130156853Abstract: A liquid composition of an insoluble medicament and a preparation method thereof are disclosed. The composition includes insoluble medicament, oil for injection, phospholipid, and solvent; the percentage by weight of each component is as follows: insoluble medicament 0.01-10%, oil for injection 0%-20%, phospholipid 10-80%, solvent 20-89%. The preparation method for the composition includes the following steps: dissolving an insoluble medicament into solvent or oil for injection or a mixture thereof firstly, and then adding other components, and mixing uniformly; or dissolving an insoluble medicament into a mixture of other components, and mixing uniformly; or dissolving an insoluble medicament into part of solvent firstly, and then adding into a mixed solvent of other components and the remaining solvent, and mixing uniformly.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: PEKING UNIVERSITYInventors: Qiang Zhang, Wenbing Dai, Jiancheng Wang, Xuan Zhang
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Publication number: 20130150422Abstract: The disclosure relates to resorcylic acid lactones and indolinone-containing compounds for use in treatment of diseases associated with aberrant protein processing, such as cystic fibrosis (CF; mucoviscidosis). The disclosure more generally relates to treatment of aberrant protein processing, such as errors in protein folding, trafficking or post-translational modification.Type: ApplicationFiled: August 19, 2011Publication date: June 13, 2013Applicant: THE HOSPITAL FOR SICK CHILDRENInventors: Daniela Rotin, Agata Trzcinska-Daneluti
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Publication number: 20130150434Abstract: Methods of treating sleep disorders by administration of low doses of doxepin in individuals seeking sustained efficacy or in need of avoiding weight gain, rebound insomnia, or sedative tolerance resulting from doxepin treatment.Type: ApplicationFiled: February 11, 2013Publication date: June 13, 2013Applicant: SOMAXON PHARMACEUTICALS, INC.Inventor: SOMAXON PHARMACEUTICALS, INC.
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Publication number: 20130150390Abstract: A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect.Type: ApplicationFiled: December 12, 2012Publication date: June 13, 2013Inventors: Mie Kaino, Hiroyuki Meguro
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Publication number: 20130143956Abstract: This invention provides for novel antiparasitic and pesticidal forms of moxidectin, including a long-acting polymeric implant. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections in animals.Type: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Applicant: Merial LimitedInventors: Susan Mancini Cady, Baoqing Ma, Robert Clark Chapman, Chunhua Yang, Uday Jain
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Patent number: 8455539Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.Type: GrantFiled: October 15, 2012Date of Patent: June 4, 2013Assignee: Wyeth LLCInventors: Joseph T. Rubino, Victoria Siskavich, Maureen M. Harrison, Pooja Gandhi
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Publication number: 20130136809Abstract: The invention discloses biologically active ingredient(s) selected from 7-hydroxyfrullanolide, its analogs, the ex-tract(s) and fraction(s) standardized to 7-hydroxyfrullanolide or its analogs or both or mixtures thereof or their composition(s) for the prevention, control and treatment of one or more obesity, overweight, metabolic syndrome, diabetes and other metabolic disorders or for producing lean body mass in a warm blooded animal in need thereof.Type: ApplicationFiled: January 28, 2013Publication date: May 30, 2013Applicant: LAILA NUTRACEUTICALSInventor: LAILA NUTRACEUTICALS
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Publication number: 20130137759Abstract: The present invention features compositions and methods for treatment of parasitic diseases and cancer. The compositions include Artemisia annua tissue and a pharmaceutically acceptable carrier. The methods provide an efficient delivery system for artemisinin and related compounds.Type: ApplicationFiled: March 4, 2011Publication date: May 30, 2013Applicant: Worcester Polytechnic InstituteInventor: Pamela J. Weathers
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Patent number: 8449866Abstract: This disclosure provides, in part, fluorocarbon imaging reagents and formulations for the ex vivo labeling of cells. Labeled cells may be detected in vivo or ex vivo by a nuclear magnetic resonance technique, such as magnetic resonance imaging (MRI) or magnetic resonance spectroscopy (MRS). The disclosure additionally provides methods for using the imaging reagents in a variety of clinical procedures.Type: GrantFiled: March 6, 2012Date of Patent: May 28, 2013Assignee: Carnegie Mellon UniversityInventor: Eric T. Ahrens
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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: 20130109654Abstract: Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.Type: ApplicationFiled: December 8, 2010Publication date: May 2, 2013Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Ravit Arav-Boger, Gary Posner
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Publication number: 20130109745Abstract: The present invention relates to an anti-angiogenic composition containing macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A, and 7-O-succinyl macrolactin A as active ingredients. The macrolactin compounds according to the present invention strongly suppress angiogenesis in in vivo experiments and can be used as a pharmaceutical composition for preventing or treating diseases caused by angiogenesis.Type: ApplicationFiled: February 23, 2011Publication date: May 2, 2013Inventors: Young-Hoon Ji, Dong-Hee Kim, Jung-Ae Kim, Jae-Seon Kang, Sung-Uk Chung, Sung-Woo Hwang, Kyung-Ran Kang, You-Ra Kang
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Patent number: 8431611Abstract: This disclosure provides improved derivatives of artemisinin; pharmaceutical compositions containing these compounds; methods for preparing these compounds and compositions; methods of using these compounds and compositions for preventing, controlling or treating infectious diseases including but not limited to parasitic infectious diseases such as T. gondii infection, trypanosome parasite infection, plasmodia parasite infection, and cryptosporidium parasite infection; methods for preventing, controlling or treating toxoplasma infection; and methods for treating psychiatric disorders associated with toxoplasma infection including but not limited to schizophrenia using the disclosed compounds and compositions alone or in combination with one or more antipsychotic drugs.Type: GrantFiled: October 19, 2007Date of Patent: April 30, 2013Assignee: Johns Hopkins UniversityInventors: Lorraine V. Brando, Gary H. Posner, John G. D'Angelo, Robert H. Yolken, Christopher P. Hencken, Lauren Woodard
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Publication number: 20130102658Abstract: The invention relates to use of the cis-(Z) isomer or isomeric mixtures containing specified ratios of the cis-(Z) and trans-(E) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disordersType: ApplicationFiled: December 3, 2012Publication date: April 25, 2013Applicants: PROCOM ONE, INC., SOMAXON PHARMACEUTICALS, INC.Inventors: Somaxon Pharmaceuticals, Inc., ProCom One, Inc.
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Publication number: 20130096188Abstract: The invention relates to use of the trans-(E) isomer or isomeric mixtures containing specified ratios of the trans-(E) and cis-(Z) isomers of doxepin, metabolites of doxepin, pharmaceutically-acceptable salts of doxepin and prodrugs of the same; compositions containing the same, for the treatment of sleep disordersType: ApplicationFiled: December 3, 2012Publication date: April 18, 2013Applicants: ProCom One, Inc., Somaxon Pharmaceuticals, Inc.Inventors: Somaxon Pharmaceuticals, Inc., ProCom One, Inc.
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Publication number: 20130096086Abstract: Methods described herein relate to mitochondria and their role in Human immunodeficiency virus type 1 (HIV-1) infection and cell-to-cell HIV-1 transmission and compositions and methods for modulating mitochondrial mediated cell-to-cell transmission of HIV-1. Methods for screening to identify inhibitors of mitochondrial mediated cell-to-cell transmission of HIV-1 are also envisioned herein.Type: ApplicationFiled: October 17, 2012Publication date: April 18, 2013Inventor: Sylvia Lee-Huang
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Patent number: 8410292Abstract: Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2?-chloroenglerin A, which has the structure (II), wherein double bond ‘a’ is E, Z, or a mixture of E and Z.Type: GrantFiled: December 30, 2008Date of Patent: April 2, 2013Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: John A. Beutler, Ranjala Ratnayake, David Covell, Tanya R. Johnson
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Publication number: 20130072550Abstract: The present disclosure relates to methods of administering compounds for treating conditions associated with amyloid processing such as Alzheimer's Disease. Methods are disclosed comprising the step of administering a macrocyclic lactone, a benzolactam, a pyrrolidinone or a combination thereof to a subject in need in an amount effective to decrease soluble A?-40 or A?-42, or to lower total amyloid precursor protein (“APP”). Methods are also disclosed further comprising the step of identifying a subject with increased soluble A?-40 or A?-42 levels, or elevated APP levels compared to a control population.Type: ApplicationFiled: September 10, 2012Publication date: March 21, 2013Inventors: Rene Etcheberrigaray, Daniel L. Alkon
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Patent number: 8399508Abstract: Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the nose are disclosed. The aqueous formulations contain approximately 0.6% (w/v) of olopatadine.Type: GrantFiled: June 30, 2011Date of Patent: March 19, 2013Assignee: Alcon Pharmaceuticals Ltd.Inventors: Onkar N. Singh, G. Michael Wall, Rajni Jani, Masood A. Chowhan, Wesley Wehsin Han
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Patent number: 8394849Abstract: In certain aspects, the invention relates to methods of treating proliferative oropharyngeal cancer, laryngeal cancer and esophageal cancer by administering artemisinin-related compounds.Type: GrantFiled: July 11, 2011Date of Patent: March 12, 2013Assignee: Georgetown UniversityInventors: Richard Schlegel, Dan-Paul Hartmann, Astrid Baege
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Publication number: 20130059019Abstract: The invention features methods of treating a subject suffering from a herpes simplex virus-induced inflammation by topically applying a composition including an effective amount of an antihistamine. The invention also features methods of treating inflammation by topically applying a base composition including essential extracts, either with or without one or more therapeutic agents. Also provided are compositions formulated for topical administration including a base composition, as well as kits including the composition.Type: ApplicationFiled: December 17, 2010Publication date: March 7, 2013Applicant: Exodus Life Sciences Limited PartnershipInventors: Harry J. Leighton, Crist J. Frangakis
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Publication number: 20130053380Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 28, 2011Publication date: February 28, 2013Applicant: PHENEX PHARMACEUTICALS AGInventors: Olaf Kinzel, Christoph Steeneck, Gerald Klaymann, Michael Albers, Thomas Hoffman, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
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Publication number: 20130053434Abstract: The present invention provides new compounds having a kinase inhibitory activity and useful for treating cancer.Type: ApplicationFiled: September 28, 2010Publication date: February 28, 2013Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE STRASBOURGInventors: Nicolas Winssinger, Sofia Barluenga
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Patent number: 8383671Abstract: 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: GrantFiled: June 18, 2009Date of Patent: February 26, 2013Assignee: Abbott Cardiovascular Systems Inc.Inventor: Paul M. Consigny
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Publication number: 20130045939Abstract: The invention relates to fatty and macrolide derivatives; compositions comprising an effective amount of fatty acid macrolide derivative; and methods for treating or preventing an autoimmune disorders and diseases with inflammation as the underlying etiology comprising the administration of an effective amount of a fatty acid macrolide derivative.Type: ApplicationFiled: March 18, 2011Publication date: February 21, 2013Applicant: CATABASIS PHARMACEUTICALS, INC.Inventors: Chi B. Vu, Jean E. Bemis, Michael R. Jirousek, Jill C. Milne
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Publication number: 20130041021Abstract: Methods of improving the pharmacokinetics of doxepin in a patient.Type: ApplicationFiled: October 16, 2012Publication date: February 14, 2013Applicant: SOMAXON PHARMACEUTICALS, INC.Inventor: SOMAXON PHARMACEUTICALS, INC.
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Publication number: 20130035302Abstract: The present invention is in the field of biomedicine pharmaceutical chemistry. Specifically, it refers to the use of yessotoxin, its derivatives and analogues, for the preparation of a medicinal drug for the prevention and/or treatment of neurodegenerative diseases related to abnormal levels of Tau and ?-amyloid proteins such as, for example, Alzheimer's disease.Type: ApplicationFiled: February 7, 2011Publication date: February 7, 2013Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELAInventors: Luis Miguel Botana López, Eva Alonso López, Carmen Vale González
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Publication number: 20130035284Abstract: The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.Type: ApplicationFiled: March 5, 2012Publication date: February 7, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Stanley J. Watowich, Suzanne M. Tomlinson, Scott Gilbertson
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Publication number: 20130030027Abstract: The present invention is directed to hemi phorboxazole A: and its stereoisomers, as well as derivatives of hemi phorboxazole A of formula I: wherein ring A is aryl or a 5- or 6-membered heteroaryl optionally substituted with one or more of halogen, —OH, or —C1-6alkyl; and R is —CN, a 5- or 6-membered heteroaryl, or halogen; and the pharmaceutically acceptable salt forms thereof, in addition to methods of using these compounds.Type: ApplicationFiled: July 23, 2010Publication date: January 31, 2013Applicants: The Regents of the University of California, The Trustes of The University of PennsylvaniaInventors: Amos B. Smith, III, Zhuqing Liu, Anne-Marie L. Hogan, Doralyn S. Dalisay, Tadeusz F. Molinski
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Publication number: 20130030044Abstract: This invention relates to the synthesis of certain novel Baylis-Hillman adducts of artremisinin derived aldehyde 2[10??-deoxoartemisininyl]-ethanal. The capabilities of introduction of three functional groups into a molecule in one step using Baylis-Hillman reaction encouraged us to synthesize some highly functionalized derivatives of artemisinin.Type: ApplicationFiled: January 20, 2011Publication date: January 31, 2013Applicant: Council of Scientific & Industrial ResearchInventors: Gakul Baishya, Nabin Chandra Barua, Abhishek Goswami, Partha Pratim Saikia, Paruchuri Gangadhar Rao, Ajit Kumar Saxena, Nitasha Suri, Madhunika Sharma
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Patent number: 8362069Abstract: Pharmaceutical/dermatological emulsions containing at least one avermectin compound, notably ivermectin, include at least one fatty phase and at least one aqueous phase, the at least one avermectin compound being solubilized in the fatty phase, which emulsions are useful for the treatment of a variety of dermatological conditions/afflictions, in particular rosacea.Type: GrantFiled: October 17, 2008Date of Patent: January 29, 2013Assignee: Galderma S.A.Inventors: Fanny Diaz-Astruc, Nathalie Barthez, Sandrine Segura-Orsoni
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Publication number: 20130023500Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.Type: ApplicationFiled: October 1, 2012Publication date: January 24, 2013Applicants: Human ServicesInventor: The United States of America, as represented by the Secretary, Department of Health and Human Services
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Publication number: 20130018090Abstract: Methods of treating sleep disorders, particularly certain aspects of insomnia, in elderly patients (65 years and older) by administering initial daily dosages of doxepin of 1-3 mg. These ultra-low initial dosages are more effective in elderly versus non-elderly patients in decreasing wake time during sleep, latency to persistent sleep and wake time after sleep, and are particularly efficacious in treating those conditions in the last hour of an 8-hour sleep cycle. Also, the dosages described herein are safe for elderly individuals.Type: ApplicationFiled: September 17, 2012Publication date: January 17, 2013Applicants: PROCOM ONE, INC., SOMAXON PHARMACEUTICALS, INC.Inventors: SOMAXON PHARMACEUTICALS, INC., PROCOM ONE, INC.
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Publication number: 20130012470Abstract: Novel compositions comprising viral fusion inhibition compounds and viral replication inhibition compounds as well as methods of their use are disclosed. The novel compositions are useful, inter alia, in the prevention, inhibition and/or treatment of Dengue Fever (DF) or Dengue Hemorrhagic Fever (DHF).Type: ApplicationFiled: July 7, 2011Publication date: January 10, 2013Applicant: Humanitas Technology, LLCInventors: John Schlafer Colman, Luis Ramon Romero
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Patent number: 8349887Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: GrantFiled: June 30, 2011Date of Patent: January 8, 2013Assignee: Tranzyme Pharma Inc.Inventors: Graeme L. Fraser, Hamid R. Hoveyda, Mark L. Peterson
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Publication number: 20130004569Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: COSMO TECHNOLOGIES LIMITEDInventors: Mauro AJANI, Roberta BOZZELLA, Giuseppe CELASCO, Roberto VILLA
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Publication number: 20130005655Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Applicant: Somaxon Pharmaceuticals, Inc.Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
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Publication number: 20120322717Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.Type: ApplicationFiled: May 22, 2009Publication date: December 20, 2012Inventors: Dakai Liu, Xiaofeng Li, Richard Jin, Yuaxin Liang, Wei Cheng, Riddhi Bhattacharyya, Guangrong Zhang
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Publication number: 20120322796Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.Type: ApplicationFiled: August 29, 2012Publication date: December 20, 2012Inventors: Bruno SCHOENTJES, Alain Philippe PONCELET, Julien Georges Pierre-Olivier DOYON, Joannes Theodorus Maria LINDERS, Lieven MEERPOEL, Luc August Laurentius VER DONCK
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Publication number: 20120316227Abstract: Embodiments of antimicrobial chrysophaentin compounds, pharmaceutical compositions including the chrysophaentin compounds, and methods for using the chrysophaentin compounds are disclosed. Some embodiments of the disclosed compounds are isolated from Chrysophaeum taylori. Certain embodiments of the chrysophaentin compounds inhibit FtsZ protein, thereby inhibiting the growth of clinically relevant bacteria, including drug-resistant strains.Type: ApplicationFiled: February 25, 2011Publication date: December 13, 2012Inventors: Carole A. Bewley, Alberto Plaza, Jessica Keffer