Nitrogen Containing Patents (Class 514/459)
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Publication number: 20140336137Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
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Publication number: 20140323530Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: March 26, 2014Publication date: October 30, 2014Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Ryo Kubota
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Publication number: 20140314857Abstract: In accordance with the present invention, there are provided compositions comprising zanamivir and at least one permeability enhancer. The compositions can increase the amount of zanamivir capable of being transported across a cell membrane (such as a Caco-2 cell membrane), and can increase this amount by at least 150% relative to the amount capable of being transported across the cell membrane in the absence of the permeability enhancer. Also provided are oral dosage forms of the compositions, which comprise a therapeutically effective amount of zanamivir and a permeability-enhancing amount of a permeability enhancer. The oral dosage forms can further comprise an enteric- or pH-sensitive coating or layer surrounding the composition. Also provided in accordance with the present invention are methods for treating or preventing influenza infection.Type: ApplicationFiled: June 30, 2014Publication date: October 23, 2014Inventors: Eric Holmes, Michael Hite, Gary K. Ostrander
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Publication number: 20140315905Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventor: Soren Ebdrup
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Publication number: 20140309208Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
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Patent number: 8858991Abstract: Disclosed herein are controlled-release oral pharmaceutical dosage forms comprising MGBG, and their application for the improved treatment of diseases with reduced side effects and/or longer time at maximum concentration.Type: GrantFiled: January 19, 2012Date of Patent: October 14, 2014Assignee: Pathologica LLCInventors: John McKearn, Jeremy Blitzer
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Patent number: 8846609Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.Type: GrantFiled: June 19, 2012Date of Patent: September 30, 2014Assignee: New York UniversityInventors: Victor J. Torres, Derya Unutmaz, Francis Alonzo, III
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Patent number: 8841290Abstract: Disclosed is a tetrahydronapthalene compound having Formula I the variables of which are as described herein, methods of preparing same and their use.Type: GrantFiled: February 12, 2010Date of Patent: September 23, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
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Publication number: 20140275043Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Publication number: 20140275008Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Patent number: 8834920Abstract: Short oligopeptides are provide which are capable of binding to the epidermal growth factor receptor on the surface of human tumor cells. Methods for using the peptides as targeting moieties in more complex compositions, such as conjugates of cytoxins, and/or structures, such as liposomal structures, for the purposes of drug delivery are also provided.Type: GrantFiled: December 20, 2007Date of Patent: September 16, 2014Assignee: Alza CorporationInventors: Ken Shi Kun Huang, Weiming Zhang, Guoyang Zhang, Francois Nicol, Anthony Huang
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Publication number: 20140255479Abstract: The present invention provides pharmaceutical compositions suitable for oral and methods of treating subjects in need thereof. The pharmaceutical compositions of the present invention enhance bioavailability of at least one compound classified as BCS Class II, BCS Class III or BCS Class IV.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Inventors: Stephen M. Carl, John Stanley Vrettos, William Stern
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Publication number: 20140256698Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Robert Booth, Jeff Dener, Michael Green
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Publication number: 20140249105Abstract: Compounds, ceramide analogues, having a cyclic structure derived from cyclopropane, cyclobutane or cyclopentane, the ring bearing two chains consisting of an amide function. Each amide function is attached to the ring by the nitrogen atom of the function and carries a hydrocarbon chain derived from a fatty acid. The amide functions can be cis or trans relative to one another. Processes for the preparation of these novel compounds as well as pharmaceutical and/or cosmetic compositions containing them.Type: ApplicationFiled: July 25, 2011Publication date: September 4, 2014Applicant: DiverchimInventors: Jean-Louis Brayer, Natacha Frison, Benoit Folleas
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Patent number: 8821876Abstract: Methods of identifying infectious disease infection prior to presentation of symptoms, assays for identifying genomic markers of infectious disease, and methods for diagnosing the underlying etiology of infectious disease.Type: GrantFiled: May 26, 2010Date of Patent: September 2, 2014Assignee: Duke UniversityInventors: Geoffrey S. Ginsburg, Joseph Lucas, Christopher W. Woods, Lawrence Carin, Aimee K. Zaas, Alfred Hero
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Publication number: 20140243374Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.Type: ApplicationFiled: October 4, 2012Publication date: August 28, 2014Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
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Patent number: 8815941Abstract: Compounds of structural formula (I) useful for the treatment or prophylaxis of viral infection, particularly viral influenza are provided Pharmaceutical preparations thereof and methods for their preparation are also described. The therapeutic effect is achieved via inhibition of viral neuraminidases, also known as viral sialidases. These neuraminidases are classified under the GH34 family of viral enzymes.Type: GrantFiled: July 15, 2010Date of Patent: August 26, 2014Assignee: The University of British ColumbiaInventors: Stephen Withers, Andrew Graham Watts, Jin Hyo Kim, Tom Wennekes
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Patent number: 8815925Abstract: The invention relates to the use of an antimycotic agent and an epithelial cell or endothelial cell adhesion inhibitor for producing a combination drug for the topical treatment of Candida mycoses selected from vulvovaginal candidiasis, oropharyngeal candidiasis (oral thrush), diaper dermatitis (diaper thrush) and intertriginous (Candida) eczema.Type: GrantFiled: October 2, 2013Date of Patent: August 26, 2014Inventors: Christian Noe, Marion Noe-Letschnig
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Publication number: 20140213617Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: January 23, 2014Publication date: July 31, 2014Applicant: ACUCELA INC.Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
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Publication number: 20140194505Abstract: Disclosed are neuraminidase inhibitor compounds and pharmaceutical compositions with improved bioavailability and/or improved efficacy and methods of treating influenza using the compounds and pharmaceuticals compositions.Type: ApplicationFiled: February 11, 2014Publication date: July 10, 2014Applicant: SineVir Therapeutics LLCInventors: John Hilfinger, Wei Shen
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Publication number: 20140179687Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: February 21, 2014Publication date: June 26, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Patent number: 8759354Abstract: Disclosed is a pharmaceutical composition comprising a pyrazine derivative represented by the general formula: [wherein R1 and R2 independently represent a hydrogen atom or a halogen atom; and R3 represents a hydrogen atom or an amino-protecting group] or a salt thereof and at least one neuraminidase inhibitor. The pharmaceutical composition is useful for a treatment including the treatment or prevention of influenza. Also disclosed is a method of using these components in combination. The method is useful for a treatment including the treatment or prevention of influenza.Type: GrantFiled: February 14, 2008Date of Patent: June 24, 2014Assignee: Toyama Chemical Co., Ltd.Inventor: Masako Maekawa
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Patent number: 8754121Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.Type: GrantFiled: August 19, 2011Date of Patent: June 17, 2014Assignee: Academia SinicaInventors: Lie-Fen Shyur, Wen-Wan Chao, Ya-Wen Cheng
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Publication number: 20140155478Abstract: Disclosed herein is a novel antifungal compound, derivatives that are used to treat fungal infections. In a specific embodiment, the compound is a small molecule. In a specific embodiment, the compound described herein inhibits yeast to hypha transition under robust hyphal inducing conditions at lower concentration of the molecule. Also disclosed is a composition comprising the antifungal compound. In a specific embodiment, the composition is a pharmaceutical composition. Also disclosed is a method of treating and/or preventing fungal infection using the disclosed compound. The disclosed compound exhibits antifungal activity against wide range of fungal species at slightly higher concentrations. Antifungal compound disclosed herein is used as anti-biofilm agent against fungal infections.Type: ApplicationFiled: December 3, 2013Publication date: June 5, 2014Applicant: The University of Hong KongInventors: Chaminda Jayampath SENEVIRATNE, Yi Tsun Richard KAO, Lakshman Perera SAMARANAYAKE, Kwok Yung YUEN, Dan YANG, Yu WANG, Sze Wah Sarah WONG
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Publication number: 20140155350Abstract: A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.Type: ApplicationFiled: November 26, 2013Publication date: June 5, 2014Applicant: SineVir Therapeutics LLCInventors: John Hilfinger, Gordon Amidon
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Publication number: 20140142137Abstract: Provided herein, inter alia, are novel compounds for the inhibition of HIV integrase. The compounds disclosed herein are useful for methods of treating HIV infection in a subject in need thereof.Type: ApplicationFiled: August 2, 2013Publication date: May 22, 2014Applicants: National Institutes of Health, The Regents of the University of CaliforniaInventors: Seth M. Cohen, Arpita Agrawal, Jamie DeSoto, Yves Pommier, Kasthuraiah Maddali
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Publication number: 20140120112Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.Type: ApplicationFiled: December 19, 2013Publication date: May 1, 2014Inventor: Kameran Lashkari
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Patent number: 8703813Abstract: Provided is a compound having a spiro chiral carbon backbone, a stereoisomer thereof, an enantiomer thereof, an in vivo hydrolysable precursor thereof, or a pharmaceutically acceptable salt thereof. The compound having the spiro chiral carbon backbone has excellent osteoblast differentiation activity, mast cell inhibitory activity, and fatty acid synthesis inhibitory activity in the liver. Therefore, the compound can be expected to play an innovative role in treatment of osteoporosis, fatty liver, and obesity.Type: GrantFiled: October 30, 2009Date of Patent: April 22, 2014Assignee: SNU R & DB FoundationInventors: Heon-Joong Kang, Jung-Rae Rho, Jeong-Ho Hong, Seung-Bum Park, Chan-Soo Shin, Jae-Hwan Lee, Jun-Young Hong, Eun-O Kim, Jeong-Ah Kim, Sang-Mi Oh
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Publication number: 20140093518Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.Type: ApplicationFiled: August 26, 2013Publication date: April 3, 2014Applicant: The Scripps Research InstituteInventor: Carlos F. Barbas, III
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Publication number: 20140088158Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: November 27, 2013Publication date: March 27, 2014Applicant: SANOFIInventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
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Patent number: 8680148Abstract: Methods for treating a bacterial infection by using a metallo-desferrioxamine complex.Type: GrantFiled: August 13, 2007Date of Patent: March 25, 2014Assignees: University of Washington, Hadasit Medical Research Services and Development Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: E. Peter Greenberg, Ehud Banin, Eyal Banin, Eduard Berenshtein, Mordechai Chevion
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Publication number: 20140073688Abstract: A compound for use in a therapeutic treatment of filariasis or a prophylactic treatment of filariasis of the general formula (1) or at least one of racemates, enantiomers, diastereomers, solvates, hydrates, pharmaceutically acceptable salts, and esters of the general formula (1), a nematicidal composition comprising as an active ingredient a compound according to the general formula (1), and a method for treating filariasis.Type: ApplicationFiled: May 4, 2012Publication date: March 13, 2014Applicant: RHEINISCHE FRIEDRICH-WILHELMS UNIVERSITAET BONNInventors: Kenneth Michael Pfarr, Achim Hoerauf, Gabriele Maria Koenig, Sabine Specht, Andrea Schiefer, Till Friedrich Schaeberle, Alexander Schmitz, Stefan Kehraus
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Publication number: 20140073611Abstract: The disclosure relates to a platform of using zebrafish in screening candidates for treating and/or preventing myopia and keratoconus disease. The disclosure is mainly based on that Lumican, one of several SLRPs, plays an important role in the regulation of fibrillogenesis or the genes affecting the size of eyeballs in zebrafish, in addition to playing an important role in clinical myopia. Therefore, the disclosure uses the established zebrafish model to further identify the drugs affecting the expression of lumican and collagen fibrillogenesis, and/or the regulation of eyeball size. These drugs are potential candidates for treating myopia and/or keratoconus disease.Type: ApplicationFiled: May 21, 2013Publication date: March 13, 2014Applicant: National Taiwan UniversityInventors: I-Jong Wang, Wei-Ting Ho, Ting-Hsuan Chiang, I-Tsen Lin
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Publication number: 20140073501Abstract: A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Inventors: Ratnakar Asolkar, Marja Koivunen, Pamela Marrone
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Publication number: 20140044661Abstract: Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DPOH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.Type: ApplicationFiled: October 23, 2013Publication date: February 13, 2014Applicant: JOHNSON & JOHNSON CONSUMER COMPANIES, INC.Inventors: Michael J. Fevola, Frank C. Sun, Stacey E. York
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Publication number: 20140039048Abstract: Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.Type: ApplicationFiled: May 3, 2013Publication date: February 6, 2014Applicant: Acucela Inc.Inventor: Acucela Inc.
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Publication number: 20140024650Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: April 5, 2012Publication date: January 23, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
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Publication number: 20140018417Abstract: A method for manufacturing a compound represented by the formula (13): wherein R2 represents a C1-C4 alkyl group and Ac represents an acetyl group, including reacting a compound represented by the following formula (12): wherein R2 represents a C1-C4 alkyl group, Ac represents an acetyl group and Boc represents a tert-butoxycarbonyl group, with water.Type: ApplicationFiled: August 14, 2013Publication date: January 16, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yoshitaka NAKAMURA, Masayuki MURAKAMI, Makoto YAMAOKA, Masakazu WAKAYAMA
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Publication number: 20140018418Abstract: A method of treating or preventing H5N1 influenza by administering to a person in need thereof a pharmacologically effective amount of 5-acetamido-4-guanidino-9-O-hexanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid, 5-acetamido-4-guanidino-9-O-decanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid, 5-acetamido-4-guanidino-9-O-dodecanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid or 5-acetamido-4-guanidino-9-O-tetradecanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid. A method of preventing H5N1 influenza by administering to a person in need thereof a pharmacologically effective amount of 5-acetamido-4-guanidino-9-O-octanoyl-2,3,4,5-tetradeoxy-7-O-methyl-D-glycero-D-galacto-non-2-enopyranosoic acid.Type: ApplicationFiled: August 27, 2013Publication date: January 16, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Makoto YAMASHITA, Yoshihiro KAWAOKA
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Publication number: 20140005181Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Applicant: Sanford-Burnham Medical Research InstituteInventors: Layton Smith, Anthony B. Pinkerton
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Publication number: 20130338117Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 27, 2013Publication date: December 19, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: Robert P. RICCIARDI
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Publication number: 20130338116Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Inventor: Irving Sucholeiki
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Publication number: 20130331413Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Patent number: 8598221Abstract: The present invention relates to a pharmaceutical composition comprising as active substances: at least one compound of the following general formula (I): and at least one inhibitor of type 2 cyclooxygenase (COX-2), notably for use in the prevention or treatment of pain.Type: GrantFiled: December 3, 2010Date of Patent: December 3, 2013Assignee: BiocodexInventors: Philippe Girard, Marie-Emmanuelle Le Guern, Jean-Marie Gillardin, Bernard Hublot
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Publication number: 20130303530Abstract: The present invention provides methods and compositions for treating chronic pelvic pain syndrome. In particular, the present invention provides methods and compositions for treating chronic pelvic pain syndrome with an agent that targets MCP-1, MIP-1?, or the CCR-2 receptor.Type: ApplicationFiled: July 8, 2013Publication date: November 14, 2013Applicant: Northwestern UniversityInventors: Anthony J. Schaeffer, David Klumpp, Praveen Thumbikat
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Publication number: 20130298291Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: November 11, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
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Publication number: 20130281490Abstract: The present invention provides compounds and pharmaceutical compositions for inhibiting N-acylethanolamine acid amidase (NAAA). Inhibition of NAAA is contemplated as a method to sustain the levels of palmitoylethanolamide (PEA) and oleylethanolamide (OEA), two substrates of NAAA, in conditions characterized by reduced concentrations of PEA and OEA. The invention also provides methods for treating inflammatory diseases and pain, and other disorders in which decreased levels of PEA and OEA are associated with the disorder.Type: ApplicationFiled: November 21, 2012Publication date: October 24, 2013Inventors: The Regents of the University of California, Fondazione Istituto Italiano Di Tecnologia, Universita Degli Studi Di Parma, Universita Degli Studi Di Urbino "Carlo Bo"
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Publication number: 20130274229Abstract: Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.Type: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Applicant: Academia SinicaInventors: Chi-Huey Wong, Jim-Min Fang, Kung-Cheng Liu, Jia-Tsrong Jan, Yih-Shyun E. Cheng, Ting-Jen R. Cheng
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Patent number: 8552033Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: December 17, 2008Date of Patent: October 8, 2013Assignee: SANOFIInventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter