Abstract: A method of treating irritable bowel syndrome in a patient in need thereof by administering to said patient a pharmaceutically effective amount of tapentadol.
Type:
Application
Filed:
April 13, 2017
Publication date:
August 3, 2017
Inventors:
Klaus SCHIENE, Petra BLOMS-FUNKE, Thomas CHRISTOPH, Wolfgang SCHROEDER
Abstract: Activity-generating delivery molecules comprising the structure R3—(C?O)-Xaa-NH—R4 wherein Xaa is any D- or L-amino acid residue with a non-hydrogen, substituted or unsubstituted side chain, R3—(C?O)— and —NH—R4 are independently a long chain group, each long chain group containing one or more carbon-carbon double bonds, and salts, compositions and methods of use thereof. The activity-generating delivery compounds and compositions are useful for generating activity of an active agent in a cell, tissue, or subject.
Type:
Application
Filed:
April 13, 2017
Publication date:
August 3, 2017
Inventors:
Renata Fam, Roger C. Adami, Kathy L. Fosnaugh, Pierrot Harvie, Rachel E. Johns, Shaguna Seth, Michael E. Houston, JR., Michael V. Templin
Abstract: The present invention is directed to a pharmaceutical submicron suspension and a method of forming the submicron suspension. The submicron suspension is useful for delivery of relatively hydrophobic and/or low solubility therapeutic agent. The submicron suspension and method of forming the submicron suspension typically employ a polymeric material that aids in preventing aggregation of the therapeutic agent.
Type:
Application
Filed:
April 21, 2017
Publication date:
August 3, 2017
Inventors:
Bahram Asgharian, Ernesto J. Castillo, Masood A. Chowhan
Abstract: Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof.
Abstract: The present invention concerns a pharmaceutical composition comprising 0.3% by weight of adapalene or a pharmaceutically acceptable salt thereof and 2.5% by weight of benzoyl peroxide, as active ingredients, for its use by topical administration in the treatment of inflammatory acne lesions. The present invention further concerns regimen for the therapeutic treatment of acne lesions in subjects afflicted with severe acne. The regimen includes topically applying to a subject's skin, as active ingredients, 0.3% by weight adapalene and 2.5% by weight benzoyl peroxide, combined in a single formula that delivers the active ingredients together. The single formula can for example be applied once or twice daily for a period of 8 to 12 weeks.
Type:
Application
Filed:
July 16, 2015
Publication date:
August 3, 2017
Inventors:
Matthew James LEONI, Michael GRAEBER, Vasant MANNA
Abstract: Methods of treating at least one condition chosen from pain, inflammation, and fever in a critically ill patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen using a first dosage regimen, wherein the first dosage regimen produces a first pharmacokinetic profile in critically ill patients that is about equivalent to a second pharmacokinetic profile produced by administration of the intravenous pharmaceutical composition using a second dosage regimen of ibuprofen to non-critically ill patients, wherein the at least one condition of the critically ill patient is thereby treated.
Abstract: This disclosure provides generally for antimicrobial compositions and methods of use comprising an anthocyanin, an anthocyanidin or metabolites thereof. Methods for promoting healing of a wound using these compositions are also disclosed. These compositions have broad spectrum antimicrobial activity and are safe for human and animal uses. Further, these compositions are safe for medical uses and industrial uses as antiseptic preparations to reduce or prevent microbial growth, including killing bacterial biofilms.
Abstract: A method for treating a subject afflicted with dementia is disclosed. The method comprises administering to the subject a composition comprising an effective amount of a benzoic acid, a salt, an ester, or a derivative thereof, and a pharmaceutically acceptable carrier or vehicle, wherein the subject is not administered any other neuropharmaceutical.
Abstract: A regimen for the safe and effective long-term treatment of acne vulgaris entails topically applying onto the affected skin area of a subject afflicted therewith, for a period of time of at least four (4) months, e.g., for at least twelve (12) months and advantageously on a daily basis and preferably once a day, a thus effective amount of a topical medicament containing adapalene and benzoyl peroxide, formulated into a pharmaceutically acceptable medium therefor.
Abstract: The present invention provides a simple and improved dose form that is capable of providing a controlled release of GABAB receptor agonist contained in the core thereof The invention also provides methods of administering the dosage form and of treating conditions that are therapeutically responsive to GABAB receptor agonist.
Type:
Application
Filed:
April 20, 2017
Publication date:
August 3, 2017
Applicant:
OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT
Inventors:
Glenn A. MEYER, Cristian R. FRANCO, Gustavo A. FISCHBEIN, Alejandro A. AGUILAR, Claude E. WRIGHT
Abstract: Compositions comprising high concentration of monounsaturated fatty acids having low melting points and high iodine values and use of such compositions as dietary supplements, nutraceuticals or pharmaceuticals for reducing atherosclerotic plaque in mammals. It has been found that high concentrations of monounsaturated fatty acids (MUFAs) having low melting point temperatures and iodine values of about 50 to about 130 can be used to effectively treat atherosclerosis. Epidemiological studies suggest that those populations consuming large quantities of C18:1 found in olive oil are protected against vascular diseases such as atherosclerosis.
Abstract: Methods of modulating healing response to vascular injury and/or vascular scarring in a subject are provided. As such, aspects of the disclosure relate to the use of pro-resolving lipid mediators to modulate inflammation and/or restenosis of a vascular wall. Another aspect of the disclosure relates to the use of pro-resolving lipid mediators to modulate a biological activity of vascular smooth muscle cells (VSMC) or vascular endothelial cells (VEC). Pro-resolving lipid mediators that fmd use in the subject methods include derivatives of omega-3 polyunsaturated fatty acids and omega-6 polyunsaturated fatty acids, such as resolvins, protectins, lipoxins and maresins and their therapeutically stable analogs. Also provided are vascular devices and compositions for use in the subject methods. Such methods, devices and compositions fmd use in a variety of applications, including applications related to treatment of vascular injuries and vascular scarring (e.g.
Type:
Application
Filed:
September 2, 2016
Publication date:
August 3, 2017
Inventors:
Michael S. Conte, Charles N. Serhan, Tejal A. Desai
Abstract: The invention is directed to microbial oils containing omega-3 polyunsaturated fatty acids comprising docosahexaenoic acid, eicosapentaenoic acid, and optionally docosapentaenoic acid and dosage forms containing such oils.
Type:
Application
Filed:
April 7, 2017
Publication date:
August 3, 2017
Inventors:
Kirk E. APT, Paul Warren Behrens, Jon Milton Hansen, Joseph W. Pfeifer, Tracey Lyy Stahl, Ross Zirkle
Abstract: Disclosed herein are methods of using polyunsaturated fatty acids and derivatives thereof (“PUFAs”) to modulate Iks channels to treat conditions associated with a disruption in Iks channel activity, such as cardiac arrhythmias. In particular, disclosed herein are negatively charged PUFAs having decreased pKa values, which can activate (i.e., open) IKs channels, and positively charged PUFAs that can inhibit (i.e., close) IKS channels.
Type:
Application
Filed:
August 4, 2015
Publication date:
August 3, 2017
Inventors:
Hans Peter Larsson, Sara Liin, Fredrik Elinder
Abstract: The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, having the structure:
Type:
Application
Filed:
February 10, 2017
Publication date:
August 3, 2017
Applicant:
The Research Foundation for The State University of New York
Inventors:
Iwao Ojima, Dale Deutsch, Martin Kaczocha, William T. Berger, Robert Rizzo, Trent E. Balius
Abstract: Pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating heart failure diseases such heart failure with preserved ejection fraction (HFPEF) alone or in combination with statins (HMG-CoA reductase inhibitors) are disclosed.
Abstract: The present invention relates to a stable, sterile, ready to administer parenteral dosage form of amiodarone or its pharmaceutically acceptable salt. Particularly, the present invention provides a stable, sterile, ready to administer parenteral dosage form of amiodarone comprising an aqueous solution comprising amiodarone or its pharmaceutically acceptable salt, an acid, and a polyol, wherein the pH of the solution is in the range of about 2.0 to 4.0, wherein the solution is filled in a plastic container and wherein the solution is free of a solubilizer.
Abstract: The present invention provides methods for treating or preventing diabetic nephropathy and its related pathologies by inhibiting podocyte Semaphorin3a (Sema3a). The invention also provides a method for identifying or characterizing a compound useful for treating or preventing diabetic nephropathy.
Abstract: The present application concerns polyphenol compositions, and the use of such compositions for preventing or treating endothelial dysfunction. The polyphenol compositions of the invention comprise at least one ellagitannin in combination with at least one proanthocyanidin.
Abstract: A method for treating Zika virus infection with a composition containing quercetin or isoquercetin, together with one or more of vitamin B3, vitamin C, and a folate compound is described. Methods of preventing microcephaly and treating and preventing infections of other Flavivridae viruses are also described.
Abstract: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and far treating or preventing iron deficiency and anemia of chronic disease.
Type:
Application
Filed:
April 13, 2017
Publication date:
August 3, 2017
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson, Todd W. Seeley, Ingrid Langsetmo Parobok
Abstract: Disclosed are methods and pharmaceutical compositions for modulating one or more steroidal receptor activities. The methods typically utilize and the pharmaceutical compositions typically include one or more substituted phenyl aziridine precursors, their respective aziridines, analogs thereof, derivatives thereof, or pharmaceutically acceptable salts thereof such as CpdA. The methods and compositions may be used for treating diseases, disorders, and conditions associated with glucocorticoid receptor activity, androgen receptor activity, or both, such as cancers, acne vulgaris, and alopecia.
Abstract: Use of a glucagon receptor antagonist in combination with a cholesterol absorption inhibitor for the treatment of diabetes and related conditions is disclosed.
Type:
Application
Filed:
April 11, 2017
Publication date:
August 3, 2017
Applicant:
Merch Sharp & Dohme Corp.
Inventors:
Hong-Ping Guan, Jose M. Castro-Perez, Harry R. Davis, Samuel E. Engel, Douglas G. Johns, Songnian Lin, Stephen F. Previs, Thomas P. Roddy, Liangsu Wang, Sheng-Ping Wang, Yusheng Xiong
Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
Type:
Application
Filed:
September 6, 2016
Publication date:
August 3, 2017
Inventors:
Anthony Alexander McKinney, Franklin Porter Bymaster
Abstract: Compounds of general formula I that are capable of inhibiting bacterial pyruvate kinase and/or bacterial growth. The compounds may find use as antibacterial agents in therapeutic and/or non-therapeutic contexts.
Type:
Application
Filed:
July 10, 2015
Publication date:
August 3, 2017
Inventors:
Robert N. YOUNG, Nag Sharwan KUMAR, Christophe LABRIERE, Jon Paul SELVAN, James Brian JAQUITH, Edith Mary DULLAGHAN
Abstract: Compositions comprising ketorolac tromethamine at a therapeutically effective concentration of less than 0.5% are disclosed herein. Methods of treating or preventing ocular pain using said compositions are also disclosed herein.
Type:
Application
Filed:
February 24, 2017
Publication date:
August 3, 2017
Inventors:
Christopher A. Muller, Janet K. Cheetham, Teresa H. Kuan, David F. Power
Abstract: The present invention relates to an FK506 derivative which has reduced immunosuppressive activity but maintains nerve regeneration activity, a preparing method thereof, and a pharmaceutical composition comprising the same for preventing or treating nervous system diseases. A composition comprising 9-deoxo-prolyl-FK506, 31-O-demethyl-FK506, or 9-deoxo-31-O-demethyl-FK506 can promote nerve regeneration and has reduced immunosuppressive activity, thereby reducing side effects in the treatment of nervous system diseases.
Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
Abstract: A method of treating a CNS disorder. The method comprises providing a water-soluble histone deacetylase inhibitor, and administering the water-soluble histone deactylase inhibitor directly into a brain via convection enhanced delivery.
Abstract: The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy.
Type:
Application
Filed:
April 20, 2017
Publication date:
August 3, 2017
Inventors:
Shuang Liu, John Frederick QUINN, Bryan Cordell DUFFY, Ruifang WANG, May Xiaowu JIANG, Gregory Scott MARTIN, He ZHAO, Michael ELLIS, Gregory Steven WAGNER, Peter Ronald YOUNG
Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.
Abstract: The invention relates to novel compounds and pharmaceutical preparations thereof, as well as methods of making an using these compounds. The invention further relates to methods of treating or preventing disease using the novel compounds of the invention.
Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
Abstract: Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
Type:
Application
Filed:
March 29, 2017
Publication date:
August 3, 2017
Inventors:
Kenneth W. BAIR, Timm R. BAUMEISTER, Peter DRAGOVICH, Xiongcai LIU, Snahel PATEL, Po-Wai YUEN, Mark ZAK, Guiling ZHAO, Yamin ZHANG, Xiaozhang ZHENG
Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
Type:
Application
Filed:
April 17, 2017
Publication date:
August 3, 2017
Inventors:
Huji Turdi, Jon J. Hangeland, R. Michael Lawrence, Dong Cheng, Saleem Ahmad, Wei Meng, Robert Paul Brigance, Pratik Devasthale, Guohua Zhao
Abstract: The present invention is directed to novel substituted macrocycles compounds, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds and compositions of the present invention have protein kinases inhibitory activities and are expected to be useful for the treatment of protein kinases mediated diseases and conditions.
Abstract: The present invention primarily relates to multi-component crystals comprising a compound of formula 1 and a second compound selected from the group consisting of co-crystal formers and solvents. The invention is further related to pharmaceutical compositions comprising such multi-component crystals. Furthermore, the invention relates to processes for preparing said multi-component crystals. The invention also relates to several aspects of using said multi-component crystals or pharmaceutical compositions to treat a disease.
Type:
Application
Filed:
August 3, 2015
Publication date:
August 3, 2017
Inventors:
MARTIN VIERTELHAUS, Tiziana CHIODO, Beate SALVADOR, Marcus VOSSEN, Andreas HAFNER, Tobias HINTERMANN, Walter WEISHAAR, Rolf HELLMANN
Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.
Abstract: The invention relates to a gel composition containing pirfenidone, which is advantageous over other cutaneously administered pharmaceutical forms known in the prior art and which can be used in treatment for the restoration of tissues with fibrotic lesions and for the prevention of fibrotic lesions.
Type:
Application
Filed:
February 17, 2017
Publication date:
August 3, 2017
Inventors:
José Agustín Rogelio MAGAÑA CASTRO, Laura VÁZQUEZ CERVANTES, Juan Socorro ARMENDÁRIZ BORUNDA
Abstract: Methods of treating developmental disorders by administering a pharmaceutical composition of pipradrol or a pharmaceutically acceptable salt thereof are provided. The methods may be used to treat conditions such as epilepsy, Landau-Kleffner Syndrome, Lennox-Gastaut syndrome (LGS) and Dravet syndrome.
Abstract: An oral methylphenidate extended release tablet is described, which can be scored and still retain its extended release profile. The tablet contains a combination of an uncoated methylphenidate-ion exchange resin complex, a barrier coated methylphenidate-ion exchange resin complex-matrix, and an uncomplexed methylphenidate active component. Following administration of a single dose of the extended release methylphenidate chewable tablet, a therapeutically effective amount of methylphenidate is reached in less than about 20 minutes and the composition provides a twelve-hour extended release profile.
Abstract: The present disclosure relates to salts of heterocyclic compounds and methods that inhibit HIF pathway activity. The compounds are designed to treat or prevent cancer and other hypoxia-mediated diseases.
Type:
Application
Filed:
April 20, 2017
Publication date:
August 3, 2017
Inventors:
Philip JONES, Maria Emilia DI FRANCESCO, Timothy MCAFOOS
Abstract: Provided herein are methods and compositions for modulating the activity or level of a sirtuin, thereby treating or preventing obesity or an insulin resistance disorder, such as diabetes in a subject. Exemplary methods comprise contacting a cell with a sirtuin activating compound or an inhibitory compound to thereby increase or decrease fat accumulation, respectively.
Type:
Application
Filed:
February 3, 2017
Publication date:
August 3, 2017
Applicants:
President and Fellows of Harvard College, The General Hospital Corporation d/b/a Massachusetts General Hospital
Inventors:
David A. Sinclair, Maria Alexander-Bridges
Abstract: This invention provides a compound selected from the group consisting of L-nicotine(X1)(X2) and D-nicotine(X1) (X2), or a pharmaceutically acceptable salt thereof, wherein (i) each of X1 and X2 is independently a pharmaceutically acceptable anion or a null set; and (ii) X1 and X2 cannot both be null sets. This invention also provides related compositions, as well as methods for treating a disorder reasonably believed to be ameliorated by the administration of nicotine.
Abstract: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
Type:
Application
Filed:
April 21, 2017
Publication date:
August 3, 2017
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Robert C. Stephenson, Todd W. Seeley, Ingrid Langsetmo Parobok
Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.
Type:
Application
Filed:
August 12, 2016
Publication date:
August 3, 2017
Inventors:
Yan FENG, Ottavio ARANCIO, Shixian DENG, Donald W. LANDRY