Abstract: This invention relates to a method of treating B cell malignancies, which involves administering to a subject a compound having a structure of formula (I) to cause cell death of a B cell malignancy, thereby treating the B cell malignancy in the subject. Also disclosed are a method of causing cell death of malignant B cells, pharmaceutical compositions and therapeutic systems comprising a compound having a structure of formula (I), and a compound having a structure of formula (I).
Abstract: Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): or a pharmaceutically acceptable salt, or ester thereof, wherein R1 and R2 are independently chosen from a hydrogen atom or linear, branched, and/or cyclic C1-C6 alkyl groups, with the proviso that R1 and R2 are not both hydrogen or a pharmaceutically acceptable salt or ester thereof. Such diseases or conditions may relate to coronary heart disease (CHD), for example atherosclerosis; metabolic syndrome/insulin resistance; and/or a dyslipidemic condition such as hypertriglyceridemia (HTG), elevated LDL-cholesterol, elevated total-cholesterol, elevated Apo B and low HDL-cholesterol. The present disclosure further provides for a method of reducing atherosclerosis development. Pharmaceutical compositions comprising a compound of Formula (I) are also disclosed.
Type:
Grant
Filed:
November 3, 2011
Date of Patent:
July 19, 2016
Assignee:
PRONOVA BIOPHARMA NORGE AS
Inventors:
Ragnar Hovland, Tore Skjæret, David Fraser
Abstract: Provided is a pharmaceutical composition that contains a 1,2-dithiolthionederivative, and is effective to prevent and treat a disease caused by overactivity of a liver X receptor? (LXR?) or a sterol response element binding protein (SREBP-1). Specifically, the pharmaceutical composition includes 1,2-dithiolthione derivatives such as 4-methyl-5-(2-pyrazinyl)-1,2-dithiol-3-thione, 3-methyl-1,2-dithiol-3-thione, or 5-(6-methoxypyrazinyl)-4-methyl-1,2-dithiol-3-thione. The pharmaceutical composition is effective for preventing and treating hypertension caused by renin, aldosteronism, adrenoleukodystrophy, glomerulosclerosis, proteinuria, nephropathy, liver steatosis, hypertriglyceridemia or hyperreninemia.
Type:
Grant
Filed:
July 30, 2009
Date of Patent:
June 21, 2016
Assignee:
SNU R&DB FOUNDATION
Inventors:
Sang Geon Kim, Sung Hwan Ki, Seong Hwan Hwang
Abstract: A combination hormone and melatonin therapy is provided to reduce the risk of developing, or to reduce the severity of, breast cancer by administering at least one estrogen hormone and optionally at least one progesterone-receptor-binding compound or composition and melatonin together, preferably at normal bed time.
Abstract: The present disclosure relates to methods and compositions for modulating the activity of KCNQ channels as a means for reducing the effects of aberrant KCNQ channel function associated with epilepsy, deafness and arrhythmias including but not limited to, Long-QT syndrome (“LQTS”), and atrial fibrillation. The present disclosure also relates to the discovery of certain regions of KCNQ channels that interact with various channel stimulating molecules such as, ATP, and PIP2, as well as KCNQ channel domains that effect voltage dependant channel activation. The disclosure is also directed to the use of small molecules to modulate KCNQ channel activity in a cell. Moreover, the present disclosure relates to the therapeutic effects of treating a subject with modulators of KCNQ channel activity.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
May 24, 2016
Assignees:
Washington University, The Research Foundation for The State University of New York, Curators of the University of Missouri
Abstract: Oral cannabinoid formulations, including an aqueous-based oral dronabinol solution, that are stable at room or refrigerated temperatures and may possess improved in vivo absorption profiles with faster onset and lower inter-subject variability.
Type:
Grant
Filed:
October 4, 2012
Date of Patent:
May 24, 2016
Assignee:
INSYS DEVELOPMENT COMPANY, INC.
Inventors:
Venkat R. Goskonda, Ashok Chavan, Amit Kokate, Howard Gill
Abstract: The present invention provide chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit host targeting functions in insects such as mosquitoes. Method of employing such agents, and articles incorporating the same, are also provided.
Type:
Grant
Filed:
October 21, 2011
Date of Patent:
May 10, 2016
Assignee:
Vanderbilt University
Inventors:
Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Patrick L. Jones
Abstract: The present invention provides formulas of elemental compositions encompassing acetate salts of calcium, magnesium and zinc along with vitamin D3. The acetate salts could be extracted from natural sources such as pearls, coral, and oyster or compounded using synthetic materials. The dosage and ratio of calcium to magnesium was estimated using in vitro and in vivo estimations. The dosage for promoting bone health and alleviation of osteoporosis is about a quarter to a third of the conventional dose.
Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the formula: wherein R is selected from one or more of the same or different of hydrogen, hydroxyl, optionally substituted alkyl, optionally substituted aryl, alkoxy, aryloxy, thiol, and optionally substituted amino, and wherein R1 is selected from one or more of the same or different of hydrogen, acetyl, optionally substituted alkyl, optionally substituted aryl, and an amino acid selected from leucine, valine, isoleucine, and glycine.
Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.
Type:
Grant
Filed:
March 14, 2011
Date of Patent:
January 5, 2016
Assignee:
Proximagen Limited
Inventors:
David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
Abstract: The invention includes compositions comprising a selective small-molecule inhibitor of RAD51 recombinase and a pharmaceutically acceptable carrier. The invention further includes methods of treating or preventing cancer in a subject, comprising the step of administering to the subject the compositions contemplated within the invention.
Abstract: A composition of alkali carbonate peroxyhydrate in a quantity of 45 to 85% by weight relative to a total amount of the composition and an alkali hydrogen carbonate is provided for combating pathogenic germs and parasites in water of aquaculture, ponds, and aquariums; for destroying thread algae in water; for processing water. The addition of alkali hydrogen carbonate to alkali percarbonate peroxyhydrate stabilizes the alkali percarbonate peroxyhydrates relative to combustible materials. The alkali carbonate peroxyhydrate is preferably Na2CO3 and xH2O2.
Abstract: The invention provides novel beta-carboline derivatives of formulae (Ia) and (Ib) useful in the treatment of proliferative disorders including cancer, intermediates used in their preparation, processes for preparing the same and uses thereof.
Type:
Grant
Filed:
June 24, 2011
Date of Patent:
October 27, 2015
Assignees:
FACULTES UNIVERSITAIRES NOTRE DAME DE LA PAIX, UNIVERSITE LIBRE BRUXELLES
Inventors:
Raphael Frederick, Bernard Masereel, Jeremy Reniers, Johan Wouters, Celine Bruyere, Robert Kiss, Céline Anne Marie Michelle Meinguet, Véronique Emmanuelle Julie Mathieu
Abstract: The invention relates to substituted pyridine compounds of Formula I: (I) or a pharmaceutically acceptable salt, prodrug, or solvate thereof wherein A1, X, A2, R1a, R1b, R1c, G, and z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
Type:
Grant
Filed:
July 15, 2011
Date of Patent:
September 1, 2015
Assignee:
Purdue Pharma, L.P.
Inventors:
Donald J. Kyle, Chiyou Ni, Minnie Park, Laykea Tafesse
Abstract: A prodrug having antioxidant activity, including a phosphorylated compound having a thiol group. A method of treating oxidative stress by administering a prodrug of a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug, and treating oxidative stress. A method of increasing bioavailability of a thiol compound by creating a prodrug by phosphorylating a thiol compound, administering the prodrug, preventing first pass metabolism of the prodrug, removing a phosphate group from the prodrug, and providing active drug to a site in need of therapy from oxidative stress. A method of preventing radiation damage to healthy tissue by administering a prodrug comprising a phosphorylated compound including a thiol group, removing a phosphate group of the prodrug to provide active drug, and preventing radiation damage to healthy tissue.
Type:
Grant
Filed:
June 27, 2008
Date of Patent:
July 21, 2015
Assignee:
Board of Trustees of Northern Illinois University
Abstract: In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
November 10, 2012
Date of Patent:
July 7, 2015
Assignee:
Vanderbilt University
Inventors:
Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney
Abstract: The present invention relates to compounds of the formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds as activators of AMPK.
Abstract: The invention relates to a pharmaceutical composition comprising a compound preventing EthR from binding to the ethA promoter, for example a compound of formula 1 wherein R1 is optionally substituted phenyl or optionally substituted pyridyl; R2 (CH2)n wherein n is 1, 2, 3 or 4; R3 is CH3(CH2)m wherein m is 0, 1, 2 or 3; X1 is O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; in particular 2-phenylethyl butyrate, and a thioamide or thiourea of formula 2 wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
Type:
Grant
Filed:
November 25, 2008
Date of Patent:
June 9, 2015
Assignee:
ETH Zurich
Inventors:
Martin Fussenegger, Wilfried Weber, Ronald Schoenmakers
Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
Type:
Grant
Filed:
October 29, 2013
Date of Patent:
April 21, 2015
Assignee:
Laboratorios del Dr. Esteve, S.A.
Inventors:
Carlos Ramon Plata Salaman, Nicolas Tesson
Abstract: Problem To provide an antioxidant, an antioxidant composition, and a method for producing the antioxidant and the antioxidant composition, which feature a high content rate and degree of extraction of substances. These substances are taurine, glycogen, protein, so-called blood platelet anticoagulant with zinc, fat-soluble vitamin with a high activation such as vitamin D, and other useful substances. The antioxidant and the antioxidant composition also feature a so-called antioxidative property, which has recently attracted attention. Solution The present invention, for example, includes 3,5-dihydroxy-4-methoxybenzyl alcohol.
Type:
Grant
Filed:
January 26, 2012
Date of Patent:
April 21, 2015
Assignees:
Watanabe Oyster Laboratory Co., Ltd., National University Corporation Hokkaido University
Inventors:
Mitsugu Watanabe, Hitoshi Chiba, Hirotoshi Fuda, Shigeki Jin