Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Type:
Grant
Filed:
June 21, 2011
Date of Patent:
July 16, 2013
Assignee:
Memory Pharmaceuticals Corporation
Inventors:
Wenge Xie, Brian Herbert, Richard A. Schumacher, Truc Minh Nguyen, Jianguo Ma, Carla Maria Gauss, Ashok Tehim
Abstract: 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:
Grant
Filed:
February 4, 2011
Date of Patent:
July 9, 2013
Assignees:
Georgua Tech Research Corporation, The Regents of the University of California
Inventors:
Julia M. Kubanek, Mark E. Hay, Karine G. Le Roch, E. Paige Stout, Amy L. Lane, An-Shen Lin
Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
Type:
Grant
Filed:
January 25, 2010
Date of Patent:
July 2, 2013
Assignee:
Targacept, Inc.
Inventors:
Merouane Bencherif, Nikolai Fedorov, Terry Hauser, Kristen Jordan, Sharon Rae Letchworth, Anatoly Mazurov, Julio A. Munoz, Jason Speake, Daniel Yohannes
Abstract: A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4?-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular a pharmaceutical composition for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.
Abstract: The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling.
Abstract: (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide has been found to have procognitive effects in humans at unexpectedly low doses. Thus, (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide and pharmaceutically acceptable salts thereof can be used at unexpectedly low doses to improve cognition.
Abstract: The present inventions relate to accurately identifying a subset of patients within a larger group with malarial parasitemia. In particular, the present inventions provide compositions and methods comprising a malarial protein, histidine rich pro-tein-2 (HRP-2) for determining the general severity of a malarial infection in patients. Specifically, the inventions provide a rapid test comprising a read-out for HRP-2 levels in bodily fluids for determining whether a comatose patient's disease is a result of malaria as opposed to coma of another cause with incidental parasitemia. Specifically, in one preferred embodiment, a rapid test is contemplated as a quantitative rapid test dipstick. Further, these inventions relate to predictive tests for patients at risk for progression of relatively mild malaria disease to the more life-threatening cerebral malaria in addition to determining the etiology of malaria infections in comatose patients.
Type:
Application
Filed:
March 22, 2011
Publication date:
May 23, 2013
Applicant:
Board of Trustees of Michigan State University
Abstract: The present disclosure relates to pharmaceutical compositions for inhalation comprising aclidinium in the form of a dry powder of a pharmaceutically acceptable salt in admixture with a pharmaceutically acceptable dry powder carrier, providing a metered nominal dose of aclidinium equivalent to about 200 micrograms aclidinium bromide.
Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.
Abstract: Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
Abstract: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X)(Y)(Px)n[R1R2C*(NR3R4)-A-R5R6C*(NR7R8)] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).
Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
Abstract: A pharmaceutical combination comprising (a) a combination of two or more bronchodilators; or (b) a combination of at least one bronchodilator in combination with at least one corticosteroid.
Abstract: Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
Abstract: A method of treating a patient who has extravasation of blood from an intravascular compartment to an extravascular compartment. An agent is administered to the patient which mitigates a harmful effect of break-down products of blood at an extravascular site, resulting in the patient having reduced morbidity and mortality. The morbidity and mortality of the patient is further reduced by concomitant administration of a suspension of submicron protein spheres having a molecular weight of ranging from 780 billion Daltons to less than 0.8 billion Daltons.
Abstract: The invention relates to the quinuclidine compounds of formula I having quaternary ammonium group, its preparation, and the pharmaceutical composition comprising an effective amount of the compound of formula I. The compound and the composition are used to prevent and treat the diseases by blocking acetylcholine receptor. Wherein: R1 is selected from C1-12 saturated straight-chain alkyl and cycloalkyl; R2 is selected from C1-12 saturated straight-chain alkyl or straight-chain alkyl; and X is selected from halogen ion, organic and inorganic acid radical.
Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
Type:
Application
Filed:
February 22, 2012
Publication date:
March 7, 2013
Applicant:
Satiogen Pharmaceuticals, Inc.
Inventors:
Bronislava Gedulin, Andrew A. Young, Howard E. Greene
Abstract: This invention relates to novel aminoquinoline derivatives of Formula (I) or Ia, or pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an aminoquinoline derivative, such as a derivative of primaquine.
Abstract: The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.
Type:
Application
Filed:
March 30, 2011
Publication date:
February 21, 2013
Inventors:
Kazuhiro Ishizaka, Tadashi Nomizu, Aya Kitao
Abstract: Compounds of formula (I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive and inflammatory diseases.
Type:
Application
Filed:
June 8, 2012
Publication date:
February 21, 2013
Applicant:
Chiesi Farmaceutici S.p.A.
Inventors:
Fabio Rancati, Andrea Rizzi, Gabriele Amari, Matteo Biagetti, Ian Linney
Abstract: Use of (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxy)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid for treating urinary incontinence is disclosed.
Abstract: The subject invention provides stereoisomeric compounds of formula (X): wherein the variables are as defined herein, and compositions for the safe and effective treatment of various gastrointestinal disorders including, but not limited to, gastroparesis, gastroesophageal reflux and related conditions. The compounds of the subject invention are also useful in treating a variety of conditions involving the central nervous system.
Type:
Application
Filed:
February 10, 2012
Publication date:
February 14, 2013
Applicant:
Armetheon, Inc.
Inventors:
Ian Irwin, Monica Palme, Cyrus Becker, Pascal Druzgala
Abstract: A combination which comprises (a) a ?2 agonist and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9-carbonyloxy)-1-azoniabicyclo[2.2.2]octane. In the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.
Type:
Application
Filed:
March 2, 2012
Publication date:
February 7, 2013
Inventors:
Jordi GRAS ESCARDO, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, 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.
Abstract: The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.
Type:
Application
Filed:
August 1, 2012
Publication date:
January 31, 2013
Applicants:
PULMAGEN THERAPEUTICS (SYNERGY) LIMITED, ASTRAZENECA AB
Inventors:
Richard James BULL, Elizabeth Anne SKIDMORE, Rhonan Lee FORD, Andrew Nigel MATHER, Antonio METE
Abstract: Compounds and compositions for reducing intracellular lipid accumulation in a cell are described herein. These compounds are useful for the treatment and prevention of lipid/glycogen disorders, as well as for the treatment and prevention of obesity. A high throughput screen for identifying compounds that reduce intracellular lipid accumulation in cells is also provided.
Abstract: A medicament delivery system is disclosed. The system comprises a descending formulation for delivering the medicament and an ascending formulation to protect a patient being treated with the medicament from the side effects thereof.
Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.
Abstract: The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation
Type:
Application
Filed:
May 15, 2012
Publication date:
January 3, 2013
Applicant:
AstraZeneca AB
Inventors:
Rhonan Ford, Andrew Mather, Antonio Mete
Abstract: Disclosed herein are quinine formulations and methods of using quinine formulations. Specifically disclosed are methods of using quinine and informing a user of information, including potential adverse effects, the effect of food on quinine's pharmacokinetics, effect of dosing various strengths of quinine, effect of maximum plasma concentrations of quinine in a patient as it relates to adverse events, effects of deviating from the prescribed dosage, etc.
Abstract: The present invention relates to a composition for preventing or treating obesity, dyslipidemia, fatty liver or insulin resistance syndrome, comprising cinchonine as an active ingredient. The composition of the present invention comprising cinchonine as an active ingredient contributes to not only inhibition of adipocyte differentiation but also reductions of body weight, visceral fat, total cholesterol level, plasma triglyceride level and liver tissue triglyceride level, thereby exerting prevention or treatment efficacies of obesity, hyperlipidemia or fatty liver. In addition, the composition of the present invention induces significant decrease in fasting glucose level and blood insulin level to improve type 2 diabetes, insulin resistance and related metabolic diseases.
Type:
Application
Filed:
December 14, 2010
Publication date:
December 20, 2012
Applicant:
YONSEI UNIVERSITY TECHNOLOGY HOLDINGS, INC.
Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
Type:
Application
Filed:
June 14, 2012
Publication date:
December 20, 2012
Applicant:
The Feinstein Institute For Medical Research
Abstract: Disclosed is a novel polymorphic form of the compound of formula (I) also known as mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)-acetate, a process for the preparation of the polymorphic form, pharmaceutical compositions comprising the polymorphic form, and the use of the polymorphic form in medicine, particularly in antibacterial therapy.
Type:
Grant
Filed:
February 28, 2006
Date of Patent:
December 18, 2012
Assignee:
Glazo Group Limited
Inventors:
Alan Collier, Michael Anthony Forth, Darren Hewitt, Paul Oxley
Abstract: The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.
Abstract: Combinations comprising (a) a POE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases.
Type:
Application
Filed:
August 17, 2012
Publication date:
December 6, 2012
Inventors:
Jordi Gras Escardo, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
Abstract: A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.
Type:
Application
Filed:
August 17, 2012
Publication date:
December 6, 2012
Inventors:
Jordi Gras Escardo, Jesus Llenas Calvo, Harnish Ryder, Pio Orviz Diaz
Abstract: Novel combinations of a muscarinic acetylcholine receptor antagonist and a beta 2 agonist for inhaled administration via the nose or mouth, and methods of using them are provided.
Type:
Application
Filed:
November 29, 2010
Publication date:
December 6, 2012
Inventors:
Darrell Baker, Mark Bruce, Glenn Crater, Brian Noga, Marian Thomas, Patrick Wire
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
Type:
Application
Filed:
October 28, 2010
Publication date:
November 29, 2012
Inventors:
Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
Abstract: A method for assessing if a subject has or is at risk of developing cardiac arrhythmia is described. The method includes determining the activity of Rap1A protein in a bodily sample of the subject and comparing the activity of Rap1A protein from the bodily sample of the subject to at least one Rap1A control. A decreased level of Rap1A activity in the bodily sample of the subject as compared to the at least one Rap1A control indicates that the subject is at risk of developing or has cardiac arrhythmia. Methods for evaluating the efficacy of treatment of a subject having decreased Rap1A activity with an antiarrhythmic agent are also described.
Type:
Application
Filed:
April 27, 2012
Publication date:
November 29, 2012
Applicant:
NATIONWIDE CHILDREN'S HOSPITAL, INC.
Inventors:
Maqsood Ahmed Chotani, John Anthony Bauer, Mandar Shankar Joshi, Selvi Chrysolyte Jeyaraj
Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.
Abstract: The present invention relates to the discovery that, in human cancer, an 11q deletion of ATM together with an increase in ATR and CHEK1 expression correlates with resistance to ionizing radiation which could be overcome by inhibition of the ATR/CHEK1 pathway. It provides for methods of identifying patients unlikely to exhibit an adequate response to radiation therapy and/or chemotherapy who may benefit from ATR/CHEK1 pathway inhibition, as well as methods of treating said patients.
Type:
Application
Filed:
May 24, 2012
Publication date:
November 22, 2012
Inventors:
Susanne M. Gollin, Rahul Atul Parikh, Xin Huang
Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.
Abstract: Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release solifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
May 21, 2012
Publication date:
November 15, 2012
Applicant:
THERAVIDA, INC.
Inventors:
Mehdi PABORJI, Wendy Jade Limayo HERNANDEZ, Kenneth L. DUCHIN, Roger S. FLUGEL
Abstract: A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.
Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
Abstract: The invention relates to a 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.
Type:
Grant
Filed:
December 7, 2011
Date of Patent:
November 6, 2012
Assignee:
Pierre Fabre Medicament
Inventors:
Charles Mioskowski, Vanessa Gonnot, Rachid Baati, Marc Nicolas