Abstract: The present invention includes a method for improving cognitive function in a human suffering from a neurodegenerative cognitive disorder. The method comprises administering to a patient a total daily dose of a cholinesterase inhibitor and a quaternary ammonium antimuscarinic compound. The total daily dose is divided into one or more doses administered before food intake. The quaternary ammonium antimuscarinic compound is administered in a first drug delivery element configured for rapid absorption into a body of the patient, and the cholinesterase inhibitor is administered in a second drug delivery element configured for a slower or delayed absorption into the body of the patient.
Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.
Type:
Grant
Filed:
May 5, 2022
Date of Patent:
July 30, 2024
Assignee:
Melior Pharmaceuticals II, LLC
Inventors:
John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
Abstract: A percutaneous absorption preparation is disclosed. The percutaneous absorption preparation contains donepezil for treatment of dementia, wherein the preparation includes: (a) donepezil or its pharmaceutically acceptable salt as active component, (b) propylene glycol monocaprylate as solubilizer, and (c) styrene-isoprene-styrene block copolymer (“SIS”) as adhesive. The percutaneous absorption preparation has low skin irritation and high skin penetration.
Type:
Grant
Filed:
November 7, 2018
Date of Patent:
May 28, 2024
Assignees:
DONG-A ST CO., LTD., KM TRANSDERM LTD.
Inventors:
Sun-Woo Jang, Chang-Yell Shin, Jeong-Soo Kim, Hae-Sun Kim, Kwang-Ho Cha, Hyun-Jung Kim, Masaoki Goto
Abstract: A compound, such as isoquinoline-6-sulfonyl chloride acid and/or addition salts thereof, may be useful as a manufacturing intermediate for an isoquinoline-6-sulfonamide compound. A method for manufacturing such compounds and/or or acid addition salts thereof, may involve subjecting 6-(benzylthio)isoquinoline to an oxidative chlorination reaction and/or reacting 6-aminoisoquinoline with a nitrite or nitrous acid ester, then with thionyl chloride, and then with an acid.
Abstract: A family of ?-glucosidase inhibitors are identified. Exemplary ?-glucosidase inhibitors may be obtained from Heterophragma adenophyllum seem. The inhibitors are used to lower blood sugar levels and thus to treat diseases related to or characterized by high blood sugar, such as diabetes.
Type:
Grant
Filed:
February 8, 2021
Date of Patent:
September 27, 2022
Assignee:
KING ABDULAZIZ UNIVERSITY
Inventors:
Abdur Rauf, Zafar Ali Shah, Yasir Anwar, Abdul Wadood, Hani Mohammed Ali, Abdurahman Labeed Almalki, Khalid Mohammed S. Al-Ghamdi
Abstract: Various compounds, compositions, and methods for inhibition of Rit1 are presented. In especially preferred aspects, contemplated compounds and compositions are suitable for treatment of cancers and other diseases associated with Rit1 signaling.
Inventors:
Shahrooz Rabizadeh, Oleksandr Buzko, Paul Weingarten, Heather McFarlane, Connie Tsai, Stephen Charles Benz, Kayvan Niazi, Patrick Soon-Shiong
Abstract: Disclosed are methods for diagnosing a myelodysplastic syndrome (MDS) in a subject. In some embodiments, the method involves assaying a sample from the subject to detect inflammasome activation, wherein an increase in inflammasome activation in the sample compared to a control is an indication of MDS in the subject. The disclosed methods can further involve treating the subject for MDS if an increase in inflammasome activation is detected.
Type:
Grant
Filed:
April 29, 2016
Date of Patent:
November 26, 2019
Assignee:
H. Lee Moffitt Cancer Center and Research Institute, Inc.
Abstract: Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration.
Abstract: The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
Type:
Grant
Filed:
January 31, 2018
Date of Patent:
September 4, 2018
Assignee:
Aquinox Pharmaceuticals (Canada) Inc.
Inventors:
Lloyd F. Mackenzie, Jeffery R. Raymond, Curtis Harwig, Ana Fernandez Casares
Abstract: Methods are presented for treating cancers and hematopoietic stem cell disorders, comprising administering to a subject with a cancer or hematopoietic stem cell disorder who is receiving a treatment regimen, a heparin derivative capable of inhibiting, reducing, abrogating or otherwise interfering with the binding of CXCL12 to CXCR4, wherein the cancer or hematopoietic stem cell disorder is one in which interaction of CXCL12 with CXCR4 privileges the cancer or disordered HSCs against therapeutic intervention. In preferred embodiments, the heparin derivative is a substantially 2-O, 3-O-desulfated heparin derivative.
Abstract: The present invention is generally directed to novel crystalline forms of the acetate salt of (1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexanol and processes for their preparation.
Type:
Grant
Filed:
June 23, 2016
Date of Patent:
April 17, 2018
Assignee:
Aquinox Pharmaceuticals (Canada) Inc.
Inventors:
Lloyd F. Mackenzie, Jeffery R. Raymond, Curtis Harwig, Ana Fernandez Casares
Abstract: Despite significant progress in the synthesis of nanocomposite materials, integration of several components with various functions remains a big challenge, which significantly limits control over nanocomposite properties. The disclosure provides a multifunctional micro particle based on incorporation of titania nanoparticles combined into a porous polylactic acid (PLA) matrix. PLA is used as a biodegradable and biocompatible polymer and titania nanoparticles represent photocatalytically active nanofillers capable of degradation of organic compounds under solar irradiation. Titania nanoparticles are integrated with PLA by using ‘mixed’ and ‘in situ grown’ approaches. The hybrid systems effectively absorbed and degraded organic impurities from water. The sorption capacity, dye degradability, and PLA disintegration were controlled by varying the concentration of incorporated titania.
Type:
Grant
Filed:
June 18, 2012
Date of Patent:
September 19, 2017
Assignee:
The UAB Research Foundation
Inventors:
Eugenia P. Kharlampieva, Benjamin Yancey
Abstract: The invention provides an ophthalmic product containing rebamipide, which has a transparency enough to be agreeable feeling on using it and has neutral so weakly acidic pH not to injury of the keratoconjunctiva of a patient suffering from dry eye. An aqueous suspension of crystalline rebamipide which has an improved transparency is provided by adding an aqueous solution of rebamipide dissolved by a base such as sodium hydroxide or an aqueous solution of a salt of rebamipide to an aqueous acidic solution such as hydrochloric acid containing at least one of the compounds selected from water-soluble polymers and surfactants, and mixing them.
Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
Type:
Application
Filed:
May 3, 2013
Publication date:
May 7, 2015
Inventors:
Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
Abstract: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.
Type:
Grant
Filed:
October 7, 2010
Date of Patent:
April 21, 2015
Assignee:
Abon Pharmaceuticals, LLC
Inventors:
Yanming Zu, Sudhir Gorukanti, Salah Uddin Ahmed
Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
Type:
Grant
Filed:
May 10, 2012
Date of Patent:
March 31, 2015
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Inventors:
John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.
Type:
Grant
Filed:
January 18, 2012
Date of Patent:
March 3, 2015
Assignee:
University of Pittsburgh—Of The Commonwealth System Of Higher Education
Inventors:
Carol A. Feghali-Bostwick, Pamela Anne Hershberger
Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
Abstract: Treatment of varying degrees of cognitive impairment associated with Alzheimer's disease with a combination of a phosphodiesterase 4 inhibitor and an acetylcholinestase inhibitor, including roflumilast and donepezil hydrochloride.
Type:
Application
Filed:
August 15, 2014
Publication date:
February 19, 2015
Inventors:
Tadataka Yamada, Jos Prickaerts, Marlies van Duinen, Anke Sambeth, Arjan Blokland
Abstract: The present invention is a screening assay for identifying inhibitors of Pseudomonas aeruginosa CFTR Inhibitory Factor as well as compounds identified by the screening assay for use in compositions and methods for ameliorating or treating a respiratory disease such as cystic fibrosis or secondary infection thereof.
Type:
Application
Filed:
April 9, 2013
Publication date:
February 12, 2015
Inventors:
Dean R. Madden, Christopher D. Bahl, Bruce D. Hammock, Christophe Morisseau
Abstract: The present invention relates to orally disintegrating tablet formulations of donepezil hydrochloride comprising magnesium aluminium silicate, and one or more pharmaceutically acceptable excipient and process for preparing such a formulation.
Type:
Application
Filed:
July 18, 2014
Publication date:
January 22, 2015
Inventors:
Ali Turkyilmaz, Fatih Cengiz Aygul, Devrim Celik
Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
Type:
Application
Filed:
September 30, 2014
Publication date:
January 22, 2015
Inventors:
Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
Abstract: The present invention provides compositions and formulations that contain active compounds as RNAi inhibitors. These compositions and formulations are useful for controlling insects and pests including mosquitoes and agricultural pests.
Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
Type:
Application
Filed:
February 21, 2013
Publication date:
January 1, 2015
Applicant:
Hoffmann-La Roche Inc.
Inventors:
Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
Abstract: The invention relates to a pharmacologically active combination and a method of enhancing cognitive performance in a patient suffering from Alzheimer's disease comprising administering to said patient a cognitive performance-enhancing amount of melatonin or a melatonin agonist in a combination therapy with a nicotine receptor agonist.
Abstract: Provided is an intraoral soluble-type film preparation in which an unpleasant taste of a drug is masked. The intraoral soluble-type film preparation comprises a drug layer containing: a drug having a bitter taste and/or an astringent taste; an alkyl sulfate at a content of ¾ mol or more with respect to 1 mol of the drug; and a water-soluble polymer.
Abstract: The invention provides a method of diagnosing Alzheimer's Disease in a subject, by determining the level of at least one miRNA in a sample derived from the subject, wherein a change in the level of the at least one miRNA relative to a suitable control is indicative of Alzheimer's Disease in the subject. Methods for monitoring the course of Alzheimer's Disease, methods of treating a subject having Alzheimer's Disease, and kits for diagnosing Alzheimer's Disease are also provided.
Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease, Alzheimer's disease related disorders, amyotrophic lateral sclerosis, multiple sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on baclofen and acamprosate combination.
Abstract: The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
Abstract: The present invention provides a transdermal drug delivery system comprising donepezil or its pharmaceutically acceptable salt and method of making the same.
Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.
Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
Type:
Grant
Filed:
August 6, 2012
Date of Patent:
December 2, 2014
Assignee:
Bristol-Myers Squibb Company
Inventors:
Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
Type:
Application
Filed:
July 24, 2014
Publication date:
November 20, 2014
Inventors:
Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
Type:
Grant
Filed:
February 18, 2012
Date of Patent:
October 21, 2014
Assignee:
Asana Biosciences, LLC
Inventors:
Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
Abstract: The present invention provides transdermal absorption preparation having a support, and a drug-containing adhesive layer formed on the support, wherein a drug-containing adhesive layer contains donepezil or a salt thereof, and a higher fatty acid salt.
Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
Type:
Application
Filed:
June 17, 2014
Publication date:
October 16, 2014
Applicant:
BIOGEN IDEC MA INC.
Inventors:
Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Ma Bin, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
Type:
Application
Filed:
December 22, 2011
Publication date:
October 9, 2014
Applicant:
LEO Laboratories Limited
Inventors:
Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
Type:
Application
Filed:
June 23, 2014
Publication date:
October 9, 2014
Inventors:
Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Adalie Motta, Gary Schiltz, Georgeta Hategan, Timothy Hagen
Abstract: This invention concerns a dosage form comprising a therapeutically neuroprotective amount of A2-73 and a neuroprotective amount of at least one cooperating acetylcholinesterase inhibitor selected from the group consisting of donepezil, galantamine, rivastigmine, or memantine and method of use.
Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
Type:
Grant
Filed:
November 24, 2010
Date of Patent:
September 23, 2014
Assignee:
Celgene Corporation
Inventors:
Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.
Type:
Application
Filed:
May 29, 2014
Publication date:
September 18, 2014
Applicant:
Chase Pharmaceuticals Corporation
Inventors:
Thomas N. CHASE, Kathleen E. CLARENCE-SMITH