Piperidines Patents (Class 514/315)
  • Patent number: 10278942
    Abstract: The present disclosure provides methods of treating pulmonary arterial hypertension (PAH) in a subject in need thereof. Compositions for use in these methods are also provided.
    Type: Grant
    Filed: March 9, 2016
    Date of Patent: May 7, 2019
    Assignee: Peloton Therapeutics, Inc.
    Inventors: John A. Josey, Eli M. Wallace, Xinlin Du, Barry Goggin
  • Patent number: 10280140
    Abstract: The present invention relates to a method for the production of a pyrrolidine derivative.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: May 7, 2019
    Assignee: Eberhard Karls Universitaet Tuebingen Medizinische Fakultaet
    Inventors: Bernhard Hirt, Claus Zeyher
  • Patent number: 10245256
    Abstract: Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: April 2, 2019
    Assignee: Mitos Pharmaceuticals, Inc.
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 10179128
    Abstract: Described herein are dosing regimens and kits for the treatment and/or prevention of lysosomal storage disorders such as Gaucher disease. Also described are dosing regimens and kits for the treatment and/or prevention of degenerative disorders of the central nervous system, such as the synucleinopathies Parkinson's disease or Lewy Body Dementia.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: January 15, 2019
    Assignee: Amicus Therapeutics, Inc.
    Inventor: Sean Clark
  • Patent number: 10159665
    Abstract: Disclosed herein are embodiments of a method of inhibiting amyloid plaque deposition. In some embodiments, the method comprises: administering to an individual known to have a decreased expression level of Bri3 an amount of a nitroxide antioxidant effective to increase the BRI3 expression level relative to the decreased expression level, whereby the increased expression level of Bri3 inhibits amyloid plaque deposition via inhibition of amyloid precursor protein processing.
    Type: Grant
    Filed: November 16, 2017
    Date of Patent: December 25, 2018
    Inventor: Louis Habash
  • Patent number: 10144727
    Abstract: The present application provide novel iminosugars and their use in treatment of viral infections, such as Dengue infection and Influenza A infection. The present inventors discovered certain deoxynojirimycin derivatives may be effective against one or more viruses, which may be, for example, a Dengue virus and/or a virus belonging to the Orthomyxoviridae family, such as an Influenza A virus. In particular, such deoxynojirimycin derivatives may be useful for treating a disease or condition caused by or associated with one or more viruses. In certain embodiments, the deoxynojirimycin derivatives may increase a survival rate or probability for a subject infected with one or more viruses, which may be, for example, a Dengue virus and/or a virus belonging to the Orthomyxoviridae family, such as an Influenza A virus.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: December 4, 2018
    Assignee: Emergent Virology LLC
    Inventors: Urban Ramstedt, Raju Penmasta, Hitesh Batra, Tam Nguyen
  • Patent number: 10077458
    Abstract: A process for the microbial synthesis of migalastat, specifically a process for the production of migalastat comprising culturing a microorganism under conditions such that at least one imino sugar is produced and detecting and/or isolating an imino sugar produced by said microorganism, and the microorganisms used in this process. The invention also comprises migalastat produced according to the above method and pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: September 18, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Emilio Alvarez-Ruiz, Andrew John Collis, Alison Sarah Dann, Andrew Peter Fosberry, Sarah Jane Ready, Maria Jesus Vazquez Muniz
  • Patent number: 10076514
    Abstract: Provided are methods of treating a patient diagnosed with Fabry disease and methods of enhancing ?-galactosidase A in a patient diagnosed with or suspected of having Fabry disease. Certain methods comprise administering to a patient a therapeutically effective dose of a pharmacological chaperone for ?-galactosidase A, wherein the patient has a splice site mutation in intron 4 of the nucleic acid sequence encoding ?-galactosidase A. Also described are uses of pharmacological chaperones for the treatment of Fabry disease and compositions for use in the treatment of Fabry disease.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: September 18, 2018
    Assignee: Amicus Therapeutics, Inc.
    Inventor: Elfrida Benjamin
  • Patent number: 10071964
    Abstract: This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: September 11, 2018
    Assignee: UNIVERZA V LJUBJIANI
    Inventors: Boris Brus, Urban Kosak, Damijan Knez, Nicolas Coquelle, Jacques-Philippe Colletier, Stanislav Gobec
  • Patent number: 10064852
    Abstract: Disclosed herein are methods for treating a human subject having a disease associated with an increased level of apoptosis using a nitroxide. Further disclosed are methods for treating a human subject in need of a reduced expression level of a gene associated with the apoptosis pathway using a nitroxide.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: September 4, 2018
    Inventor: Louis Habash
  • Patent number: 10035766
    Abstract: The present invention provides novel compositions as well as methods for preventing and/or treating lysosomal storage disorders. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.
    Type: Grant
    Filed: November 19, 2013
    Date of Patent: July 31, 2018
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Robert Boyd, Gary Lee, Philip Rybczynski
  • Patent number: 10028943
    Abstract: Nitrone, nitroso, and nitroxide spintraps and spin labels and their reduction products are claimed for the treatment of dense breasts.
    Type: Grant
    Filed: July 5, 2015
    Date of Patent: July 24, 2018
    Inventors: Peter Herbert Proctor, Donna Marie RollingProctor
  • Patent number: 9968596
    Abstract: Compounds of formula I for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: May 15, 2018
    Assignee: Celgene Corporation
    Inventors: Brian E. Cathers, Matthew Daniel Correa, Joshua Hansen, Antonia Lopez-Girona, Ehab M. Khalil, Kyle MacBeth, Hon-Wah Man, George W. Muller, Michael Pourdehnad, Raj Raheja
  • Patent number: 9944600
    Abstract: The present invention relates to novel piperidine derivatives, stereoisomers thereof or pharmaceutically acceptable salts thereof; methods for preparing the compound; and pharmaceutical compositions comprising the compound. The novel piperidine derivatives, according to the present invention, having an effect as GPR119 agonist can be used for treatment of metabolic disorders, including diabetes mellitus (especially type II) and related disorders.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: April 17, 2018
    Assignee: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: ChangSik Lee, TaegSu Jang, DaeKyu Choi, MooSung Ko, DoHoon Kim, SoYoung Kim, JaeKi Min, WooSik Kim, YoungTae Lim
  • Patent number: 9931353
    Abstract: The present invention relates to a method for treating an individual having Cerebral Amyloid Angiopathy by using pharmacological chaperones to increase the activity of gangliosidase and/or sialidase enzymes involved in ganglioside catabolism.
    Type: Grant
    Filed: May 5, 2015
    Date of Patent: April 3, 2018
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Brandon Alan Wustman, Kenneth Valenzano, Robert Boyd
  • Patent number: 9808451
    Abstract: Compounds of formula I for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed.
    Type: Grant
    Filed: September 23, 2016
    Date of Patent: November 7, 2017
    Assignee: Celgene Corporation
    Inventors: Brian E. Cathers, Matthew Daniel Correa, Joshua Hansen, Antonia Lopez-Girona, Ehab M. Khalil, Kyle MacBeth, Hon-Wah Man, George W. Muller, Michael Pourdehnad, Raj Raheja
  • Patent number: 9750733
    Abstract: Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease.
    Type: Grant
    Filed: October 10, 2016
    Date of Patent: September 5, 2017
    Assignee: AMICUS THERAPEUTICS, INC.
    Inventors: Robert Boyd, Philip J. Rybczynski, Kamlesh Sheth
  • Patent number: 9717718
    Abstract: Compositions comprising isolated ido-BR1 are described for use in therapy or prophylaxis, including the treatment of inflammatory diseases (for example as anti-inflammatory drugs) and to reduce inflammation. Also described are methods for monitoring the quality of a Cucurbitaceae extract, to processes for producing a Cucurbitaceae extract as well as to Cucurbitaceae extracts obtainable by such processes.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: August 1, 2017
    Assignee: Phytoquest Limited
    Inventor: Robert James Nash
  • Patent number: 9700550
    Abstract: Disclosed herein are methods for treating a human subject having a disease associated with an increased level of apoptosis using a nitroxide. Further disclosed are methods for treating a human subject in need of a reduced expression level of a gene associated with the apoptosis pathway using a nitroxide.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: July 11, 2017
    Inventor: Louis Habash
  • Patent number: 9688633
    Abstract: The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 27, 2017
    Assignee: INSTITUT DE RECHERCHE POUR LE DEVELOPPEMENT
    Inventors: Ignacio Aldana Moraza, Silvia Victoria Blair Trujillo, Eric Deharo, Giovanny Garavito, Adela Mendoza Lizaldez, Silvia Perez-Silanes
  • Patent number: 9675551
    Abstract: The present invention relates to a stable pharmaceutical composition for sublingual administration comprising a therapeutically effective quantity of an antihistamine agent, in particular Dimenhydnnate and a process for the preparation thereof.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: June 13, 2017
    Assignee: EXPERMED S.A.
    Inventors: Evangelos Karavas, Efthimios Koutris, Vicky Samara, Amalia Diakidou, Aggelos Karatzas
  • Patent number: 9623016
    Abstract: Provided are iminosugars having antibacterial properties and methods of treating and/or preventing bacterial infections with such iminosugars. The present disclosure relates to antibacterial compounds and, in particular, to iminosugars having antibacterial activity. One embodiment is a method of treating or preventing a bacterial infection comprising administering to a subject in need thereof an antibacterial effective amount of a compound of the following formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 18, 2017
    Assignee: EMERGENT VIROLOGY LLC
    Inventors: Urban Ramstedt, Kelly Warfield
  • Patent number: 9579311
    Abstract: Disclosed herein are methods for treating a human subject having a disease associated with an increased level of apoptosis using a nitroxide. Further disclosed are methods for treating a human subject in need of a reduced expression level of a gene associated with the apoptosis pathway using a nitroxide.
    Type: Grant
    Filed: May 16, 2016
    Date of Patent: February 28, 2017
    Inventor: Louis Habash
  • Patent number: 9545398
    Abstract: Disclosed herein are methods for counteracting age-related decrease in gene expression or treating age-related diseases, for example cancers and autoimmune diseases, caused by decreased expression levels of a gene associated with the apoptosis pathway, using a nitroxide. Further disclosed are methods for treating a human subject in need of an increased expression level of a gene associated with the apoptosis pathway using a nitroxide.
    Type: Grant
    Filed: March 23, 2016
    Date of Patent: January 17, 2017
    Inventor: Louis Habash
  • Patent number: 9527816
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: December 27, 2016
    Assignee: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 9522876
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 20, 2016
    Assignee: ZYMEWORKS INC.
    Inventors: Geoffrey C. Winters, Alexander L. Mandel, Bradley J. Hedberg, John Babcook, James R. Rich, Tom Han Hsiao Hsieh, Elyse Marie Josée Bourque
  • Patent number: 9522144
    Abstract: Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: December 20, 2016
    Assignee: Mitos Pharmaceuticals, Inc.
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 9522883
    Abstract: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-?-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-?-D-glucopyranoside (O-GlcNAc).
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: December 20, 2016
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Patent number: 9499514
    Abstract: Compounds of formula I for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: November 22, 2016
    Assignee: Celgene Corporation
    Inventors: Joshua Hansen, Matthew Daniel Correa, Raj Raheja, Antonia Lopez-Girona, Hon-Wah Man, George W. Muller, Ehab M. Khalil, Kyle MacBeth, Brian E. Cathers, Michael Pourdehnad
  • Patent number: 9326977
    Abstract: Compositions comprising isolated ido-BR1 are described for use in therapy or prophylaxis, including the treatment of inflammatory diseases (for example as anti-inflammatory drugs) and to reduce inflammation. Also described are methods for monitoring the quality of a Cucurbitaceae extract, to processes for producing a Cucurbitaceae extract as well as to Cucurbitaceae extracts obtainable by such processes.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: May 3, 2016
    Assignee: Phytoquest Limited
    Inventor: Robert James Nash
  • Patent number: 9301527
    Abstract: The present invention relates to methods of applying an insect repellent composition containing, in a physiologically acceptable medium, as active insect repellent material, at least 20% by weight of 1-methylpropyl (2-(2-hydroxyethyl)piperidine-1-carboxylate, said active insect repellent material being used in an aqueous medium with about 5% by weight of at least one copolymer of vinylpyrrolidone and hexadecene and at least one silicone oil.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 5, 2016
    Assignee: DAKEM
    Inventor: Marc Esculier
  • Patent number: 9194011
    Abstract: Multimeric protein structures comprising at least two alpha-galactosidase monomers being covalently linked to one another via a linking moiety are disclosed herein, as well a process for preparing same, and methods of treating Fabry disease via administration of a multimeric protein structure. The disclosed multimeric protein structures exhibit an improved performance, in terms of enhanced activity and/or a longer lasting activity under both lysosomal conditions and in a serum environment.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: November 24, 2015
    Assignee: Protalix Ltd.
    Inventors: Avidor Shulman, Ilya Ruderfer, Tehila Ben-Moshe, Talia Shekhter, Yaniv Azulay, Yoseph Shaaltiel, Tali Kizhner
  • Patent number: 9187735
    Abstract: Compositions comprising peptides that are capable of binding a metal are disclosed. Such compositions can be used for binding metal in a variety of contexts and environments. In various embodiments, peptides are used for antioxidant activity, anti-inflammatory activity, anti-pain therapy, as chemical reagents, and/or as superoxide dismutase mimics.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: November 17, 2015
    Assignees: UNIVERSITY OF KANSAS, ECHOGEN, INC.
    Inventors: Jennifer Ann Stowell Laurence, Mary Elizabeth Krause, Timothy A. Jackson, Amanda Michelle Glass, George Laurence
  • Patent number: 9133172
    Abstract: This invention recites dihydrofuran substituted azetidine derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in mammals and birds. The substituents A, R1a, R1b, R1c, R2, R3, R4, R6, and n are as described herein.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: September 15, 2015
    Assignee: Zoetis Services LLC
    Inventors: Nathan Anthony Logan Chubb, Valerie A. Vaillancourt
  • Patent number: 9101619
    Abstract: Pharmaceutical compositions are provided that are useful in treating diabetes. The compositions comprise a pharmaceutically acceptable carrier, and an effective therapeutic or prophylactic amount of a nitroxide antioxidant that alters the expression of genes related to diabetes. Methods are also provided for the use of the pharmaceutical compositions in the treatment or prevention of diabetes. In a preferred embodiment, the nitroxide antioxidant is Tempol (4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl).
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: August 11, 2015
    Assignee: Mitos Pharmaceuticals, Inc.
    Inventors: Louis Habash, Clarence Jones
  • Patent number: 9089515
    Abstract: Long chain N-alkyl amino and imino compounds, oxa-substituted derivatives thereof, and pharmaceutical compositions including such compounds are described. The long chain N-alkyl group is a C8-C16 alkyl group. The long chain N-alkyl compounds and oxa-substituted derivatives thereof can be used in the treatment of viral infections, in particular hepatitis B virus or hepatitis C virus, in a cell or an individual. For example, the long chain N-alkyl compounds or oxa-substituted derivatives thereof can be derived from piperidines, pyrrolidines, phenylamines, pyridines, pyrroles, or amino acids.
    Type: Grant
    Filed: March 7, 2011
    Date of Patent: July 28, 2015
    Assignees: Thomas Jefferson University, The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Nicole Zitzmann, Terry D. Butters, Frances M. Platt, Gary S. Jacob, Donald H. Picker, Sandra Carrouee, George W. J. Fleet, Raymond A. Dwek, David Durantel, Anand Mehta, Timothy M. Block
  • Patent number: 9079856
    Abstract: Process for the preparation of an iminosugar, and the intermediates thereof, having known activity as a glycosyltransferase inhibitor and used, for example, in the treatment of Gaucher's disease.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: July 14, 2015
    Assignee: Dipharma Francis S.r.l.
    Inventors: Emanuele Attolino, Andrea Malvestiti
  • Patent number: 9056101
    Abstract: The present invention provides dosing regimens for administering pharmacological chaperones to a subject in need thereof. The dosing regimens can be used to treat disorders caused by improper protein misfolding, such as lysosomal storage disorders.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: June 16, 2015
    Assignee: Amicus Therapeutics, Inc.
    Inventors: David J. Lockhart, Brandon Wustman
  • Patent number: 9044470
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: June 2, 2015
    Assignees: United Therapeutics Corporation, The Chancellor, Masters and Scholars of The University of Oxford
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Publication number: 20150148317
    Abstract: A drug delivery system is provided for treatment of oxidative stress. The drug delivery system can include a therapeutic agent and a matrix. The therapeutic agent can include an antioxidant or steroid. The matrix can include a hydrogel, particle, microparticle, or nanoparticle. A method of treating injury, including peripheral nerve injury or spinal cord injury, is also provided. The method includes injecting the drug delivery system at the site of injury.
    Type: Application
    Filed: November 26, 2014
    Publication date: May 28, 2015
    Applicants: InVivo Therapeutics Corporation, Massachusetts Institute of Technology
    Inventors: Christopher D. Pritchard, Robert S. Langer, Francis M. Reynolds, Eric J. Woodard
  • Publication number: 20150141460
    Abstract: The invention relates to 3-(2?,2?-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and their use as a medicament intended to prevent or treat inflammatory disorders.
    Type: Application
    Filed: October 6, 2014
    Publication date: May 21, 2015
    Inventors: David John Grainger, David Fox
  • Publication number: 20150133496
    Abstract: Described is a method for treating an individual having a neurological disorder with an associated mutation or mutations in a gene encoding a lysosomal enzyme. Specifically, the individual is administered a specific pharmacological chaperone for the lysosomal enzyme which increases trafficking of the protein from the ER to the lysosome in neural cells, with or without concomitantly increasing enzyme activity in neural cells. Restoration of trafficking relieves cell stress and other toxicities associated with accumulation of mutant proteins. Restoration of enzyme activity relieves substrate accumulation and pathologies associated with lipid accumulation. In a specific embodiment, the neurological disorder is Parkinson's disease or parkinsonism which is associated with mutations in glucocerebrosidase.
    Type: Application
    Filed: October 3, 2014
    Publication date: May 14, 2015
    Inventor: Brandon Alan Wustman
  • Publication number: 20150118221
    Abstract: The present invention relates to the field of cardiology. More specifically, the present invention provides methods and compositions useful for treating cardiac hypertrophy. In a specific embodiment, a method for treating or preventing cardiac hypertrophy in a patient comprises the step of administering a therapeutically effective amount of a glycolipid synthesis inhibitor.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Applicant: The John Hopkins University
    Inventor: Subroto Chatterjee
  • Patent number: 9018381
    Abstract: The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Robert Bruce Diebold, Thomas Gero, Paul Grover, Shan Huang, Stephanos Ioannidis, Claude Afona Ogoe, Jamal Carlos Saeh
  • Publication number: 20150111749
    Abstract: Methods and compositions for controlling plant pests, particularly weeds and/or plant phytopathogens using sarmentine and/or analogs thereof are disclosed.
    Type: Application
    Filed: December 31, 2014
    Publication date: April 23, 2015
    Inventors: Huazhang Huang, Ratnakar Asolkar
  • Patent number: 9012647
    Abstract: Disclosed are nitroxide modified NSAID compounds of the formula (I) or a pharmaceutically acceptable salt or enantiomer thereof: in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and n are defined herein and pharmaceutical compositions thereof. Further disclosed is a method of treating or preventing various disorders, such as inflammation, cancer, diabetes, a cardiovascular disorder, weight gain, polyps, and/or chronic pain, in a patient comprising administering an effective amount of a compound or pharmaceutically acceptable salt or enantiomer of formula (I). A method of imaging the compound or pharmaceutically acceptable salt or enantiomer of formula (I) in the body of the animal is also provided.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: April 21, 2015
    Assignees: The United States of America, as Represented by the Secretary, Department of Health and Human Services, Wake Forest University
    Inventors: David A. Wink, Wilmarie Flores-Santana, S. Bruce King, Murali Krishna Cherukuri, James B. Mitchell
  • Patent number: 9012475
    Abstract: A method for treating a tumor by combining a piperidine compound of formula (I) or salt thereof and a microtubule-targeting drug, in which the microtubule-targeting drug is administered once per 7 days or more one cycle, and the piperidine compound is administered once or more per day for 4 days or more: R1 represents a carboxyl group, —C(?O)NR5R6, or an oxadiazolyl group optionally substituted with a C1-C6 alkyl group or trifluoromethyl group; R2 represents a halogen atom or C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 groups, selected from a halogen atom, and a C1-C6 alkyl, C1-C6 alkoxy, or trifluoromethyl group; R4 represents a hydrogen atom or C1-C6 alkyl group; and R5 and R6, each represent a hydrogen atom, a C1-C6 alkyl or C3-C6 cycloalkyl group; or R5 and R6, together with a nitrogen atom, optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: April 21, 2015
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Hirai, Hiroshi Sootome
  • Publication number: 20150099015
    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.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • Publication number: 20150099709
    Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 9, 2015
    Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
  • Patent number: 8993596
    Abstract: 4-(Azacycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and uses thereof in pharmaceutical or cosmetic compositions to treat pigmentary disorders.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: March 31, 2015
    Assignee: Galderma Research & Development
    Inventors: Jean-Guy Boiteau, Karine Bouquet, Sandrine Talano, Corinne Millois Barbuis