Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/329)
  • Patent number: 10377744
    Abstract: The invention discloses a new series of inhibitors of soluble epoxide hydrolase (sEH) with improved physical properties that enhance their druglikeness to treat sEH associated diseases such as chronic diabetic neuropathic pain.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: August 13, 2019
    Assignee: Eicosis, LLC
    Inventors: Bruce D. Hammock, Kin Sing Stephen Lee, Ahmet Bora Inceoglu
  • Patent number: 10207984
    Abstract: The disclosure relates to cyclopropyl derivatives and methods of use. In some embodiments, the disclosure relates to methods of managing medical disorders with pharmaceutical compositions disclosed herein administered to subject in need thereof. In certain embodiments, the disclosure relates to methods of managing mental disorders, mood disorders, pain, and fibromyalgia and related conditions with pharmaceutical compositions disclosed herein.
    Type: Grant
    Filed: May 3, 2016
    Date of Patent: February 19, 2019
    Assignees: Emory University, Wake Forest University Health Services
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Thomas J. Martin, Steven R. Childers
  • Patent number: 10117862
    Abstract: A remifentanil injection solution formulation contains remifentanil and or physiologically acceptable salts thereof, water, and a stabilizer, the remifentanil injection solution formulation contains said water at a rate of 0.007 to 0.025 mL per 1 mg of said remifentanil.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: November 6, 2018
    Assignee: TERUMO KABUSHIKI KAISHA
    Inventors: Aiko Horiuchi, Shigeru Suzuki
  • Patent number: 9757366
    Abstract: Methods for the treatment of Parkinson's disease psychosis which comprise the administration of pimavanserin.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: September 12, 2017
    Assignee: ACADIA Pharmaceuticals Inc.
    Inventors: Roger Mills, Hilde Williams
  • Patent number: 9663428
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Grant
    Filed: August 8, 2014
    Date of Patent: May 30, 2017
    Assignee: NeOnc Technologies Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Patent number: 9499461
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: November 22, 2016
    Assignee: NeOnc Technologies, Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Puppali
  • Patent number: 9428489
    Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: August 30, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Robert Murray McKinnell, Lan Jiang, Daniel D. Long
  • Patent number: 9353091
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: May 31, 2016
    Assignee: ABBVIE INC.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Patent number: 9296693
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: March 29, 2016
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Tristan Rose, Christophe Morisseau, Kin Sing Lee
  • Patent number: 9216967
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: December 22, 2015
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Publication number: 20150147282
    Abstract: The present invention relates to topical bioadhesive formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: November 24, 2014
    Publication date: May 28, 2015
    Inventors: Fredrik JOABSSON, Margareta LINDEN, Krister THURESSON, Fredrik TIBERG
  • Publication number: 20150141461
    Abstract: Methods and compositions of treating a subject for cancer pain are provided. In the subject methods, a subject is treated for cancer pain by administering to the subject an effective amount of a narcotic emulsion, e.g., fentanyl elmulsion, formulation. In certain embodiments, the emulsion formulations include a narcotic active agent, oil, water and a surfactant. Also provided are methods of making the subject emulsion formulations as well as kits that include the emulsion formulations.
    Type: Application
    Filed: September 22, 2014
    Publication date: May 21, 2015
    Inventors: Kiichiro Nabeta, Toru Hibi
  • Patent number: 9034903
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: May 19, 2015
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
  • Patent number: 9018231
    Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: April 28, 2015
    Assignee: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
  • Publication number: 20150098909
    Abstract: A soluble fiber lozenge provided herein includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and one or more additives dispersed in the soluble-fiber matrix. In some cases, a soluble fiber lozenge provided herein includes at least 40 weight percent of soluble fiber. In some cases, soluble fiber in soluble fiber lozenge provided herein can include maltodextrin. The soluble fiber lozenge is adapted to release one or more additives from the body when the body is received within the oral cavity of a consumer and exposed to saliva. A method of making soluble fiber lozenges provided herein includes forming a molten mixture of at least 40 weight percent soluble fiber, one or more additives, and less than 15 weight percent water while maintaining a mixture temperature of less than 200° C. and portioning the molten mixture into a plurality of soluble fiber lozenges. In some cases, the ingredients can be mixed to form the molten mixture in an extruder.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Feng Gao, Diane L. Gee, Shuzhong Zhuang, Phillip M. Hulan, William J. Burke, Gerd Kobal
  • Patent number: 9000174
    Abstract: The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: April 7, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Elfrida R. Benjamin, Zhengming Chen, Deyou Sha, Laykea Tafesse, Samuel F. Victory, John W. F. Whitehead
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Patent number: 8987290
    Abstract: The present invention concerns a needle-less drug delivery device being suitable for delivering drugs through a skin surface into a human or animal body comprising a pharmaceutical composition with at least one analgesic agent preferably being an opioid. The present invention also relates to the use of at least one analgesic agent, preferably being at least one opioid in a needle-less drug delivery device being suitable for injecting medication through a skin surface into the human or animal body. Further, the invention is concerned with a method of treating breakthrough pain by injecting at least one analgesic agent preferably being an opioid into the human or animal body using a needle-less drug delivery device.
    Type: Grant
    Filed: August 29, 2007
    Date of Patent: March 24, 2015
    Assignee: Purdue Pharma L.P.
    Inventor: Jo Woodward
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Patent number: 8980305
    Abstract: There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: March 17, 2015
    Assignee: Orexo AB
    Inventor: Anders Pettersson
  • Publication number: 20150064118
    Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: September 15, 2014
    Publication date: March 5, 2015
    Inventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
  • Publication number: 20150057259
    Abstract: A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion.
    Type: Application
    Filed: October 17, 2014
    Publication date: February 26, 2015
    Applicant: Auxilium US Holdings, LLC
    Inventors: Michael M. Crowley, Justin M. Keen, John J. Koleng, Feng Zhang
  • Publication number: 20150057313
    Abstract: This document provides methods and materials for modulating afferent nerve signals to treat medical conditions such as CHF, CHF respiration, dyspnea, peripheral vascular disease (e.g., peripheral arterial disease or venous insufficiency), hypertension (e.g., age-associated hypertension, resistant hypertension, or chronic refractory hypertension), COPD, sleep apnea, and chronic forms of lung disease where muscle dysfunction is a part of the disease pathophysiology. For example, methods and materials involved in using electrical and/or chemical techniques to block or reduce afferent nerve signals (e.g., nerve signals of group III and/or IV afferents coming from skeletal muscle and/or the kidneys) are provided.
    Type: Application
    Filed: March 8, 2013
    Publication date: February 26, 2015
    Inventors: Michael J. Joyner, Bruce D. Johnson, Thomas P. Olson
  • Publication number: 20150045389
    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
  • Patent number: 8952031
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: February 10, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Publication number: 20150030685
    Abstract: A sugar-free, pharmaceutical composition comprising an oral transmucosal solid dosage form which includes an adherent carrier preblend mixture of a highly potent pharmaceutical agent, and dextrates, hydrated the composition further including a pharmaceutically acceptable sugar-free excipient.
    Type: Application
    Filed: July 23, 2013
    Publication date: January 29, 2015
    Inventors: Lynn J. Maland, Brian I. Hague
  • Publication number: 20150031655
    Abstract: The disclosure provides a method of treating a mammal afflicted with an age-related disorder, comprising administering to the mammal a combination of liver X receptor (LXR) modulator and estrogen receptor (ER) modulator, in an amount effective to treat the mammal. Further disclosed are the LXR modulators and ER modulators used in the combination therapy.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NORTH DAKOTA
    Inventor: Othman Ghribi
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Patent number: 8937181
    Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
  • Publication number: 20150011586
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases. In some embodiments, the present invention provides a method for monitoring the activity of a soluble epoxide hydrolase, the method including contacting the soluble epoxide hydrolase with an amount of a compound of the present invention sufficient to produce a detectable change in the fluorescence of the soluble epoxide hydrolase by interacting with one or more tryptophan residues present in the catalytic site of said sEH.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 8, 2015
    Inventors: Bruce D. Hammock, Kin Sing Lee, Christophe Morisseau
  • Publication number: 20150005328
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 1, 2015
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Publication number: 20150005337
    Abstract: The invention relates to a transdermal or transmucosal non-occlusive, semi-solid pharmaceutical formulation that includes at least one systemically active agent that acts on the Central Nervous System (CNS) of a mammal; and a permeation enhancing solvent system present in an amount sufficient to solubilize the at least one active ingredient.
    Type: Application
    Filed: September 17, 2014
    Publication date: January 1, 2015
    Inventors: Dario Norberto R. Carrara, Arbaud Grenier, Igno Alberti, Laetitia Henry, Celine Decaudin
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140371238
    Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: FLATLEY DISCOVERY LAB
    Inventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
  • Publication number: 20140370077
    Abstract: The present invention provides a transdermal drug delivery system comprising fentanyl or its pharmaceutically acceptable salt and method of making the same.
    Type: Application
    Filed: March 12, 2014
    Publication date: December 18, 2014
    Inventors: Hoo-Kyun Choi, Je Phil Ryoo
  • Publication number: 20140364449
    Abstract: The invention relates to a method for identifying compounds that bind and preferably activate a target opioid receptor in a pH-dependent manner.
    Type: Application
    Filed: January 7, 2013
    Publication date: December 11, 2014
    Applicant: MATHPHARM GMBH
    Inventors: Christoph Stein, Marcus Weber, Olga Scharkol, Peter Deuflhard
  • Publication number: 20140349976
    Abstract: As disclosed herein, co-administration of pimavanserin with an agent that ameliorates one or more cholinergic abnormalities can have a synergistic effect on the efficacy of the agent. Disclosed herein are compositions which include pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities. Also disclosed herein are methods for ameliorating or treating a disease condition characterized by one or more cholinergic abnormalities that can include administering pimavanserin in combination with an agent that ameliorates one or more cholinergic abnormalities.
    Type: Application
    Filed: May 28, 2014
    Publication date: November 27, 2014
    Applicant: Acadia Pharmaceuticals Inc.
    Inventors: Uli HACKSELL, Krista MCFARLAND
  • Publication number: 20140350053
    Abstract: The present invention provides high-concentration formulations of opioids such as fentanyl or fentanyl congeners. The formulation of the invention comprises fentanyl or a fentanyl congener in concentrations significantly in excess of conventional formulations, e.g., on the order about 2-fold to about 10,000-fold greater than conventional formulations, e.g., currently commercially available formulations. These formulations are particularly useful for long-term delivery to a subject suffering from pain. The invention further provides drug delivery devices comprising the high-concentration opioid formulations, and further provides methods of alleviating pain in a subject, comprising administering the high-concentration formulations to a subject in need thereof.
    Type: Application
    Filed: April 23, 2014
    Publication date: November 27, 2014
    Applicant: DURECT CORPORATION
    Inventors: Dana Litmanovitz, Barbara J. F. Laidlaw
  • Publication number: 20140343100
    Abstract: The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable salt thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: S. George Kottayil, Venkat R. Goskonda, Zhongyuan Zhu, Linet Kattookaran, Neha Parikh
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140335153
    Abstract: A method of preparing a thin film, the method comprising: (a) mixing a lipid, emulsifier, and solvent to provide a uniform first mixture; (b) contacting an active ingredient with the uniform first mixture to provide a thickened second mixture; (c) contacting a binder with the thickened second mixture to provide a slurry; and (d) hot extruding, casting, and condensing the slurry to provide the thin film; or cooling, shearing, mixing, casting, and condensing the slurry to provide the thin film.
    Type: Application
    Filed: October 31, 2013
    Publication date: November 13, 2014
    Applicant: CURE Pharmaceutical Corporation
    Inventors: Eric Allen, Robert Steven Davidson, Jose Bernardo
  • Publication number: 20140336214
    Abstract: The present invention relates generally to the co-administration of an opioid agonist compound and an analgesic compound. In addition, the invention relates to, among other things, dosage forms for co-administration of an opioid agonist compound and an analgesic compound, methods for administering an opioid agonist compound and an analgesic compound, compositions comprising an opioid agonist compound and an analgesic compound, dosage forms comprising an opioid agonist compound and an analgesic compound, and so on.
    Type: Application
    Filed: November 6, 2012
    Publication date: November 13, 2014
    Inventors: Timothy A. Riley, Juergen W. Pfeiffer, Hema Gursahani
  • Publication number: 20140329857
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20140329835
    Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.
    Type: Application
    Filed: June 19, 2014
    Publication date: November 6, 2014
    Inventors: Je Phil Ryoo, Chun Kwong Chu, Zheng Wang
  • Publication number: 20140323487
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Patent number: 8871791
    Abstract: Methods and compositions of treating a subject for cancer pain are provided. In the subject methods, a subject is treated for cancer pain by administering to the subject an effective amount of a narcotic emulsion, e.g., fentanyl elmulsion, formulation. In certain embodiments, the emulsion formulations include a narcotic active agent, oil, water and a surfactant. Also provided are methods of making the subject emulsion formulations as well as kits that include the emulsion formulations.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: October 28, 2014
    Assignees: Teikoku Pharma USA, Inc., Techno Guard Co., Ltd.
    Inventors: Kiichiro Nabeta, Toru Hibi
  • Patent number: 8865745
    Abstract: The compound 1-(2-{4-[3-(3,4-dimethoxyphenyl)-4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]piperidin-1-yl}-2-oxoethyl)pyrrolidine-2,5-dione is a novel effective inhibitor of the type 4 phosphodiesterase.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Takeda GmbH
    Inventors: Beate Schmidt, Christian Scheufler, Juergen Volz, Martin Feth, Rolf-Peter Hummel, Armin Hatzelmann, Christof Zitt, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley, Deborah Ockert, Anke Heuser, Johannes A. M. Christiaans, Geert Jan Sterk, Wiro M. P. B. Menge
  • Publication number: 20140288040
    Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyc
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Gianni Chessari, Gilbert Ebai Besong, Maria Grazia Carr, Steven Douglas Hiscock, Michael Alistair O'Brien, David Charles Rees, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson
  • Publication number: 20140271799
    Abstract: A method and a non-rate controlled, monolithic, subsaturated patch for transdermally administering fentanyl and analogs thereof, for analgetic purposes, to a subject through skin over an extended period of time are disclosed.
    Type: Application
    Filed: June 2, 2014
    Publication date: September 18, 2014
    Applicant: ALZA Corporation
    Inventors: SUBRAMANIAN S. VENKATRAMAN, SHAOLING LI, ROBERT M. GALE, JANE STEPIC, WILLIAM W. VAN OSDOL
  • Patent number: 8835459
    Abstract: The present invention is directed to sublingual formulations containing fentanyl, a pharmaceutically acceptable sale thereof, or derivative thereof, suitable for administration to a patient, and methods for treatment with the formulations.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: September 16, 2014
    Assignee: Insys Therapeutics, Inc.
    Inventors: S. George Kottayil, Venkat R. Goskonda, Zhongyuan Zhu, Linet Kattookaran, Neha Parikh