Tropanes (including Nor Or Dehydro Form) Patents (Class 514/304)
  • Publication number: 20150056163
    Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 26, 2015
    Inventors: Victor J. Torres, Derya Unutmaz, Francis Alonzo, III
  • Patent number: 8962653
    Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides 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: October 1, 2013
    Date of Patent: February 24, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
  • Publication number: 20150050294
    Abstract: The present invention relates to a method for diagnosing neuroendocrine cancers via detecting the presence of N-methyl D-asparate-associated (NMDA) glutamate receptors type 1 and/or type 2. Methods for preventing and treating neuroendocrine cancers are also disclosed.
    Type: Application
    Filed: October 27, 2014
    Publication date: February 19, 2015
    Inventor: William G. North
  • Patent number: 8946258
    Abstract: Methods of performing non-gastrointestinal endoscopic procedures with concomitant dosing with rapidly disintegrating oral formulations of single active ingredient L-Hyoscyamine rapidly dissolving tablets.
    Type: Grant
    Filed: August 13, 2013
    Date of Patent: February 3, 2015
    Inventor: Jugal K. Taneja
  • Publication number: 20150030683
    Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Varghese John, Dale E. Bredesen, Stelios Tzannis
  • 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
  • Patent number: 8940762
    Abstract: The present invention is directed to methods of treating pain by administering a therapeutically effective amount of an ?7 nAChR ligand or a pharmaceutically acceptable salt thereof, to a mammal in need of treatment thereof and to pharmaceutical compositions comprising such a compound or salt.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: January 27, 2015
    Assignee: AbbVie Inc.
    Inventors: Chih-Hung Lee, Michael R. Schrimpf, Timothy A. Esbenshade, Chang Z. Zhu
  • 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
  • Publication number: 20150025107
    Abstract: This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected.
    Type: Application
    Filed: February 14, 2013
    Publication date: January 22, 2015
    Inventors: Henrik Björk Hansen, Morten Grunnet, Bo Hjorth Bentzen, Lars Hyveled-Nielsen, Jorgen Buus Lassen, Claus Sundgreen
  • Publication number: 20150018342
    Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 15, 2015
    Applicant: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Patent number: 8933236
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: January 13, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Publication number: 20150010632
    Abstract: Aerosol formulations of granisetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Applicant: Luxena Pharmaceuticals, Inc.
    Inventors: George Lu, Xiaodong Li
  • Patent number: 8927573
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: January 15, 2014
    Date of Patent: January 6, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20140364451
    Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.
    Type: Application
    Filed: August 1, 2012
    Publication date: December 11, 2014
    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 8906392
    Abstract: Compositions, methods of making, and methods of using nanoclusters in which the nanoclusters comprise a plurality of nanoparticles having a core of nanoparticles arranged such that the surfaces of the nanoparticles contact adjacent nanoparticles, the nanoparticles comprise an active ingredient, and the nanocluster has a mass median aerodynamic diameter of from about 0.25 ?m to about 20 ?m.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: December 9, 2014
    Assignee: University of Kansas
    Inventors: Cory J. Berkland, Lianjun Shi, Nashwa El Gendy, Carl Plumley, Mark Bailey
  • Publication number: 20140343091
    Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Applicant: NOVARTIS AG
    Inventors: Bernard Cuenoud, Ian Bruce, Robin Alec Fairhurst, David Beattie
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Publication number: 20140336218
    Abstract: Compositions and methods for the prevention and/or treatment of airway and/or respiratory disorders are provided. The compositions comprise arformoterol (the (R,R)-formoterol isomer) and tiotropium.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Holly HUANG, Elizabeth B. GOODWIN, Kendyl M. SCHAEFER, John P. HANRAHAN, William T. ANDREWS, Paul MCGLYNN
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Publication number: 20140329809
    Abstract: A process for the characterization of rosacea is disclosed. The process can include identifying for the first time new markers in leukocyte recruitment as well as the therapeutic applications targeting rosacea.
    Type: Application
    Filed: October 26, 2012
    Publication date: November 6, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Isabelle Carlavan, Martin Steinhoff
  • Patent number: 8877251
    Abstract: The present invention relates to methods of making a powder for inhalation comprising a first step of mixing particles of a force-controlling agent selected from the group consisting of phospholipids, titanium dioxide, aluminum dioxide, silicon dioxide, starch, and salts of fatty acids, with particles of one or more pharmacologically active materials, wherein the mixing is achieved by one or more of the processes of sieving, mixing or blending, and wherein the mixing results in the particles of the force-controlling agent being disposed on the surface of the particles of the one or more pharmacologically active materials as either a particulate coating or as a continuous or discontinuous film.
    Type: Grant
    Filed: September 5, 2012
    Date of Patent: November 4, 2014
    Assignee: Jagotec AG
    Inventor: Rudi Mueller-Walz
  • Publication number: 20140322242
    Abstract: Methods of treating or preventing cancer, or ameliorating a symptom thereof, by administering a muscarinic receptor inhibitor to inhibit cancer metastasis and/or a ? adrenergic receptor inhibitor to inhibit tumor initiation are provided. Also provided are pharmaceutical compositions for treating or preventing cancer comprising a muscarinic receptor inhibitor and/or a ? adrenergic receptor inhibitor.
    Type: Application
    Filed: November 24, 2011
    Publication date: October 30, 2014
    Applicant: Icahn School of Medicine at Mount Sinai
    Inventors: Paul S. Frenette, Claire Magnon
  • Publication number: 20140323473
    Abstract: Organophosphate (OP) nerve agents and pesticides are potent inhibitors of acetylcholinesterase (AChE). Though oxime nucleophiles can reactivate an AChE-phosphyl adduct, the adduct can undergo a reaction called aging, leading to an aged-AChE adduct. The invention provides compounds and methods that can be used to reactivate an aged-AChE adduct. Such compounds and methods are useful to counteract organophosphorus poisoning.
    Type: Application
    Filed: January 24, 2014
    Publication date: October 30, 2014
    Applicant: University of Iowa Research Foundation
    Inventors: Daniel Quinn, Joseph John Topczewski
  • Publication number: 20140315884
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 23, 2014
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Dane Goff, Donald Payan, Rajinder Singh, Simon Shaw, David Carroll, Yasumichi Hitoshi
  • Patent number: 8865641
    Abstract: A method of treating a fatty liver disease in a subject. The method comprises administering to the subject an effective amount of a cholinergic pathway stimulating agent, wherein the fatty liver disease is selected from non-alcoholic fatty liver (NAFL), alcoholic fatty liver (AFL), non-alcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), NASH-associated liver fibrosis, ASH-associated liver fibrosis, non-alcoholic cirrhosis, and alcoholic cirrhosis.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: October 21, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Valentin A. Pavlov, Kevin J. Tracey
  • Patent number: 8859585
    Abstract: Provided are methods and compositions for the treatment of depression and anxiety. The compositions contain scopolamine, or an analog thereof, and can optionally include one or more psychoactive agents. Further provided is an inhaler containing scopolamine, or an analog thereof, in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 25, 2005
    Date of Patent: October 14, 2014
    Assignee: The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Maura L. Furey, Wayne C. Drevets
  • Patent number: 8859535
    Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: October 14, 2014
    Assignee: Novartis AG
    Inventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
  • Publication number: 20140303143
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Patent number: 8853241
    Abstract: The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Jianguo Ji, Tao Li, Kevin B. Sippy, Chih-Hung Lee, Murali Gopalakrishnan
  • Patent number: 8846609
    Abstract: The present invention relates to methods for preventing or treating Human Immunodeficiency Virus (HIV) infection, inflammatory conditions, and graft-versus-host-disease (GVHD) in a subject. Therapeutic compositions of the present invention comprise Leukocidin E (LukE) and/or D proteins or polypeptides. The invention further relates to methods of treating Staphylococcus aureus infection by administering a composition comprising a CCR5 antagonist or any molecule that blocks LukE/D interaction with CCR5+ cells in an amount effective to treat the S. aureus infection in the subject.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: September 30, 2014
    Assignee: New York University
    Inventors: Victor J. Torres, Derya Unutmaz, Francis Alonzo, III
  • Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8846675
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 30, 2014
    Assignee: Cymabay Therapeutics, Inc.
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • Publication number: 20140288112
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: Application
    Filed: January 15, 2014
    Publication date: September 25, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20140288117
    Abstract: The subject invention provides materials and methods for treating neurodegenerative diseases. In one embodiment of the invention, a cysteamine compound is administered to a patient to treat Parkinson's Disease and/or complications associated with Parkinson's Disease. In another embodiment, a cysteamine compound is administered to a patient to prevent the onset of Parkinson's Disease in an at-risk patient and/or treat or prevent the onset of Parkinson's Disease-associated symptoms.
    Type: Application
    Filed: June 5, 2014
    Publication date: September 25, 2014
    Inventor: Bill Piu CHAN
  • Publication number: 20140271527
    Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 18, 2014
    Applicant: Serina Therapeutics, Inc.
    Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
  • Publication number: 20140275020
    Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
  • Publication number: 20140271680
    Abstract: The present invention relates to uses, methods and compositions for the treatment of pulmonary hypertension.
    Type: Application
    Filed: August 10, 2012
    Publication date: September 18, 2014
    Applicant: UNIVERSITE PARIS-EST CRETEIL VAL DE MARNE
    Inventors: Serge Adnot, Valerie Amsellem
  • Patent number: 8835456
    Abstract: The invention provides compounds of Formula I and the pharmaceutically salts thereof. These compounds may be generally described as bridged-bicyclo indole-containing compounds. The variables shown in Formula I are defined herein. Certain compounds of Formula I are useful as antiviral agents. Compounds as disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I and at least one pharmaceutically acceptable carrier. Such pharmaceutical compositions may contain a compound of Formula I as the only active agent or may contain a combination of a compound of Formula I and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in patients.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: September 16, 2014
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Gadhachanada, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8835457
    Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: September 16, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John W. Lampe, Paul S. Watson, David J. Slade
  • Publication number: 20140256769
    Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
    Type: Application
    Filed: January 8, 2014
    Publication date: September 11, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
  • Patent number: 8829027
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1, Y1 to Y4, V, W, and X are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
  • Publication number: 20140248357
    Abstract: A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.
    Type: Application
    Filed: April 7, 2014
    Publication date: September 4, 2014
    Applicant: PULMAGEN THERAPEUTICS (INFLAMMATION) LIMITED
    Inventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
  • Patent number: 8821877
    Abstract: This method provides a method for reducing HIV-1 viral load in an HIV-1-infected human subject which comprises administering to the subject at a predefined interval effective HIV-1 viral load-reducing doses of (a) a humanized antibody designated PRO 140, or of (b) an anti-CCR5 receptor monoclonal antibody. This invention also provides a method for inhibiting in a human subject the onset or progression of an HIV-1-associated disorder, the inhibition of which is effected by inhibiting fusion of HIV-1 to CCR5+CD4+ target cells in the subject. This invention also provides a method for treating a subject infected with HIV-1 comprising administering to the subject (a) a monoclonal antibody which (i) binds to a CCR5 receptor on the surface of the subject's CD4+ cells and (ii) inhibits fusion of HIV-1 to the subject's CCR5+CD4+ cells, and (b) a non-antibody CCR5 receptor antagonist, in amounts effective to treat the subject.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 2, 2014
    Assignee: CytoDyn Inc.
    Inventors: William C. Olson, Paul J. Maddon, Daniel C. Pevear, Robert J. Israel, Jose D. Murga
  • Publication number: 20140235669
    Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: ANIONA APS
    Inventors: Dan PETERS, Gordon MUNRO, Elsebet Ostergaard NIELSEN, Karin Sandager NIELSEN
  • Publication number: 20140234443
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: March 10, 2014
    Publication date: August 21, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter R. GUZZO, David D. MANNING, William EARLEY
  • Publication number: 20140228397
    Abstract: The present invention relates to propellant-free aerosol formulations for inhalation containing ipratropium bromide and salbutamol.
    Type: Application
    Filed: November 22, 2013
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Silvia Weitzel
  • Patent number: 8802698
    Abstract: The invention provides 8-azabicyclo[3.2.1]octyl-2-hydroxybenzamide compounds of formula (I): wherein R2, R7, and m 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: June 10, 2013
    Date of Patent: August 12, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daisuke Roland Saito, Daniel D. Long, Lan Jiang, Bryan Frieman
  • Publication number: 20140221420
    Abstract: Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.
    Type: Application
    Filed: March 18, 2011
    Publication date: August 7, 2014
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Venkateswararao Kalapala, Jianfeng Li
  • Publication number: 20140221341
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Application
    Filed: April 15, 2014
    Publication date: August 7, 2014
    Applicant: NAEJA PHARMACEUTICAL INC.
    Inventors: Samarendra N. MAITI, Dai NGUYEN, Jehangir KHAN, Rong LING
  • Patent number: RE45364
    Abstract: A chemical compound represented by the formula [I]: (wherein R1 represents a hydroxyl group or the like, m represents 0 or an integer of 1 to 5, R2 represents a halogen atom or the like, k represents 0 or an integer of 1 to 4, R3, R31, R4, R41, R5, R51, R6, R61, and R7 each independently represents a hydrogen atom or the like, X represents an oxygen atom or the like, and n represents 1), a salt, an N-oxide of the chemical compound represented by formula [I], and a pest control agent containing the formula [I] as its active constituent.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: February 3, 2015
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Daisuke Hanai, Takao Iwasa