WO 2013/142184 Al 26 September 2013 (26.09.2013) P O P C T
Total Page:16
File Type:pdf, Size:1020Kb
Load more
Recommended publications
-
Hyperforin Inhibits Cell Growth by Inducing Intrinsic and Extrinsic
ANTICANCER RESEARCH 37 : 161-168 (2017) doi:10.21873/anticanres.11301 Hyperforin Inhibits Cell Growth by Inducing Intrinsic and Extrinsic Apoptotic Pathways in Hepatocellular Carcinoma Cells I-TSANG CHIANG 1,2,3* , WEI-TING CHEN 4* , CHIH-WEI TSENG 5, YEN-CHUNG CHEN 2,6 , YU-CHENG KUO 7, BI-JHIH CHEN 8, MAO-CHI WENG 9, HWAI-JENG LIN 10,11# and WEI-SHU WANG 2,12,13# Departments of 1Radiation Oncology, 6Pathology, and 13 Medicine, and 2Cancer Medical Care Center, National Yang-Ming University Hospital, Yilan, Taiwan, R.O.C.; 3Department of Radiological Technology, Central Taiwan University of Science and Technology, Taichung, Taiwan, R.O.C.; 4Department of Psychiatry, Zuoying Branch of Kaohsiung Armed Forces General Hospital, Kaohsiung, Taiwan, R.O.C.; 5Division of Gastroenterology, Department of Internal Medicine, Dalin Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, Chia-Yi, Taiwan, R.O.C.; 7Radiation Oncology, Show Chwan Memorial Hospital, Changhua, Taiwan, R.O.C.; 8Department of Laboratory Medicine, Changhua Christian Hospital, Changhua Christian Medical Foundation, Changhua, Taiwan, R.O.C.; 9Institute of Nuclear Energy Research, Atomic Energy Council, Taoyuan, Taiwan, R.O.C.; 10 Department of Internal Medicine, Division of Gastroenterology and Hepatology, College of Medicine, School of Medicine, Taipei Medical University, Taipei, Taiwan, R.O.C.; 11 Department of Internal Medicine, Division of Gastroenterology and Hepatology, Shuang-Ho Hospital, New Taipei, Taiwan, R.O.C.; 12 National Yang-Ming University School of Medicine, Taipei, Taiwan, R.O.C. Abstract. The aim of the present study was to investigate the (c-FLIP), X-linked inhibitor of apoptosis protein (XIAP), antitumor effect and mechanism of action of hyperforin in myeloid cell leukemia 1(MCL1), and cyclin-D1] were hepatocellular carcinoma (HCC) SK-Hep1 cells in vitro. -
(19) United States (12) Patent Application Publication (10) Pub
US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist. -
St. John's Wort 2018
ONLINE SERIES MONOGRAPHS The Scientific Foundation for Herbal Medicinal Products Hyperici herba St. John's Wort 2018 www.escop.com The Scientific Foundation for Herbal Medicinal Products HYPERICI HERBA St. John's Wort 2018 ESCOP Monographs were first published in loose-leaf form progressively from 1996 to 1999 as Fascicules 1-6, each of 10 monographs © ESCOP 1996, 1997, 1999 Second Edition, completely revised and expanded © ESCOP 2003 Second Edition, Supplement 2009 © ESCOP 2009 ONLINE SERIES ISBN 978-1-901964-61-5 Hyperici herba - St. John's Wort © ESCOP 2018 Published by the European Scientific Cooperative on Phytotherapy (ESCOP) Notaries House, Chapel Street, Exeter EX1 1EZ, United Kingdom www.escop.com All rights reserved Except for the purposes of private study, research, criticism or review no part of this text may be reproduced, stored in a retrieval system or transmitted, in any form or by any means, without the written permission of the publisher. Important Note: Medical knowledge is ever-changing. As new research and clinical experience broaden our knowledge, changes in treatment may be required. In their efforts to provide information on the efficacy and safety of herbal drugs and herbal preparations, presented as a substantial overview together with summaries of relevant data, the authors of the material herein have consulted comprehensive sources believed to be reliable. However, in view of the possibility of human error by the authors or publisher of the work herein, or changes in medical knowledge, neither the authors nor the publisher, nor any other party involved in the preparation of this work, warrants that the information contained herein is in every respect accurate or complete, and they are not responsible for any errors or omissions or for results obtained by the use of such information. -
Synaptic Action of Anandamide and Related Substances in Mammalian Brain
SYNAPTIC ACTION OF ANANDAMIDE AND RELATED SUBSTANCES IN MAMMALIAN BRAIN by Chengyong Liao M.Sc., Sichuan University, 1991 B.Sc., Sichuan University, 1984 THESIS SUBMITTED IN PARTIAL FULFILLMENT OF THE REQUIREMENTS FOR THE DEGREE OF DOCTOR OF PHILOSOPHY Inthe Department of Biological Sciences © Chengyong Liao 2007 SIMON FRASER UNIVERSITY 2007 All rights reserved. This work may not be reproduced in whole or in part, by photocopy or other means, without permission ofthe author. APPROVAL Name: Chengyong Liao Degree: Doctor of Philosophy Title of Thesis: Synaptic Actions of Anandamide and Related Substances in Mammalian Brain Examining Committee: Chair: Dr. Z. Punja Professor ofDepartment ofBiological Sciences, SFU. Dr. R. A. Nicholson Senior Supervisor Associate Professor ofDepartment ofBiological Sciences, SFU. Dr. C. J. Kennedy, Supervisor Associate Professor of Department ofBiological Sciences, SFU Dr. F. C. P. Law, Supervisor Professor ofDepartment ofBiological Sciences, SFU Dr. M. A. Silverman Public Examiner Associate Professor ofDepartment ofBiological Sciences, SFU Dr. J. Church External Examiner Professor ofDepartment ofCellular and Physiological Sciences, UBC Date Defended/Approved: 11 SIMON FRASER UNIVERSITY LIBRARY Declaration of Partial Copyright Licence The author, whose copyright is declared on the title page of this work, has granted to Simon Fraser University the right to lend this thesis, project or extended essay to users of the Simon Fraser University Library, and to make partial or single copies only for such users or -
Compositions and Methods for Selective Delivery of Oligonucleotide Molecules to Specific Neuron Types
(19) TZZ ¥Z_T (11) EP 2 380 595 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 26.10.2011 Bulletin 2011/43 A61K 47/48 (2006.01) C12N 15/11 (2006.01) A61P 25/00 (2006.01) A61K 49/00 (2006.01) (2006.01) (21) Application number: 10382087.4 A61K 51/00 (22) Date of filing: 19.04.2010 (84) Designated Contracting States: • Alvarado Urbina, Gabriel AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Nepean Ontario K2G 4Z1 (CA) HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL • Bortolozzi Biassoni, Analia Alejandra PT RO SE SI SK SM TR E-08036, Barcelona (ES) Designated Extension States: • Artigas Perez, Francesc AL BA ME RS E-08036, Barcelona (ES) • Vila Bover, Miquel (71) Applicant: Nlife Therapeutics S.L. 15006 La Coruna (ES) E-08035, Barcelona (ES) (72) Inventors: (74) Representative: ABG Patentes, S.L. • Montefeltro, Andrés Pablo Avenida de Burgos 16D E-08014, Barcelon (ES) Edificio Euromor 28036 Madrid (ES) (54) Compositions and methods for selective delivery of oligonucleotide molecules to specific neuron types (57) The invention provides a conjugate comprising nucleuc acid toi cell of interests and thus, for the treat- (i) a nucleic acid which is complementary to a target nu- ment of diseases which require a down-regulation of the cleic acid sequence and which expression prevents or protein encoded by the target nucleic acid as well as for reduces expression of the target nucleic acid and (ii) a the delivery of contrast agents to the cells for diagnostic selectivity agent which is capable of binding with high purposes. -
Note: the Letters 'F' and 'T' Following the Locators Refers to Figures and Tables
Index Note: The letters ‘f’ and ‘t’ following the locators refers to figures and tables cited in the text. A Acyl-lipid desaturas, 455 AA, see Arachidonic acid (AA) Adenophostin A, 71, 72t aa, see Amino acid (aa) Adenosine 5-diphosphoribose, 65, 789 AACOCF3, see Arachidonyl trifluoromethyl Adlea, 651 ketone (AACOCF3) ADP, 4t, 10, 155, 597, 598f, 599, 602, 669, α1A-adrenoceptor antagonist prazosin, 711t, 814–815, 890 553 ADPKD, see Autosomal dominant polycystic aa 723–928 fragment, 19 kidney disease (ADPKD) aa 839–873 fragment, 17, 19 ADPKD-causing mutations Aβ, see Amyloid β-peptide (Aβ) PKD1 ABC protein, see ATP-binding cassette protein L4224P, 17 (ABC transporter) R4227X, 17 Abeele, F. V., 715 TRPP2 Abbott Laboratories, 645 E837X, 17 ACA, see N-(p-amylcinnamoyl)anthranilic R742X, 17 acid (ACA) R807X, 17 Acetaldehyde, 68t, 69 R872X, 17 Acetic acid-induced nociceptive response, ADPR, see ADP-ribose (ADPR) 50 ADP-ribose (ADPR), 99, 112–113, 113f, Acetylcholine-secreting sympathetic neuron, 380–382, 464, 534–536, 535f, 179 537f, 538, 711t, 712–713, Acetylsalicylic acid, 49t, 55 717, 770, 784, 789, 816–820, Acrolein, 67t, 69, 867, 971–972 885 Acrosome reaction, 125, 130, 301, 325, β-Adrenergic agonists, 740 578, 881–882, 885, 888–889, α2 Adrenoreceptor, 49t, 55, 188 891–895 Adult polycystic kidney disease (ADPKD), Actinopterigy, 223 1023 Activation gate, 485–486 Aframomum daniellii (aframodial), 46t, 52 Leu681, amino acid residue, 485–486 Aframomum melegueta (Melegueta pepper), Tyr671, ion pathway, 486 45t, 51, 70 Acute myeloid leukaemia and myelodysplastic Agelenopsis aperta (American funnel web syndrome (AML/MDS), 949 spider), 48t, 54 Acylated phloroglucinol hyperforin, 71 Agonist-dependent vasorelaxation, 378 Acylation, 96 Ahern, G. -
(12) United States Patent (10) Patent No.: US 9.402,830 B2 Cialella Et Al
USOO940283OB2 (12) United States Patent (10) Patent No.: US 9.402,830 B2 Cialella et al. (45) Date of Patent: * Aug. 2, 2016 (54) METHODS OF TREATING DYSKINESIA AND FOREIGN PATENT DOCUMENTS RELATED DSORDERS WO 93.18767 A1 9, 1993 (71) Applicant: Melior Discovery, Inc., Exton, PA (US) OTHER PUBLICATIONS (72) Inventors: John Ciallella, Exton, PA (US); John Afanasev et al., Effects of amphetamine and Sydnocarbon dopamine Gruner, Exton, PA (US); Andrew G. release and free radical generation in rat striatum, Pharmacol Reaume, Exton, PA (US); Michael S. Biochem Behav, 2001, 69(3-4):653-8. Saporito, Exton, PA (US) Anderzhanova et al., Effect of d-amphetamine and Sydnocarb on the extracellular level of dopamine, 3,4-dihydroxyphenylacetic acid, and (73) Assignee: Melior Discovery, Inc., Exton, PA (US) hydroxyl radicals generation in rat striatum, Ann NY AcadSci, 2000, 914:137-45. Anderzhanova et al., Effects of Sydnocarb and D-amphetamine on the (*) Notice: Subject to any disclaimer, the term of this extracellular levels of amino acids in the rat caudate-putamen, Eur J patent is extended or adjusted under 35 Pharmacol, 2001, 428(1):87-95. U.S.C. 154(b) by 0 days. Bashkatova et al., Neuroshemical changes and neurotoxic effects of This patent is Subject to a terminal dis an acute treatment with Sydnocarb, a novel psychostimulant: com claimer. parison with D-amphetamine, Ann NY AcadSci, 2002,965: 180-192. Cody, Precursor medications as a source of methamphetamine and/or amphetamine positive drug testing results, J Occup Environ Med, (21) Appl. No.: 14/702,242 2002, 44(5):435-50. -
Study Protocol 64565111EDI1002
NCT03586830 Janssen Research & Development * Clinical Protocol Protocol Title A Randomized, Double-blind Placebo-controlled, Parallel-group, Multicenter, Dose- ranging Study to Evaluate the Safety and Efficacy of JNJ-64565111 in Severely Obese Subjects with Type 2 Diabetes Mellitus Short Title Evaluation of JNJ-64565111 in Severely Obese Subjects with Type 2 Diabetes Mellitus Protocol 64565111OBE2002; Phase 2b AMENDMENT 1 JNJ-64565111 *Janssen Research & Development is a global organization that operates through different legal entities in various countries. Therefore, the legal entity acting as the sponsor for Janssen Research & Development studies may vary, such as, but not limited to Janssen Biotech, Inc.; Janssen Products, LP; Janssen Biologics, BV; Janssen-Cilag International NV; Janssen, Inc; Janssen Pharmaceutica NV; Janssen Sciences Ireland UC; or Janssen Research & Development, LLC. The term “sponsor” is used throughout the protocol to represent these various legal entities; the sponsor is identified on the Contact Information page that accompanies the protocol. US sites of this study will be conducted under US Food & Drug Administration IND regulations (21 CFR Part 312).] Status: Approved Date: 23 August 2018 Prepared by: Janssen Research & Development, LLC EDMS number: EDMS-ERI-156156741, 2.0 GCP Compliance: This study will be conducted in compliance with Good Clinical Practice, and applicable regulatory requirements. Confidentiality Statement The information in this document contains trade secrets and commercial information that are privileged or confidential and may not be disclosed unless such disclosure is required by applicable law or regulations. In any event, persons to whom the information is disclosed must be informed that the information is privileged or confidential and may not be further disclosed by them. -
(12) United States Patent (10) Patent N0.: US 7,964,607 B2 Verhoest Et A1
US007964607B2 (12) United States Patent (10) Patent N0.: US 7,964,607 B2 Verhoest et a1. (45) Date of Patent: Jun. 21, 2011 (54) PYRAZOLO[3,4-D]PYRIMIDINE FOREIGN PATENT DOCUMENTS COMPOUNDS EP 1460077 9/2004 WO 02085904 10/2002 (75) Inventors: Patrick Robert Verhoest, Old Lyme, CT WO 2004037176 5/2004 (US); Caroline ProulX-Lafrance, Ledyard, CT (US) OTHER PUBLICATIONS Wunder et a1, M01. PharmacoL, v01. 28, N0. 6, (2005), pp. 1776 (73) Assignee: P?zer Inc., New York, NY (U S) 1781. van der Staay et a1, Neuropharmacology, v01. 55 (2008), pp. 908 ( * ) Notice: Subject to any disclaimer, the term of this 918. patent is extended or adjusted under 35 USC 154(b) by 562 days. Primary Examiner * Susanna Moore (74) Attorney, Agent, or Firm * Jennifer A. Kispert; (21) Appl.No.: 12/118,062 Michael Herman (22) Filed: May 9, 2008 (57) ABSTRACT (65) Prior Publication Data The invention provides PDE9-inhibiting compounds of For US 2009/0030003 A1 Jan. 29, 2009 mula (I), Related US. Application Data (60) Provisional application No. 60/917,333, ?led on May 11, 2007. (51) Int. Cl. C07D 48 7/04 (2006.01) A61K 31/519 (2006.01) A61P 25/28 (2006.01) (52) US. Cl. ................................... .. 514/262.1; 544/262 (58) Field of Classi?cation Search ................ .. 544/262; 5 1 4/2 62 .1 See application ?le for complete search history. and pharmaceutically acceptable salts thereof, Wherein R, R1, (56) References Cited R2 and R3 are as de?ned herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in U.S. -
Download Product Insert (PDF)
Product Information Benocyclidine-d10 Item No. 9001493 Formal Name: 1-(1-benzo[b]thien-2-ylcyclohexyl)- 2,2,3,3,4,4,5,5,6,6-d10-piperidine D D Synonyms: BCP-d10, Benzothiophenylcyclohexylpiperidine-d10, D D BTCP-d10, GK 13-d10 D D S MF: C19H15D10NS FW: 309.5 D N Chemical Purity: ≥98% D Deuterium DD Incorporation: ≥99% deuterated forms (d1-d10); ≤1% d0 Stability: ≥2 years at -20°C Supplied as: A crystalline solid λ UV/Vis.: max: 229, 270, 300 nm Laboratory Procedures Benocyclidine-d10 (BCP-d10) contains ten deuterium atoms at the 2, 2’, 3, 3’, 4, 4’, 5, 5’, 6, and 6’ positions. It is intended for use as an internal standard for the quantification of BCP by GC- or LC-mass spectrometry (MS). For long term storage, we suggest that BCP-d10 be stored as supplied at -20°C. It should be stable for at least two years. BCP-d10 is supplied as a crystalline solid. A stock solution may be made by dissolving the BCP-d10 in the solvent of choice. BCP-d10 is soluble in organic solvents such as ethanol and dimethyl formamide, which should be purged with an inert gas. The solubility of BCP-d10 in these solvents is approximately 2 and 5 mg/ml, respectively. BCP-d10 is used as an internal standard for the quantification of BCP by stable isotope dilution MS. The accuracy of the sample weight in this vial is between 5% over and 2% under the amount shown on the vial. If better precision is required, the deuterated standard should be quantitated against a more precisely weighed unlabeled standard by constructing a standard curve of peak intensity ratios (deuterated versus unlabeled). -
Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances Joshua Zolton Seither [email protected]
Florida International University FIU Digital Commons FIU Electronic Theses and Dissertations University Graduate School 4-25-2018 Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances Joshua Zolton Seither [email protected] DOI: 10.25148/etd.FIDC006565 Follow this and additional works at: https://digitalcommons.fiu.edu/etd Part of the Chemistry Commons Recommended Citation Seither, Joshua Zolton, "Application of High Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances" (2018). FIU Electronic Theses and Dissertations. 3823. https://digitalcommons.fiu.edu/etd/3823 This work is brought to you for free and open access by the University Graduate School at FIU Digital Commons. It has been accepted for inclusion in FIU Electronic Theses and Dissertations by an authorized administrator of FIU Digital Commons. For more information, please contact [email protected]. FLORIDA INTERNATIONAL UNIVERSITY Miami, Florida APPLICATION OF HIGH RESOLUTION MASS SPECTROMETRY FOR THE SCREENING AND CONFIRMATION OF NOVEL PSYCHOACTIVE SUBSTANCES A dissertation submitted in partial fulfillment of the requirements for the degree of DOCTOR OF PHILOSOPHY in CHEMISTRY by Joshua Zolton Seither 2018 To: Dean Michael R. Heithaus College of Arts, Sciences and Education This dissertation, written by Joshua Zolton Seither, and entitled Application of High- Resolution Mass Spectrometry for the Screening and Confirmation of Novel Psychoactive Substances, having been approved in respect to style and intellectual content, is referred to you for judgment. We have read this dissertation and recommend that it be approved. _______________________________________ Piero Gardinali _______________________________________ Bruce McCord _______________________________________ DeEtta Mills _______________________________________ Stanislaw Wnuk _______________________________________ Anthony DeCaprio, Major Professor Date of Defense: April 25, 2018 The dissertation of Joshua Zolton Seither is approved. -
General Pharmacology
GENERAL PHARMACOLOGY Winners of “Nobel” prize for their contribution to pharmacology Year Name Contribution 1923 Frederick Banting Discovery of insulin John McLeod 1939 Gerhard Domagk Discovery of antibacterial effects of prontosil 1945 Sir Alexander Fleming Discovery of penicillin & its purification Ernst Boris Chain Sir Howard Walter Florey 1952 Selman Abraham Waksman Discovery of streptomycin 1982 Sir John R.Vane Discovery of prostaglandins 1999 Alfred G.Gilman Discovery of G proteins & their role in signal transduction in cells Martin Rodbell 1999 Arvid Carlson Discovery that dopamine is neurotransmitter in the brain whose depletion leads to symptoms of Parkinson’s disease Drug nomenclature: i. Chemical name ii. Non-proprietary name iii. Proprietary (Brand) name Source of drugs: Natural – plant /animal derivatives Synthetic/semisynthetic Plant Part Drug obtained Pilocarpus microphyllus Leaflets Pilocarpine Atropa belladonna Atropine Datura stramonium Physostigma venenosum dried, ripe seed Physostigmine Ephedra vulgaris Ephedrine Digitalis lanata Digoxin Strychnos toxifera Curare group of drugs Chondrodendron tomentosum Cannabis indica (Marijuana) Various parts are used ∆9Tetrahydrocannabinol (THC) Bhang - the dried leaves Ganja - the dried female inflorescence Charas- is the dried resinous extract from the flowering tops & leaves Papaver somniferum, P album Poppy seed pod/ Capsule Natural opiates such as morphine, codeine, thebaine Cinchona bark Quinine Vinca rosea periwinkle plant Vinca alkaloids Podophyllum peltatum the mayapple