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Complete Dissertation
VU Research Portal Histamine H-receptor agonists and antagonists ter Laak, A.M. 1995 document version Publisher's PDF, also known as Version of record Link to publication in VU Research Portal citation for published version (APA) ter Laak, A. M. (1995). Histamine H-receptor agonists and antagonists: molecular modeling and drug design. General rights Copyright and moral rights for the publications made accessible in the public portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognise and abide by the legal requirements associated with these rights. • Users may download and print one copy of any publication from the public portal for the purpose of private study or research. • You may not further distribute the material or use it for any profit-making activity or commercial gain • You may freely distribute the URL identifying the publication in the public portal ? Take down policy If you believe that this document breaches copyright please contact us providing details, and we will remove access to the work immediately and investigate your claim. E-mail address: [email protected] Download date: 06. Oct. 2021 Histamine H1~receptor Agonists and Antagonists Molecular Modeling and Drug Design , Ton tel' Laak Histamine HI-receptor Agonists and Antagonists Molecular Modeling and Drug Design VRIJE UNIVERSlTEIT Histamine HI-receptor Agonists and Antagonists Molecular Modeling and Drug Design ACADEMISCH PROEFSCHRIFT ter verkrijging van de graad van doctor aan de Vrije Universiteit te Amsterdam, op gezag van de rector magnificus prof.dr E. Boeker, in het openbaar te verdedigen ten overstaan van de promotiecommissie van de faculteit der scheikunde op maandag 16 oktober 1995 te 13.45 uur in het hoofdgebouw van de universiteit, De Boelelaan 1105 door Antonius Marinus ter Laak geboren te Delft Promotor prof.dr H. -
Paediatric Drug Development: an Opportunity for Academia to Close the Gap
Paediatric drug development: an opportunity for academia to close the gap Pauline De Bruyne Promotor: Prof. dr. J. Vande Walle Copromotor: Prof. dr. M. Van Winckel Ghent University Faculty of Medicine and Health Sciences Department of Paediatrics and Medical Genetics Paediatric drug development: an opportunity for academia to close the gap Pauline De Bruyne This thesis is submitted as fulfillment of the requirements for the degree of Doctor in Health Sciences. Academic year 2015 – 2016 Promotors: Prof. dr. Johan Vande Walle Prof. dr. Myriam Van Winckel Promotors: Prof. dr. Johan Vande Walle Prof. dr. Myriam Van Winckel Members of the Supervisory Board: Prof. dr. Dirk Matthys dr. Lieve Nuytinck Prof. dr. Luc Van Bortel Members of the Examination Committee: Prof. dr. Johan Van de Voorde (chair) Prof. dr. Karel Allegaert Prof. dr. ir. Sofie Bekaert Prof. dr. Daniel Brasseur Prof. dr. Sylvie Rottey Prof. dr. Jan Van Bocxlaer Prof. dr. John van den Anker The research reported in this thesis was supported by a doctoral grant for Strategic Basic Research (IWT SB-111279) awarded to Pauline De Bruyne, and a grant for Strategic Basic Research (IWT SBO-130033) awarded to the SAFE-PEDRUG project; both of the Agency for Innovation by Science and Technology in Flanders. Voor Sara, Emile en Julie Table of contents TABLE OF CONTENTS Table of contents ............................................................................................................ 1 List of abbreviations ...................................................................................................... -
The Organic Chemistry of Drug Synthesis
THE ORGANIC CHEMISTRY OF DRUG SYNTHESIS VOLUME 3 DANIEL LEDNICER Analytical Bio-Chemistry Laboratories, Inc. Columbia, Missouri LESTER A. MITSCHER The University of Kansas School of Pharmacy Department of Medicinal Chemistry Lawrence, Kansas A WILEY-INTERSCIENCE PUBLICATION JOHN WILEY AND SONS New York • Chlchester • Brisbane * Toronto • Singapore Copyright © 1984 by John Wiley & Sons, Inc. All rights reserved. Published simultaneously in Canada. Reproduction or translation of any part of this work beyond that permitted by Section 107 or 108 of the 1976 United States Copyright Act without the permission of the copyright owner is unlawful. Requests for permission or further information should be addressed to the Permissions Department, John Wiley & Sons, Inc. Library of Congress Cataloging In Publication Data: (Revised for volume 3) Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." Includes bibliographical references and index. 1. Chemistry, Pharmaceutical. 2. Drugs. 3. Chemistry, Organic—Synthesis. I. Mitscher, Lester A., joint author. II. Title. [DNLM 1. Chemistry, Organic. 2. Chemistry, Pharmaceutical. 3. Drugs—Chemical synthesis. QV 744 L473o 1977] RS403.L38 615M9 76-28387 ISBN 0-471-09250-9 (v. 3) Printed in the United States of America 10 907654321 With great pleasure we dedicate this book, too, to our wives, Beryle and Betty. The great tragedy of Science is the slaying of a beautiful hypothesis by an ugly fact. Thomas H. Huxley, "Biogenesis and Abiogenisis" Preface Ihe first volume in this series represented the launching of a trial balloon on the part of the authors. In the first place, wo were not entirely convinced that contemporary medicinal (hemistry could in fact be organized coherently on the basis of organic chemistry. -
United States Patent 19 11 Patent Number: 5,446,070 Mantelle (45) Date of Patent: "Aug
USOO544607OA United States Patent 19 11 Patent Number: 5,446,070 Mantelle (45) Date of Patent: "Aug. 29, 1995 54 COMPOST ONS AND METHODS FOR 4,659,714 4/1987 Watt-Smith ......................... 514/260 TOPCAL ADMNSTRATION OF 4,675,009 6/1987 Hymes .......... ... 604/304 PHARMACEUTICALLY ACTIVE AGENTS 4,695,465 9/1987 Kigasawa .............................. 424/19 4,748,022 5/1988 Busciglio. ... 424/195 75 Inventor: Juan A. Mantelle, Miami, Fla. 4,765,983 8/1988 Takayanagi. ... 424/434 4,789,667 12/1988 Makino ............ ... 514/16 73) Assignee: Nover Pharmaceuticals, Inc., Miami, 4,867,970 9/1989 Newsham et al. ... 424/435 Fla. 4,888,354 12/1989 Chang .............. ... 514/424 4,894,232 1/1990 Reul ............. ... 424/439 * Notice: The portion of the term of this patent 4,900,552 2/1990 Sanvordeker .... ... 424/422 subsequent to Aug. 10, 2010 has been 4,900,554 2/1990 Yanagibashi. ... 424/448 disclaimed. 4,937,078 6/1990 Mezei........... ... 424/450 Appl. No.: 112,330 4,940,587 7/1990 Jenkins ..... ... 424/480 21 4,981,875 l/1991 Leusner ... ... 514/774 22 Filed: Aug. 27, 1993 5,023,082 6/1991 Friedman . ... 424/426 5,234,957 8/1993 Mantelle ........................... 514/772.6 Related U.S. Application Data FOREIGN PATENT DOCUMENTS 63 Continuation-in-part of PCT/US92/01730, Feb. 27, 0002425 6/1979 European Pat. Off. 1992, which is a continuation-in-part of Ser. No. 0139127 5/1985 European Pat. Off. 813,196, Dec. 23, 1991, Pat. No. 5,234,957, which is a 0159168 10/1985 European Pat. -
(12) Patent Application Publication (10) Pub. No.: US 2006/0078604 A1 Kanios Et Al
US 20060078604A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0078604 A1 Kanios et al. (43) Pub. Date: Apr. 13, 2006 (54) TRANSDERMAL DRUG DELIVERY DEVICE Related U.S. Application Data INCLUDING AN OCCLUSIVE BACKING (60) Provisional application No. 60/616,861, filed on Oct. 8, 2004. (75) Inventors: David Kanios, Miami, FL (US); Juan A. Mantelle, Miami, FL (US); Viet Publication Classification Nguyen, Miami, FL (US) (51) Int. Cl. Correspondence Address: A 6LX 9/70 (2006.01) DCKSTEIN SHAPRO MORN & OSHINSKY (52) U.S. Cl. .............................................................. 424/449 LLP (57) ABSTRACT 2101 L Street, NW Washington, DC 20037 (US) A transdermal drug delivery system for the topical applica tion of one or more active agents contained in one or more (73) Assignee: Noven Pharmaceuticals, Inc. polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can (21) Appl. No.: 11/245,180 control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmis (22) Filed: Oct. 7, 2005 sion rate of the polymeric backing layer. Patent Application Publication Apr. 13, 2006 Sheet 1 of 2 US 2006/0078604 A1 Fis ZZZZZZZZZZZZZZZZZZZ :::::::::::::::::::::::::::::::: Patent Application Publication Apr. 13, 2006 Sheet 2 of 2 US 2006/0078604 A1 3. s s 3. a 3 : 8 g US 2006/0078604 A1 Apr. 13, 2006 TRANSIDERMAL DRUG DELVERY DEVICE 0008. In the “classic' reservoir-type device, the active INCLUDING AN OCCLUSIVE BACKING agent is typically dissolved or dispersed in a carrier to yield a non-finite carrier form, Such as, for example, a fluid or gel. -
Perspectives in Drug Discovery a Collection of Essays on the History and Development of Pharmaceutical Substances
Perspectives in Drug Discovery A Collection of Essays on the History and Development of Pharmaceutical Substances Professor Alan Wayne Jones Department of Forensic Genetics and Forensic Toxicology, National Board of Forensic Medicine Perspectives in Drug Discovery A Collection of Essays on the History and Development of Pharmaceutical Substances Professor Alan Wayne Jones Department of Forensic Genetics and Forensic Toxicology National Board of Forensic Medicine Perspectives in Drug Discovery A Collection of Essays on the History and Development of Pharmaceutical Substances Professor Alan Wayne Jones Department of Forensic Genetics and Forensic Toxicology, National Board of Forensic Medicine Artillerigatan 12 • SE-587 58 Linköping • Sweden E-mail: [email protected] Internet: www.rmv.se RMV-report 2010:1 ISSN 1103-7660 Copyright © 2010 National Board of Forensic Medicine and Professor Alan Wayne Jones Design and graphic original: Forma Viva, Linköping • Sweden Printed by Centraltryckeriet, Linköping • Sweden, October 2010 Contents Preface Introduction 1. The First Sedative Hypnotics . 13 2. The Barbiturates ......................... 19 3. The Benzodiazepines ..................... 25 4. Narcotic Analgesics . 31 5. Central Stimulant Amines . 39 6. The First Antidepressants .................. 45 7. Antipsychotic Medication ................. 51 8. Aspirin and Other NSAID .................. 59 9. General Anesthetics . 65 10. SSRI Antidepressants . 71 11. Histamine Antagonists .................... 79 12. Anticonvulsants ......................... 87 -
PRODUCT MONOGRAPH ALLERTIN Loratadine Capsules, 10 Mg Histamine H1 Receptor Antagonist APOTEX INC. DATE of REVISION: 150 Signet
PRODUCT MONOGRAPH ALLERTIN Loratadine Capsules, 10 mg Histamine H1 receptor antagonist APOTEX INC. DATE OF REVISION: 150 Signet Drive September 25, 2019 Toronto, Ontario Canada M9L 1T9 Control #: 231181 Page 2 of 20 Table of Contents PART I: HEALTH PROFESSIONAL INFORMATION ....................................................................... 4 SUMMARY PRODUCT INFORMATION ............................................................................................. 4 INDICATIONS AND CLINICAL USE ................................................................................................... 4 CONTRAINDICATIONS ........................................................................................................................ 4 WARNINGS AND PRECAUTIONS ....................................................................................................... 4 ADVERSE REACTIONS ......................................................................................................................... 5 DRUG INTERACTIONS ......................................................................................................................... 6 DOSAGE AND ADMINISTRATION ..................................................................................................... 7 OVERDOSAGE ....................................................................................................................................... 7 ACTION AND CLINICAL PHARMACOLOGY.................................................................................... 8 STORAGE -
Ep 2425858 A2
(19) & (11) EP 2 425 858 A2 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 07.03.2012 Bulletin 2012/10 A61K 45/06 (2006.01) A61K 31/167 (2006.01) A61K 31/085 (2006.01) A61K 31/165 (2006.01) (2006.01) (21) Application number: 11007950.6 A61P 29/00 (22) Date of filing: 19.11.2007 (84) Designated Contracting States: (72) Inventors: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR • Bean, Bruce P. HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE Waban, MA 02468 (US) SI SK TR • Woolf, Clifford J. Newton, MA 02458 (US) (30) Priority: 20.11.2006 US 860124 P 06.07.2007 US 958594 P (74) Representative: Lahrtz, Fritz 03.10.2007 US 997510 P Isenbruck Bösl Hörschler LLP Patentanwälte (62) Document number(s) of the earlier application(s) in Prinzregentenstraße 68 accordance with Art. 76 EPC: DE-81675 München (DE) 07862114.1 / 2 101 819 Remarks: (71) Applicants: This application was filed on 30-09-2011 as a • President and Fellows of Harvard College divisional application to the application mentioned Cambridge, MA 02138 (US) under INID code 62. • The General Hospital Corporation Boston, MA 02114 (US) (54) Compositions for treating pain and pruritus (57) The invention features a method for inhibiting through the channel-forming receptor when the receptor one or more voltage-gated ion channels in a cell by con- is activated. The invention also features a quarternary tacting the cell with (i) a first compound that activates a amine derivative or other permanently or transiently channel-forming receptor that is present on nociceptors charged derivative of a compound that inhibits one or and/or pruriceptors; and (ii) a second compound that in- more voltage-gated ion channels when applied to the in- hibits one or more voltage-gated ion channels when ap- ternal face of the channels but does not substantially in- plied to the internal face of the channels but does not hibit said channels when applied to the external face of substantially inhibit said channels when applied to the the channels. -
Permanently Charged Sodium and Calcium Channel Blockers As Anti-Inflammatory Agents
(19) TZZ ¥Z¥_T (11) EP 2 995 303 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 16.03.2016 Bulletin 2016/11 A61K 31/165 (2006.01) A61K 31/277 (2006.01) A61K 45/06 (2006.01) A61P 25/00 (2006.01) (2006.01) (2006.01) (21) Application number: 15002768.8 A61P 11/00 A61P 13/00 A61P 17/00 (2006.01) A61P 1/00 (2006.01) (2006.01) (2006.01) (22) Date of filing: 09.07.2010 A61P 27/02 A61P 29/00 A61P 37/08 (2006.01) (84) Designated Contracting States: (72) Inventors: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB • WOOLF, Clifford, J. GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO Newton, MA 02458 (US) PL PT RO SE SI SK SM TR • BEAN, Bruce, P. Waban, MA 02468 (US) (30) Priority: 10.07.2009 US 224512 P (74) Representative: Lahrtz, Fritz (62) Document number(s) of the earlier application(s) in Isenbruck Bösl Hörschler LLP accordance with Art. 76 EPC: Patentanwälte 10797919.7 / 2 451 944 Prinzregentenstrasse 68 81675 München (DE) (71) Applicants: • President and Fellows of Harvard College Remarks: Cambridge, MA 02138 (US) This application was filed on 25-09-2015 as a • THE GENERAL HOSPITAL CORPORATION divisional application to the application mentioned Boston, MA 02114 (US) under INID code 62. • CHILDREN’S MEDICAL CENTER CORPORATION Boston, Massachusetts 02115 (US) (54) PERMANENTLY CHARGED SODIUM AND CALCIUM CHANNEL BLOCKERS AS ANTI-INFLAMMATORY AGENTS (57) The present invention relates to a composition or a kit comprising N-methyl etidocaine for use in a method for treating neurogenic inflammation in a patient, wherein the kit further comprises instructions for use. -
Analysis for Commonly Prescribed Non-Sedating Antihistamines ⇑ Michael E
Analytical Chemistry Research 3 (2015) 1–12 Contents lists available at ScienceDirect Analytical Chemistry Research journal homepage: www.elsevier.com/locate/ancr Analysis for commonly prescribed non-sedating antihistamines ⇑ Michael E. El-Kommos, Samia M. El-Gizawy, Noha N. Atia, Noha M. Hosny Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt article info abstract Keywords: A comprehensive review with 185 references for the analysis of commonly prescribed members of an Cetirizine important class of drugs, non-sedating antihistamines (NSAs), is presented. The review covers most of Ebastine the methods described for the analysis of cetirizine (CTZ), ebastine (EBS), fexofenadine (FXD), ketotifen Fexofenadine (KET) and loratadine (LOR) in pure forms, in different pharmaceutical dosage forms and in biological Ketotifen fluids. The review covers the period from 1991 till now. Loratadine Ó 2014 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/3.0/). Contents 1. Introduction. ........................................................................................................ 2 2. Chemistry . ........................................................................................................ 2 3. Pharmacokinetics of NSAs . ..................................................................................... 2 4. Official methods of analysis . .................................................................................... -
The Effects of Acute and Chronic Diphenhydramine and Cetirizine Use on Learning and Memory in Rats
T.C. REPUBLIC OF TURKEY HACETTEPE UNIVERSITY INSTITUTE OF HEALTH SCIENCES THE EFFECTS OF ACUTE AND CHRONIC DIPHENHYDRAMINE AND CETIRIZINE USE ON LEARNING AND MEMORY IN RATS Sadık Taşkın TAŞ, MD Medical Pharmacology Program DOCTOR OF PHILOSOPHY THESIS ANKARA 2018 T.C. REPUBLIC OF TURKEY HACETTEPE UNIVERSITY INSTITUTE OF HEALTH SCIENCES THE EFFECTS OF ACUTE AND CHRONIC DIPHENHYDRAMINE AND CETIRIZINE USE ON LEARNING AND MEMORY IN RATS Sadık Taşkın TAŞ, MD Medical Pharmacology Program DOCTOR OF PHILOSOPHY THESIS ADVISOR OF THE THESIS Prof. Mehmet Yıldırım SARA, MD, PhD ANKARA 2018 iii The Effects of Acute and Chronic Diphenhydramine and Cetirizine Use on Learning and Memory in Rats Sadık Taşkın Taş, MD This study has been approved and accepted as a PhD dissertation in the program of “Medical Pharmacology” by the examining committee, whose members are listed below, on 18.01.2018. Chairman of the Committee : Prof. Dr. Alper Bektaş İskit Hacettepe University Advisor of the Dissertation : Prof. Dr. Mehmet Yıldırım Sara Hacettepe University Member : Prof. Dr. Emine Demirel Yılmaz Ankara University Member : Doç. Dr. Güray Soydan Hacettepe University Member : Doç. Dr. Ergin Dileköz Gazi University This dissertation has been approved by the committee above in conformity to the regulations and by laws of Hacettepe University Graduate Programs. Prof. Dr. Diclehan Orhan Institute Director iv YAYIMLAMA VE FİKRİ MÜLKİYET HAKLARI BEYANI Enstitü tarafından onaylanan lisansüstü tezimin/raporumun tamamını veya herhangi bir kısmını, basılı (kağıt) ve elektronik formatta arşivleme ve aşağıda verilen koşullarla kullanıma açma iznini Hacettepe Üniversitesine verdiğimi bildiririm. Bu izinle Üniversiteye verilen kullanım hakları dışındaki tüm fikri mülkiyet haklarım bende kalacak, tezimin tamamının ya da bir bölümünün gelecekteki çalışmalarda (makale, kitap, lisans ve patent vb.) kullanım hakları bana ait olacaktır. -
Ep001815846a2*
(19) *EP001815846A2* (11) EP 1 815 846 A2 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 08.08.2007 Bulletin 2007/32 A61K 9/127 (2006.01) A61K 31/192 (2006.01) A61K 31/196 (2006.01) A61K 31/405 (2006.01) (2006.01) (21) Application number: 06023465.5 A61K 31/5415 (22) Date of filing: 09.10.2003 (84) Designated Contracting States: (72) Inventors: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR • Cevc, Gregor HU IE IT LI LU MC NL PT RO SE SI SK TR 82131 Gauting (DE) Designated Extension States: • Vierl, Ulrich AL LT LV MK 82194 Gröbenzell (DE) (30) Priority: 11.10.2002 US 417874 P (74) Representative: Maiwald Patentanwalts GmbH 04.02.2003 US 357617 Elisenhof 04.02.2003 US 357618 Elisenstraße 3 80335 München (DE) (62) Document number(s) of the earlier application(s) in accordance with Art. 76 EPC: Remarks: 03757944.8 / 1 551 370 This application was filed on 10-11-2006 as a divisional application to the application mentioned (71) Applicant: IDEA AG under INID code 62. 80807 Munich (DE) (54) Aggregate with increased deformability, comprising at least three amphipats, for improved transport through semi-permeable barriers and for the non-invasive drug application in vivo, especially through the skin (57) The application describes combinations of at least three amphipatic substances forming aggregate suspensions in a polar liquid. Judicious choice of system components, which differ at least 2-times to 10-times in solubility, ensures said aggregates to have extended, un- usually adaptable surfaces.