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An Introduction to Medicinal
An Introduction to Medicinal Chemistry FIFTH EDITION Graham L. Patrick 1 Patrick97397.indb iii 11/28/2012 9:11:45 PM 1 Great Clarendon Street, Oxford, OX2 6DP, United Kingdom Oxford University Press is a department of the University of Oxford. It furthers the University’s objective of excellence in research, scholarship, and education by publishing worldwide. Oxford is a registered trade mark of Oxford University Press in the UK and in certain other countries © Graham L. Patrick 2013 Th e moral rights of the author have been asserted Second Edition copyright 2001 Th ird Edition copyright 2005 Fourth Edition copyright 2009 Impression: 1 All rights reserved. No part of this publication may be reproduced, stored in a retrieval system, or transmitted, in any form or by any means, without the prior permission in writing of Oxford University Press, or as expressly permitted by law, by licence or under terms agreed with the appropriate reprographics rights organization. Enquiries concerning reproduction outside the scope of the above should be sent to the Rights Department, Oxford University Press, at the address above You must not circulate this work in any other form and you must impose this same condition on any acquirer British Library Cataloguing in Publication Data Data available ISBN 978–0–19–969739–7 Printed in Italy by L.E.G.O. S.p.A.—Lavis TN Links to third party websites are provided by Oxford in good faith and for information only. Oxford disclaims any responsibility for the materials contained in any third party website referenced in this work. -
Stems for Nonproprietary Drug Names
USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
Pharmacokinetics and Related Topics
Pharmacokinetics and 11 related topics 11.1 The three phases of drug may be absorbed through the mucosal membranes of the mouth, but most passes down into the stomach where action it encounters gastric juices and hydrochloric acid. Th ese chemicals aid in the digestion of food and will treat a Th ere are three phases involved in drug action. Th e drug in a similar fashion if it is susceptible to breakdown fi rst of these is the pharmaceutical phase . For an orally and is not protected within an acid-resistant pill or cap- administered drug, this includes the disintegration of a sule. For example, the fi rst clinically useful penicillin was pill or capsule in the gastrointestinal tract (GIT), the broken down in the stomach and had to be administered release of the drug, and its dissolution. Th e pharmaceu- by injection. Other acid-labile drugs include the local tical phase is followed by the pharmacokinetic phase , anaesthetics and insulin . If the drug does survive the which includes absorption from the GIT into the blood stomach, it enters the upper intestine where it encoun- supply, and the various factors that aff ect a drug’s survival ters digestive enzymes that serve to break down food. and progress as it travels to its molecular target. Th e fi nal Assuming the drug survives this attack, it then has to pharmacodynamic phase involves the mechanism by pass through the cells lining the gut wall. Th is means that which a drug interacts with its molecular target and the it has to pass through a cell membrane on two occasions: resulting pharmacological eff ect. -
Pharmaceutical Appendix to the Tariff Schedule 2
Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9 -
Downloaded from Survive Nursing | Survivenursing.Com V20110426
Generic Stem Stem Definition Examples -abine (see -arabine, -citabine) decitabine -ac Anti-inflammatory agents (acetic acid derivatives) bromfenac; dexpemedolac -acetam See -racetam -actide Synthetic corticotropins seractide -adol or -aldol- Analgesics (mixed opiate receptor agonists/ antagonists) tazadolene; spiradolene; levonantradol -adox Antibacterials (quinoline dioxide derivatives) carbadox -afenone Antiarrhythmics (propafenone derivatives) alprafenone; diprafenone -afil PDE5 inhibitors tadalafil -aj- Antiarrhythmics (ajmaline derivatives) lorajmine -aldrate Antacid aluminum salts magaldrate -algron Alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol Combined alpha and beta blockers labetalol; medroxalol -amivir (see -vir) -ampa Ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) -ampanel Ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) ; becampanel antagonists -ampator Ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) ; forampator modulators -andr- Androgens nandrolone -anib Angiogenesis inhibitors semaxanib -anserin Serotonin 5-HT2 receptor antagonists altanserin; tropanserin; adatanserin -antel Anthelmintics (undefined group) carbantel -antrone Antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine Antineoplastics (arabinofuranosyl derivatives) fazarabine; fludarabine aril-, -aril, -aril- Antiviral (arildone derivatives) pleconaril; arildone; fosarilate -arit Antirheumatics (lobenzarit type) lobenzarit; clobuzarit -arol -
(12) Patent Application Publication (10) Pub. No.: US 2004/0019025A1 Gavin (43) Pub
US 20040019025A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0019025A1 Gavin (43) Pub. Date: Jan. 29, 2004 (54) MEDICAL COMPOSITIONS COMPRISING (30) Foreign Application Priority Data (R,R)-FORMOTEROLAND ROFLEPONIDE Apr. 18, 2000 (GB).......................................... OOO96O73 (76) Inventor: Brian Charles Gavin, Rathfarnfam (IE) Publication Classification Correspondence Address: DAVIDJ LEVY, CORPORATE (51) Int. Cl." ............................ A61L 9/04; A61K 31/58; INTELLECTUAL PROPERTY A61K 31/4745 GLAXOSMITHKLINE (52) U.S. Cl. ............................. 514/171; 424/45; 514/291 FIVE MOORE DR., PO BOX 13398 RESEARCH TRIANGLE PARK, NC 27709-3398 (US) (57) ABSTRACT (21) Appl. No.: 10/257,702 The present invention is concerned with pharmaceutical formulations comprising a combination of (R,R)-formoterol (22) PCT Filed: Apr. 11, 2001 and rofileponide and the use of Such formulations in medi cine, particularly in the prophylaxis and treatment of respi (86) PCT No.: PCT/GB01/01629 ratory diseases. US 2004/0019025 A1 Jan. 29, 2004 MEDICAL COMPOSITIONS COMPRISING 0010 AS would be appreciated by the skilled person, (R,R)-FORMOTEROLAND ROFLEPONIDE rofileponide contains Several asymmetric centres. The 0001. The present invention is concerned with combina present invention includes each isomer of rofileponide, par tions of (R,R)-formoterol and rofleponide, particularly com ticularly the (22R) and (22S) isomers, either in substantially positions containing a combination of (R,R)-formoterol and pure form or admixed in any proportions. The isomers of rofileponide and the use of Such compositions in medicine, rofileponide have been described previously in WO particularly in the prophylaxis and treatment of respiratory 92/13872. diseases. 0011. By the term “physiologically functional derivative” 0002 Formoterol, i.e. -
Providing for Duty-Free Treatment for Specified Pharmaceutical Active
13 . 3 . 97 I EN I Official Journal of the European Communities No L 71 / 1 I (Acts whose publication is obligatory) COUNCIL REGULATION (EC) No 467/97 of 3 March 1997 providing for duty-free treatment for specified pharmaceutical active ingredients bearing an 'international non-proprietary name' (INN) from the World Health Organization and specified products used for the manufacture of finished pharmaceuticals and withdrawing duty-free treatment as pharmaceutical products from certain INNs whose predominant use is not pharmaceutical THE COUNCIL OF THE EUROPEAN UNION , whereas in the context of the review it was concluded that it was appropriate to rectify the situation with regard Having regard to the Treaty establishing the European to certain INNs whose use was predominantly non Community, and in particular Article 113 thereof, pharmaceutical and which had been inadvertently included among those INNs already receiving duty-free treatment, Having regard to the proposal from the Commission , Whereas, in the course of the Uruguay Round negotia HAS ADOPTED THIS REGULATION : tions the Community and a number of countries discussed duty-free treatment of pharmaceutical products ; Article 1 Whereas the participants in those discussions concluded that in addition to products falling within the Harm From 1 April 1997 the Community shall also accord onized System (HS) Chapter 30 and HS headings 2936 , duty-free treatment for the INNs listed in Annex I as well 2937, 2939 and 2941 , duty-free treatment should be given as the salts, esters and hydrates of such products . to designated pharmaceutical active ingredients bearing an 'international non-proprietary name' (INN) from the Article 2 World Health Organization as well as specified salts , esters and hydrates of such INNs, and also to designated From 1 April 1997 the Community shall also grant duty products used for the production and manufacture of free treatment for the products used in the production finished products ; and manufacture of pharmaceutical products listed in Annex II . -
BMJ Open Is Committed to Open Peer Review. As Part of This Commitment We Make the Peer Review History of Every Article We Publish Publicly Available
BMJ Open: first published as 10.1136/bmjopen-2018-027935 on 5 May 2019. Downloaded from BMJ Open is committed to open peer review. As part of this commitment we make the peer review history of every article we publish publicly available. When an article is published we post the peer reviewers’ comments and the authors’ responses online. We also post the versions of the paper that were used during peer review. These are the versions that the peer review comments apply to. The versions of the paper that follow are the versions that were submitted during the peer review process. They are not the versions of record or the final published versions. They should not be cited or distributed as the published version of this manuscript. BMJ Open is an open access journal and the full, final, typeset and author-corrected version of record of the manuscript is available on our site with no access controls, subscription charges or pay-per-view fees (http://bmjopen.bmj.com). If you have any questions on BMJ Open’s open peer review process please email [email protected] http://bmjopen.bmj.com/ on September 26, 2021 by guest. Protected copyright. BMJ Open BMJ Open: first published as 10.1136/bmjopen-2018-027935 on 5 May 2019. Downloaded from Treatment of stable chronic obstructive pulmonary disease: a protocol for a systematic review and evidence map Journal: BMJ Open ManuscriptFor ID peerbmjopen-2018-027935 review only Article Type: Protocol Date Submitted by the 15-Nov-2018 Author: Complete List of Authors: Dobler, Claudia; Mayo Clinic, Evidence-Based Practice Center, Robert D. -
(12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr
US008158152B2 (12) United States Patent (10) Patent No.: US 8,158,152 B2 Palepu (45) Date of Patent: Apr. 17, 2012 (54) LYOPHILIZATION PROCESS AND 6,884,422 B1 4/2005 Liu et al. PRODUCTS OBTANED THEREBY 6,900, 184 B2 5/2005 Cohen et al. 2002fOO 10357 A1 1/2002 Stogniew etal. 2002/009 1270 A1 7, 2002 Wu et al. (75) Inventor: Nageswara R. Palepu. Mill Creek, WA 2002/0143038 A1 10/2002 Bandyopadhyay et al. (US) 2002fO155097 A1 10, 2002 Te 2003, OO68416 A1 4/2003 Burgess et al. 2003/0077321 A1 4/2003 Kiel et al. (73) Assignee: SciDose LLC, Amherst, MA (US) 2003, OO82236 A1 5/2003 Mathiowitz et al. 2003/0096378 A1 5/2003 Qiu et al. (*) Notice: Subject to any disclaimer, the term of this 2003/OO96797 A1 5/2003 Stogniew et al. patent is extended or adjusted under 35 2003.01.1331.6 A1 6/2003 Kaisheva et al. U.S.C. 154(b) by 1560 days. 2003. O191157 A1 10, 2003 Doen 2003/0202978 A1 10, 2003 Maa et al. 2003/0211042 A1 11/2003 Evans (21) Appl. No.: 11/282,507 2003/0229027 A1 12/2003 Eissens et al. 2004.0005351 A1 1/2004 Kwon (22) Filed: Nov. 18, 2005 2004/0042971 A1 3/2004 Truong-Le et al. 2004/0042972 A1 3/2004 Truong-Le et al. (65) Prior Publication Data 2004.0043042 A1 3/2004 Johnson et al. 2004/OO57927 A1 3/2004 Warne et al. US 2007/O116729 A1 May 24, 2007 2004, OO63792 A1 4/2004 Khera et al. -
PHARMACEUTICAL APPENDIX to the HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2008) (Rev
Harmonized Tariff Schedule of the United States (2008) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2008) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM GADOCOLETICUM 280776-87-6 ABAFUNGIN 129639-79-8 ACIDUM LIDADRONICUM 63132-38-7 ABAMECTIN 65195-55-3 ACIDUM SALCAPROZICUM 183990-46-7 ABANOQUIL 90402-40-7 ACIDUM SALCLOBUZICUM 387825-03-8 ABAPERIDONUM 183849-43-6 ACIFRAN 72420-38-3 ABARELIX 183552-38-7 ACIPIMOX 51037-30-0 ABATACEPTUM 332348-12-6 ACITAZANOLAST 114607-46-4 ABCIXIMAB 143653-53-6 ACITEMATE 101197-99-3 ABECARNIL 111841-85-1 ACITRETIN 55079-83-9 ABETIMUSUM 167362-48-3 ACIVICIN 42228-92-2 ABIRATERONE 154229-19-3 ACLANTATE 39633-62-0 ABITESARTAN 137882-98-5 ACLARUBICIN 57576-44-0 ABLUKAST 96566-25-5 ACLATONIUM NAPADISILATE 55077-30-0 ABRINEURINUM 178535-93-8 ACODAZOLE 79152-85-5 ABUNIDAZOLE 91017-58-2 ACOLBIFENUM 182167-02-8 ACADESINE 2627-69-2 ACONIAZIDE 13410-86-1 ACAMPROSATE -
WO 2007/061529 Al
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date (10) International Publication Number 31 May 2007 (31.05.2007) PCT WO 2007/061529 Al (51) International Patent Classification: GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, A61K 9/14 (2006.01) KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV,LY,MA, MD, MG, MK, MN, MW, MX, MY, MZ, (21) International Application Number: NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, PCT/US2006/040197 SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW (22) International Filing Date: 13 October 2006 (13.10.2006) (84) Designated States (unless otherwise indicated, for every (25) Filing Language: English kind of regional protection available): ARIPO (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, (26) Publication Language: English ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), European (AT,BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV,MC, NL, PL, PT, (30) Priority Data: RO, SE, SI, SK, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, 11/282,507 18 November 2005 (18.1 1.2005) US GN, GQ, GW, ML, MR, NE, SN, TD, TG). (71) Applicant (for all designated States except US): SCI- Declarations under Rule 4.17: DOSE PHARMA INC.