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(12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe Et Al
US 2011 01 05536A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe et al. (43) Pub. Date: May 5, 2011 (54) DOSING REGIMENASSOCATED WITH Publication Classification LONG-ACTING INUECTABLE PALIPERDONE ESTERS (51) Int. Cl. A 6LX 3/59 (2006.01) (76) Inventors: Peter H. Lewyn-Briscoe, A6IP 25/18 (2006.01) Newtown, PA (US); Cristiana Gassmann-Mayer, Pennington, NJ (US); Srihari Gopal, Belle Meade, (52) U.S. Cl. ................................................... S14/259.41 NJ (US); David W. Hough, Wallingford, PA (US); Bart M.M. Remmerie, Gent (BE); Mahesh N. (57) ABSTRACT Samtani, Flemington, NJ (US) The present application provides a method for treating (21) Appl. No.: 12/916,910 patients in need of psychiatric treatment, wherein said patient (22) Filed: Nov. 1, 2010 misses a stabilized dose of a monthly maintenance regimen of paliperidone palmitate. The present application also provides Related U.S. Application Data a method for treating psychiatric patients in need of a Switch (60) Provisional application No. 61/256,696, filed on Oct. ing treatment to paliperidone palmitate in a Sustained release 30, 2009. formulation. Patent Application Publication May 5, 2011 Sheet 1 of 6 US 2011/O105536 A1 FIG. 1 First-Order PrOCeSS Cp V CL Central (2) Zero-Order PrOCeSS Patent Application Publication May 5, 2011 Sheet 2 of 6 US 2011/O105536 A1 FIG. 2 25mgeq 50mgeq m-100mde::::: Missed doSe On WK 4. Patient returns On WK5 Missed doSe On WK 4. Patient returns On WK 6 -8-4 O 4 8 12 16 2024 -8-4 O 4 8 12 1620 24 Missed doSe On WK 4. -
Known Active Compounds Used in This Article
Known active compounds used in this article As COX-2 active compounds, 12 inhibitors and 2 natural ligands were selected. The two natural ligands were arachidonic acid and prostaglandin H2. The 12 inhibitors were diclofenac, etodolac, suprofen, diflunisal, piroxicam, sulindac, indomethacin, ketoprofen, naproxen, nimesulide, rofecoxib, and 1-phenylsulfonamide-3-trifluoromethyl-5-parabromophenylpyrazole. The names of the thermolysin inhibitors used in the present study are as follows, with the PDB code in parentheses representing the complex structure from which the compound originated: l-benzylsuccinate (1hyt), phenylalanine phosphinic acid - deamino-methyl-phenylalanine (1os0), (6-methyl-3,4-dihydro-2H-chromen-2-Yl) methylphosphonate (1pe5), 2-(4-methylphenoxy) ethylphosphonate - 3-methylbutan-1-amine (1pe7), 2-ethoxyethylphosphonate - 3-methylbutan-1-amine (1pe8), (2-sulfanyl-3-phenylpropanoyl)-Phe-Tyr (1qf0), [2(R,S)-2-sulfanylheptanoyl]-Phe-Ala (1qf1), [(2S)-2-sulfanyl-3-phenylpropanoyl]-Gly-(5-phenylproline) (1qf2), n-(1-(2(R, S)-carboxy-4-phenylbutyl) cyclopentylcarbonyl)- (S)-tryptophan (1thl), (R)-retrothiorphan (1z9g), (S)-thiorphan (1zdp), hydroxamic acid (4tln), phenylalanine phosphinic acid (4tmn), Honh-benzylmalonyl-L-alanylglycine-P-nitroanilide (5tln), 1 Cbz-GlyP-Leu-Leu (ZgPLl) (5tmn), Cbz-GlyP-(O)-Leu-Leu (ZgP(O)Ll) (6tmn), CH2CO(N-OH)Leu-OCH3 (7tln), benzyloxycarbonyl-D-Ala (1kto), benzyloxycarbonyl-L-Ala (1kl6), benzyloxycarbonyl-D-Thr (1kro), benzyloxycarbonyl-L-Thr (1kj0), benzyloxycarbonyl-D-Asp (1ks7), benzyloxycarbonyl-L-Asp -
(12) United States Patent (10) Patent No.: US 8,138,169 B2 Oronsky Et Al
USOO8138169B2 (12) United States Patent (10) Patent No.: US 8,138,169 B2 Oronsky et al. (45) Date of Patent: Mar. 20, 2012 (54) COMBINATION THERAPY FOR BIPOLAR 6,863,901 B2 3/2005 Hirsh et al. 7,201.920 B2 4/2007 Kumar et al. DSORDER 2007/0213394 A1 9/2007 Beguin et al. (75) Inventors: Bryan T. Oronsky, Los Altos Hills, CA FOREIGN PATENT DOCUMENTS (US); Neil C. Oronsky, Los Altos Hills, WO WO-200806691.6 A1 6, 2008 CA (US) OTHER PUBLICATIONS (73) Assignee: ComgenRx, Inc., Mountain View, CA Boothby et al. Buprenorphine for the treatment of opioid depen (US) dence. American Journal of Health-System Pharamcy, 2007, 64 (3), pp. 266-272, abstract.* (*) Notice: Subject to any disclaimer, the term of this Brown, et al., “Naltrexone in Patients with Bipolar Disorder and patent is extended or adjusted under 35 Alcohol Dependence.” Depression and Anxiety, 2006, vol. 23, No. 8, pp. 492-495. U.S.C. 154(b) by 424 days. Carlezon, et al., “Kappa-Opioid Ligands in the Study and Treatment of Mood Disorders.” Pharmacology and Therapeutics, (21) Appl. No.: 12/422,156 XP002548302, Sep. 2009, vol. 123, No. 3, pp. 334-343. International Search Report and Written Opinion mailed on Jan. 25. (22) Filed: Apr. 10, 2009 2010, for PCT Application No. PCT/US2009/040272, 17 pages. Kamin, et al., “Extrapyramidal Side Effects in the Psychiatric Emer (65) Prior Publication Data gency Service.” Psychiatric Service, Mar. 2000, vol. 51, No. 3, pp. US 2009/0311347 A1 Dec. 17, 2009 287-289. Levin, et al., "Bipolar Disorder and Substance abuse.” Biological Psychiatry, XP004649079, vol. -
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. -
Fluphenazine Decanoate (Timing of Administration) for People with Schizophrenia (Protocol)
Cochrane Database of Systematic Reviews Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) Abbas F, Rajab T, Alsamarrai O, Alhalabi N, Zaher Addeen S, Mheish O, Aljojo A, Essali A Abbas F, Rajab T, Alsamarrai O, Alhalabi N, Zaher Addeen S, Mheish O, Aljojo A, Essali A. Fluphenazine decanoate (timing of administration) for people with schizophrenia. Cochrane Database of Systematic Reviews 2017, Issue 10. Art. No.: CD012810. DOI: 10.1002/14651858.CD012810. www.cochranelibrary.com Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) Copyright © 2017 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. TABLE OF CONTENTS HEADER....................................... 1 ABSTRACT ...................................... 1 BACKGROUND .................................... 1 Figure1. ..................................... 3 OBJECTIVES ..................................... 4 METHODS ...................................... 4 ACKNOWLEDGEMENTS . 11 REFERENCES ..................................... 11 CONTRIBUTIONSOFAUTHORS . 14 DECLARATIONSOFINTEREST . 14 SOURCESOFSUPPORT . 15 Fluphenazine decanoate (timing of administration) for people with schizophrenia (Protocol) i Copyright © 2017 The Cochrane Collaboration. Published by John Wiley & Sons, Ltd. [Intervention Protocol] Fluphenazine decanoate (timing of administration) for people with schizophrenia Fatima Abbas1, Tawfik Rajab1, Omar Alsamarrai1, Nawras Alhalabi2, Sarah Zaher Addeen1, Oubadah Mheish1, Aisha Aljojo3, -
The Organic Chemistry of Drug Synthesis
The Organic Chemistry of Drug Synthesis VOLUME 2 DANIEL LEDNICER Mead Johnson and Company Evansville, Indiana 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 • Chichester • Brisbane • Toronto Copyright © 1980 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 Sections 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: Lednicer, Daniel, 1929- The organic chemistry of drug synthesis. "A Wiley-lnterscience publication." 1. Chemistry, Medical and pharmaceutical. 2. Drugs. 3. Chemistry, Organic. I. Mitscher, Lester A., joint author. II. Title. RS421 .L423 615M 91 76-28387 ISBN 0-471-04392-3 Printed in the United States of America 10 987654321 It is our pleasure again to dedicate a book to our helpmeets: Beryle and Betty. "Has it ever occurred to you that medicinal chemists are just like compulsive gamblers: the next compound will be the real winner." R. L. Clark at the 16th National Medicinal Chemistry Symposium, June, 1978. vii Preface The reception accorded "Organic Chemistry of Drug Synthesis11 seems to us to indicate widespread interest in the organic chemistry involved in the search for new pharmaceutical agents. We are only too aware of the fact that the book deals with a limited segment of the field; the earlier volume cannot be considered either comprehensive or completely up to date. -
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 -
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. -
(12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley Et Al
USOO6197764B1 (12) United States Patent (10) Patent No.: US 6,197,764 B1 Bradley et al. (45) Date of Patent: *Mar. 6, 2001 (54) CLOZAPINE COMPOSITIONS AND USES FOREIGN PATENT DOCUMENTS THEREOF 0599 576A1 1/1994 (EP). (75) Inventors: Matthews O. Bradley, Laytonsville, 693498 1/1996 (EP). MD (US); Victor E. Shashoua, 61204136 11/1984 (JP). Belmont, MA (US); Charles S. 06-072868 3/1994 (JP). Swindell, Merion; Nigel L. Webb, 6072868 3/1994 (JP). Bryn Mawr, both of PA (US) 7082146 3/1996 (JP). 8151334 6/1996 (JP). (73) Assignee: Protarga, Inc., Conshohocken, PA (US) 9030963 2/1997 (JP). (*) Notice: Subject to any disclaimer, the term of this WO 89/07938 9/1989 (WO). patent is extended or adjusted under 35 WO 96/04001 2/1996 (WO). U.S.C. 154(b) by 0 days. WO 96/22303 7/1996 (WO). WO 96/27380 9/1996 (WO). This patent is Subject to a terminal dis WO98/17325 4/1998 (WO). claimer. OTHER PUBLICATIONS (21) Appl. No.: 08/978,541 (22) Filed: Nov. 26, 1997 Bourat, et al., "Long Chain Esters of Pipotiazine as Lon g-Acting Psychotropic Pro-Drug, Med. Chem. Proc. Int. (51) Int. Cl. .............................................. A61K 31/00 Symp. 5th (1976) pp. 105-114. (52) U.S. Cl. ........................... 514/218; 514/219; 514/220 Lohr, et al., “Neuroleptic-Induced Movement Disorders . (58) Field of Search ..................................... 514/218, 219, ..", Psychiatry, vol. 3, (1989). 514/220 Makino, et al., Chemical Abstracts, vol. 106, No. 12, (56) References Cited (90.177x) issued Mar. 23, 1987, “Pharmaceuticals Permeable to Blood-Brain Barrier'. -
Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0 -
Stembook 2018.Pdf
The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data. -
Technical Commentary
TECHNICAL COMMENTARY Metiapine Introduction When multiple copies of reviews were found and/or when findings conflict, we present the First generation ‘typical’ antipsychotics are an most recent version and the most recent older class of antipsychotic than second conclusions. generation ‘atypical’ antipsychotics. They are used primarily to treat positive symptoms Evidence was graded using the Grading of including the experiences of perceptual Recommendations Assessment, Development abnormalities (hallucinations) and fixed, false, and Evaluation (GRADE) Working Group irrational beliefs (delusions). approach where high quality evidence such as that gained from RCTs may be downgraded to First generation antipsychotics may cause side moderate or low if review and study quality is effects which can differ depending on which limited, if there is inconsistency in results, antipsychotic is being administered and on indirect comparisons, imprecise or sparse data individual differences in reaction to the drug. and high probability of reporting bias. It may Reactions may include dyskinesias such as also be downgraded if risks associated with the repetitive, involuntary, and purposeless body or intervention or other matter under review are facial movements, Parkinsonism (cogwheel high. Conversely, low quality evidence such as muscle rigidity, pill-rolling tremor and reduced that gained from observational studies may be or slowed movements), akathisia (motor upgraded if effect sizes are large, there is a restlessness, especially in the legs, and dose dependent response or if results are resembling agitation) and dystonias such as reasonably consistent, precise and direct with muscle contractions causing unusual twisting of low associated risks2. The resulting table parts of the body, most often in the neck.