Afloqualone SAFETY DATA SHEET Section 2. Hazards Identification
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Eu^^esP— || | MMMMI 1 1 1 1 1 1|||| 1 1 1||| || J European Patent Office _ _ _ _ _ © Publication number: 0 665 009 A1 Office europeen desj brevets © EUROPEAN PATENT APPLICATION published in accordance with Art. 158(3) EPC © Application number: 93922625.4 © Int. CI.6: A61 K 9/00 @ Date of filing: 13.10.93 © International application number: PCT/JP93/01469 © International publication number: WO 94/08561 (28.04.94 94/10) ® Priority: 14.10.92 JP 303085/92 Koga-gun, Shiga 520-32 (JP) @ Date of publication of application: Inventor: IZUMI, Shougo 02.08.95 Bulletin 95/31 3-94, Nlshltsutsujlgaoka Mlyamadal 1-chome Kameoka-shl, © Designated Contracting States: Kyoto 621 (JP) AT BE CH DE DK ES FR GB GR IE IT LI LU MC Inventor: OKA, Masaakl NL PT SE 18-8-207, Hoshlgaoka 1-chome Hlrakata-shl, © Applicant: NIPPON SHINYAKU COMPANY, Osaka 573 (JP) LIMITED 14, Klssholn Nlshlnosho Monguchlcho Mlnaml-ku © Representative: Vogeser, Werner, Dipl.-lng. et Kyoto-shl al Kyoto 601 (JP) Patent- und Rechtsanwalte Hansmann, Vogeser, Dr. Boecker, © Inventor: NAKAMICHI, Koulchl Alber, Dr. Strych, Lledl 13-16, Kltayamadal 1-chome, Albert-Rosshaupter-Strasse 65 Koselcho D-81369 Munchen (DE) © CRYSTALLINE CONDITION DISLOCATING METHOD. © An object of this invention is to provide a meth- od of the crystalline condition of dislocating cry- \A/ < stalline medicine simply, speedily and homoge- 4 ^ 0 at neously, and, moreover, in large quantities at once. A X. X O O x.X o °o This invention is directed to a method using an x x.x O outlet side melting zonex cooling zone. -
Marrakesh Agreement Establishing the World Trade Organization
No. 31874 Multilateral Marrakesh Agreement establishing the World Trade Organ ization (with final act, annexes and protocol). Concluded at Marrakesh on 15 April 1994 Authentic texts: English, French and Spanish. Registered by the Director-General of the World Trade Organization, acting on behalf of the Parties, on 1 June 1995. Multilat ral Accord de Marrakech instituant l©Organisation mondiale du commerce (avec acte final, annexes et protocole). Conclu Marrakech le 15 avril 1994 Textes authentiques : anglais, français et espagnol. Enregistré par le Directeur général de l'Organisation mondiale du com merce, agissant au nom des Parties, le 1er juin 1995. Vol. 1867, 1-31874 4_________United Nations — Treaty Series • Nations Unies — Recueil des Traités 1995 Table of contents Table des matières Indice [Volume 1867] FINAL ACT EMBODYING THE RESULTS OF THE URUGUAY ROUND OF MULTILATERAL TRADE NEGOTIATIONS ACTE FINAL REPRENANT LES RESULTATS DES NEGOCIATIONS COMMERCIALES MULTILATERALES DU CYCLE D©URUGUAY ACTA FINAL EN QUE SE INCORPOR N LOS RESULTADOS DE LA RONDA URUGUAY DE NEGOCIACIONES COMERCIALES MULTILATERALES SIGNATURES - SIGNATURES - FIRMAS MINISTERIAL DECISIONS, DECLARATIONS AND UNDERSTANDING DECISIONS, DECLARATIONS ET MEMORANDUM D©ACCORD MINISTERIELS DECISIONES, DECLARACIONES Y ENTEND MIENTO MINISTERIALES MARRAKESH AGREEMENT ESTABLISHING THE WORLD TRADE ORGANIZATION ACCORD DE MARRAKECH INSTITUANT L©ORGANISATION MONDIALE DU COMMERCE ACUERDO DE MARRAKECH POR EL QUE SE ESTABLECE LA ORGANIZACI N MUND1AL DEL COMERCIO ANNEX 1 ANNEXE 1 ANEXO 1 ANNEX -
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Harmonized Tariff Schedule of the United States (2009) (Rev. 1) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2009) (Rev. 1) 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 ACEXAMIC ACID 57-08-9 ABAFUNGIN 129639-79-8 ACICLOVIR 59277-89-3 ABAMECTIN 65195-55-3 ACIFRAN 72420-38-3 ABANOQUIL 90402-40-7 ACIPIMOX 51037-30-0 ABAPERIDONE 183849-43-6 ACITAZANOLAST 114607-46-4 ABARELIX 183552-38-7 ACITEMATE 101197-99-3 ABATACEPT 332348-12-6 ACITRETIN 55079-83-9 ABCIXIMAB 143653-53-6 ACIVICIN 42228-92-2 ABECARNIL 111841-85-1 ACLANTATE 39633-62-0 ABETIMUS 167362-48-3 ACLARUBICIN 57576-44-0 ABIRATERONE 154229-19-3 ACLATONIUM NAPADISILATE 55077-30-0 ABITESARTAN 137882-98-5 ACODAZOLE 79152-85-5 ABLUKAST 96566-25-5 ACOLBIFENE 182167-02-8 ABRINEURIN 178535-93-8 ACONIAZIDE 13410-86-1 ABUNIDAZOLE 91017-58-2 ACOTIAMIDE 185106-16-5 ACADESINE 2627-69-2 ACOXATRINE 748-44-7 ACAMPROSATE 77337-76-9 ACREOZAST 123548-56-1 ACAPRAZINE 55485-20-6 -
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 -
GABA Receptor Gamma-Aminobutyric Acid Receptor; Γ-Aminobutyric Acid Receptor
GABA Receptor Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties. www.MedChemExpress.com 1 GABA Receptor Agonists, Antagonists, Inhibitors, Activators & Modulators (+)-Bicuculline (+)-Kavain (d-Bicuculline) Cat. No.: HY-N0219 Cat. No.: HY-B1671 (+)-Bicuculline is a light-sensitive competitive (+)-Kavain, a main kavalactone extracted from Piper antagonist of GABA-A receptor. methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Purity: 99.97% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg (-)-Bicuculline methobromide (-)-Bicuculline methochloride (l-Bicuculline methobromide) Cat. No.: HY-100783 (l-Bicuculline methochloride) Cat. No.: HY-100783A (-)-Bicuculline methobromide (l-Bicuculline (-)-Bicuculline methochloride (l-Bicuculline methobromide) is a potent GABAA receptor methochloride) is a potent GABAA receptor antagonist. -
Supplement Ii to the Japanese Pharmacopoeia Seventeenth Edition
SUPPLEMENT II TO THE JAPANESE PHARMACOPOEIA SEVENTEENTH EDITION O‹cial from June 28, 2019 English Version THE MINISTRY OF HEALTH, LABOUR AND WELFARE Notice: This English Version of the Japanese Pharmacopoeia is published for the convenience of users unfamiliar with the Japanese language. When and if any discrepancy arises between the Japanese original and its English translation, the former is authentic. Printed in Japan The Ministry of Health, Labour and Welfare Ministerial Notification No. 49 Pursuant to Paragraph 1, Article 41 of Act on Securing Quality, Efficacy and Safety of Products Including Pharmaceuticals and Medical Devices (Act No. 145, 1960), this notification stated that a part of the Japanese Pharmacopoeia was revised as follows*. NEMOTO Takumi The Minister of Health, Labour and Welfare June 28, 2019 A part of the Japanese Pharmacopoeia (Ministerial Notification No. 64, 2016) was revised as follows*. (The text referred to by the term ``as follows'' are omitted here. All of the revised Japanese Pharmacopoeia in accordance with this notification (hereinafter referred to as ``new Pharmacopoeia'' in Supplement 2) are made available for public exhibition at the Pharmaceutical Evaluation Division, Pharmaceutical Safety and Environmen- tal Health Bureau, Ministry of Health, Labour and Welfare, at each Regional Bureau of Health and Welfare, and at each Prefectural Office in Japan). Supplementary Provisions (Effective Date) Article 1 This Notification is applied from June 28, 2019. (Transitional measures) Article 2 In the case of drugs which are listed in the Japanese Pharmacopoeia (hereinafter referred to as ``previous Pharmacopoeia'') [limited to those listed in new Pharmacopoeia] and drugs which have been approved as of June 28, 2019 as prescribed under Paragraph 1, Article 14 of Act on Securing Quality, Efficacy and Safety of Products Including Pharmaceuticals and Medical Devices [including drugs the Minister of Health, Labour and Welfare specifies (the Ministry of Health and Welfare Ministerial Notification No. -
Design, Synthesis, Molecular Docking and Anticonvulsant Evaluation of Novel 6-Iodo-2-Phenyl- 3-Substituted-Quinazolin-4(3H)-Ones
Bulletin of Faculty of Pharmacy, Cairo University (2015) 53, 101–116 HOSTED BY Cairo University Bulletin of Faculty of Pharmacy, Cairo University www.elsevier.com/locate/bfopcu www.sciencedirect.com ORIGINAL ARTICLE Design, synthesis, molecular docking and anticonvulsant evaluation of novel 6-iodo-2-phenyl- 3-substituted-quinazolin-4(3H)-ones Mohamed-Kamal Ibrahim, Khaled El-Adl *, Ahmed A. Al-Karmalawy Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt Received 20 July 2014; accepted 11 May 2015 Available online 28 May 2015 KEYWORDS Abstract A new series of 6-iodo-2-phenyl-3-substituted-quinazolin-4(3H)-one (5–12a–b) derivatives Quinazolin-4(3H)-ones; were synthesized, evaluated for their anticonvulsant activity against pentylenetetrazole (PTZ)- 6-Iodoquinazoline induced seizures and maximal electroshock test and compared with the reference drugs phenobar- derivatives; bital sodium and methaqualone. The neurotoxicity was assessed using rotarod test. The molecular Anticonvulsant agents docking was performed for all the synthesized compounds to assess their binding affinities to GABA-A receptor in order to rationalize their anticonvulsant activities in a qualitative way. The data obtained from the molecular modeling were correlated with those obtained from the biological screening. Compounds 9a, 9b, 12a and 7a showed the highest anticonvulsant activities of this series with relatively low neurotoxicity and low toxicity in the median lethal dose test when compared with the reference drugs. The obtained results proved that the most active compounds could be a useful model for future design, adaptation and investigation to construct more active analogs. ª 2015 Production and hosting by Elsevier B.V. -
Infrared Reference Spectra
INFRARED REFERENCE SPECTRA The infrared reference spectra presented here were obtained by the use of Fourier-trans- form infrared spectrophotometers under the conditions specified in the individual mono- graphs. The horizontal axis indicates the wave numbers (cm－1) and the vertical axis indicates the transmittance (z). A spectrum of polystyrene obtained in the same manner is also presented for reference. Polystyrene JP XVI Infrared Reference Spectra 1775 Acebutolol Hydrochloride Acemetacin Acetaminophen 1776 Infrared Reference Spectra JP XVI Acetohexamide Acetylcholine Chloride for Injection Acetylcysteine JP XVI Infrared Reference Spectra 1777 Aciclovir Aclarubicin Hydrochloride Acrinol Hydrate 1778 Infrared Reference Spectra JP XVI Adrenaline Afloqualone Alacepril JP XVI Infrared Reference Spectra 1779 L-Alanine Alendronate Sodium Hydrate Allopurinol 1780 Infrared Reference Spectra JP XVI Alminoprofen Alprenolol Hydrochloride Alprostadil JP XVI Infrared Reference Spectra 1781 Amantadine Hydrochloride Ambenonium Chloride Amidotrizoic Acid 1782 Infrared Reference Spectra JP XVI Amikacin Sulfate Amiodarone Hydrochloride Amlexanox JP XVI Infrared Reference Spectra 1783 Amlodipine Besilate Amosulalol Hydrochloride Amoxapine 1784 Infrared Reference Spectra JP XVI Amoxicillin Hydrate Anhydrous Ampicillin Ampicillin Hydrate JP XVI Infrared Reference Spectra 1785 Ampicillin Sodium Amyl Nitrite Aprindine Hydrochloride 1786 Infrared Reference Spectra JP XVI Argatroban Hydrate L-Arginine L-Arginine Hydrochloride JP XVI Infrared Reference Spectra -
Accidental Afloqualone Intoxication in Two Dogs
NOTE Internal Medicine Accidental afloqualone intoxication in two dogs Jin-Ok AHN1), Won-Joung JAUNG1), Sang-Heum WON1), Min-Ok RYU1), Woo-Jin SONG1), Kee-Ok JEON1), Jin-Young CHUNG2) and Hwa-Young YOUN1)* 1)Department of Veterinary Internal Medicine and Institute of Veterinary Science, College of Veterinary Medicine, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Republic of Korea 2)Department of Veterinary Internal Medicine and Geriatrics, College of Veterinary Medicine, Kangwon National University, Chuncheon 200-701, Republic of Korea J. Vet. Med. Sci. 80(1): 152–155, 2018 ABSTRACT. Two dogs presented to the emergency service after accidental ingestion of afloqualone tablets, a muscle relaxant used for back pain in humans. Toxic effects of the drug in doi: 10.1292/jvms.17-0305 these dogs included vomiting, respiratory depression, seizures, ataxia, bradycardia, and hematuria. Treatment consisted of fluid diuresis, furosemide, and propofol. Flumazenil, a gamma-amino butyric acid antagonist, was administered intravenously; however, it was not effective in stopping Received: 5 June 2017 the seizures in these dogs. Both dogs recovered with supportive treatment. To the authors’ Accepted: 31 October 2017 knowledge, this is the first documented report of afloqualone intoxication in dogs. Published online in J-STAGE: 14 November 2017 KEY WORDS: afloqualone, canine, flumazenil, intoxication, seizure Afloqualone [6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone] is a quinazolinone family gamma-amino butyric acid (GABA)ergic drug and an analogue of methaqualone that was developed in the 1970s. It has muscle-relaxant and sedative effects resulting from its agonist activity at the GABAA receptor and is commonly used clinically in humans to relieve back pain and spastic muscle disorders [14]. -
Florencio Zaragoza Dörwald Lead Optimization for Medicinal Chemists
Florencio Zaragoza Dorwald¨ Lead Optimization for Medicinal Chemists Related Titles Smith, D. A., Allerton, C., Kalgutkar, A. S., Curry, S. H., Whelpton, R. van de Waterbeemd, H., Walker, D. K. Drug Disposition and Pharmacokinetics and Metabolism Pharmacokinetics in Drug Design From Principles to Applications 2012 2011 ISBN: 978-3-527-32954-0 ISBN: 978-0-470-68446-7 Gad, S. C. (ed.) Rankovic, Z., Morphy, R. Development of Therapeutic Lead Generation Approaches Agents Handbook in Drug Discovery 2012 2010 ISBN: 978-0-471-21385-7 ISBN: 978-0-470-25761-6 Tsaioun, K., Kates, S. A. (eds.) Han, C., Davis, C. B., Wang, B. (eds.) ADMET for Medicinal Chemists Evaluation of Drug Candidates A Practical Guide for Preclinical Development 2011 Pharmacokinetics, Metabolism, ISBN: 978-0-470-48407-4 Pharmaceutics, and Toxicology 2010 ISBN: 978-0-470-04491-9 Sotriffer, C. (ed.) Virtual Screening Principles, Challenges, and Practical Faller, B., Urban, L. (eds.) Guidelines Hit and Lead Profiling 2011 Identification and Optimization ISBN: 978-3-527-32636-5 of Drug-like Molecules 2009 ISBN: 978-3-527-32331-9 Florencio Zaragoza Dorwald¨ Lead Optimization for Medicinal Chemists Pharmacokinetic Properties of Functional Groups and Organic Compounds The Author All books published by Wiley-VCH are carefully produced. Nevertheless, authors, Dr. Florencio Zaragoza D¨orwald editors, and publisher do not warrant the Lonza AG information contained in these books, Rottenstrasse 6 including this book, to be free of errors. 3930 Visp Readers are advised to keep in mind that Switzerland statements, data, illustrations, procedural details or other items may inadvertently be Cover illustration: inaccurate. -
The Effect of Different Doses of Oral Tizanidine, on the Minimum Alveolar Concentration of Isoflurane and Stress Response
Alexandria Journal of Anaesthesia and Intensive Care 67 The Effect of Different Doses of Oral Tizanidine, on the Minimum Alveolar Concentration of Isoflurane and Stress Response. Montaser S. Abo Elkassem,MD Lecturer of Anesthesia, Faculty of Medicine, Menoufiya University. ABSTRACT α2-ADRENERGIC receptor agonists bind to peripheral and central nervous system sites modulating autonomic nervous system function. These effects may explain the clinically observed attenuation of sympathetically mediated responses to perioperative stress. They also have an antinociceptive effect in animals. In humans premedicated with oral tizanidine an α2-adrenoceptor agonist, attenuated the increase in blood pressure associated with laryngoscopy and intubation and the amount of midazolam required for loss of consciousness was significantly reduced. We speculated that the oral administration of tizanidine might reduce the minimum alveolar anesthetic concentration (MAC) of isoflurane. Eighty ASA physical status I–II patients, aged 24–56 yr, were randomly allocated into 4 groups ( 20 for each): a Control group and a 2mg Tizanidine group, 4mg Tizanidine group, 10mg Tizanidine group. As premedication, the Control group received a placebo, and the Tizanidine groups received oral tizanidine 70 min. before surgical skin incision. Anesthesia was induced in all patients by propofol 2-2.5 mg/kg intravenously mixed with lidocaine 0.3 mg/kg, given over 30s. until loss of eyelid reflex (determined every 15 s). After loss of consciousness, appropriate size of laryngeal mask was introduced by Brain method. Then administration of isoflurane was begun; the patients were spontaneously ventilated using a non—rebreathing system. MAC was determined by a technique adapted from the conventional up-down method for quantal responses. -
Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes
Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 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. Product CAS No. Product CAS No. ABACAVIR 136470-78-5 ACEXAMIC ACID 57-08-9 ABAFUNGIN 129639-79-8 ACICLOVIR 59277-89-3 ABAMECTIN 65195-55-3 ACIFRAN 72420-38-3 ABANOQUIL 90402-40-7 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABCIXIMAB 143653-53-6 ACITEMATE 101197-99-3 ABECARNIL 111841-85-1 ACITRETIN 55079-83-9 ABIRATERONE 154229-19-3 ACIVICIN 42228-92-2 ABITESARTAN 137882-98-5 ACLANTATE 39633-62-0 ABLUKAST 96566-25-5 ACLARUBICIN 57576-44-0 ABUNIDAZOLE 91017-58-2 ACLATONIUM NAPADISILATE 55077-30-0 ACADESINE 2627-69-2 ACODAZOLE 79152-85-5 ACAMPROSATE 77337-76-9 ACONIAZIDE 13410-86-1 ACAPRAZINE 55485-20-6 ACOXATRINE 748-44-7 ACARBOSE 56180-94-0 ACREOZAST 123548-56-1 ACEBROCHOL 514-50-1 ACRIDOREX 47487-22-9 ACEBURIC ACID 26976-72-7