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Cyclohexyl Amide Derivatives As Crf Receptor
(19) TZZ ¥_Z_T (11) EP 2 531 490 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/4155 (2006.01) A61P 25/24 (2006.01) 15.10.2014 Bulletin 2014/42 C07D 213/82 (2006.01) C07D 231/12 (2006.01) C07D 231/14 (2006.01) C07D 231/16 (2006.01) (2006.01) (2006.01) (21) Application number: 11701824.2 C07D 231/20 C07D 231/38 C07D 231/54 (2006.01) C07D 231/56 (2006.01) C07D 249/08 (2006.01) C07D 401/04 (2006.01) (22) Date of filing: 31.01.2011 C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/04 (2006.01) C07D 471/04 (2006.01) C07D 473/00 (2006.01) C07D 491/052 (2006.01) C07C 233/79 (2006.01) (86) International application number: PCT/EP2011/051293 (87) International publication number: WO 2011/095450 (11.08.2011 Gazette 2011/32) (54) CYCLOHEXYL AMIDE DERIVATIVES AS CRF RECEPTOR ANTAGONISTS CYCLOHEXYLAMIDDERIVATE ALS CRF-REZEPTORANTAGONISTEN DÉRIVÉS DE CYCLOHEXYLAMIDE À TITRE D’ANTAGONISTES DU RÉCEPTEUR CRF (84) Designated Contracting States: • COLSON, Anny-Odile AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Horsham GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO Sussex RH12 5AB (GB) PL PT RO RS SE SI SK SM TR • CULSHAW, Andrew James Horsham (30) Priority: 17.12.2010 US 424258 P Sussex RH12 5AB (GB) 02.02.2010 US 300576 P • SHARP, Thomas Horsham (43) Date of publication of application: Sussex RH12 5AB (GB) 12.12.2012 Bulletin 2012/50 (74) Representative: Woodcock-Bourne, Heather (73) Proprietor: Novartis AG Novartis Pharma AG 4056 Basel (CH) Patent Department Postfach (72) Inventors: 4002 Basel (CH) •BEATTIE,David Horsham (56) References cited: Sussex RH12 5AB (GB) WO-A1-2010/015655 • BRUCE, Ian Horsham • GILLIGAN, P. -
Cardiac Drug Therapy
Series Editor: Christopher P. Cannon ebook M. Gabriel Khan Cardiac Drug Therapy Contemporary Cardiology 8th Edition Disclaimer: This book is meant only for academic reference purpose only We acknowledge the Author and the Publisher www.pubrica.com +91-9884350006 [email protected] CONTEMPORARY CARDIOLOGY CHRISTOPHER P. C ANNON, MD SERIES EDITOR More information about this series at http://www.springer.com/series/7677 M. Gabriel Khan Cardiac Drug Therapy 8th Edition M. Gabriel Khan, MD, FRCPC, FRCP (London), FACC University of Ottawa The Ottawa Hospital Ottawa , ON , Canada ISSN 2196-8969 ISSN 2196-8977 (electronic) ISBN 978-1-61779-961-7 ISBN 978-1-61779-962-4 (eBook) DOI 10.1007/978-1-61779-962-4 Springer Totowa Heidelberg New York Dordrecht London Library of Congress Control Number: 2014952818 © Springer Science+Business Media New York 2015 This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifi cally the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfi lms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. Exempted from this legal reservation are brief excerpts in connection with reviews or scholarly analysis or material supplied specifi cally for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Duplication of this publication or parts thereof is permitted only under the provisions of the Copyright Law of the Publisher’s location, in its current version, and permission for use must always be obtained from Springer. -
Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix
United States International Trade Commission Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix USITC Publication 4208 December 2010 U.S. International Trade Commission COMMISSIONERS Deanna Tanner Okun, Chairman Irving A. Williamson, Vice Chairman Charlotte R. Lane Daniel R. Pearson Shara L. Aranoff Dean A. Pinkert Address all communications to Secretary to the Commission United States International Trade Commission Washington, DC 20436 U.S. International Trade Commission Washington, DC 20436 www.usitc.gov Modifications to the Harmonized Tariff Schedule of the United States to Implement Changes to the Pharmaceutical Appendix Publication 4208 December 2010 (This page is intentionally blank) Pursuant to the letter of request from the United States Trade Representative of December 15, 2010, set forth at the end of this publication, and pursuant to section 1207(a) of the Omnibus Trade and Competitiveness Act, the United States International Trade Commission is publishing the following modifications to the Harmonized Tariff Schedule of the United States (HTS) to implement changes to the Pharmaceutical Appendix, effective on January 1, 2011. Table 1 International Nonproprietary Name (INN) products proposed for addition to the Pharmaceutical Appendix to the Harmonized Tariff Schedule INN CAS Number Abagovomab 792921-10-9 Aclidinium Bromide 320345-99-1 Aderbasib 791828-58-5 Adipiplon 840486-93-3 Adoprazine 222551-17-9 Afimoxifene 68392-35-8 Aflibercept 862111-32-8 Agatolimod -
Efficacy of Amiodarone in the Treatment of Ventricular
EFFICACY OF AMIODARONE IN THE TREATMENT OF VENTRICULAR ARRHYTHMIAS IN PATIENTS WITH CORONARY ARTERY DISEASE IN BANGLADESH 1 2 3 1 4 5 ADHIKARY DK , SAHA SK , MAHMOOD M , SALIM A , JOARDER AI , SINGHA CK , RAHMAN 6 7 8 9 10 11 MW , AHASAN MH , KHALED MFI , BANERJEE SK , MAHBUBA F , AHMED A Abstract Background: Ventricular arrhythmias (VA) are among the most feared complications of coronary artery disease (CAD) and one of the major contributors of death in CAD patients. Antiarrhythmic drug (AAD) therapy is required for recurrent significant VA in the absence of need for further revascularization. But all AADs do not have the same efficacy against life threatening VA and supraventricular arrhythmias (SVAs). Methodology: All (50) patients admitted in the department of Cardiology, BSMMU with ventricular arrhythmias with CAD fulfilling the inclusion and exclusion criteria were included in the study. Informed written consent was taken from each patient before enrollment. Detailed history was taken and relevant physical examinations were done. Loading dose followed by maintenance dose of amiodarone was given and recorded. Relevant lab investigations were performed and recorded in predesigned semi-structured data collection sheet. Symptomatic improvement was assessed, relevant physical examination was done and lab investigations were performed at 1, 3 and 6 month follow up. After editing data analysis was carried out by using the Statistical Package for Social Science (SPSS) version 23.0 windows software. Results: The mean age was found 57.7±8.0 years with a range of 45 to 78 years. Almost two third (62.0%) patients were male and 19(38.0%) patients were female. -
Potential Cannabis Antagonists for Marijuana Intoxication
Central Journal of Pharmacology & Clinical Toxicology Bringing Excellence in Open Access Review Article *Corresponding author Matthew Kagan, M.D., Cedars-Sinai Medical Center, 8730 Alden Drive, Los Angeles, CA 90048, USA, Tel: 310- Potential Cannabis Antagonists 423-3465; Fax: 310.423.8397; Email: Matthew.Kagan@ cshs.org Submitted: 11 October 2018 for Marijuana Intoxication Accepted: 23 October 2018 William W. Ishak, Jonathan Dang, Steven Clevenger, Shaina Published: 25 October 2018 Ganjian, Samantha Cohen, and Matthew Kagan* ISSN: 2333-7079 Cedars-Sinai Medical Center, USA Copyright © 2018 Kagan et al. Abstract OPEN ACCESS Keywords Cannabis use is on the rise leading to the need to address the medical, psychosocial, • Cannabis and economic effects of cannabis intoxication. While effective agents have not yet been • Cannabinoids implemented for the treatment of acute marijuana intoxication, a number of compounds • Antagonist continue to hold promise for treatment of cannabinoid intoxication. Potential therapeutic • Marijuana agents are reviewed with advantages and side effects. Three agents appear to merit • Intoxication further inquiry; most notably Cannabidiol with some evidence of antipsychotic activity • THC and in addition Virodhamine and Tetrahydrocannabivarin with a similar mixed receptor profile. Given the results of this research, continued development of agents acting on cannabinoid receptors with and without peripheral selectivity may lead to an effective treatment for acute cannabinoid intoxication. Much work still remains to develop strategies that will interrupt and reverse the effects of acute marijuana intoxication. ABBREVIATIONS Therapeutic uses of cannabis include chronic pain, loss of appetite, spasticity, and chemotherapy-associated nausea and CBD: Cannabidiol; CBG: Cannabigerol; THCV: vomiting [8]. Recreational cannabis use is on the rise with more Tetrahydrocannabivarin; THC: Tetrahydrocannabinol states approving its use and it is viewed as no different from INTRODUCTION recreational use of alcohol or tobacco [9]. -
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 -
Synopsis Style Clinical Study Report 18-Nov-2011 SSR149744 - DRI10936 - Celivarone Version Number: 1 (Electronic 1.0)
Synopsis Style Clinical Study Report 18-Nov-2011 SSR149744 - DRI10936 - celivarone Version number: 1 (electronic 1.0) SYNOPSIS Title of the study: Double blind placebo controlled dose ranging study of the efficacy and safety of celivarone 50, 100 or 300 mg OD with amiodarone as calibrator for the prevention of ICD interventions or death (DRI10936 – ALPHEE) Investigator(s): Study centers: 151 active centers in 26 countries across Europe (Belgium, Czech Republic, Denmark, Finland, France, Germany, Hungary, Italy, Netherlands, Poland, Portugal, Slovakia, Spain, Sweden), Argentina, Australia, Canada, Chile, Israel, Japan, Mexico, Norway, Russian Federation, South Africa, Turkey, and the USA. Publications (reference): Kowey PR, Crijns HJGM, Aliot EM, Capucci A, Kulakowski P, Radzik D, et al, on behalf of the ALPHEE study Investigators. Efficacy and safety of celivarone, with amiodarone as calibrator, in patients with an implantable cardioverter- defibrillator for prevention of implantable cardioverter-defibrillator interventions or death: The ALPHEE study. Circulation, published online November 14, 2011. Study period: Date first patient enrolled: 21 September 2009 Date last patient completed: 12 May 2011 Phase of development: 2b Objectives: Primary: To assess the efficacy of celivarone for the prevention of implantable cardioverter defibrillator (ICD) interventions or death. Secondary: To assess the tolerability and safety of the different dose regimens of celivarone in the selected population. To document SSR149744 plasma levels during the study. Methodology: This was a dose-finding, multicenter, multinational, randomized, double-blind, placebo-controlled, parallel-arm study including a positive control calibrator arm. Eligible patients were randomized (2:2:2:2:1) via an interactive voice response system (IVRS) to placebo, celivarone 50 mg, celivarone 100 mg, celivarone 300 mg, or amiodarone group. -
Possible Therapeutic Doses of Cannabinoid Type 1 Receptor Antagonist Reverses Key Alterations in Fragile X Syndrome Mouse Model
G C A T T A C G G C A T genes Article Possible Therapeutic Doses of Cannabinoid Type 1 Receptor Antagonist Reverses Key Alterations in Fragile X Syndrome Mouse Model Maria Gomis-González 1, Arnau Busquets-Garcia 1,†, Carlos Matute 2,3,4, Rafael Maldonado 1,‡, Susana Mato 2,3,4,‡ and Andrés Ozaita 1,*,‡ 1 Laboratory of Neuropharmacology-NeuroPhar, Department of Experimental and Health Sciences, Program of Genetics and Neurosciences, University Pompeu Fabra, Barcelona 08003, Spain; [email protected] (M.G.-G.); [email protected] (A.B.-G.); [email protected] (R.M.) 2 Department of Neurosciences, University of the Basque Country UPV/EHU, Leioa 48940, Spain; [email protected] (C.M.); [email protected] (S.M.) 3 Achucarro Basque Center for Neuroscience, Zamudio 48170, Spain 4 Centro de Investigación Biomédica en Red de Enfermedades Neurodegenerativas (CIBERNED), Madrid 28031, Spain * Correspondence: [email protected]; Tel.: +34-93-316-0823 † Present affiliation: Endocannabinoids and Neuroadaptation Group, NeuroCentre Magendie, INSERM U1215, Bordeaux 33077, France. ‡ These authors contributed equally to this work. Academic Editor: Mark Hirst Received: 21 July 2016; Accepted: 22 August 2016; Published: 31 August 2016 Abstract: Fragile X syndrome (FXS) is the most common monogenetic cause of intellectual disability. The cognitive deficits in the mouse model for this disorder, the Fragile X Mental Retardation 1 (Fmr1) knockout (KO) mouse, have been restored by different pharmacological approaches, among those the blockade of cannabinoid type 1 (CB1) receptor. In this regard, our previous study showed that the CB1 receptor antagonist/inverse agonist rimonabant normalized a number of core features in the Fmr1 knockout mouse. -
Cannabinoid-1 Receptor Inverse Agonists: Current Understanding of Mechanism of Action and Unanswered Questions
International Journal of Obesity (2009) 33, 947–955 & 2009 Macmillan Publishers Limited All rights reserved 0307-0565/09 $32.00 www.nature.com/ijo REVIEW Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions TM Fong1 and SB Heymsfield2 1Merck Research Laboratories, Department of Metabolic Disorders, Rahway, NJ, USA and 2Merck Research Laboratories, Global Center of Scientific Affairs, Rahway, NJ, USA Rimonabant and taranabant are two extensively studied cannabinoid-1 receptor (CB1R) inverse agonists. Their effects on in vivo peripheral tissue metabolism are generally well replicated. The central nervous system site of action of taranabant or rimonabant is firmly established based on brain receptor occupancy studies. At the whole-body level, the mechanism of action of CB1R inverse agonists includes a reduction in food intake and an increase in energy expenditure. At the tissue level, fat mass reduction, liver lipid reduction and improved insulin sensitivity have been shown. These effects on tissue metabolism are readily explained by CB1R inverse agonist acting on brain CB1R and indirectly influencing the tissue metabolism through the autonomic nervous system. It has also been hypothesized that rimonabant acts directly on adipocytes, hepatocytes, pancreatic islets or skeletal muscle in addition to acting on brain CB1R, although strong support for the contribution of peripherally located CB1R to in vivo efficacy is still lacking. This review will carefully examine the published literature -
Pdf4 Complex I and the Aryl Palladium Precursor II Underwent Sequential Single Electron Abstraction from Aryl Pd(II) Complex
Design, synthesis, methodology development, and evaluation of PET imaging agents targeting cancer and CNS disorders By Gengyang Yuan B.S. in Chemical Engineering and Technology, Zhejiang University of Technology M.S. in Pharmaceutical Engineering, Zhejiang University A dissertation submitted to The Faculty of the College of Science of Northeastern University in partial fulfillment of the requirements for the degree of Doctor of Philosophy April 21, 2017 Dissertation directed by Michael P. Pollastri Associate Professor and Chair of Chemistry and Chemical Biology Co-directed by Neil Vasdev Adjunct Associate Professor of Chemsitry and Chemical Biology Associate Professor of Radiology, Massachusetts General Hospital and Harvard Medical School Dedication To my parents Zhijun and Yongmian and my wife Ran and daughter Isabella ii Acknowledgements This dissertation would not have been possible without the support, guidance and encouragement of numerous people who have helped me along the way. First and foremost, I would like to thank Northeastern University and the Department of Chemistry and Chemical Biology for supporting me to pursue my doctoral study. I would like to especially thank my current advisor Professor Michael Pollastri for helping me out when I needed it the most. I appreciate you for taking me into your group and giving me full support to finish my thesis projects. I also especially thank my co-advisor Professor Neil Vasdev for taking me into his group at Mass. General Hospital & Harvard Medical School and teaching me the PET radiochemistry and PET imaging. I could not image how I could accomplish this work without your help. I also got a lot of help from Dr. -
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. -
Cannabinoid Receptor Cannabinoid Receptor
Cannabinoid Receptor Cannabinoid Receptor Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol. www.MedChemExpress.com 1 Cannabinoid Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators (S)-MRI-1867 (±)-Ibipinabant Cat. No.: HY-141411A ((±)-SLV319; (±)-BMS-646256) Cat. No.: HY-14791A (S)-MRI-1867 is a peripherally restricted, orally (±)-Ibipinabant ((±)-SLV319) is the racemate of bioavailable dual cannabinoid CB1 receptor and SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent inducible NOS (iNOS) antagonist. (S)-MRI-1867 and selective cannabinoid-1 (CB-1) receptor ameliorates obesity-induced chronic kidney disease antagonist with an IC50 of 22 nM. (CKD). Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg 2-Arachidonoylglycerol 2-Palmitoylglycerol Cat. No.: HY-W011051 (2-Palm-Gl) Cat. No.: HY-W013788 2-Arachidonoylglycerol is a second endogenous 2-Palmitoylglycerol (2-Palm-Gl), an congener of cannabinoid ligand in the central nervous system. 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.