Computational Drug Repurposing Algorithm Targeting TRPA1 Calcium Channel As a Potential Therapeutic Solution for Multiple Sclerosis
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The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances" WHO/EMP/RHT/TSN/2018.1
INN Working Document 19.450 04/02/2019 Addendum1 to "The use of stems in the selection of International Nonproprietary names (INN) for pharmaceutical substances" WHO/EMP/RHT/TSN/2018.1 Programme on International Nonproprietary Names (INN) Technologies Standards and Norms (TSN) Regulation of Medicines and other health technologies (RHT) World Health Organization, Geneva © World Health Organization 2019 - All rights reserved. The contents of this document may not be reviewed, abstracted, quoted, referenced, reproduced, transmitted, distributed, translated or adapted, in part or in whole, in any form or by any means, without explicit prior authorization of the WHO INN Programme. This document contains the collective views of the INN Expert Group and does not necessarily represent the decisions or the stated policy of the World Health Organization. Addendum1 to "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances" - WHO/EMP/RHT/TSN/2018.1 1 This addendum is a cumulative list of all new stems selected by the INN Expert Group since the publication of "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances" 2018. ------------------------------------------------------------------------------------------------------------ -calcet/-calcet- calcium-sensing receptors (CaSR) agonists cinacalcet (88), etelcalcetide (112), evocalcet (113), tecalcet (87), upacicalcet (118) ------------------------------------------------------------------------------------------------------------ -
Classification Decisions Taken by the Harmonized System Committee from the 47Th to 60Th Sessions (2011
CLASSIFICATION DECISIONS TAKEN BY THE HARMONIZED SYSTEM COMMITTEE FROM THE 47TH TO 60TH SESSIONS (2011 - 2018) WORLD CUSTOMS ORGANIZATION Rue du Marché 30 B-1210 Brussels Belgium November 2011 Copyright © 2011 World Customs Organization. All rights reserved. Requests and inquiries concerning translation, reproduction and adaptation rights should be addressed to [email protected]. D/2011/0448/25 The following list contains the classification decisions (other than those subject to a reservation) taken by the Harmonized System Committee ( 47th Session – March 2011) on specific products, together with their related Harmonized System code numbers and, in certain cases, the classification rationale. Advice Parties seeking to import or export merchandise covered by a decision are advised to verify the implementation of the decision by the importing or exporting country, as the case may be. HS codes Classification No Product description Classification considered rationale 1. Preparation, in the form of a powder, consisting of 92 % sugar, 6 % 2106.90 GRIs 1 and 6 black currant powder, anticaking agent, citric acid and black currant flavouring, put up for retail sale in 32-gram sachets, intended to be consumed as a beverage after mixing with hot water. 2. Vanutide cridificar (INN List 100). 3002.20 3. Certain INN products. Chapters 28, 29 (See “INN List 101” at the end of this publication.) and 30 4. Certain INN products. Chapters 13, 29 (See “INN List 102” at the end of this publication.) and 30 5. Certain INN products. Chapters 28, 29, (See “INN List 103” at the end of this publication.) 30, 35 and 39 6. Re-classification of INN products. -
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 -
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. -
Adverse Drug Reaction News Published by the Health Products Regulation Group, HSA and the HSA Pharmacovigilance Advisory Committee
ISSN: 0219 - 2152 April 2011 Vol.13 No.1 Adverse Drug Reaction News Published by the Health Products Regulation Group, HSA and the HSA Pharmacovigilance Advisory Committee Consumer health product recalls Voluntary recalls of mouth rinses and cleansing wipes Over the recent months, the following four products were voluntarily recalled by their Reports of B. cepacia-contaminated distributors following detection of Burkholderia cepacia (B. cepacia) in certain batches of products overseas1-3 the products: B. cepacia is known to contaminate health ■ “Oral Guard Antiseptic-Antiplaque Mouthwash” by Medimex Singapore products. There have been reported cases ■ “Trihexid Chlorhexidine 0.2% Mouth Rinse” by Trident Pharm Pte Ltd of B. cepacia detected in a variety of ■ “Pearlie White Fluorinze Fluoride Mouth Rinse” by Corlison Pte Ltd products in other countries such as the United States (US), Australia and Canada. ■ “Care Wipes” by Tai Sun Paper Products Pte Ltd (Singapore) The types of products affected include mouthwashes, mouth gels, nasal sprays and hand sanitisers. A recent case in November 2009 involved the recall of three lots of Vicks Sinex Nasal Spray by Procter & Gamble2 in the US, Germany and the United Kingdom. The company detected B. cepacia in the product during routine quality control at its plant located in Germany. The company’s analysis showed that the problem was limited to a single batch of raw material mixture involving three lots of product sold in the US, Germany and the UK. No reports of illness were received by The consumer level recall was initiated as a precautionary measure to safeguard public the company. -
Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG . -
(12) Patent Application Publication (10) Pub. No.: US 2015/0202317 A1 Rau Et Al
US 20150202317A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0202317 A1 Rau et al. (43) Pub. Date: Jul. 23, 2015 (54) DIPEPTDE-BASED PRODRUG LINKERS Publication Classification FOR ALPHATIC AMNE-CONTAINING DRUGS (51) Int. Cl. A647/48 (2006.01) (71) Applicant: Ascendis Pharma A/S, Hellerup (DK) A638/26 (2006.01) A6M5/9 (2006.01) (72) Inventors: Harald Rau, Heidelberg (DE); Torben A 6LX3/553 (2006.01) Le?mann, Neustadt an der Weinstrasse (52) U.S. Cl. (DE) CPC ......... A61K 47/48338 (2013.01); A61 K3I/553 (2013.01); A61 K38/26 (2013.01); A61 K (21) Appl. No.: 14/674,928 47/48215 (2013.01); A61M 5/19 (2013.01) (22) Filed: Mar. 31, 2015 (57) ABSTRACT The present invention relates to a prodrug or a pharmaceuti Related U.S. Application Data cally acceptable salt thereof, comprising a drug linker conju (63) Continuation of application No. 13/574,092, filed on gate D-L, wherein D being a biologically active moiety con Oct. 15, 2012, filed as application No. PCT/EP2011/ taining an aliphatic amine group is conjugated to one or more 050821 on Jan. 21, 2011. polymeric carriers via dipeptide-containing linkers L. Such carrier-linked prodrugs achieve drug releases with therapeu (30) Foreign Application Priority Data tically useful half-lives. The invention also relates to pharma ceutical compositions comprising said prodrugs and their use Jan. 22, 2010 (EP) ................................ 10 151564.1 as medicaments. US 2015/0202317 A1 Jul. 23, 2015 DIPEPTDE-BASED PRODRUG LINKERS 0007 Alternatively, the drugs may be conjugated to a car FOR ALPHATIC AMNE-CONTAINING rier through permanent covalent bonds. -
Recent Development of Non-Peptide Gnrh Antagonists
Review Recent Development of Non-Peptide GnRH Antagonists Feng-Ling Tukun 1, Dag Erlend Olberg 1,2, Patrick J. Riss 2,3,4, Ira Haraldsen 4, Anita Kaass 5 and Jo Klaveness 1,* 1 School of Pharmacy, University of Oslo, 0316 Oslo, Norway; [email protected] (F.-L.T.); [email protected] (D.E.O.) 2 Norsk Medisinsk Syklotronsenter AS, Postboks 4950 Nydalen, 0424 Oslo, Norway; [email protected] 3 Realomics SFI, Department of Chemistry, University of Oslo, 0316 Oslo, Norway 4 Department of neuropsychiatry and psychosomatic medicine, Oslo University Hospital, 4950 Oslo, Norway; [email protected] 5 Betanien Hospital, 3722 Skien, Norway; [email protected] * Correspondence: [email protected]; Tel.: +47-9177-6204 Received: 16 November 2017; Accepted: 4 December 2017; Published: 9 December 2017 Abstract: The decapeptide gonadotropin-releasing hormone, also referred to as luteinizing hormone-releasing hormone with the sequence (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) plays an important role in regulating the reproductive system. It stimulates differential release of the gonadotropins FSH and LH from pituitary tissue. To date, treatment of hormone-dependent diseases targeting the GnRH receptor, including peptide GnRH agonist and antagonists are now available on the market. The inherited issues associate with peptide agonists and antagonists have however, led to significant interest in developing orally active, small molecule, non-peptide antagonists. In this review, we will summarize all developed small molecule GnRH antagonists along with the most recent clinical data and therapeutic applications. Keywords: GnRH receptor; non-peptide GnRH antagonist 1. -
Antiepileptic Drugs in Development Pipeline: a Recent Update
eNeurologicalSci 4 (2016) 42–51 Contents lists available at ScienceDirect eNeurologicalSci journal homepage: http://ees.elsevier.com/ensci/ Review article Antiepileptic drugs in development pipeline: A recent update Harjeet Kaur, Baldeep Kumar, Bikash Medhi ⁎ Department of Pharmacology, Postgraduate Institute of Medical Education and Research, Chandigarh 160012, India article info abstract Article history: Epilepsy is the most common neurological disorder which significantly affects the quality of life and poses a Received 16 September 2015 health as well as economic burden on society. Epilepsy affects approximately 70 million people in the world. Received in revised form 16 April 2016 The present article reviews the scientific rationale, brief pathophysiology of epilepsy and newer antiepileptic Accepted 15 June 2016 drugs which are presently under clinical development. We have searched the investigational drugs using the Available online 17 June 2016 key words ‘antiepileptic drugs,’‘epilepsy,’‘Phase I,’‘Phase II’ and ‘Phase III’ in American clinical trial registers Keywords: (clinicaltrials.gov), the relevant published articles using National Library of Medicine's PubMed database, compa- Seizures ny websites and supplemented results with a manual search of cross-references and conference abstracts. This Epilepsy review provides a brief description about the antiepileptic drugs which are targeting different mechanisms Drug development and the clinical development status of these drugs. Besides the presence of old as well as new AEDs, still there Neuroprotection is a need of new drugs or the modified version of old drugs in order to make affected people free of seizures. Clinical trial An optimistic approach should be used to translate the success of preclinical testing to clinical practice. -
First Principles and Their Application to Drug Discovery
REVIEWS Drug Discovery Today Volume 17, Numbers 1/2 January 2012 The utilization of the kinetic and thermodynamic signatures of preclinical leads is proving pivotal in their triage and rational optimization towards clinical candidates with maximal in vivo efficacy devoid of adverse events. Reviews KEYNOTE REVIEW Target–drug interactions: first principles and their application to drug discovery 1 1 Sara Nu´n˜ez studied organic Sara Nu´n˜ ez , Jennifer Venhorst and Chris G. Kruse chemistry at the University of Barcelona (Spain) and the Abbott Healthcare Products, 1381 CP Weesp, The Netherlands University of London (UK). She received her Ph.D. in 2003 from the University of Manchester (UK), and thereafter did a In this review, we begin by introducing the basic principles of kinetics postdoc in Biophysics at the and thermodynamics of target–drug binding within the context of Albert Einstein College of Medicine (USA). In 2005, she drug discovery. In addition, we present a meta-analysis of the recent joined Solvay Pharmaceuticals (now Abbott Healthcare) in The Netherlands as a postdoctoral fellow; and in 2008, she literature describing the kinetic and thermodynamic resolution of was promoted to Sr. Computational Medicinal Chemist. At Abbott, she has supported the medicinal chemistry efforts successful clinical candidates with diverse mechanisms of action. for neuroscience drug discovery programs, from target We finish by discussing the best practices in the triage and chemical discovery up to and including clinical proof of principle studies. She has supported more than 15 programs optimization towards clinical candidates with maximal in vivo internationally, and was project manager of the D2-103 Top Institute Pharma innitiative. -
WO 2011/089216 Al
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date t 28 July 2011 (28.07.2011) WO 2011/089216 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 47/48 (2006.01) C07K 1/13 (2006.01) kind of national protection available): AE, AG, AL, AM, C07K 1/1 07 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, (21) Number: International Application DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, PCT/EP201 1/050821 HN, HR, HU, ID, J , IN, IS, JP, KE, KG, KM, KN, KP, (22) International Filing Date: KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, 2 1 January 201 1 (21 .01 .201 1) ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, (25) Filing Language: English SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 1015 1465. 1 22 January 2010 (22.01 .2010) EP kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, (71) Applicant (for all designated States except US): AS- ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, CENDIS PHARMA AS [DK/DK]; Tuborg Boulevard TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 12, DK-2900 Hellerup (DK). -
High-Density Lipoproteins in Kidney Disease
International Journal of Molecular Sciences Review High-Density Lipoproteins in Kidney Disease Valentina Kon 1, Hai-Chun Yang 1,2, Loren E. Smith 3, Kasey C. Vickers 4 and MacRae F. Linton 4,5,* 1 Department of Pediatrics, Vanderbilt University Medical Center, Nashville, TN 37232, USA; [email protected] (V.K.); [email protected] (H.-C.Y.) 2 Department of Pathology, Microbiology and Immunology, Vanderbilt University Medical Center, Nashville, TN 37232, USA 3 Department of Anesthesiology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; [email protected] 4 Atherosclerosis Research Unit, Department of Medicine, Division of Cardiovascular Medicine, Vanderbilt University Medical Center, Nashville, TN 37232, USA; [email protected] 5 Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA * Correspondence: [email protected] Abstract: Decades of epidemiological studies have established the strong inverse relationship be- tween high-density lipoprotein (HDL)-cholesterol concentration and cardiovascular disease. Recent evidence suggests that HDL particle functions, including anti-inflammatory and antioxidant func- tions, and cholesterol efflux capacity may be more strongly associated with cardiovascular disease protection than HDL cholesterol concentration. These HDL functions are also relevant in non- cardiovascular diseases, including acute and chronic kidney disease. This review examines our current understanding of the kidneys’ role in HDL metabolism and homeostasis, and the effect of kidney disease on HDL composition and functionality. Additionally, the roles of HDL particles, proteins, and small RNA cargo on kidney cell function and on the development and progression of both acute and chronic kidney disease are examined. The effect of HDL protein modification Citation: Kon, V.; Yang, H.-C.; Smith, by reactive dicarbonyls, including malondialdehyde and isolevuglandin, which form adducts with L.E.; Vickers, K.C.; Linton, M.F.