Clofibrate Causes an Upregulation of PPAR- Target Genes but Does Not
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(12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao Et Al
USOO9498481 B2 (12) United States Patent (10) Patent No.: US 9,498,481 B2 Rao et al. (45) Date of Patent: *Nov. 22, 2016 (54) CYCLOPROPYL MODULATORS OF P2Y12 WO WO95/26325 10, 1995 RECEPTOR WO WO99/O5142 2, 1999 WO WOOO/34283 6, 2000 WO WO O1/92262 12/2001 (71) Applicant: Apharaceuticals. Inc., La WO WO O1/922.63 12/2001 olla, CA (US) WO WO 2011/O17108 2, 2011 (72) Inventors: Tadimeti Rao, San Diego, CA (US); Chengzhi Zhang, San Diego, CA (US) OTHER PUBLICATIONS Drugs of the Future 32(10), 845-853 (2007).* (73) Assignee: Auspex Pharmaceuticals, Inc., LaJolla, Tantry et al. in Expert Opin. Invest. Drugs (2007) 16(2):225-229.* CA (US) Wallentin et al. in the New England Journal of Medicine, 361 (11), 1045-1057 (2009).* (*) Notice: Subject to any disclaimer, the term of this Husted et al. in The European Heart Journal 27, 1038-1047 (2006).* patent is extended or adjusted under 35 Auspex in www.businesswire.com/news/home/20081023005201/ U.S.C. 154(b) by Od en/Auspex-Pharmaceuticals-Announces-Positive-Results-Clinical M YW- (b) by ayS. Study (published: Oct. 23, 2008).* This patent is Subject to a terminal dis- Concert In www.concertpharma. com/news/ claimer ConcertPresentsPreclinicalResultsNAMS.htm (published: Sep. 25. 2008).* Concert2 in Expert Rev. Anti Infect. Ther. 6(6), 782 (2008).* (21) Appl. No.: 14/977,056 Springthorpe et al. in Bioorganic & Medicinal Chemistry Letters 17. 6013-6018 (2007).* (22) Filed: Dec. 21, 2015 Leis et al. in Current Organic Chemistry 2, 131-144 (1998).* Angiolillo et al., Pharmacology of emerging novel platelet inhibi (65) Prior Publication Data tors, American Heart Journal, 2008, 156(2) Supp. -
(12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn Et Al
US 2004O224012A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0224012 A1 Suvanprakorn et al. (43) Pub. Date: Nov. 11, 2004 (54) TOPICAL APPLICATION AND METHODS Related U.S. Application Data FOR ADMINISTRATION OF ACTIVE AGENTS USING LIPOSOME MACRO-BEADS (63) Continuation-in-part of application No. 10/264,205, filed on Oct. 3, 2002. (76) Inventors: Pichit Suvanprakorn, Bangkok (TH); (60) Provisional application No. 60/327,643, filed on Oct. Tanusin Ploysangam, Bangkok (TH); 5, 2001. Lerson Tanasugarn, Bangkok (TH); Suwalee Chandrkrachang, Bangkok Publication Classification (TH); Nardo Zaias, Miami Beach, FL (US) (51) Int. CI.7. A61K 9/127; A61K 9/14 (52) U.S. Cl. ............................................ 424/450; 424/489 Correspondence Address: (57) ABSTRACT Eric G. Masamori 6520 Ridgewood Drive A topical application and methods for administration of Castro Valley, CA 94.552 (US) active agents encapsulated within non-permeable macro beads to enable a wider range of delivery vehicles, to provide longer product shelf-life, to allow multiple active (21) Appl. No.: 10/864,149 agents within the composition, to allow the controlled use of the active agents, to provide protected and designable release features and to provide visual inspection for damage (22) Filed: Jun. 9, 2004 and inconsistency. US 2004/0224012 A1 Nov. 11, 2004 TOPCAL APPLICATION AND METHODS FOR 0006 Various limitations on the shelf-life and use of ADMINISTRATION OF ACTIVE AGENTS USING liposome compounds exist due to the relatively fragile LPOSOME MACRO-BEADS nature of liposomes. Major problems encountered during liposome drug Storage in vesicular Suspension are the chemi CROSS REFERENCE TO OTHER cal alterations of the lipoSome compounds, Such as phos APPLICATIONS pholipids, cholesterols, ceramides, leading to potentially toxic degradation of the products, leakage of the drug from 0001) This application claims the benefit of U.S. -
Coronary Effect of Fibrates on Proteins and Enzymes Which Hydrolyze Triacylglycerols
Acta Poloniae Pharmaceutica ñ Drug Research, Vol. 73 No. 3 pp. 579ñ588, 2016 ISSN 0001-6837 Polish Pharmaceutical Society CORONARY EFFECT OF FIBRATES ON PROTEINS AND ENZYMES WHICH HYDROLYZE TRIACYLGLYCEROLS RENATA FRANCIK 1,2*, JADWIGA KRYCZYK 3 and S£AWOMIR FRANCIK 4 1 Department of Bioorganic Chemistry, 2 Department of Food Chemistry and Nutrition, Jagiellonian University, Medical College, Faculty of Pharmacy, 9 Medyczna St., 30-688 KrakÛw, Poland 2 Institute of Health, State Higher Vocational School, 1 Staszica St., 33-300 Nowy Sπcz, Poland 3 Jagiellonian University Medical College, Department of Food Chemistry and Nutrition, 9 Medyczna St., 30-688 KrakÛw, Poland 4 Department of Mechanical Engineering and Agrophysics, University of Agriculture in Krakow, Faculty of Production Engineering and Energetics, 116 B Balicka St., 30-149, KrakÛw, Poland Abstract: Clofibric acid derivatives called fibrates, are quite commonly used lipid-lowering drugs, so it is nec- essary to know beneficial and adverse effects of these compounds on the body. The European Medicines Agencyís Committee for Medicinal Products for Human Use (CHMP) has concluded that benefits of four fibrates such as: bezafibrate, ciprofibrate, fenofibrate and gemfibrozil continue outweigh their risk in treatment of people with blood lipid disorders. According to recommendations of the CHMP fibrates should not be used as first-line drugs, except in patients with severe hypertriglyceridemia and patients who cannot use statins. In this paper, we focused on effect of clofibric acid derivatives -
PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1
Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2020) Revision 19 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. -
A Toxicogenomic Study of the Hepatocarcinogen Furan
A Toxicogenomic Study of the Hepatocarcinogen Furan by Anna Francina Webster (Jackson) A thesis submitted to the Faculty of Graduate and Postdoctoral Affairs in partial fulfillment of the requirements for the degree of Doctor of Philosophy in Biology Carleton University Ottawa, Ontario © 2015, Anna Francina Webster Abstract A major goal in human health risk assessment is the identification and management of chemicals that may cause cancer in human populations. The current gold- standard for assessing chemical carcinogenicity is the two-year rodent cancer bioassay, which is animal, time, and resource intensive. The use of toxicogenomics for chemical risk assessment was first proposed over 15 years ago because of its potential to produce toxicologically relevant data more quickly, using fewer animals, and at a lower cost than the two-year cancer bioassay. While the two-year cancer bioassay produces a detailed inventory of chemical-dependent lesions, toxicogenomics analyzes chemical-dependent changes to global gene expression. Moreover, toxicogenomics provides comprehensive mechanistic data that are not obtained using standard tests. In this thesis quantitative, predictive, and mechanistic approaches were applied to a toxicogenomic case study of the rodent hepatocarcinogen furan. Female B3C6F1 mice were exposed for three weeks to non-carcinogenic or carcinogenic doses of furan. The dose response of a variety of transcriptional endpoints produced benchmark doses (BMDs) similar to the furan- dependent cancer BMDs. Bioinformatic analysis of disease datasets showed strong similarity between global gene expression changes induced by furan and those associated with the appropriate hepatic pathologies. The molecular pathways that were enriched in the liver following furan exposure facilitated the development of a molecular mode of action (MoA) for furan-induced liver cancer. -
Addition of Peroxisome Proliferator-Activated Receptor to Guinea Pig Hepatocytes Confers Increased Responsiveness to Peroxisome
[CANCER RESEARCH 59, 4776–4780, October 1, 1999] Advances in Brief Addition of Peroxisome Proliferator-activated Receptor a to Guinea Pig Hepatocytes Confers Increased Responsiveness to Peroxisome Proliferators Neil Macdonald, Peter R. Holden, and Ruth A. Roberts1 AstraZeneca Central Toxicology Laboratory, Alderley Park, Macclesfield SK10 4TJ, United Kingdom Abstract humans are considered to be nonresponsive to the adverse effects of PPs associated with increased b-oxidation and peroxisome prolifera- The fibrate drugs, such as nafenopin and fenofibrate, show efficacy in tion (3, 7, 11, 12). In guinea pigs, there is no increased DNA synthesis hyperlipidemias but cause peroxisome proliferation and liver tumors in or liver enlargement and only a small increase in peroxisome prolif- rats and mice via nongenotoxic mechanisms. However, humans and b guinea pigs appear refractory to these adverse effects. The peroxisome eration, and peroxisomal -oxidation enzyme activity is weak (12) proliferator (PP)-activated receptor a (PPARa) mediates the effects of even at very high PP concentrations (13). Similarly, cultured human PPs by heterodimerizing with the retinoid X receptor (RXR) to bind to hepatocytes are refractory to the adverse effects of PPs (14) because DNA at PP response elements (PPREs) upstream of PP-regulated genes, the induction of peroxisomal b-oxidation by PPs weak (15) or absent such as acyl-CoA oxidase. Hepatic expression of PPARa in guinea pigs (15), and PPs cannot induce DNA synthesis (reviewed in Ref. 11) or and humans is low, suggesting that species differences in response to PPs suppress apoptosis (16). In addition, there appears to be no increased may be due at least in part to quantity of PPARa. -
Partial Agreement in the Social and Public Health Field
COUNCIL OF EUROPE COMMITTEE OF MINISTERS (PARTIAL AGREEMENT IN THE SOCIAL AND PUBLIC HEALTH FIELD) RESOLUTION AP (88) 2 ON THE CLASSIFICATION OF MEDICINES WHICH ARE OBTAINABLE ONLY ON MEDICAL PRESCRIPTION (Adopted by the Committee of Ministers on 22 September 1988 at the 419th meeting of the Ministers' Deputies, and superseding Resolution AP (82) 2) AND APPENDIX I Alphabetical list of medicines adopted by the Public Health Committee (Partial Agreement) updated to 1 July 1988 APPENDIX II Pharmaco-therapeutic classification of medicines appearing in the alphabetical list in Appendix I updated to 1 July 1988 RESOLUTION AP (88) 2 ON THE CLASSIFICATION OF MEDICINES WHICH ARE OBTAINABLE ONLY ON MEDICAL PRESCRIPTION (superseding Resolution AP (82) 2) (Adopted by the Committee of Ministers on 22 September 1988 at the 419th meeting of the Ministers' Deputies) The Representatives on the Committee of Ministers of Belgium, France, the Federal Republic of Germany, Italy, Luxembourg, the Netherlands and the United Kingdom of Great Britain and Northern Ireland, these states being parties to the Partial Agreement in the social and public health field, and the Representatives of Austria, Denmark, Ireland, Spain and Switzerland, states which have participated in the public health activities carried out within the above-mentioned Partial Agreement since 1 October 1974, 2 April 1968, 23 September 1969, 21 April 1988 and 5 May 1964, respectively, Considering that the aim of the Council of Europe is to achieve greater unity between its members and that this -
Title Page Alcohol Use, Vascular Disease and Lipid-Lowering Drugs
JPET Fast Forward. Published on April 20, 2006 as DOI: 10.1124/jpet.106.102269 JPET ThisFast article Forward. has not been Published copyedited andon formatted.April 20, The 2006 final versionas DOI:10.1124/jpet.106.102269 may differ from this version. JPET #102269 PiP Title page Alcohol use, Vascular Disease and Lipid-Lowering Drugs Genovefa D. Kolovou Klelia D. Salpea Downloaded from Katherine K. Anagnostopoulou Dimitri P. Mikhailidis jpet.aspetjournals.org (G.D.K., K.D.S., K.K.A.): 1st Cardiology Department, Onassis Cardiac Surgery Center, Athens, at ASPET Journals on September 24, 2021 Greece (D.P.M.): Department of Clinical Biochemistry, Vascular Disease Prevention Clinics, Royal Free Hospital, Royal Free and University College Medical School, London, UK 1 Copyright 2006 by the American Society for Pharmacology and Experimental Therapeutics. JPET Fast Forward. Published on April 20, 2006 as DOI: 10.1124/jpet.106.102269 This article has not been copyedited and formatted. The final version may differ from this version. JPET #102269 PiP Running title page Alcohol and Lipid-Lowering Drugs Corresponding author: Genovefa D. Kolovou, MD, PhD, FESC, SFASA 1st Cardiology Department, Onassis Cardiac Surgery Center 356 Sygrou Ave, 176 74 Athens, Greece Tel: +30 210 9493520, Fax: +30 210 9493336 Downloaded from E-mail: [email protected] Document statistics: Number of text pages: 13 double spaced pages jpet.aspetjournals.org Tables: 0 Figures: 2 References: 67 at ASPET Journals on September 24, 2021 Number of words in the abstract: 136 words Number of words in the introduction: 217 words Number of words in the body article (excluding introduction): 3725 words Abbreviations: Alc: alcohol, CHD: coronary heart disease, HDL: high density lipoprotein, LDL: low density lipoprotein, VLDL: very low density lipoprotein, TG: triglyceride, AST: aspartate aminotransferase, ALT: alanine aminotransferase, NAD: nicotinamide adenine dinucleotide, NADP: nicotinamide adenine dinucleotide phosphate, NA: nicotinic acid. -
BREAST CANCER METASTATIC DORMANCY and EMERGENCE, a ROLE for ADJUVANT STATIN THERAPY by Colin Henry Beckwitt Bachelor of Science
BREAST CANCER METASTATIC DORMANCY AND EMERGENCE, A ROLE FOR ADJUVANT STATIN THERAPY by Colin Henry Beckwitt Bachelor of Science in Biological Engineering, Massachusetts Institute of Technology, 2013 Submitted to the Graduate Faculty of The School of Medicine in partial fulfillment of the requirements for the degree of Doctor of Philosophy University of Pittsburgh 2018 UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE This dissertation was presented by Colin Henry Beckwitt It was defended on May 22, 2018 and approved by Chairperson: Donna Beer Stolz, PhD, Associate Professor, Department of Cell Biology Zoltán N. Oltvai, MD, Associate Professor, Department of Pathology Partha Roy, PhD, Associate Professor, Departments of Bioengineering and Pathology Kari N. Nejak-Bowen, MBA, PhD, Assistant Professor, Department of Pathology Linda G. Griffith, PhD, School of Engineering Teaching Innovation Professor, Departments of Biological and Mechanical Engineering Dissertation Advisor: Alan Wells, MD, DMSc, Thomas J. Gill III Professor, Department of Pathology ii Copyright © by Colin Henry Beckwitt 2018 iii BREAST CANCER METASTATIC DORMANCY AND EMERGENCE, A ROLE FOR ADJUVANT STATIN THERAPY Colin Henry Beckwitt University of Pittsburgh, 2018 Breast cancer is responsible for the most new cancer cases and is the second highest cause of cancer related deaths among women. Localized breast cancer is effectively treated surgically. In contrast, metastatic cancers often remain undetected as dormant micrometastases for years to decades after primary surgery. Emergence of micrometastases to form clinically evident metastases complicates therapeutic intervention, making survival rates poor. The often long lag time between primary tumor diagnosis and emergence of metastatic disease motivates the development or repurposing of agents to act as safe, long term adjuvants to prevent disease progression. -
Pharmaceuticals Appendix
)&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 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. ABAMECTIN 65195-55-3 ADAPALENE 106685-40-9 ABANOQUIL 90402-40-7 ADAPROLOL 101479-70-3 ABECARNIL 111841-85-1 ADEMETIONINE 17176-17-9 ABLUKAST 96566-25-5 ADENOSINE PHOSPHATE 61-19-8 ABUNIDAZOLE 91017-58-2 ADIBENDAN 100510-33-6 ACADESINE 2627-69-2 ADICILLIN 525-94-0 ACAMPROSATE 77337-76-9 ADIMOLOL 78459-19-5 ACAPRAZINE 55485-20-6 ADINAZOLAM 37115-32-5 ACARBOSE 56180-94-0 ADIPHENINE 64-95-9 ACEBROCHOL 514-50-1 ADIPIODONE 606-17-7 ACEBURIC ACID 26976-72-7 ADITEREN 56066-19-4 ACEBUTOLOL 37517-30-9 ADITOPRIME 56066-63-8 ACECAINIDE 32795-44-1 ADOSOPINE 88124-26-9 ACECARBROMAL 77-66-7 ADOZELESIN 110314-48-2 ACECLIDINE 827-61-2 ADRAFINIL 63547-13-7 ACECLOFENAC 89796-99-6 ADRENALONE 99-45-6 ACEDAPSONE 77-46-3 AFALANINE 2901-75-9 ACEDIASULFONE SODIUM 127-60-6 AFLOQUALONE 56287-74-2 ACEDOBEN 556-08-1 AFUROLOL 65776-67-2 ACEFLURANOL 80595-73-9 AGANODINE 86696-87-9 ACEFURTIAMINE 10072-48-7 AKLOMIDE 3011-89-0 ACEFYLLINE CLOFIBROL 70788-27-1 -
Ehealth DSI [Ehdsi V2.2.2-OR] Ehealth DSI – Master Value Set
MTC eHealth DSI [eHDSI v2.2.2-OR] eHealth DSI – Master Value Set Catalogue Responsible : eHDSI Solution Provider PublishDate : Wed Nov 08 16:16:10 CET 2017 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 1 of 490 MTC Table of Contents epSOSActiveIngredient 4 epSOSAdministrativeGender 148 epSOSAdverseEventType 149 epSOSAllergenNoDrugs 150 epSOSBloodGroup 155 epSOSBloodPressure 156 epSOSCodeNoMedication 157 epSOSCodeProb 158 epSOSConfidentiality 159 epSOSCountry 160 epSOSDisplayLabel 167 epSOSDocumentCode 170 epSOSDoseForm 171 epSOSHealthcareProfessionalRoles 184 epSOSIllnessesandDisorders 186 epSOSLanguage 448 epSOSMedicalDevices 458 epSOSNullFavor 461 epSOSPackage 462 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 2 of 490 MTC epSOSPersonalRelationship 464 epSOSPregnancyInformation 466 epSOSProcedures 467 epSOSReactionAllergy 470 epSOSResolutionOutcome 472 epSOSRoleClass 473 epSOSRouteofAdministration 474 epSOSSections 477 epSOSSeverity 478 epSOSSocialHistory 479 epSOSStatusCode 480 epSOSSubstitutionCode 481 epSOSTelecomAddress 482 epSOSTimingEvent 483 epSOSUnits 484 epSOSUnknownInformation 487 epSOSVaccine 488 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 3 of 490 MTC epSOSActiveIngredient epSOSActiveIngredient Value Set ID 1.3.6.1.4.1.12559.11.10.1.3.1.42.24 TRANSLATIONS Code System ID Code System Version Concept Code Description (FSN) 2.16.840.1.113883.6.73 2017-01 A ALIMENTARY TRACT AND METABOLISM 2.16.840.1.113883.6.73 2017-01 -
Regulation of Pharmaceutical Prices: Evidence from a Reference Price Reform in Denmark
A Service of Leibniz-Informationszentrum econstor Wirtschaft Leibniz Information Centre Make Your Publications Visible. zbw for Economics Kaiser, Ulrich; Mendez, Susan J.; Rønde, Thomas Working Paper Regulation of pharmaceutical prices: Evidence from a reference price reform in Denmark ZEW Discussion Papers, No. 10-062 Provided in Cooperation with: ZEW - Leibniz Centre for European Economic Research Suggested Citation: Kaiser, Ulrich; Mendez, Susan J.; Rønde, Thomas (2010) : Regulation of pharmaceutical prices: Evidence from a reference price reform in Denmark, ZEW Discussion Papers, No. 10-062, Zentrum für Europäische Wirtschaftsforschung (ZEW), Mannheim This Version is available at: http://hdl.handle.net/10419/41440 Standard-Nutzungsbedingungen: Terms of use: Die Dokumente auf EconStor dürfen zu eigenen wissenschaftlichen Documents in EconStor may be saved and copied for your Zwecken und zum Privatgebrauch gespeichert und kopiert werden. personal and scholarly purposes. Sie dürfen die Dokumente nicht für öffentliche oder kommerzielle You are not to copy documents for public or commercial Zwecke vervielfältigen, öffentlich ausstellen, öffentlich zugänglich purposes, to exhibit the documents publicly, to make them machen, vertreiben oder anderweitig nutzen. publicly available on the internet, or to distribute or otherwise use the documents in public. Sofern die Verfasser die Dokumente unter Open-Content-Lizenzen (insbesondere CC-Lizenzen) zur Verfügung gestellt haben sollten, If the documents have been made available under an Open gelten abweichend von diesen Nutzungsbedingungen die in der dort Content Licence (especially Creative Commons Licences), you genannten Lizenz gewährten Nutzungsrechte. may exercise further usage rights as specified in the indicated licence. www.econstor.eu Dis cus si on Paper No. 10-062 Regulation of Pharmaceutical Prices: Evidence from a Reference Price Reform in Denmark Ulrich Kaiser, Susan J.