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Nitrate Prodrugs Able to Release Nitric Oxide in a Controlled and Selective
Europäisches Patentamt *EP001336602A1* (19) European Patent Office Office européen des brevets (11) EP 1 336 602 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.7: C07C 205/00, A61K 31/00 20.08.2003 Bulletin 2003/34 (21) Application number: 02425075.5 (22) Date of filing: 13.02.2002 (84) Designated Contracting States: (71) Applicant: Scaramuzzino, Giovanni AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU 20052 Monza (Milano) (IT) MC NL PT SE TR Designated Extension States: (72) Inventor: Scaramuzzino, Giovanni AL LT LV MK RO SI 20052 Monza (Milano) (IT) (54) Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases (57) New pharmaceutical compounds of general effects and for this reason they are useful for the prep- formula (I): F-(X)q where q is an integer from 1 to 5, pref- aration of medicines for prevention and treatment of in- erably 1; -F is chosen among drugs described in the text, flammatory, ischemic, degenerative and proliferative -X is chosen among 4 groups -M, -T, -V and -Y as de- diseases of musculoskeletal, tegumental, respiratory, scribed in the text. gastrointestinal, genito-urinary and central nervous sys- The compounds of general formula (I) are nitrate tems. prodrugs which can release nitric oxide in vivo in a con- trolled and selective way and without hypotensive side EP 1 336 602 A1 Printed by Jouve, 75001 PARIS (FR) EP 1 336 602 A1 Description [0001] The present invention relates to new nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without the side effects typical of nitrate vasodilators drugs. -
268 Part 522—Implantation Or Injectable Dosage Form
§ 520.2645 21 CFR Ch. I (4–1–18 Edition) (ii) Indications for use. For the control 522.82 Aminopropazine. of American foulbrood (Paenibacillus 522.84 Beta-aminopropionitrile. larvae). 522.88 Amoxicillin. 522.90 Ampicillin injectable dosage forms. (iii) Limitations. The drug should be 522.90a Ampicillin trihydrate suspension. fed early in the spring or fall and con- 522.90b Ampicillin trihydrate powder for in- sumed by the bees before the main jection. honey flow begins, to avoid contamina- 522.90c Ampicillin sodium. tion of production honey. Complete 522.144 Arsenamide. treatments at least 4 weeks before 522.147 Atipamezole. main honey flow. 522.150 Azaperone. 522.161 Betamethasone. [40 FR 13838, Mar. 27, 1975, as amended at 50 522.163 Betamethasone dipropionate and FR 49841, Dec. 5, 1985; 59 FR 14365, Mar. 28, betamethasone sodium phosphate aque- 1994; 62 FR 39443, July 23, 1997; 68 FR 24879, ous suspension. May 9, 2003; 70 FR 69439, Nov. 16, 2005; 73 FR 522.167 Betamethasone sodium phosphate 76946, Dec. 18, 2008; 75 FR 76259, Dec. 8, 2010; and betamethasone acetate. 76 FR 59024, Sept. 23, 2011; 77 FR 29217, May 522.204 Boldenone. 17, 2012; 79 FR 37620, July 2, 2014; 79 FR 53136, 522.224 Bupivacaine. Sept. 8, 2014; 79 FR 64116, Oct. 28, 2014; 80 FR 522.230 Buprenorphine. 34278, June 16, 2015; 81 FR 48702, July 26, 2016] 522.234 Butamisole. 522.246 Butorphanol. § 520.2645 Tylvalosin. 522.275 N-Butylscopolammonium. 522.300 Carfentanil. (a) Specifications. Granules containing 522.304 Carprofen. 62.5 percent tylvalosin (w/w) as 522.311 Cefovecin. -
Active Pharmaceutical Ingredients
Active Pharmaceutical Ingredients Catalog HPD-5E ® CREATING A HEALTHY WORLDTM Active Pharmaceutical Ingredients (APIs) Available for International Markets Human Pharmaceutical Department www.Pharmapex.net Catalog HPD-5E *Not all products referred to on this site are available in all countries and our products are subject to different regulatory requirements depending on the country of use. Consequently, certain sections of this site may be indicated as being intended only for users in specic countries. Some of the products may also be marketed under different trade names. You should not construe anything on this site as a promotion or solicitation for any product or for the use of any product that is not authorized by the laws and regulations of your country of residence. For inquiries about the availability of any specic product in your country, you may simply contact us at [email protected]. **Products currently covered by valid US Patents may be offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk. ©2016, Pharmapex USA, A member of Apex Group of Companies, All Rights Reserved. Toll-Free: 1.844.PHARMAPEX Fax: + 1.619.881.0035 ACTIVE PHARMACEUTICAL [email protected] CREATING A HEALTHY WORLD™ www.Pharmapex.net INGREDIENTS About Pharmapex’s Human Pharmaceuticals Department: Pharmapex’s Human Pharmaceuticals Department (HPD) is a leading source for high-quality Active Pharmaceutical Ingredients (APIs) and Finished Pharmaceutical Products (FPPs) in various markets across the globe. With an extensive product portfolio, our consortium of companies is dedicated to addressing and solving the most important medical needs of our time, including oncology (e.g., multiple myeloma and prostate cancer), neuroscience (e.g., schizophrenia, dementia and pain), infectious disease (e.g., HIV/AIDS, Hepatitis C and tuberculosis), and cardiovascular and metabolic diseases (e.g., diabetes). -
Product Portfolio
API Product Portfolio Hovione has developed a range of particle engineered Particle Engineered APIs APIs with superior powder properties that will address the challenges of your formulation development. Corticosteroids PRODUCT ROUTE OF CAS CUSTOMIZED REGULATORY ADMINISTRATION NUMBER PARTICLE SIZE STATUS Beclomethasone Dipropionate Anhydrous Inhalation Nasal Oral Topical 5534-09-08 Beclomethasone Dipropionate Monohydrate Inhalation Nasal 77011-63-3 US DMF Betamethasone Acetate Ophtalmic Injectable 987-24-6 US DMF Betamethasone Disodium Phosphate Ophtalmic Injectable Topical 151-73-5 US DMF, JP DMF Fluticasone Furoate Inhalation Nasal 397864-44-7 US DMF CEP, US DMF, JP DMF, Fluticasone Propionate Inhalation Nasal Topical 80474-14-2 CN DMF Halobetasol Propionate Topical 66852-54-8 US DMF Hydrocortisone Aceponate Topical 74050-20-7 ASMF & VMF Mometasone Furoate Anhydrous Inhalation Nasal Topical 83919-23-7 CEP, US DMF, JP DMF Mometasone Furoate Monohydrate Inhalation Nasal 141646-00-6 CEP, US DMF, JP DMF LABA/LAMA PRODUCT ROUTE OF CAS CUSTOMIZED REGULATORY ADMINISTRATION NUMBER PARTICLE SIZE STATUS Aclidinium Bromide Inhalation 320345-99-1 US DMF Glycopyrronium Bromide Inhalation 51186-83-5 US DMF Salmeterol Xinafoate Inhalation 94749-08-3 CEP, US DMF Indacaterol Maleate Inhalation 312753-06-3 DEV Olodaterol Sulphate Inhalation 869477-96-3 DEV Salbutamol Inhalation 18559-94-9 GMP, TECH PACK Tiotropium Bromide Monohydrate Inhalation 136310-93-5 DEV Umeclidinium Bromide Inhalation 869113-09-7 DEV, TECH PACK Vilanterol Trifenatate Inhalation 503070-58-4 GMP, TECH PACK Hovione provides the peace of mind of a high quality Security of supply manufacturer who is a founding member of Rx-360 and has an unblemished regulatory track record. -
Product List
Arena Product List A Cabazitaxel (Under Development) Acebutolol HCl Calcitriol N-Acetyl-L-Asparagine Calcifediol N-Acetyl-L-Aspartic Acid Calcipotriol Monohydrate Acexamic Acid (Upon Request) Canrenoate K Aesculin Canrenone micronised Agomelatine (Under Development) Capecitabine Alfacalcidol Captopril Alimemazine Tartrate Carbamizole Aliskiren Fumarate (Under Development) Carbasalate Calcium Altizide Carbomers Amcinonide Acetyl Thiazolidin Carboxylic Acid Amifostine L-Carnitine Base Amiodarone HCl (Upon Request) Acetyl-L-Carnitine HCl Amisulpride (Upon Request) Acetyl Carnosine Amitriptyline HCl L-Carnosine Apomorphine HCl Cefaclor L-Arginine Base Cefalexin Monohydrate L-Arginine-L-Aspartate Cefamandole Nafate Sterile L-Arginine-L-Glutamate Cefazedone Sodium Sterile Aripiprazole (Under Development) Cefepime HCL Artesunate (Upon Request) Cefmetazole Artemether (Upon Request) Cefmetazole Sodium Sterile Articaine HCl Cefminox Sodium Sterile L-Asparagine Anyhdrous Cefodizime Disodium L-Asparagine Monohydrate Cefodizime Sodium Sterile DL-Aspartic Acid Magnesium Salt Cefotetan DL-Aspartic Acid Magnesium + Potassium Salt Cefotetan Sodium Sterile DL-Aspartic Acid Potassium Salt Cefozopran (Under Development) L-Aspartic Acid Sodium Salt Monohydrate Cefsulodin (Under Development) Atovaquone (Under Development) Cefsulodin Sodium Sterile Azacitidine (Under Development) Cefuroxime Sodium Azathioprine Powder Cefuroxime Sodium Sterile Centella Asiatica Extract B Cephacetrile Sodium Sterile Baclofen Cetirizine HCl Beclomethasone Base Cetrimide Powder -
A New Robust Technique for Testing of Glucocorticosteroids in Dogs and Horses Terry E
Iowa State University Capstones, Theses and Retrospective Theses and Dissertations Dissertations 2007 A new robust technique for testing of glucocorticosteroids in dogs and horses Terry E. Webster Iowa State University Follow this and additional works at: https://lib.dr.iastate.edu/rtd Part of the Veterinary Toxicology and Pharmacology Commons Recommended Citation Webster, Terry E., "A new robust technique for testing of glucocorticosteroids in dogs and horses" (2007). Retrospective Theses and Dissertations. 15029. https://lib.dr.iastate.edu/rtd/15029 This Thesis is brought to you for free and open access by the Iowa State University Capstones, Theses and Dissertations at Iowa State University Digital Repository. It has been accepted for inclusion in Retrospective Theses and Dissertations by an authorized administrator of Iowa State University Digital Repository. For more information, please contact [email protected]. A new robust technique for testing of glucocorticosteroids in dogs and horses by Terry E. Webster A thesis submitted to the graduate faculty in partial fulfillment of the requirements for the degree of MASTER OF SCIENCE Major: Toxicology Program o f Study Committee: Walter G. Hyde, Major Professor Steve Ensley Thomas Isenhart Iowa State University Ames, Iowa 2007 Copyright © Terry Edward Webster, 2007. All rights reserved UMI Number: 1446027 Copyright 2007 by Webster, Terry E. All rights reserved. UMI Microform 1446027 Copyright 2007 by ProQuest Information and Learning Company. All rights reserved. This microform edition is protected against unauthorized copying under Title 17, United States Code. ProQuest Information and Learning Company 300 North Zeeb Road P.O. Box 1346 Ann Arbor, MI 48106-1346 ii DEDICATION I want to dedicate this project to my wife, Jackie, and my children, Shauna, Luke and Jake for their patience and understanding without which this project would not have been possible. -
Steroid Use in Prednisone Allergy Abby Shuck, Pharmd Candidate
Steroid Use in Prednisone Allergy Abby Shuck, PharmD candidate 2015 University of Findlay If a patient has an allergy to prednisone and methylprednisolone, what (if any) other corticosteroid can the patient use to avoid an allergic reaction? Corticosteroids very rarely cause allergic reactions in patients that receive them. Since corticosteroids are typically used to treat severe allergic reactions and anaphylaxis, it seems unlikely that these drugs could actually induce an allergic reaction of their own. However, between 0.5-5% of people have reported any sort of reaction to a corticosteroid that they have received.1 Corticosteroids can cause anything from minor skin irritations to full blown anaphylactic shock. Worsening of allergic symptoms during corticosteroid treatment may not always mean that the patient has failed treatment, although it may appear to be so.2,3 There are essentially four classes of corticosteroids: Class A, hydrocortisone-type, Class B, triamcinolone acetonide type, Class C, betamethasone type, and Class D, hydrocortisone-17-butyrate and clobetasone-17-butyrate type. Major* corticosteroids in Class A include cortisone, hydrocortisone, methylprednisolone, prednisolone, and prednisone. Major* corticosteroids in Class B include budesonide, fluocinolone, and triamcinolone. Major* corticosteroids in Class C include beclomethasone and dexamethasone. Finally, major* corticosteroids in Class D include betamethasone, fluticasone, and mometasone.4,5 Class D was later subdivided into Class D1 and D2 depending on the presence or 5,6 absence of a C16 methyl substitution and/or halogenation on C9 of the steroid B-ring. It is often hard to determine what exactly a patient is allergic to if they experience a reaction to a corticosteroid. -
The Inhaled Steroid Ciclesonide Blocks SARS-Cov-2 RNA Replication by Targeting Viral
bioRxiv preprint doi: https://doi.org/10.1101/2020.08.22.258459; this version posted August 24, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. 1 The inhaled steroid ciclesonide blocks SARS-CoV-2 RNA replication by targeting viral 2 replication-transcription complex in culture cells 3 4 Shutoku Matsuyamaa#, Miyuki Kawasea, Naganori Naoa, Kazuya Shiratoa, Makoto Ujikeb, Wataru 5 Kamitanic, Masayuki Shimojimad, and Shuetsu Fukushid 6 7 aDepartment of Virology III, National Institute of Infectious Diseases, Tokyo, Japan 8 bFaculty of Veterinary Medicine, Nippon Veterinary and Life Science University, Tokyo, Japan 9 cDepartment of Infectious Diseases and Host Defense, Gunma University Graduate School of 10 Medicine, Gunma, Japan 11 dDepartment of Virology I, National Institute of Infectious Diseases, Tokyo, Japan. 12 13 Running Head: Ciclesonide blocks SARS-CoV-2 replication 14 15 #Address correspondence to Shutoku Matsuyama, [email protected] 16 17 Word count: Abstract 149, Text 3,016 bioRxiv preprint doi: https://doi.org/10.1101/2020.08.22.258459; this version posted August 24, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. 18 Abstract 19 We screened steroid compounds to obtain a drug expected to block host inflammatory responses and 20 MERS-CoV replication. Ciclesonide, an inhaled corticosteroid, suppressed replication of MERS-CoV 21 and other coronaviruses, including SARS-CoV-2, the cause of COVID-19, in cultured cells. The 22 effective concentration (EC90) of ciclesonide for SARS-CoV-2 in differentiated human bronchial 23 tracheal epithelial cells was 0.55 μM. -
Kentucky Horse Racing Commission Withdrawal Guidelines Thoroughbred; Standardbred; Quarter Horse, Appaloosa, and Arabian KHRC 8-020-2 (11/2018)
Kentucky Horse Racing Commission Withdrawal Guidelines Thoroughbred; Standardbred; Quarter Horse, Appaloosa, and Arabian KHRC 8-020-2 (11/2018) General Notice Unless otherwise specified in these withdrawal guidelines or the applicable regulations and statutes, the following withdrawal guidelines are voluntary and advisory. The guidelines are recommendations based on current scientific knowledge that may change over time. A licensee may present evidence of full compliance with these guidelines to the Kentucky Horse Racing Commission (the “Commission” or “KHRC”) and the stewards as a mitigating factor to be used in determining violations and penalties. These withdrawal interval guidelines assume that administration of medications will be performed at doses that are not greater than the manufacturer’s maximum recommended dosage. Medications administered at dosages above manufacturer’s recommendations, in compounded formulations and/or in combination with other medications and/or administration inside the withdrawal interval may result in test sample concentrations above threshold concentrations that could lead to positive test results and the imposition of penalties. The time of administration of an orally administered substance, for the purposes of withdrawal interval, shall be considered to be the time of complete ingestion of the medication by the horse via eating or drinking. Brand names of medications, where applicable, are listed in parentheses or brackets following the generic name of a drug. In addition to the requirements contained in KRS Chapter 13A, the KHRC shall give notice of an amendment or addition to these withdrawal guidelines by posting the change on the KHRC website and at all Kentucky racetracks at least two weeks before the amendment or addition takes legal effect. -
Effects of Three Corticosteroids on Equine Articular Cocultures in Vitro
Effects of Three Corticosteroids on Equine Articular Cocultures In Vitro Richard Angellas Trahan Thesis submitted to the faculty of the Virginia Polytechnic Institute and State University in partial fulfillment of the requirements for the degree of Master of Science In Biomedical and Veterinary Sciences Christopher R. Byron, Chair Linda A. Dahlgren R. Scott Pleasant April 27th, 2018 Blacksburg, VA Keywords: osteoarthritis, corticosteroid, osteochondral explant, isoflupredone acetate Effects of Three Corticosteroids on Equine Articular Cocultures In Vitro Richard Angellas Trahan Academic Abstract The objective was to compare the effects of three corticosteroids at various equimolar concentrations on equine articular explant co-cultures in an inflammatory environment. Synovial and osteochondral explant co-cultures from 6 equine cadavers were exposed to IL-1β (10 ng/mL) and various concentrations (10-4, 10-7, or 10-10 M) of MPA, TA, IPA. Concentrations of PGE2, MMP-13, LDH, and GAG in media were determined at 48 and 96 hours. Results indicated wells with low concentrations of MPA (10-7 and 10-10 M at 48 and 96 hours), TA (10-7 M at 48 hours and 10-7 and 10-10 M at 48 and 96 hours), and IPA -10 (10 M at 48 hours) had significantly less PGE2 than positive control samples. Groups -7 -10 with low concentrations (10 and 10 M) of MPA and TA had significantly less PGE2 than the highest concentration (10-4 M) at 48 hours. Significantly less MMP-13 was detected for all concentrations of MPA, TA, and IPA at 96 hours. The LDH assay results indicated cytotoxicity only for samples treated with IPA at 10-4 M at 48 and 96 hours. -
Therapeutic Drug Class
BUREAU FOR MEDICAL SERVICES EFFECTIVE WEST VIRGINIA MEDICAID PREFERRED DRUG LIST WITH PRIOR AUTHORIZATION CRITERIA 07/01/2018 This is not an all-inclusive list of available covered drugs and includes only Version 2018.3e managed categories. Refer to cover page for complete list of rules governing this PDL. • Prior authorization for a non-preferred agent in any class will be given only if there has been a trial of the preferred brand/generic equivalent or preferred formulation of the active ingredient, at a therapeutic dose, that resulted in a partial response with a documented intolerance. • Prior authorization of a non-preferred isomer, pro-drug, or metabolite will be considered with a trial of a preferred parent drug of the same chemical entity, at a therapeutic dose, that resulted in a partial response with documented intolerance or a previous trial and therapy failure, at a therapeutic dose, with a preferred drug of a different chemical entity indicated to treat the submitted diagnosis. (The required trial may be overridden when documented evidence is provided that the use of these preferred agent(s) would be medically contraindicated.) • Unless otherwise specified, the listing of a particular brand or generic name includes all legend forms of that drug. OTC drugs are not covered unless specified. • PA criteria for non-preferred agents apply in addition to general Drug Utilization Review policy that is in effect for the entire pharmacy program, including, but not limited to, appropriate dosing, duplication of therapy, etc. • The use of pharmaceutical samples will not be considered when evaluating the members’ medical condition or prior prescription history for drugs that require prior authorization. -
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