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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. -
Specifications of Approved Drug Compound Library
Annexure-I : Specifications of Approved drug compound library The compounds should be structurally diverse, medicinally active, and cell permeable Compounds should have rich documentation with structure, Target, Activity and IC50 should be known Compounds which are supplied should have been validated by NMR and HPLC to ensure high purity Each compound should be supplied as 10mM solution in DMSO and at least 100µl of each compound should be supplied. Compounds should be supplied in screw capped vial arranged as 96 well plate format. -
(12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub
US 2010O221245A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0221245 A1 Kunin (43) Pub. Date: Sep. 2, 2010 (54) TOPICAL SKIN CARE COMPOSITION Publication Classification (51) Int. Cl. (76) Inventor: Audrey Kunin, Mission Hills, KS A 6LX 39/395 (2006.01) (US) A6II 3L/235 (2006.01) A638/16 (2006.01) Correspondence Address: (52) U.S. Cl. ......................... 424/133.1: 514/533: 514/12 HUSCH BLACKWELL SANDERS LLP (57) ABSTRACT 4801 Main Street, Suite 1000 - KANSAS CITY, MO 64112 (US) The present invention is directed to a topical skin care com position. The composition has the unique ability to treat acne without drying out the user's skin. In particular, the compo (21) Appl. No.: 12/395,251 sition includes a base, an antibacterial agent, at least one anti-inflammatory agent, and at least one antioxidant. The (22) Filed: Feb. 27, 2009 antibacterial agent may be benzoyl peroxide. US 2010/0221 245 A1 Sep. 2, 2010 TOPCAL SKIN CARE COMPOSITION stay of acne treatment since the 1950s. Skin irritation is the most common side effect of benzoyl peroxide and other anti BACKGROUND OF THE INVENTION biotic usage. Some treatments can be severe and can leave the 0001. The present invention generally relates to composi user's skin excessively dry. Excessive use of some acne prod tions and methods for producing topical skin care. Acne Vul ucts may cause redness, dryness of the face, and can actually garis, or acne, is a common skin disease that is prevalent in lead to more acne. Therefore, it would be beneficial to provide teenagers and young adults. -
Lymphoid Organs of Neonatal and Adult Mice Preferentially Produce Active Glucocorticoids from Metabolites, Not Precursors ⇑ Matthew D
Brain, Behavior, and Immunity 57 (2016) 271–281 Contents lists available at ScienceDirect Brain, Behavior, and Immunity journal homepage: www.elsevier.com/locate/ybrbi Full-length Article Lymphoid organs of neonatal and adult mice preferentially produce active glucocorticoids from metabolites, not precursors ⇑ Matthew D. Taves a,b, , Adam W. Plumb c, Anastasia M. Korol a, Jessica Grace Van Der Gugten d, Daniel T. Holmes d, Ninan Abraham b,c,1, Kiran K. Soma a,b,e,1 a Department of Psychology, University of British Columbia, 2136 West Mall, Vancouver V6T 1Z4, Canada b Department of Zoology, University of British Columbia, 4200-6270 University Blvd, Vancouver V6T 1Z4, Canada c Department of Microbiology and Immunology, University of British Columbia, 1365-2350 Health Sciences Mall, Vancouver V6T 1Z3, Canada d Department of Laboratory Medicine, St Paul’s Hospital, 1081 Burrard St, Vancouver, BC V6Z 1Y6, Canada e Djavad Mowafaghian Centre for Brain Health, University of British Columbia, 2215 Wesbrook Mall, Vancouver, BC V6T 1Z3, Canada article info abstract Article history: Glucocorticoids (GCs) are circulating adrenal steroid hormones that coordinate physiology, especially the Received 4 March 2016 counter-regulatory response to stressors. While systemic GCs are often considered immunosuppressive, Received in revised form 22 April 2016 GCs in the thymus play a critical role in antigen-specific immunity by ensuring the selection of competent Accepted 7 May 2016 T cells. Elevated thymus-specific GC levels are thought to occur by local synthesis, but the mechanism of Available online 7 May 2016 such tissue-specific GC production remains unknown. Here, we found metyrapone-blockable GC produc- tion in neonatal and adult bone marrow, spleen, and thymus of C57BL/6 mice. -
Effects of Androgenic-Anabolic Steroids on Apolipoproteins and Lipoprotein (A) F Hartgens, G Rietjens, H a Keizer, H Kuipers, B H R Wolffenbuttel
253 Br J Sports Med: first published as 10.1136/bjsm.2003.000199 on 21 May 2004. Downloaded from ORIGINAL ARTICLE Effects of androgenic-anabolic steroids on apolipoproteins and lipoprotein (a) F Hartgens, G Rietjens, H A Keizer, H Kuipers, B H R Wolffenbuttel ............................................................................................................................... Br J Sports Med 2004;38:253–259. doi: 10.1136/bjsm.2003.000199 Objectives: To investigate the effects of two different regimens of androgenic-anabolic steroid (AAS) administration on serum lipid and lipoproteins, and recovery of these variables after drug cessation, as indicators of the risk for cardiovascular disease in healthy male strength athletes. Methods: In a non-blinded study (study 1) serum lipoproteins and lipids were assessed in 19 subjects who self administered AASs for eight or 14 weeks, and in 16 non-using volunteers. In a randomised double blind, placebo controlled design, the effects of intramuscular administration of nandrolone decanoate (200 mg/week) for eight weeks on the same variables in 16 bodybuilders were studied (study 2). Fasting serum concentrations of total cholesterol, triglycerides, HDL-cholesterol (HDL-C), HDL2-cholesterol (HDL2- C), HDL3-cholesterol (HDL3-C), apolipoprotein A1 (Apo-A1), apolipoprotein B (Apo-B), and lipoprotein (a) (Lp(a)) were determined. Results: In study 1 AAS administration led to decreases in serum concentrations of HDL-C (from 1.08 (0.30) to 0.43 (0.22) mmol/l), HDL2-C (from 0.21 (0.18) to 0.05 (0.03) mmol/l), HDL3-C (from 0.87 (0.24) to 0.40 (0.20) mmol/l, and Apo-A1 (from 1.41 (0.27) to 0.71 (0.34) g/l), whereas Apo-B increased from 0.96 (0.13) to 1.32 (0.28) g/l. -
Anabolic Androgenic Steroid Use Prevalence, Knowledge, and Practice Among Male Athletes in Eastern Province of Saudi Arabia
Electronic Journal of General Medicine 2020, 17(2), em187 e-ISSN: 2516-3507 https://www.ejgm.co.uk/ Original Article OPEN ACCESS Anabolic Androgenic Steroid Use Prevalence, Knowledge, and Practice among Male Athletes in Eastern Province of Saudi Arabia Huda Hassan Aldarweesh 1, Alyaa Hassan Alhajjaj 1* 1 Qatif Central Hospital, SAUDI ARABIA *Corresponding Author: [email protected] Citation: Aldarweesh HH, AlHajjaj AH. Anabolic Androgenic Steroid Use Prevalence, Knowledge, and Practice among Male Athletes in Eastern Province of Saudi Arabia. Electron J Gen Med. 2020;17(2):em187. https://doi.org/10.29333/ejgm/7617 ARTICLE INFO ABSTRACT Received: 25 Oct. 2019 Background: Anabolic androgenic steroids (AAS) are synthetic testosterone like hormones. AAS usage by athletes Accepted: 30 Dec. 2019 has increased dramatically over the past decade. Material and Methods: This study was designed to examine the prevalence, attitude and awareness of AAS abuse among athletes n the Eastern province of Saud Arabia. This was a cross-sectional survey that was conducted among male athletes attending twenty fitness centres in the Eastern Province. It was done during the period from April to August, 2018. Results: A total of 573 questionnaires were distributed but only 503 participants were included n the final analysis. The frequency of AAS use was 17.69%. The man reason for AAS use was muscle building (68.54%). The man source of AAS was the coaches. 56.18% of the users recognize the harmful effects of AAS. The most commonly used oral AAS form was oxandrolone (61.80%). The most commonly used substance for post cycle therapy was Tamoxifen citrate n 67.42% of the users. -
)&F1y3x PHARMACEUTICAL APPENDIX to THE
)&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 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE -
Pp375-430-Annex 1.Qxd
ANNEX 1 CHEMICAL AND PHYSICAL DATA ON COMPOUNDS USED IN COMBINED ESTROGEN–PROGESTOGEN CONTRACEPTIVES AND HORMONAL MENOPAUSAL THERAPY Annex 1 describes the chemical and physical data, technical products, trends in produc- tion by region and uses of estrogens and progestogens in combined estrogen–progestogen contraceptives and hormonal menopausal therapy. Estrogens and progestogens are listed separately in alphabetical order. Trade names for these compounds alone and in combination are given in Annexes 2–4. Sales are listed according to the regions designated by WHO. These are: Africa: Algeria, Angola, Benin, Botswana, Burkina Faso, Burundi, Cameroon, Cape Verde, Central African Republic, Chad, Comoros, Congo, Côte d'Ivoire, Democratic Republic of the Congo, Equatorial Guinea, Eritrea, Ethiopia, Gabon, Gambia, Ghana, Guinea, Guinea-Bissau, Kenya, Lesotho, Liberia, Madagascar, Malawi, Mali, Mauritania, Mauritius, Mozambique, Namibia, Niger, Nigeria, Rwanda, Sao Tome and Principe, Senegal, Seychelles, Sierra Leone, South Africa, Swaziland, Togo, Uganda, United Republic of Tanzania, Zambia and Zimbabwe America (North): Canada, Central America (Antigua and Barbuda, Bahamas, Barbados, Belize, Costa Rica, Cuba, Dominica, El Salvador, Grenada, Guatemala, Haiti, Honduras, Jamaica, Mexico, Nicaragua, Panama, Puerto Rico, Saint Kitts and Nevis, Saint Lucia, Saint Vincent and the Grenadines, Suriname, Trinidad and Tobago), United States of America America (South): Argentina, Bolivia, Brazil, Chile, Colombia, Dominican Republic, Ecuador, Guyana, Paraguay, -
2013 House Judiciary Hb 1070
2013 HOUSE JUDICIARY HB 1070 2013 HOUSE STANDING COMMITTEE MINUTES House Judiciary Committee Prairie Room, State Capitol HB 1070 January 14, 2013 Job #17167 D Conference Committee � · Committee Clerk Signature A-. .;' /) .1� ' I A.J4-��'N'f?4<'71<P2/ I Explanation or reason for introduction of bill/resolution: Relating to the scheduling of controlled substances. Minutes: Chairman Koppelman: Opened the hearing on HB 1070. Mark Hardy, Assistant Executive Director of the NO State Board of Pharmacy: (See testimony #1and 2) He went over these handouts. Rep. Klemin: I don't see an emergency clause in the bill and there is none in the amendment. Did I miss it? Mark Hardy: I want to put an emergency clause on the bill. Rep. Klemin: I think you have to have another section at the end of the bill saying this is an emergency. Rep. Kretschmar: How often do these new drugs come out and should be on it? Mark Hardy: As far as the schedule 1 substances; it is a revolving door and we are always trying to stay in front of what the chemists and what the drug makers are doing. As far as schedule 2 through 5; it is a continuous thing through the DEA. When it becomes a federally controlled substance it takes precedence. Rep. Larson: You have not been aware of the bill I was sponsoring regarding synthetic drugs yet? Mark Hardy: No. The Attorney General briefed me on the Bill #1133. Rep. Larson: The reason for my bill is not get into all of the pharmaceutical names of the chemicals, but anybody that possess or manufacturers a analog in order to try and copy these drugs would be guilty of those offences without having to know the specific chemical compound that might be morphed by unscrupulous people trying to see these products. -
61/2003, Uredbeni
Stran 7380 / Št. 61 / 26. 06. 2003 Uradni list Republike Slovenije ODDELEK VI PROIZVODI KEMIČNE INDUSTRIJE ALI PODOBNIH INDUSTRIJ OPOMBE: 1. (a) Proizvodi (razen radioaktivnih rud), ki ustrezajo poimenovanjem v tar. št. 2844 ali 2845, se uvrščajo v omenjeni tarifni številki, ne pa v druge tariFne številke Nomenklature. (b) V skladu s prejšnjim odstavkom se proizvodi, ki ustrezajo poimenovanjem v tar.št. 2843 ali 2846., uvrščajo samo v omenjeni tarifni številki, ne pa v druge tariFne številke tega oddelka. 2. V skladu z opombo št.1 se proizvodi, ki bi se zaradi pakiranja na drobno ali v odmerjene količine uvrstili v tar. št. 3004, 3005, 3006, 3212, 3303, 3304, 3305, 3306, 3307, 3506, 3707 ali 3808, se uvrščajo samo v omenjeni tar. št., (2844 ali 2845) ne pa v druge tariFne številke Nomenklature. 3. Proizvodi, pripravljeni v garniturah, ki sestoje iz dveh ali več ločenih sestavin, od katerih se neka- tere ali vse uvrščajo v ta oddelek in so namenjene za to, da se pomešajo skupaj, da bi se dobil proizvod VI. ali VII. oddelka, se uvrščajo v ustrezno tarifno številko za ta proizvod pod pogojem, da so sestavine: (a) take, da je iz tega, kako so pripravljene, razvidno, da so namenjene za uporabo skupaj brez poprejšnjega prepakiranja, (b) da se skupaj carinijo in (c) da so take, da je razvidno iz njihove narave ali po sorazmernih količinah, v katerih so zasto- pane, da se med seboj dopolnjujejo. SPLOŠNA DOLOČILA Opomba št. 1 Skladno z določili točke (a) opombe št. 1 se vsi radioaktivni kemični elementi, radioaktivni izotopi in spojine teh elementov in izotopov (anorganskih ali organskih, kemično določenih ali nedoločenih) uvrščajo v tar. -
Us Anti-Doping Agency
2019U.S. ANTI-DOPING AGENCY WALLET CARDEXAMPLES OF PROHIBITED AND PERMITTED SUBSTANCES AND METHODS Effective Jan. 1 – Dec. 31, 2019 CATEGORIES OF SUBSTANCES PROHIBITED AT ALL TIMES (IN AND OUT-OF-COMPETITION) • Non-Approved Substances: investigational drugs and pharmaceuticals with no approval by a governmental regulatory health authority for human therapeutic use. • Anabolic Agents: androstenediol, androstenedione, bolasterone, boldenone, clenbuterol, danazol, desoxymethyltestosterone (madol), dehydrochlormethyltestosterone (DHCMT), Prasterone (dehydroepiandrosterone, DHEA , Intrarosa) and its prohormones, drostanolone, epitestosterone, methasterone, methyl-1-testosterone, methyltestosterone (Covaryx, EEMT, Est Estrogens-methyltest DS, Methitest), nandrolone, oxandrolone, prostanozol, Selective Androgen Receptor Modulators (enobosarm, (ostarine, MK-2866), andarine, LGD-4033, RAD-140). stanozolol, testosterone and its metabolites or isomers (Androgel), THG, tibolone, trenbolone, zeranol, zilpaterol, and similar substances. • Beta-2 Agonists: All selective and non-selective beta-2 agonists, including all optical isomers, are prohibited. Most inhaled beta-2 agonists are prohibited, including arformoterol (Brovana), fenoterol, higenamine (norcoclaurine, Tinospora crispa), indacaterol (Arcapta), levalbuterol (Xopenex), metaproternol (Alupent), orciprenaline, olodaterol (Striverdi), pirbuterol (Maxair), terbutaline (Brethaire), vilanterol (Breo). The only exceptions are albuterol, formoterol, and salmeterol by a metered-dose inhaler when used -
Part I Biopharmaceuticals
1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modifications 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays