DOCSLIB.ORG

United States Patent (19) 11 Patent Number: 5,861,142 Schick (45) Date of Patent: *Jan

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
United States Patent (19) 11 Patent Number: 5,861,142 Schick (45) Date of Patent: *Jan USOO586 1142A United States Patent (19) 11 Patent Number: 5,861,142 Schick (45) Date of Patent: *Jan. 19, 1999 54 METHOD FOR PROMOTING HAIR, NAIL, 0 090 368 10/1983 European Pat. Off.. AND SKIN KERATINIZATION 0 187 012 7/1986 European Pat. Off.. 0 224 249 6/1987 European Pat. Off.. 76 Inventor: Mary Pichler Schick, 2027 Old Forge b 5. g i. As E. Way, Marietta, Ga. 30068 0 0 W.e "9CO * Notice: This patent issued on a continued pros- 95/16447 6/1995 WIPO. ecution application filed under 37 CFR OTHER PUBLICATIONS 1.53(d), and is subject to the twenty year patent term provisions of 35 U.S.C. Biochemistry Pharm., The interaction of benzimidazole Cat 154(a)(2). bamates with mammalian microtobule protein Vol. 28, p. 268O-2682. Davidse and Flach, “Differential Binding of Methyl 21 Appl. No.: 621,473 Benzimidazol-2-yl Carbamate to Fungal iustin S y 22 Filed: Mar. 25, 1996 Mechanism of Resistance to this Antimitotic Agent in 6 Mutant Strains of Aspergillus Nidulans”, Journal of Cell 51 Int. Cl. ....................................................... A61K 7/06 Biology, vol. 72, 1977, pp. 174-193. 52 U.S. Cl. ............................ 424/61; 424/701; 424/451; Fisher, et. al., “Efficacy of fenbenzalole and piperazine 424/464; 424/484; 424/489; 514/365; 514/395; against developing Stages of toxocara and toxascaris in 514/937; 514/944 dogs”, The Veterinary Record, vol. 132, No. 19, May 8, 58 Field of Search ..................................... 424/401, 701, 1943, pp. 473–475. 424/451, 464, 484, 489; 514/365, 395, 937, 944 (List continued on next page.) Primary Examiner Jvothsna Venkat 56) References Cited AOC, Agent, Or E". & Askew, LLP U.S. PATENT DOCUMENTS 57 ABSTRACT 35: 1919. E. s m r 5.83. A method for promoting keratinization of the hair, nails, and 3,954,791 5/1976 Loewe et al. ..... 260/309.2 skin on the body of an animal or human in which a 4,145,431 3/1979 Haugwitz et al. ... 424/273 B therapeutic amount of a benzimidazole Sufficient to cause 4,159,337 6/1979 Rowlands ...... ... 424/273 B keratinization is administered either Systemically or directly 4,166,858 9/1979 Rowlands ............................ 424/273 B to the site on the body at which keratinization is desired. The 4,792,610 12/1988 Lachhein et al. - - - - - - - - - - - - - - - - - - - - - - - 548/329 method is useful for the treatment of wide variety of hair 4,871.544 10/1989 Eckenhoff ..... ... 424/438 loSS disorders in humans Such as alopecia, is useful for the 4,925,669 5/1990 Dyer et al. ... ... 424/438 treatment of hair loSS disorders in animals, is useful for 5,169,8465,036,069 12/19927/1991 CrooksAndrews ................................. et al. ...si,50s 514/249 enhancing the strength and length of fingernails and toenails 5340804 s/1994 wickiser. siso in humans, and is useful for enhancing the strength and 5,432,187 7/1995 Gazzard ........ ... 514/388 length of claws, horns, hooves and antlers in animals. The 5,434,163 7/1995 Edlind et al. ........................... 514/310 method is also useful for the topical treatment of fungal infections, for Skin replacement or grafting, and for wound FOREIGN PATENT DOCUMENTS healing. 1 132906 10/1982 Canada. O O25 696 3/1981 European Pat. Off.. 5 Claims, 10 Drawing Sheets 3 4 5 time (weeks) 5,861,142 Page 2 OTHER PUBLICATIONS J.P. Seiler, “The Mutagenicity of Benzimidazole and Benz HammerSchlag, et. al., “Benomyl and imidazole Derivatives’, Mutation Research, Vol. 17, 1973, Methyl-2-benzimidazolecarbamate (MBC): Biomedical, pp. 21-25. Cytological and Chemical Aspects of Toxicity to Ustilago maydis and Saccharomyces cerevisae', Pesticide Biochem. J.P. Seiler, “Toxicology and Genetic Effects of Benzimida and Physiology, vol. 3, pp. 42-54. Zole Compounds”, Mutation Research, vol. 32 1975, pp. R.J. Horton, “Benzimidazoles in a Wormy World”, Parasi 151-167. tology Today, vol. 6, No. 4, 1990 p. 106. Townsend and Wise, “The Synthesis and Chemistry Anthel D.W. Woolley, “Some Biological Effects Produced by Ben mintic Benzimidazoles”, Parasitology Today, vol. 6, No. 4, Zimidazole and Their Reversal by Purines”, (Laboratories of 1990, pp. 107-111. The Rockefeller Institute for Medical Research, New York) E. Lacey, “Mode of Action of Benzimidazoles”, Parasitol No. 17, 1943. ogy Today, vol. 6, No. 4, 1990, pp. 112-124. Jordan, et. al., “Endoparasitism in dogs: 21,583 cases B.L. Blagburn et. al., National Prevalence of Canine Para (1981-1990), IAVMA, vol. 203, No. 4, Aug. 1993, pp. sites based on Centrifugal Sucrose Flotation Examination of 547-549. Fecal Specimens: Preliminary Report (18); Proc. AAVP G.C. Coles, “The Biochemical Mode of Action of Some 1994, p. 57. Modern Anthelmintics”, Pestic. Sci. vol. 8, 1977, pp. C.K. Fenger et. al., “The Phylogenetic Relationship of 536-543. D. Diwel, “Fenbendazole. II. Biological Properties and Sarcocystic Neurona to Other Coccidia Determined by Activity”, Pestic. Sci., vol. 8, 1977, pp. 550-555. Molecular Comparisons” (82), Proc. AAVP 1994, p. 57. H. Loewe, et. al. “Fenbendazole. I. Structure-Activity S.C. Barret. al. “Clinical Experience of Treating Cyrptospo Relationships", Pestic. Sci., vol. 8, 1977, pp. 544–549. ridiosis in Cats and Dogs with Paromomycin', (79) Proc. D.W. Gottschall, et. al., “The Metabolism of Benzimidazole Anthelmintics”, Parasitology Today, vol. 6, No. 4, 1990, pp. AAVP 1994, p. 56. 115-124. P.M. Schantz et. al., “Intestinal Parasites are Common in O.A. McKellar et al., “The Benzimidazole Anthelmintic Pound Dogs in Fulton County, Georgia” (80); Proc. AAVP Agents-a review”, J. Pharmacol. Therap. Vol. 13, 1990, pp. 223-247. 1994 p. 56. M. Murray et al., “Hepatic Microsomal Metabolism of the B.T. Huss et al., “Fatal Cerebral Coenurosis in a Cat”, (70), Anthelmintic Benzimidazole Fenbendazole: Enhanced Inhi Proc. AAVP, 1994. bition of Cytochrome P450 Reactions by Oxidized Metabo lites of the Drug, Chem. Res. Toxicol. Vol. 5, 1992, pp. C.T. Faulkner et. al., “Gastrointestinal Parasitism in Dogs in 60-66. Tennessee (1986–1992)” (71), Proc. AAVP 1994. U.S. Patent Jan. 19, 1999 Sheet 1 of 10 5,861,142 SnstSo 9 i CN d v o O y O U.S. Patent Jan. 19, 1999 Sheet 2 of 10 5,861,142 i r CN O CO CO r CN C) ym sleus Igeq snoa Jo Jequnu U.S. Patent Jan. 19, 1999 Sheet 3 of 10 5,861,142 i N. co to Yi ca c\ O O. O. O. O. O. s (ULIULI) SSeUXoup easp oped feu U.S. Patent Jan. 19, 1999 Sheet 4 of 10 5,861,142 CO 3. r sS S CO h-d opm s CN T 3 O y OO co N. c O O O O O (uu) sseuxoup ?ensip oped lieu U.S. Patent Jan. 19, 1999 Sheet S of 10 5,861,142 c lf 2 39 8 3. () .s E CN 9 O Lo N. c. c. C. Cd O O (uu) SSeucoup ensip oped leu U.S. Patent Jan. 19, 1999 Sheet 6 of 10 5,861,142 i | - Co. c. r. c. 6 O O O O (uu) sseuxorup reasp oped leu U.S. Patent Jan. 19, 1999 Sheet 7 of 10 5,861,142 r c) N d e S. s - CN O ld O O CN CN y v (uu) unmora Ileu eulpmauo U.S. Patent Jan. 19, 1999 Sheet 8 of 10 5,861,142 i O C) O c5 O O CN CN t n (uru) upAora IIeu eulpmauo U.S. Patent Jan. 19, 1999 Sheet 9 of 10 5,861,142 c) i o O O (uu) unmous leu. Ieupnuo U.S. Patent Jan. 19, 1999 Sheet 10 of 10 5,861,142 (uu) uplmous IIeu eulpnguo 5,861,142 1 2 METHOD FOR PROMOTING HAIR, NAIL, resemble Vellus hairs. In addition, as androgenic alopecia AND SKIN KERATINIZATION continues, the number of hairs in the active growth anagen phase decreases while there is an increase the number of The present method relates to the field of dermatology hairs in the telogen phase. and more specifically relates to a method for promoting the Telogen effluvium is a type of non-Scarring alopecia in which the anagen hairs prematurely move into the telogen keratinization of hair, nails, and Skin of an animal or human. phase. One most easily recognizable cause of telogen efflu BACKGROUND OF THE INVENTION Vium is the postpartum State in humans and other mammals. In the postpartum period, an increased number of hairs go For centuries, humans have been preoccupied with the into telogen due to the physical StreSS or hormonal changes length, thickness, color, and quantity of hair. Hair thinning, associated with delivery. Three to four months later, there is receding hairlines, and hair loSS can detrimentally affect considerable, but usually temporary hairloSS. The hair uSu appearance and Self-image and can even result in Significant ally returns to its normal state in six to twelve months. Other emotional consequences. causes of telogen effluvium in humans and other mammals Hair is a cylinder of keratinized cells protruding from a 15 include physical StreSS and Systemic illness, psychological hair follicle that anchors the hair in the skin. All hair follicles StreSS caused by major life events Such as a family death or in mammals have the same basic Structure. Hair follicles in divorce, medical nutritional deficiencies (kwashiorkor), or an adult human are generally arranged in groups of three. No absolute calorie deprivation (marasmus, crash diets), Vita new follicles are created or destroyed after birth, however, min and trace element deficiencies (Zinc, biotin, essential the type of hair produced by a given follicle can change.
Load more

Recommended publications
  • Chemotherapy of Gastrointestinal Helminths
    Chemotherapy of Gastrointestinal Helminths Contributors J. H. Arundel • J. H. Boersema • C. F. A. Bruyning • J. H. Cross A. Davis • A. De Muynck • P. G. Janssens • W. S. Kammerer IF. Michel • M.H. Mirck • M.D. Rickard F. Rochette M. M. H. Sewell • H. Vanden Bossche Editors H. Vanden Bossche • D.Thienpont • P.G. Janssens UNIVERSITATS- BlfiUOTHElC Springer-Verlag Berlin Heidelberg New York Tokyo Contents CHAPTER 1 Introduction. A. DAVIS A. Pathogenic Mechanisms in Man 1 B. Modes of Transmission 2 C. Clinical Sequelae of Infection 3 D. Epidemiological Considerations 3 E. Chemotherapy 4 F. Conclusion 5 References 5 CHAPTER 2 Epidemiology of Gastrointestinal Helminths in Human Populations C. F. A. BRUYNING A. Introduction 7 B. Epidemiological or "Mathematical" Models and Control 8 C. Nematodes 11 I. Angiostrongylus costaricensis 11 II. Anisakis marina 12 III. Ascaris lumbricoides 14 IV. Capillaria philippinensis 21 V. Enterobius vermicularis 23 VI. Gnathostoma spinigerum 25 VII. Hookworms: Ancylostoma duodenale and Necator americanus . 26 VIII. Oesophagostoma spp 32 IX. Strongyloides stercoralis 33 X. Ternidens deminutus 34 XI. Trichinella spiralis 35 XII. Trichostrongylus spp 38 XIII. Trichuris trichiura 39 D. Trematodes 41 I. Echinostoma spp 41 II. Fasciolopsis buski 42 III. Gastrodiscoides hominis 44 IV. Heterophyes heterophyes 44 V. Metagonimus yokogawai 46 X Contents E. Cestodes 47 I. Diphyllobothrium latum 47 II. Dipylidium caninum 50 III. Hymenolepis diminuta 51 IV. Hymenolepis nana 52 V. Taenia saginata 54 VI. Taenia solium 57 VII. Cysticercosis cellulosae 58 References 60 CHAPTER 3 Epidemiology and Control of Gastrointestinal Helminths in Domestic Animals J. F. MICHEL. With 20 Figures A. Introduction 67 I.
    [Show full text]
  • 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.
    [Show full text]
  • 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
    [Show full text]
  • Comparative Genomics of the Major Parasitic Worms
    Comparative genomics of the major parasitic worms International Helminth Genomes Consortium Supplementary Information Introduction ............................................................................................................................... 4 Contributions from Consortium members ..................................................................................... 5 Methods .................................................................................................................................... 6 1 Sample collection and preparation ................................................................................................................. 6 2.1 Data production, Wellcome Trust Sanger Institute (WTSI) ........................................................................ 12 DNA template preparation and sequencing................................................................................................. 12 Genome assembly ........................................................................................................................................ 13 Assembly QC ................................................................................................................................................. 14 Gene prediction ............................................................................................................................................ 15 Contamination screening ............................................................................................................................
    [Show full text]
  • 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
    [Show full text]
  • C.8. C.9. /S.II G Courses Prof
    Cursuri Romeo T. Cristina T. Romeo Cursuri C.8. C.9. Image soure: ®® http://www.colonlove.com/assets/images/Parasites.jpg /S.II Antiparasitic medication Courses Prof. Romeo T. Cristina® Introduction thethetheantiparasitic therapy isisis based ononon aaa large number ofofof substances, thethethe majority ofofof them areareare syntheticsynthetic.... Most antiparasitic drugs affect thethethe neuromuscular system ofofof thethethe parasite bybyby blocking thethethe neuromuscular junctions, with thethethefinal result ofofof: of ::: paralysis, death and disposaldisposal.... itititisisis known that helminths have also aaa reversible paralysis, sososothat ififif they areareare not eliminated ininin due time, they will recoverrecover. ... Courses Prof. Romeo T. Cristina® The substances ofofof tehthe tehorganophosphorus group eraare era knownforfor fortheir effectiveness onon onboth helminths and ectoparasitesaerare aergrafted ininin their useuse usebybyby relative high toxicity ... Their mechanism isisis based onon on blocking ehtthe eht acetylcholinesterase enzyme, which isisis tehthe tehenzyme necessaryforfor the forthe thehydrolysis ofofof acetylcholineacetylcholine. ... ByBy Byblocking this enzyme, tehthe tehmediator can onno onlongerbebe be releasedreleased,teh,,, the tehstimulus remains open resulting htethe hte exhaustion and death theofofof the theparasiteparasite. ... Courses Prof. Romeo T. Cristina® Other substances interfere with thethethe processes ofofofATP phosphorylationphosphorylation.... dichlorophenol, niclosamide, benzimidazoles
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • United States Patent (19) 11 Patent Number: 5,872,013 Leunissen Et Al
    USOO5872O13A United States Patent (19) 11 Patent Number: 5,872,013 Leunissen et al. (45) Date of Patent: *Feb. 16, 1999 54 UNIVERSALLY APPLICABLE DETECTION 56) References Cited SYSTEM BASED ON ULTRA SMALL COLLOIDAL METAL PARTICLES U.S. PATENT DOCUMENTS 4,206,094 6/1980 Yen et al.. 75 Inventors: Johannes Leonardus Maria 4,313,734 2/1982 Leuvering. Leunissen, Merksplas; Marc Joris De 4.420,558 12/1983 De Mey et al.. Brabander, Zoersel, both of Belgium; 4,446,238 5/1984 De Mey et al. ........................ 436/527 Petrus Franciscus Elisabeth Maria 4,752,567 6/1988 DeBrabander et al. 436/525 X 4,775,636 10/1988 Moeremans et al. ................... 436/518 Van de Plas, Breda, Netherlands 4,877,647 10/1989 Klabunde ................................ 427/123 73 Assignee: Janssen Pharmaceutica N.V., Beerse, 5,120,643 6/1992 Ching et al. ........................... 435/7.92 Belgium FOREIGN PATENT DOCUMENTS * Notice: This patent issued on a continued pros 158 746 10/1985 European Pat. Off.. ecution application filed under 37 CFR 165 643 12/1985 European Pat. Off.. 1.53(d), and is subject to the twenty year 167834 1/1986 European Pat. Off.. patent term provisions of 35 U.S.C. 154(a)(2). OTHER PUBLICATIONS Horisberger, “Colloidal Gold as a tool in molecular biol 21 Appl. No.: 539,131 ogy”, TIBS, Nov., 1983 pp. 395-397. Roth, “The Colloidal Gold Marker System for Light and 22 Filed: Oct. 4, 1995 Electron Microscopic Cytochemistry,” in Immunocytochem Related U.S. Application Data istry 2, Academic Press, London, (1984), pp. 217-284.
    [Show full text]
  • The Synthesis and Chemistry of Certain Anthelmintic Benzimidazoles LB
    Parasitology Today, vol. 6, no. 4. I990 107 The Synthesis and Chemistry of Certain Anthelmintic Benzimidazoles LB. Townsend and D.S. Wise A basis for interest in the benzimidazole ring system as a nucleus Benzimidazole, as the name implies, is a bicyclic ring system in from which to develop potential chemotherapeutic agents was which benzene has been fused to the 4- and 5-position of the established in the I95Os when it was found that 5,6-dimethyl- I - heterocycle (imidazole; Box I). Benzimidazole compounds in (a-D-ribofiranosyljbenzimidazole (I) was an integral part ofthe general, and benzimidazole carbamates in particular, are crys- talline materials, with fairly high melting points and are relatively insoluble in water. Compounds that are unsubstituted on either of the imidazole nitrogen atoms possess both acidic and basic characteristics. Modifications of the benzimidazole ring system that have been made during the search for anthelmintic activity are summarized in Box 2. Combinations of the modifications at positions 2- and 5- of the molecule has provided the most active drugs. The synthetic pathways to the various benzimi- structure of vitamin 6,~ As a result of these interests and dazoles usually proceeds through two steps, first the construc- extensive studies, one health related arena that has benefited tion of a benzene ring containing the desired substituents and a greatly has been the treatment ofparasitic diseases. The discovery I ,2-diamine grouping, followed by the ring closure of the of thiabendazole in I96 I further spurred chemists around the I ,2-diaminobenzene (o-phenylenediamine) derivative to con- world to design and synthesize several thousand benzimidazoles struct the imidazole ring.
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • WHO-EMP-RHT-TSN-2018.1-Eng.Pdf
    WHO/EMP/RHT/TSN/2018.1 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization [2018] Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO.
    [Show full text]
  • Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes
    Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2004) -- Supplement 1 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. Product CAS No. Product CAS No. ABACAVIR 136470-78-5 ACEXAMIC ACID 57-08-9 ABAFUNGIN 129639-79-8 ACICLOVIR 59277-89-3 ABAMECTIN 65195-55-3 ACIFRAN 72420-38-3 ABANOQUIL 90402-40-7 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABCIXIMAB 143653-53-6 ACITEMATE 101197-99-3 ABECARNIL 111841-85-1 ACITRETIN 55079-83-9 ABIRATERONE 154229-19-3 ACIVICIN 42228-92-2 ABITESARTAN 137882-98-5 ACLANTATE 39633-62-0 ABLUKAST 96566-25-5 ACLARUBICIN 57576-44-0 ABUNIDAZOLE 91017-58-2 ACLATONIUM NAPADISILATE 55077-30-0 ACADESINE 2627-69-2 ACODAZOLE 79152-85-5 ACAMPROSATE 77337-76-9 ACONIAZIDE 13410-86-1 ACAPRAZINE 55485-20-6 ACOXATRINE 748-44-7 ACARBOSE 56180-94-0 ACREOZAST 123548-56-1 ACEBROCHOL 514-50-1 ACRIDOREX 47487-22-9 ACEBURIC ACID 26976-72-7
    [Show full text]