DOCSLIB.ORG

(12) United States Patent (10) Patent No.: US 7,199,151 B2 Shashoua Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(12) United States Patent (10) Patent No.: US 7,199,151 B2 Shashoua Et Al US007 1991.51B2 (12) United States Patent (10) Patent No.: US 7,199,151 B2 Shashoua et al. (45) Date of Patent: *Apr. 3, 2007 (54) DHA-PHARMACEUTICAL AGENT 4,692,441 A 9, 1987 Alexander et al. CONUGATES OF TAXANES 4,704,393 A 11/1987 Wakabayashi et al. 4,729,989 A 3, 1988 Alexander (75) Inventors: Victor E. Shashoua, Brookline, MA 4,788,063 A 11/1988 Fisher et al. (US); Charles E. Swindell, Merion, PA is: A RE s al (US); Nigel L. Webb, Bryn Mawr, PA 4s68161. A 9, 1989 Roberts (US); Matthews O. Bradley, 4.902,505 A 2/1990 Pardridge et al. Laytonsville, MD (US) 4,933,324. A 6/1990 Shashoua 4,939,174 A 7, 1990 Shashoua (73) Assignee: Luitpold Pharmaceuticals, Inc., 4,943,579 A 7, 1990 Vishnuvajala et al. Shirley, NY (US) 4,968,672 A 1 1/1990 Jacobson et al. 5,059,699 A 10/1991 Kingston et al. (*) Notice: Subject to any disclaimer, the term of this 5,068,224. A 11/1991 Fryklund et al. patent is extended or adjusted under 35 5, 112,596 A 5/1992 Malfroy-Camine U.S.C. 154(b) by 81 days. 5, 112,863 A 5/1992 Hashimoto et al. 5,116,624 A 5/1992 Horrobin et al. This patent is Subject to a terminal dis- 5, 120,760 A 6/1992 Horrobin claimer. 5,141,958 A 8, 1992 Crozier-Willi et al. 5,169,762 A 12/1992 Grey et al. (21) Appl. No.: 10/618,884 5,169,764 A 12/1992 Shooter et al. 5,194,654 A 3, 1993 Hostetler et al. (22) Filed: Jul. 14, 2003 5,214,062 A 5/1993 Mark et al. 5,216,023 A 6/1993 Literati-Nagy et al. (65) Prior Publication Data 5,216,142 A 6/1993 Horribin et al. 5,223,263. A 6/1993 Hostetler et al. US 2004/O180949 A1 Sep. 16, 2004 5,246,726 A 9, 1993 Horribin et al. 5,250,722 A 10, 1993 Bombardelli et al. Related U.S. Application Data 5,276,020 A 1/1994 Horribin et al. (63) Continuation of application No. 09/846,838, filed on 5,278.324 A 1/1994 Kingston et al. 5,284,876 A 2, 1994 Shashoua et al. May 1, 2001, now Pat. No. 6,602,902, which is a 5,308,832 A 5/1994 Garleb et al. continuation of application No. 09/135,291, filed on 5.314.991 A 5/1994 Oka et all Aug. 17, 1998, now abandoned, which is a continu- 5,336,684 A 8/1994 Murray et al ation of application No. 08/651.312, filed on May 22, 5,352.596 A 10, 1994 Cheung et al. 1996, now Pat. No. 5,795,909. 5,356,928 A 10/1994 Murray et al. 5,362,831 A 11/1994 Mongelli et al. (51) Int. Cl. A 6LX 3/59 (2006.01) A 6LX 3/592 (2006.01) (Continued) A6 IK 9/42 (2006.01) FOREIGN PATENT DOCUMENTS A6 IK 47/48 (2006.01) A61 K 47/00 (2006.01) AU T46472 6, 1999 (52) U.S. Cl. ...................... 514/449; 514/560; 514/558: 514/552; 514/549; 514/943 (Continued) (58) Field of Classification Search ................ 514/449, OTHER PUBLICATIONS 514/560, 558,552,549; 549/510 See application file for complete search history. Chen, et al. “Taxol Structure-Activity Relationships: Synthesis and Biological Evaluation of Taxol Analogs Modified at C-7.” (56) References Cited Bioorganic & Medicinal Chemistry Letters, vol. 4. No. 18, pp. 2223-2228, 1994. U.S. PATENT DOCUMENTS 3,539,573 A 11/1970 Schmutz (Continued) 3,621,048 A 11/1971 Bauman Primary Examiner Ardin H. Marschel 4,088.646 A 5, 1978 Ishida et al. Assistant Examiner—Donna Jagoe 4,097,597 A 6, 1978 Horrom et al. (74) Attorney, Agent, or Firm Wolf, Greenfield & Sacks, 4,185,095 A 1/1980 Young P.C. 4,218,234 A 8/1980 Nadasy et al. 4,287.184 A 9/1981 Young (57) ABSTRACT 4,346,085 A 8, 1982 Growdon et al. 4,351,831 A 9, 1982 Growden et al. 4,407,744 A 10/1983 Young The invention provides conjugates of cis-docosahexaenoic 4.550,109 A 10, 1985 Folkers et al. acid and pharmaceutical agents useful in treating noncentral 4,554,272 A 11, 1985 Bock et al. nervous system conditions. Methods for selectively target 4,558,049 A 12/1985 Bernardi et al. ing pharmaceutical agents to desired tissues are provided. 4,636,494. A 1, 1987 Growden et al. 4,684,646 A 8/1987 Chang et al. 12 Claims, 14 Drawing Sheets US 7,199,151 B2 Page 2 U.S. PATENT DOCUMENTS 2001 OOO6962 A1 7/2001 Myhren et al. 5,411,947 A 5, 1995 Hostetler et al. FOREIGN PATENT DOCUMENTS 5,420,276 A 5, 1995 Norbeck 5.447,936 A 9, 1995 Hausheer et al. AU 770519 4/2001 5.453.520 A 9, 1995 Bombardelli et al. DE 24 56947 A1 6, 1975 5.453.521 A 9, 1995 Gaullier et al. DE 2602175 7, 1976 5,459.256 A 10/1995 Marquez et al. DE 2932 869 A1 2/1980 5,466,841. A 1 1/1995 Horrobin et al. DE 4224.737 2, 1994 5,468,754. A 1 1/1995 Hausheer et al. EP 0 030 009 A1 6, 1981 5,473,055 A 12/1995 Mongelli et al. EP O O35 375 A1 9, 1981 5,476,954. A 12/1995 Bourzat et al. EP 0 091 694 A1 10, 1983 5,484.809 A 1/1996 Hostetler et al. EP O 311 100 A2 4, 1989 5,494,999 A 2, 1996 Hale et al. EP O 350 287 10, 1990 EP O 599 576 A1 6, 1994 5,496,714 A 3, 1996 Comb et al. EP O 615 T52 A1 9, 1994 5,504,102 A 4, 1996 Agharkar et al. EP O 693 498 A1 1/1996 5,516,800 A 5, 1996 Horrobin EP O 761 644 A 3, 1997 5,532,374 A 7, 1996 Lee et al. EP O909183 B1 8, 2004 5.534499 A 7, 1996 Ansell FR 2592 883. A 7, 1987 5,545,719 A 8, 1996 Shashoua FR 2 698 269 A 8, 1997 5,580,556 A 12/1996 Horribin JP T6-9469 1, 1975 5,580,899 A 12/1996 Mayhew et al. JP T5-9469 7, 1976 5,597,719 A 1/1997 Freed et al. JP 55053208 A 4f1980 5,603,959 A 2f1997 Horrobin et al. JP T5-427/1983 4f1983 5,604,198 A 2f1997 Poduslo et al. JP 59025327 A 2, 1984 5,604,216 A 2, 1997 Horrobin JP 59-2041.75 11, 1984 5,646,180 A 7, 1997 Chaturvedi JP 61204136 9, 1986 5,654,290 A 8/1997 Bayon et al. JP 1153629. A 6, 1989 5,716,614 A 2, 1998 Katz et al. JP 1203331 A 8, 1989 5,750,572 A 5/1998 Bruzzese JP 1287022. A 11, 1989 5,795,909 A * 8/1998 Shashoua et al. ........... 514,449 E. 33. g 5,814,456 A 9, 1998 O’Rand et al. JP 6O72868 3, 1994 5,824,701 A 10, 1998 Greenwald et al. JP TO82146 3, 1995 5,827,819 A 10/1998 Yatvin et al. JP 8027010 A 1, 1996 5,919,815 A * 7, 1999 Bradley et al. ............. 514,449 JP 815133 6, 1996 5,922,695 A 7, 1999 Arimilli et al. JP 8163991 A 6, 1996 5,925,669 A * 7/1999 Katz et al. .................. 514,449 JP 8245378 A 9, 1996 5,952,317 A 9, 1999 Deluca et al. JP 9025231 A 1, 1997 5,955.459 A 9/1999 Bradley et al. JP 9030963 2, 1997 5,976,784. A 1 1/1999 DeLuca et al. JP 10168047 A 6, 1998 5,977,061 A 1 1/1999 Holy et al. SU 477159. A 10, 1976 5,977,089 A 11/1999 Arimilli et al. WO WO 85,00520 4f1989 5,977,174 A 11/1999 Bradley et al. WO WO 89.02733 4f1989 5,985,854. A 11/1999 Kozak WO WO 89,07938 9, 1989 5,994,392 A 1 1/1999 Shashoua WO WO 90/OO555 1, 1990 6,005,004 A 12/1999 Katz et al. WO WO92/06089 A 4f1992 6,024,977 A 2/2000 Yatvin et al. WO WO 92.16554 10, 1992 6,043,230 A 3/2000 Arimilli et al. WO WO 92,20362 11, 1992 6,069,249 A 5/2000 Arimilli et al. W Wi. E. 6,077,837 A 6, 2000 Kozak WO WO 93/11668 6, 1993 6,080,877 A * 6/2000 Swindell et al. ............ 549/510 WO WO 94,07880 4f1994 6,107,499 A 8, 2000 Shashoua WO WO 94,11547 5, 1994 6,153,653 A 11/2000 Shashoua WO WO 94,13654 6, 1994 6,166,089 A 12/2000 Kozak WO WO 94,22887 10, 1994 6, 197,764 B1 3/2001 Bradley et al. WO WO 94,24107 10, 1994 6,225,444 B1 5, 2001 Shashoua WO WO95/O1969 1, 1995 6.225,460 B1 5/2001 Bischofberger et al. WO WO95/13270 5, 1995 6,245,811 B1 6/2001 Horrobin et al. WO WO95/13271 5, 1995 6,252,060 B1 6/2001 Hostetler WO WO95/33736 12/1995 6,258,836 B1 7/2001 Shashoua WO WO 96.01259 1, 1996 6,281,376 B1 8/2001 Whittaker et al.
Load more

Recommended publications
  • A Comparative Study of Neuromuscular Blocking Effects
    IndianJournalofAnesthesiaandAnalgesia OriginalResearchArticle January–February2020;7(1)(Part-I):58-63 DOI:http://dx.doi.org/10.21088/ijaa.2349.8471.7120.9 AComparativeStudyofNeuromuscularBlockingEffectsandReversibility ofCisatracuriumandVecuronium DivyaNKheskani1,HeenaSChhanwal2,BhaktiSJain3 1AssistantProfessor,2ProfessorandHead,3rdYearResident,DepartmentofAnaesthesia,GCSMedicalCollege,Hospital&Research Centre,NearChamundaBridge,Ahmedabad,Gujarat380025,India. Abstract Context: Cisatracurium is a cis isomer of parent compound atracurium, devoid of histamine release, thus possessing hemodynamic & cardiovascular stability. Aims: We compared the intubating conditions, hemodynamic stability & recovery of atracurium & vecuronium. Settings and Design: We carried out prospective, double blind randomized study after approval of ethical committee. 100 adult patients of ASA 1 &2with comparable demographicdatawereselected. Dividedin TwoGroupsC(Cisatracurium) &V(Vecuronium).Standardmonitoringwasdone&followingroutinepremedication&inductionagents, patientswereintubatedat2minsafteradministrationofcisatracurium0.15mg/kg&vecuronium0.1mg/ kgrespectively,maintainedonintermittentdoseofcisatracurium:0.03mg/kg&vecuronium:0.02mg/kg. IntubationconditionswereassessedaccordingtoTimeto25%recoveryoft1/tcfollowinginitialdoses,Time to25%recoveryoft1/tcfollowingrepeatedboluses,Timeto25%recoveryoft1/tcfollowinglastdose,Return oft4/t1ratio0.8spontaneousrecoveryatendofoperation.Statisticalanalysisused:Theresultswereevaluated byapplyingpairedt-testandp-valueusingSPSSStatisticalSoftware.Results:Intubatingconditionsat2mins
    [Show full text]
  • Full Text in Pdf Format
    DISEASES OF AQUATIC ORGANISMS Published July 30 Dis Aquat Org Oral pharmacological treatments for parasitic diseases of rainbow trout Oncorhynchus mykiss. 11: Gyrodactylus sp. J. L. Tojo*, M. T. Santamarina Department of Microbiology and Parasitology, Laboratory of Parasitology, Faculty of Pharmacy, Universidad de Santiago de Compostela, E-15706 Santiago de Compostela, Spain ABSTRACT: A total of 24 drugs were evaluated as regards their efficacy for oral treatment of gyro- dactylosis in rainbow trout Oncorhj~nchusmykiss. In preliminary trials, all drugs were supplied to infected fish at 40 g per kg of feed for 10 d. Twenty-two of the drugs tested (aminosidine, amprolium, benznidazole, b~thionol,chloroquine, diethylcarbamazine, flubendazole, levamisole, mebendazole, n~etronidazole,mclosamide, nitroxynil, oxibendazole, parbendazole, piperazine, praziquantel, roni- dazole, secnidazole, tetramisole, thiophanate, toltrazuril and trichlorfon) were ineffective Triclabenda- zole and nitroscanate completely eliminated the infection. Triclabendazole was effective only at the screening dosage (40 g per kg of feed for 10 d), while nitroscanate was effective at dosages as low as 0.6 g per kg of feed for 1 d. KEY WORDS: Gyrodactylosis . Rainbow trout Treatment. Drugs INTRODUCTION to the hooks of the opisthohaptor or to ulceration as a result of feeding by the parasite. The latter is the most The monogenean genus Gyrodactylus is widespread, serious. though some individual species have a restricted distri- Transmission takes place largely as a result of direct bution. Gyrodactyloses affect numerous freshwater contact between live fishes, though other pathways species including salmonids, cyprinids and ornamen- (contact between a live fish and a dead fish, or with tal fishes, as well as marine fishes including gadids, free-living parasites present in the substrate, or with pleuronectids and gobiids.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2014/0100249 A1 Sears Et Al
    US 201401.00249A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0100249 A1 Sears et al. (43) Pub. Date: Apr. 10, 2014 (54) THERAPEUTIC TREATMENT A63/37 (2006.01) A613 L/45 (2006.01) (71) Applicants: Douglas Sears, Oak Park, CA (US); A613 L/4458 (2006.01) Michael Reilly, Oak Park, CA (US) (52) U.S. Cl. CPC ............... A61K 45/06 (2013.01); A61 K3I/451 (72) Inventors: Douglas Sears, Oak Park, CA (US); (2013.01): A613 L/4458 (2013.01); A61 K Michael Reilly, Oak Park, CA (US) 3 1/137 (2013.01); A61 K31/165 (2013.01) USPC .......................................................... S14/325 (21) Appl. No.: 14/046,528 (57) ABSTRACT (22) Filed: Oct. 4, 2013 This invention discloses a treatment for a patient receiving O O medication to treat an attention deficit disorder Such as Related U.S. Application Data ADHD wherein the treatment results in a loss of appetite and (60) Provisional application No. 61/744,948, filed on Oct. impairment of the patient's attentiveness. The treatment com 9, 2012, now abandoned. bines a treatment for an attention deficit disorder with an appetite stimulant, wherein the appetite stimulant increases Publication Classification the caloric intake of a patient, which can increase the patients attentiveness. The combination treatment can be given for an (51) Int. Cl. indefinite, including, without limitation, life-long, to allow a A6 IK 45/06 (2006.01) patient to maintain normal caloric intake during treatment for A6 IK3I/65 (2006.01) an attention deficit disorder. 8aasaias: Patent Application Publication Apr. 10, 2014 Sheet 1 of 22 US 2014/010O249 A1 Figure i: improvement in Atiention with increased Caiotic intake 8aakast Patent Application Publication Apr.
    [Show full text]
  • Product List March 2019 - Page 1 of 53
    Wessex has been sourcing and supplying active substances to medicine manufacturers since its incorporation in 1994. We supply from known, trusted partners working to full cGMP and with full regulatory support. Please contact us for details of the following products. Product CAS No. ( R)-2-Methyl-CBS-oxazaborolidine 112022-83-0 (-) (1R) Menthyl Chloroformate 14602-86-9 (+)-Sotalol Hydrochloride 959-24-0 (2R)-2-[(4-Ethyl-2, 3-dioxopiperazinyl) carbonylamino]-2-phenylacetic 63422-71-9 acid (2R)-2-[(4-Ethyl-2-3-dioxopiperazinyl) carbonylamino]-2-(4- 62893-24-7 hydroxyphenyl) acetic acid (r)-(+)-α-Lipoic Acid 1200-22-2 (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 207557-35-5 1,1'-Carbonyl diimidazole 530-62-1 1,3-Cyclohexanedione 504-02-9 1-[2-amino-1-(4-methoxyphenyl) ethyl] cyclohexanol acetate 839705-03-2 1-[2-Amino-1-(4-methoxyphenyl) ethyl] cyclohexanol Hydrochloride 130198-05-9 1-[Cyano-(4-methoxyphenyl) methyl] cyclohexanol 93413-76-4 1-Chloroethyl-4-nitrophenyl carbonate 101623-69-2 2-(2-Aminothiazol-4-yl) acetic acid Hydrochloride 66659-20-9 2-(4-Nitrophenyl)ethanamine Hydrochloride 29968-78-3 2,4 Dichlorobenzyl Alcohol (2,4 DCBA) 1777-82-8 2,6-Dichlorophenol 87-65-0 2.6 Diamino Pyridine 136-40-3 2-Aminoheptane Sulfate 6411-75-2 2-Ethylhexanoyl Chloride 760-67-8 2-Ethylhexyl Chloroformate 24468-13-1 2-Isopropyl-4-(N-methylaminomethyl) thiazole Hydrochloride 908591-25-3 4,4,4-Trifluoro-1-(4-methylphenyl)-1,3-butane dione 720-94-5 4,5,6,7-Tetrahydrothieno[3,2,c] pyridine Hydrochloride 28783-41-7 4-Chloro-N-methyl-piperidine 5570-77-4
    [Show full text]
  • Strategies for Managing Sexual Dysfunction Induced by Antidepressant Medication
    King’s Research Portal DOI: 10.1002/14651858.CD003382.pub3 Document Version Publisher's PDF, also known as Version of record Link to publication record in King's Research Portal Citation for published version (APA): Taylor, M. J., Rudkin, L., Bullemor-Day, P., Lubin, J., Chukwujekwu, C., & Hawton, K. (2013). Strategies for managing sexual dysfunction induced by antidepressant medication. Cochrane Database of Systematic Reviews, (5). https://doi.org/10.1002/14651858.CD003382.pub3 Citing this paper Please note that where the full-text provided on King's Research Portal is the Author Accepted Manuscript or Post-Print version this may differ from the final Published version. If citing, it is advised that you check and use the publisher's definitive version for pagination, volume/issue, and date of publication details. And where the final published version is provided on the Research Portal, if citing you are again advised to check the publisher's website for any subsequent corrections. General rights Copyright and moral rights for the publications made accessible in the Research Portal are retained by the authors and/or other copyright owners and it is a condition of accessing publications that users recognize and abide by the legal requirements associated with these rights. •Users may download and print one copy of any publication from the Research Portal for the purpose of private study or research. •You may not further distribute the material or use it for any profit-making activity or commercial gain •You may freely distribute the URL identifying the publication in the Research Portal Take down policy If you believe that this document breaches copyright please contact [email protected] providing details, and we will remove access to the work immediately and investigate your claim.
    [Show full text]
  • The Study Programme for the Quality Management of Essential Medicines - Good Manufacturing Practical (GMP) and Inspection
    The Study Programme for the Quality Management of Essential Medicines - Good Manufacturing Practical (GMP) and Inspection - Country Reports Japan International Corporation of Welfare Services (JICWELS) Contents 1. Cambodia 1 2. Indonesia 70 3. Malaysia 91 4. Philippines 116 5. Sri Lanka 141 6. Thailand 161 The Study Programme for the Quality Management of Essential Medicines - Good Manufacturing Practical (GMP) and Inspection - Cambodia -1- KINGDOM OF CAMBODIA Nation Religion King Ministry of Health Department of Drugs and Food Country Report The Study Program on Quality Management of Essential Medicines Good Manufacturing Practice (GMP) and Inspection November 4, 2012 – November 30, 2012 Sponsored by : The Government of Japan Japan International Cooperation Agency (JICA) Department of Drugs and Food Ministry of Health, Cambodia. -2- I- COUNTRY PROFILE -3- A-Geography Cambodia is an agricultural country located in South East Asia which bordering the Gulf of Thailand, between Thailand, Vietnam, and Laos. Its approximate geographical coordinates are 13°N 105°E. Its 2,572 km border is split among Vietnam (1,228 km), Thailand (803 km) and Laos (541 km), as well as 443 km of coastline. Cambodia covers 181,035 square kilometers in the southwestern part of the Indochina, Cambodia lies completely within the tropics; its southernmost points are only slightly more than 10° above the equator. The country is bounded on the north by Thailand and by Laos, on the east and southeast by Vietnam, and on the west by the Gulf of Thailand and by Thailand. It consists of the Tonle Sap Basin and the Mekong Lowlands. To the southeast of this great basin is the Mekong Delta, which extends through Vietnam to the South China Sea.
    [Show full text]
  • Totalcare Medicaid 2017 Q2 GB
    Preferred Drug List Molina Healthcare of New York, Inc. 2017 *Molina mandates the use of generic drugs, if available. Brand names listed are for reference only. THIS LIST IS SUBJECT TO CHANGE. You can get more information and updates to this document on our website at www.molinahealthcare.com MCD_CO_ESIPREFDRUGQ3_0817_08/27/2017 6025633NY0417 Table of Contents Anti - Infectives....................................................................................................................................................3 Antineoplastic / Immunosuppressant Drugs ......................................................................................................12 Autonomic / Cns Drugs, Neurology / Psych ......................................................................................................17 Cardiovascular, Hypertension / Lipids...............................................................................................................34 Dermatologicals/Topical Therapy......................................................................................................................41 Diagnostics / Miscellaneous Agents ..................................................................................................................56 Ear, Nose / Throat Medications..........................................................................................................................64 Endocrine/Diabetes ............................................................................................................................................66
    [Show full text]
  • 1-(4-Amino-Cyclohexyl)
    (19) & (11) EP 1 598 339 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07D 211/04 (2006.01) C07D 211/06 (2006.01) 24.06.2009 Bulletin 2009/26 C07D 235/24 (2006.01) C07D 413/04 (2006.01) C07D 235/26 (2006.01) C07D 401/04 (2006.01) (2006.01) (2006.01) (21) Application number: 05014116.7 C07D 401/06 C07D 403/04 C07D 403/06 (2006.01) A61K 31/44 (2006.01) A61K 31/48 (2006.01) A61K 31/415 (2006.01) (22) Date of filing: 18.04.2002 A61K 31/445 (2006.01) A61P 25/04 (2006.01) (54) 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS NOCICEPTIN ANALOGS AND ORL1 LIGANDS FOR THE TREATMENT OF PAIN 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ON DERIVATE UND VERWANDTE VERBINDUNGEN ALS NOCICEPTIN ANALOGE UND ORL1 LIGANDEN ZUR BEHANDLUNG VON SCHMERZ DERIVÉS DE LA 1-(4-AMINO-CYCLOHEXYL)-1,3-DIHYDRO-2H-BENZIMIDAZOLE-2-ONE ET COMPOSÉS SIMILAIRES POUR L’UTILISATION COMME ANALOGUES DU NOCICEPTIN ET LIGANDES DU ORL1 POUR LE TRAITEMENT DE LA DOULEUR (84) Designated Contracting States: • Victory, Sam AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU Oak Ridge, NC 27310 (US) MC NL PT SE TR • Whitehead, John Designated Extension States: Newtown, PA 18940 (US) AL LT LV MK RO SI (74) Representative: Maiwald, Walter (30) Priority: 18.04.2001 US 284666 P Maiwald Patentanwalts GmbH 18.04.2001 US 284667 P Elisenhof 18.04.2001 US 284668 P Elisenstrasse 3 18.04.2001 US 284669 P 80335 München (DE) (43) Date of publication of application: (56) References cited: 23.11.2005 Bulletin 2005/47 EP-A- 0 636 614 EP-A- 0 990 653 EP-A- 1 142 587 WO-A-00/06545 (62) Document number(s) of the earlier application(s) in WO-A-00/08013 WO-A-01/05770 accordance with Art.
    [Show full text]
  • Drug Antioxidant Effects a Basis for Drug Selection?
    REVIEW ARTI LE Drugs 42 (4): 569-605, 1991 00 12-6667/ 91/ 00 I0-0569/ $ 18.50/0 © Adis International Limited. All rights reserved. DRU161 Drug Antioxidant Effects A Basis for Drug Selection? Barry Halliwell Pulmonary Medicine, UC Davis Medical Center, Sacramento , California, USA Contents 570 Summary 570 I. What is a Free Radical? 570 1.1 Definition of a Free Radical 57/ 1.2 Hydroxyl Radical 572 1.3 Formation of Oxygen Radicals In Vivo 574 1.4 Reactive Oxygen Species 575 1.5 Transition Metal Ions and Free Radical Reactions 575 1.6 Antioxidant Defence In Vivo: Intracellular 576 1.7 Antioxidant Defence In Vivo: Extracellular 579 2. Free Radical Damage to Cells and the Protective Ability of Antioxidants 579 2.1 Mechanisms of Cell Damage: The Molecular Targets 58/ 2.2 How to Characterise an Antioxidant 5 2 3. The Role of Free Radicals in Human Disease 582 3.1 Causation of Disease 582 3.2 A Significant Consequence of Disease Pathology 584 3.3 A General Consequence of Tissue Injury 585 3.4 What Can We Expect from Antioxidant Therapy? 586 586 4. Antioxidants in Disease Therapy 586 4.1 Use of Naturally Occurring Antioxidants and Derived Compounds 587 4.1.1 Superoxide Dismutase 587 4.1.2 Superoxide Dismutase 'Mimics' 588 4.1.3 a-Tocopherol 589 4.1.4 Ascorbic Acid (Vitamin C) 589 4.1.5 Adenosine 589 4.1.6 Lactoferrin 590 4.1.7 Nicotinamide 59/ 4.1.8 Glutathione and its Precursors 59/ 4.1.9 Carotenoids 59/ 4.2 'Synthetic' Antioxidants 59/ 4.2.1 Mercaptopropionylglycine and Other Thiols 592 4.2.2 Ebselen: A Glutathione Peroxidase Mimic? 593 4.2.3 Allopurinol, Oxypurinol and Other Xanth ine Oxidase Inhibitors 593 4.2.4 Inhibitors of the Generation of Reactive Oxygen Species by Phagocytes 595 4.2.5 Chelating Agents: Deferoxamine 595 4.2.6 Other Iron Chelators: Hydroxypyridones 596 4.2.7 Other Iron Chelators: ICRF-187 and the 'Lazaroids' 4.2.8 Probucol and Other Chain-Breaking Antioxidants 570 Drugs 42 (4) 1991 596 5.
    [Show full text]
  • )&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
    [Show full text]
  • Review Article
    Free Radical Biology & Medicine, Vol. 33, No. 6, pp. 774–797, 2002 Copyright © 2002 Elsevier Science Inc. Printed in the USA. All rights reserved 0891-5849/02/$–see front matter PII S0891-5849(02)00956-5 Review Article STRUCTURE AND FUNCTION OF XANTHINE OXIDOREDUCTASE: WHERE ARE WE NOW? ROGER HARRISON Department of Biology and Biochemistry, University of Bath, Bath, UK (Received 11 February 2002; Accepted 16 May 2002) Abstract—Xanthine oxidoreductase (XOR) is a complex molybdoflavoenzyme, present in milk and many other tissues, which has been studied for over 100 years. While it is generally recognized as a key enzyme in purine catabolism, its structural complexity and specialized tissue distribution suggest other functions that have never been fully identified. The publication, just over 20 years ago, of a hypothesis implicating XOR in ischemia-reperfusion injury focused research attention on the enzyme and its ability to generate reactive oxygen species (ROS). Since that time a great deal more information has been obtained concerning the tissue distribution, structure, and enzymology of XOR, particularly the human enzyme. XOR is subject to both pre- and post-translational control by a range of mechanisms in response to hormones, cytokines, and oxygen tension. Of special interest has been the finding that XOR can catalyze the reduction of nitrates and nitrites to nitric oxide (NO), acting as a source of both NO and peroxynitrite. The concept of a widely distributed and highly regulated enzyme capable of generating both ROS and NO is intriguing in both physiological and pathological contexts. The details of these recent findings, their pathophysiological implications, and the requirements for future research are addressed in this review.
    [Show full text]
  • Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
    Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate.
    [Show full text]