DOCSLIB.ORG

(12) United States Patent (10) Patent No.: US 7,678,363 B2 Barlow 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 7,678,363 B2 Barlow Et Al USOO7678.363B2 (12) United States Patent (10) Patent No.: US 7,678,363 B2 Barlow et al. (45) Date of Patent: Mar. 16, 2010 (54) METHODS OF TREATING PSYCHIATRIC 5,093,333 A 3, 1992 Saab CONDITIONS COMPRISING 5,110,828 A 5/1992 Bromidge et al. ADMINISTRATION OF MUSCARINC 5,124,460 A 6/1992 Humphrey AGENTS IN COMBINATION WITH SSRIS 5,132,316 A 7/1992 Hadley et al. 5,137,895 A 8/1992 Munson, Jr. et al. (75) Inventors: Carrolee Barlow, Del Mar, CA (US); 4. S.4-1 1 YE Rabarti al. et al. Todd A.Carter, San Diego, CA (US); 5,260.314 A 1 1/1993 Sauerberg et al. Kym I Lorrain San Diego, CA (US); 5,262.427 A 1 1/1993 Nielson et al. Jammieson C. Pires, San Diego, CA 5,278,170 A 1/1994 Orlek et al. (US); Andrew Morse, San Diego, CA 5,286,864 A 2f1994 Walther et al. (US); Dana Gitnick, San Marcos, CA 5,314,901 A 5/1994 Bromidge et al. (US); Kai Treuner, San Diego, CA 5,324,724 A 6/1994 Orlek et al. (US); Alex Broadhead, San Diego, CA RE34,653 E 7, 1994 Tsukamoto et al. (US) 5,340,821 A 8, 1994 Abe et al. 5,356,912 A 10, 1994 Nielsen et al. 5,356,914 A 10/1994 Bromidge et al. (73) Assignee: BrainCells Inc, San Diego, CA (US) 5,362,739 A 11/1994 Orlek et al. 5,362,860 A 11, 1994 H tal. (*) Notice: Subject to any disclaimer, the term of this 5,384,408 A 1/1995 E. patent is extended or adjusted under 35 5,403,931 A 4, 1995 Tsukamoto et al. U.S.C. 154(b) by 409 days. 5,407,938 A 4, 1995 Fisher et al. 5,412,096 A 5/1995 Tsukamoto et al. (21) Appl. No.: 11/467,527 5,424.301 A 6/1995 Huang et al. 5,451,587 A 9, 1995 Walther et al. (22) Filed: Aug. 25, 2006 5,468.875 A 11, 1995 Sabb et al. 5,508.405 A 4/1996 Walther et al. (65) Prior Publication Data 5,510,478 A 4, 1996 Sabb 5,512,574 A 4/1996 Husbands et al. US 2007/OO49.576A1 Mar. 1, 2007 5,527,813 A 6/1996 Sauerberg et al. 5,534,520 A 7/1996 Fisher et al. Related U.S. Application Data 5,534,522 A 7/1996 Ando et al. 5,541,194 A 7/1996 Orlek et al. (60) Provisional application No. 60/71 1,846, filed on Aug. 5,545,740 A 8/1996 Hughes et al. 26, 2005, provisional application No. 60/727,127, 5,571,819 A 1 1/1996 Sabb filed on Oct. 14, 2005, provisional application No. 5,571,826. A 1 1/1996 Sauerberg et al. 60/738,133, filed on Nov. 17, 2005, provisional appli- 5,574,043 A 11/1996 Sauerberg et al. cation No. 60/803,826, filed on Jun. 2, 2006. 5,578,602 A 1 1/1996 Sauerberg et al. 5,580,880 A 12/1996 Handa et al. (51) Int. Cl. 5,599,937 A 2f1997 Glaset al. A6 IK 49/00 (2006.01) 5,605.908 A 2f1997 Merritt et al. A61 K 43/00 (2006.01) (Continued) AOIN 43/00 (2006.01) CO7C 213/OO (2006.01) FOREIGN PATENT DOCUMENTS (52) U.S. Cl. ................... 424/9.1: 514/183: 514/214.03; EP O32325 A1 T, 1989 564/347 (Continued) (58) Field of Classification Search ....................... None See application file for complete search history. OTHER PUBLICATIONS (56) References Cited Drugbank accession No. DB00472.* U.S. PATENT DOCUMENTS (Continued) 4,067,971 A 1/1978 Francis et al. Primary Examiner John D. Ulm 4,710,508 A 12/1987 Bergmeier et al. Assistant Examiner Stacey MacFarlane 4.786,648 A 1 1/1988 Bergmeier et al. (74) Attorney, Agent, or Firm Sughrue Mion, PLLC 4,855,290 A 8, 1989 Fisher et al. 4.866,077 A 9/1989 Bogeso et al. (57) ABSTRACT 4,870,081 A 9, 1989 Orlek et al. The instant disclosure describes methods for treating diseases 4,925,858 A 5/1990 Bogeso et al. and conditions of the central and peripheral nervous system 3. 38. St. et al. by stimulating or increasing neurogenesis. The disclosure 497,975 A 1 1/1990 Hadley et al. includes compositions and methods based on muscarinic 498 is 58 A 1/1991 Fisher et al. receptor modulation, Such as via inhibition of acetylcholine 4992.457 A 2f1991 Schulman et al. esterase (AChE) activity, alone or in combination with 4,996.210 A 2, 1991 Tsukamoto et al. another neurogenic agent to stimulate or activate the forma 5,041,455 A 8/1991 Sauerberg et al. tion of new nerve cells. 5,041,549 A 8, 1991 Tsukamoto et al. 5,043,345 A 8/1991 Sauerberg et al. 2 Claims, 15 Drawing Sheets US 7,678,363 B2 Page 2 U.S. PATENT DOCUMENTS WO WO99, 17771 A1 4f1999 WO WO99.5O247 A1 10, 1999 5,641,791 A 6/1997 Sauerberg et al. WO WOO1/O5763 A2 1, 2001 5,646.289 A 7/1997 Alt et al. WO WOO1,76571 A2 10, 2001 5,650,174 A 7, 1997 Muhammad et al. WO WOO1,83472 A1 11, 2001 RE35,593 E 8, 1997 Orlek et al. WO WO O2/OO3684 * 10/2002 5,665,745. A 9/1997 Alt et al. WO WOO2/O78629 A2 10, 2002 5,668,174 A 9, 1997 Kawagishi et al. WO WOO3,O28650 A2 4/2003 5,672,709 A 9/1997 Alt et al. WO WOO3/031412 A1 4, 2003 5,675,007 A 10/1997 Keogh et al. WO WOO3,057672 A2 7, 2003 5,756,501 A 5/1998 Sabb WO WOO3,057698 A2 7, 2003 5,773,458 A 6, 1998 Sabb et al. WO WOO3,059882 A1 T 2003 5,773,619 A 6, 1998 Bromidge et al. WO WOO3,091220 A1 11, 2003 5,808,075 A 9/1998 Bromidge et al. WO WO2004/034963 A2 4/2004 5,834,458. A 1 1/1998 Mitch WO WO2004/087158 A2 10, 2004 5,852,029 A 12/1998 Fisher et al. WO WO2004/089942 A2 10, 2004 5,902,814 A 5/1999 Gordon et al. WO WO2004/101603 A2 11/2004 RE36,374 E 11/1999 Bogeso et al. WO WO2005/041979 A1 5, 2005 5,981,545 A 11/1999 Jenkins et al. WO WO2005, O72713. A 8, 2005 6,051,581 A 4/2000 Gordon et al. WO WO2006/067494. A 6, 2006 6,103,734. A 8/2000 Ibanez WO WO2006/067496 A 6, 2006 6,174,886 B1 1/2001 Pineiro et al. 6,235,745 B1 5/2001 Megens OTHER PUBLICATIONS 6,237,645 B1 5/2001 Pountey 6,297.262 B1 10/2001 Sams-Dodd et al. Bromidge, Steven M., et al. “Design of R-(Z)-(+)-O- 6,468,560 B2 10/2002 Sauer et al. (Methoxyimino)-1-azabicyclo 2.2.2]octane-3-acetonitrile (SB 6,528,529 B1 3/2003 Brann et al. 202026), a Functionally Selective AZabicyclic Muscarinic M1 6,596,869 B2 7/2003 Hughes et al. Agonist Incorporating the N-Methoxy Imidoyl Nitrile Group as a 6,911,452 B2 6/2005 Schlienger Novel Ester Bioisostere”. J. Med. Chem. (1997) 19:40(26):4268 6,911.477 B2 6, 2005 Villalobos et al. 4280. 6.951,849 B2 10/2005 Kelly et al. Brown, Jason, et al. “Enriched environment and physical activity 2001/0003588 A1 6, 2001 Sauer et al. stimulate hippocampal but not olfactory bulb neurogenesis'. Eur 2001/0018074 A1 8/2001 Napper et al. Neurosci. (2003) 17(10):2042-2046. 2001/0036949 A1 11/2001 Coe et al. Cameron, H.A., et al. "Adult neurogenesis is regulated by adrenal 20O2/O127 271 A1 9, 2002 Van-Schie steroids in the dentate gyrus'. Neuroscience (1994) 61 (2):203-209. 2002/0150618 A1 10/2002 Napper et al. Cao, Y, et al. “Synthesis and biological characterization of 1-methyl 2003/0100545 A1 5/2003 Kelly et al. 1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives aS 2003/0129246 A1 7/2003 Napper et al. muscarinic agonists for the treatment of neurological disorders'. J. 2003. O144285 A1 7/2003 Brann et al. Med. Chem (2003) 46(20):4273-4286. 2003. O157169 A1 8, 2003 Sauer et al. Camps, P. et al. “Cholinergic Drugs in Pharmacotherapy of 2003/0176418 A1 9/2003 Skjaerbaek et al. Alzheimer's Disease'. Minireviews in Medicinal Chemistry (2002) 2005/O113357 A1 5/2005 Anderson et al. 2:11-25. 2005. O130961 A1 6, 2005 Davis et al. Eglen, Richard M., et al. “Selective Muscarinic Receptor Agonistand 2005/0209226 A1 9/2005 Skjaerbaek et al. Antagonists'. Pharmacol. Toxicol. (1996)78:59-68. 2007/00999.47 A1 5, 2007 Dean et al. Eisch, Amelia, J., et al. "Drug dependence and addiction II: Adult neurogenesis and drug addiction'. Am J Psychiatry (2004) FOREIGN PATENT DOCUMENTS 161(3):426. Fisher, Abraham "Muscarinic Receptor Agonists in Alzheimer's EP 311313 A2 12/1989 Disease—More Than Just Symptomatic Treatment?', CNS Drugs EP 370415 A1 5, 1990 (1999) 12(3): 197-214. EP 384285 A2 8, 1990 Fujimoto, J.M., et al. Intracerebroventricular Physostigmine-In EP 384288 A2 8, 1990 duced Analgesia: Enhancement by Naloxone, f-Funaltrexamine and EP 429.344 A1 5, 1991 Nor-Binaltorphimine and Antagonism by Dynorphin A (1-17)".
Load more

Recommended publications
  • [3H]-Piclamilast and [3H]-Rolipram
    JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 JPET FastThis articleForward. has not Published been copyedited on and January formatted. 24,The final2003 version as DOI:10.1124/jpet.102.047407 may differ from this version. Inhibitor Binding to Type 4 Phosphodiesterase (PDE4) Assessed Using [3H]-Piclamilast and [3H]-Rolipram Yu Zhao, Han-Ting Zhang, and James M. O’Donnell Department of Pharmacology University of Tennessee Health Science Center Downloaded from Memphis, Tennessee jpet.aspetjournals.org at ASPET Journals on September 27, 2021 1 Copyright 2003 by the American Society for Pharmacology and Experimental Therapeutics. JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 This article has not been copyedited and formatted. The final version may differ from this version. Running title: Inhibitor binding to PDE4 Correspondence should be addressed to: James M. O’Donnell, Ph.D. Department of Pharmacology University of Tennessee Health Science Center 874 Union Avenue Downloaded from Memphis, TN 38163 jpet.aspetjournals.org Phone: 901-448-3621 Fax: 901-448-3849 Email: [email protected] at ASPET Journals on September 27, 2021 Number of text page: 31 Number of tables: 3 Number of figures: 7 Number of references: 50 Number of words: Abstract (241); Introduction (716); Discussion (1544) Abbreviations: EHNA, erythro-9-(2-hydroxy-3-nonyl)adenine; HARBS, high-affinity rolipram binding site; LARBS, low-affinity rolipram binding site; IBMX, 3-isobutyl-1- methylxanthine; PDE, phosphodiesterase Section: Neuropharmacology 2 JPET Fast Forward. Published on January 24, 2003 as DOI: 10.1124/jpet.102.047407 This article has not been copyedited and formatted.
    [Show full text]
  • Calcium Channel Blocker As a Drug Candidate for the Treatment of Generalised Epilepsies
    UNIVERSITAT DE BARCELONA Faculty of Pharmacy and Food Sciences Calcium channel blocker as a drug candidate for the treatment of generalised epilepsies Final degree project Author: Janire Sanz Sevilla Bachelor's degree in Pharmacy Primary field: Organic Chemistry, Pharmacology and Therapeutics Secondary field: Physiology, Pathophysiology and Molecular Biology March 2019 This work is licensed under a Creative Commons license ABBREVIATIONS AED antiepileptic drug AMPA α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid ANNA-1 antineuronal nuclear antibody 1 BBB blood-brain barrier Bn benzyl BnBr benzyl bromide BnNCO benzyl isocyanate Boc tert-butoxycarbonyl Bu4NBr tetrabutylammonium bromide Ca+2 calcium ion CACNA1 calcium channel voltage-dependent gene cAMP cyclic adenosine monophosphate CCB calcium channel blocker cGMP cyclic guanosine monophosphate CH3CN acetonitrile Cl- chlorine ion Cmax maximum concentration CMV cytomegalovirus CTScan computed axial tomography DCM dichloromethane DIPEA N,N-diisopropylethylamine DMF dimethylformamide DMPK drug metabolism and pharmacokinetics DNET dysembryoplastic neuroepithelial tumours EEG electroencephalogram EPSP excitatory post-synaptic potential FDA food and drug administration Fe iron FLIPR fluorescence imaging plate reader fMRI functional magnetic resonance imaging GABA γ-amino-α-hydroxybutyric acid GAD65 glutamic acid decarboxylase 65 GAERS generalised absence epilepsy rat of Strasbourg GluR5 kainate receptor GTC generalised tonic-clonic H+ hydrogen ion H2 hydrogen H2O dihydrogen dioxide (water)
    [Show full text]
  • The Single Cyclic Nucleotide-Specific Phosphodiesterase of the Intestinal Parasite Giardia Lamblia Represents a Potential Drug Target
    RESEARCH ARTICLE The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target Stefan Kunz1,2*, Vreni Balmer1, Geert Jan Sterk2, Michael P. Pollastri3, Rob Leurs2, Norbert MuÈ ller1, Andrew Hemphill1, Cornelia Spycher1¤ a1111111111 1 Institute of Parasitology, Vetsuisse Faculty, University of Bern, Bern, Switzerland, 2 Division of Medicinal Chemistry, Faculty of Sciences, Amsterdam Institute of Molecules, Medicines and Systems (AIMMS), Vrije a1111111111 Universiteit Amsterdam, Amsterdam, The Netherlands, 3 Department of Chemistry and Chemical Biology, a1111111111 Northeastern University, Boston, Massachusetts, United States of America a1111111111 a1111111111 ¤ Current address: Euresearch, Head Office Bern, Bern, Switzerland * [email protected] Abstract OPEN ACCESS Citation: Kunz S, Balmer V, Sterk GJ, Pollastri MP, Leurs R, MuÈller N, et al. (2017) The single cyclic Background nucleotide-specific phosphodiesterase of the Giardiasis is an intestinal infection correlated with poverty and poor drinking water quality, intestinal parasite Giardia lamblia represents a potential drug target. PLoS Negl Trop Dis 11(9): and treatment options are limited. According to the Center for Disease Control and Preven- e0005891. https://doi.org/10.1371/journal. tion, Giardia infections afflict nearly 33% of people in developing countries, and 2% of the pntd.0005891 adult population in the developed world. This study describes the single cyclic nucleotide- Editor: Aaron R. Jex, University of Melbourne, specific phosphodiesterase (PDE) of G. lamblia and assesses PDE inhibitors as a new gen- AUSTRALIA eration of anti-giardial drugs. Received: December 5, 2016 Accepted: August 21, 2017 Methods Published: September 15, 2017 An extensive search of the Giardia genome database identified a single gene coding for a class I PDE, GlPDE.
    [Show full text]
  • Signal Transduction Guide
    Signal Transduction Product Guide | 2007 NEW! Selective T-type Ca2+ channel blockers, NNC 55-0396 and Mibefradil ZM 447439 – Novel Aurora Kinase Inhibitor NEW! Antibodies for Cancer Research EGFR-Kinase Selective Inhibitors – BIBX 1382 and BIBU 1361 DRIVING RESEARCH FURTHER Calcium Signaling Agents ...................................2 G Protein Reagents ...........................................12 Cell Cycle and Apoptosis Reagents .....................3 Ion Channel Modulators ...................................13 Cyclic Nucleotide Related Tools ...........................7 Lipid Signaling Agents ......................................17 Cytokine Signaling Agents ..................................9 Nitric Oxide Tools .............................................19 Enzyme Inhibitors/Substrates/Activators ..............9 Protein Kinase Reagents....................................22 Glycobiology Agents .........................................12 Protein Phosphatase Reagents ..........................33 Neurochemicals | Signal Transduction Agents | Peptides | Biochemicals Signal Transduction Product Guide Calcium Signaling Agents ......................................................................................................................2 Calcium Binding Protein Modulators ...................................................................................................2 Calcium ATPase Modulators .................................................................................................................2 Calcium Sensitive Protease
    [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]
  • Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Cr
    Drug Name Plate Number Well Location % Inhibition, Screen Axitinib 1 1 20 Gefitinib (ZD1839) 1 2 70 Sorafenib Tosylate 1 3 21 Crizotinib (PF-02341066) 1 4 55 Docetaxel 1 5 98 Anastrozole 1 6 25 Cladribine 1 7 23 Methotrexate 1 8 -187 Letrozole 1 9 65 Entecavir Hydrate 1 10 48 Roxadustat (FG-4592) 1 11 19 Imatinib Mesylate (STI571) 1 12 0 Sunitinib Malate 1 13 34 Vismodegib (GDC-0449) 1 14 64 Paclitaxel 1 15 89 Aprepitant 1 16 94 Decitabine 1 17 -79 Bendamustine HCl 1 18 19 Temozolomide 1 19 -111 Nepafenac 1 20 24 Nintedanib (BIBF 1120) 1 21 -43 Lapatinib (GW-572016) Ditosylate 1 22 88 Temsirolimus (CCI-779, NSC 683864) 1 23 96 Belinostat (PXD101) 1 24 46 Capecitabine 1 25 19 Bicalutamide 1 26 83 Dutasteride 1 27 68 Epirubicin HCl 1 28 -59 Tamoxifen 1 29 30 Rufinamide 1 30 96 Afatinib (BIBW2992) 1 31 -54 Lenalidomide (CC-5013) 1 32 19 Vorinostat (SAHA, MK0683) 1 33 38 Rucaparib (AG-014699,PF-01367338) phosphate1 34 14 Lenvatinib (E7080) 1 35 80 Fulvestrant 1 36 76 Melatonin 1 37 15 Etoposide 1 38 -69 Vincristine sulfate 1 39 61 Posaconazole 1 40 97 Bortezomib (PS-341) 1 41 71 Panobinostat (LBH589) 1 42 41 Entinostat (MS-275) 1 43 26 Cabozantinib (XL184, BMS-907351) 1 44 79 Valproic acid sodium salt (Sodium valproate) 1 45 7 Raltitrexed 1 46 39 Bisoprolol fumarate 1 47 -23 Raloxifene HCl 1 48 97 Agomelatine 1 49 35 Prasugrel 1 50 -24 Bosutinib (SKI-606) 1 51 85 Nilotinib (AMN-107) 1 52 99 Enzastaurin (LY317615) 1 53 -12 Everolimus (RAD001) 1 54 94 Regorafenib (BAY 73-4506) 1 55 24 Thalidomide 1 56 40 Tivozanib (AV-951) 1 57 86 Fludarabine
    [Show full text]
  • Phosphodiesterase (PDE)
    Phosphodiesterase (PDE) Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules. www.MedChemExpress.com 1 Phosphodiesterase (PDE) Inhibitors, Activators & Modulators (+)-Medioresinol Di-O-β-D-glucopyranoside (R)-(-)-Rolipram Cat. No.: HY-N8209 ((R)-Rolipram; (-)-Rolipram) Cat. No.: HY-16900A (+)-Medioresinol Di-O-β-D-glucopyranoside is a (R)-(-)-Rolipram is the R-enantiomer of Rolipram. lignan glucoside with strong inhibitory activity Rolipram is a selective inhibitor of of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM phosphodiesterase. and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg (R)-DNMDP (S)-(+)-Rolipram Cat. No.: HY-122751 ((+)-Rolipram; (S)-Rolipram) Cat. No.: HY-B0392 (R)-DNMDP is a potent and selective cancer cell (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, AMP(cAMP)-specific phosphodiesterase (PDE) binds PDE3A directly.
    [Show full text]
  • A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache
    University of South Florida Masthead Logo Scholar Commons School of Information Faculty Publications School of Information 7-2015 A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache Authors: Jeffrey L. Jackson, Elizabeth Cogbill, Rafael Santana-Davila, Christina Eldredge, William Collier, Andrew Gradall, Neha Sehgal, and Jessica Kuester OBJECTIVE: To compare the effectiveness and side effects of migraine prophylactic medications. DESIGN: We performed a network meta-analysis. Data were extracted independently in duplicate and quality was assessed using both the JADAD and Cochrane Risk of Bias instruments. Data were pooled and network meta-analysis performed using random effects models. DATA SOURCES: PUBMED, EMBASE, Cochrane Trial Registry, bibliography of retrieved articles through 18 May 2014. ELIGIBILITY CRITERIA FOR SELECTING STUDIES: We included randomized controlled trials of adults with migraine headaches of at least 4 weeks in duration. RESULTS: Placebo controlled trials included alpha blockers (n = 9), angiotensin converting enzyme inhibitors (n = 3), angiotensin receptor blockers (n = 3), anticonvulsants (n = 32), beta-blockers (n = 39), calcium channel blockers (n = 12), flunarizine (n = 7), serotonin reuptake inhibitors (n = 6), serotonin norepinephrine reuptake inhibitors (n = 1) serotonin agonists (n = 9) and tricyclic antidepressants (n = 11). In addition there were 53 trials comparing different drugs. Drugs with at least 3 trials that were more effective than placebo for episodic migraines
    [Show full text]
  • Medicine for Prevention of and Treatment for Arteriosclerosis and Hypertension
    Europäisches Patentamt *EP001604664A1* (19) European Patent Office Office européen des brevets (11) EP 1 604 664 A1 (12) EUROPEAN PATENT APPLICATION published in accordance with Art. 158(3) EPC (43) Date of publication: (51) Int Cl.7: A61K 31/4422, A61K 45/06, 14.12.2005 Bulletin 2005/50 A61P 9/00, A61P 9/10, A61P 43/00, A61P 9/12, (21) Application number: 04706359.9 A61P 13/12 (22) Date of filing: 29.01.2004 (86) International application number: PCT/JP2004/000861 (87) International publication number: WO 2004/067003 (12.08.2004 Gazette 2004/33) (84) Designated Contracting States: • IWAI, Masaru AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Shigenobu-cho, Onsen-gun, HU IE IT LI LU MC NL PT RO SE SI SK TR Ehime 791-0204 (JP) Designated Extension States: • SADA, Toshio, Sankyo Company, Limited AL LT LV MK Tokyo 140-8710 (JP) • MIZUNO, Makoto, Sankyo Company, Limited (30) Priority: 31.01.2003 JP 2003022990 Tokyo 140-8710 (JP) 07.02.2003 JP 2003030830 (74) Representative: Gibson, Christian John Robert (71) Applicant: Sankyo Company, Limited Marks & Clerk Tokyo 103-8426 (JP) 90 Long Acre London WC2E 9RA (GB) (72) Inventors: • HORIUCHI, Masatsugu Onsen-gun, Ehime 791-0204 (JP) (54) MEDICINE FOR PREVENTION OF AND TREATMENT FOR ARTERIOSCLEROSIS AND HYPERTENSION (57) A medicament comprising the following composition: (A) an angiotensin II receptor antagonist selected from the group of a compound having a general formula (I), pharmacologically acceptable esters thereof and pharmacolog- ically acceptable salts thereof (for example, olmesartan medoxomil and the like); EP 1 604 664 A1 Printed by Jouve, 75001 PARIS (FR) (Cont.
    [Show full text]
  • Original Article the Effects of Azelnidipine and Amlodipine in Treatment of Mild to Moderate Hypertension: a Systematic Review
    Int J Clin Exp Med 2017;10(7):11273-11281 www.ijcem.com /ISSN:1940-5901/IJCEM0010270 Original Article The effects of azelnidipine and amlodipine in treatment of mild to moderate hypertension: a systematic review Yu Xiao1, Gang Hu2 1Research Institute of Philosophy & Culture, Sichuan Academy of Social Sciences, Chengdu, Sichuan, China; 2De- partment of Breast Surgery, Sichuan Provincial People’s Hospital, Sichuan Academy of Medical Science, China Received May 16, 2015; Accepted June 27, 2017; Epub July 15, 2017; Published July 30, 2017 Abstract: Hypertension is an important risk factor for patients with cardiovascular disease. Long-acting calcium channel blockers are frequently used to treat patients with mild to moderate hypertension, among which azelnidip- ine and amlodipine are two dihydropyridine (DHP) type calcium channel blockers that are widely used in Japan and China. We offer a current evaluation and comparison of the efficacy and safety of azelnidipine with amlodipine. To confirm location of all relevant trials databases including Cochrane Handbook 5.1, CBM (1966 to December 2014), CNKI (1911 to December 2014), EMBASE (1966 to December 2014), and Medline (1950 to December 2014), were searched to identify randomized controlled trials (RCT) assessing the effects and safety of azelnidipine. Studies included were assessed using the RevMan 5.1. STATA 10.0 for meta-analysis. Based on study quality and other selection criteria, 19 of 405 studies were selected for the meta-analysis (subjects=1,482). Data show that lowered systolic pressure of azelnidipine were similar to those of amlodipine and there were no significant differences be- tween azelnidipine and amlodipine for mild to moderate hypertension (relative risk=1.00, 95% confidence interval 0.92-1.10).
    [Show full text]
  • General Pharmacology
    GENERAL PHARMACOLOGY Winners of “Nobel” prize for their contribution to pharmacology Year Name Contribution 1923 Frederick Banting Discovery of insulin John McLeod 1939 Gerhard Domagk Discovery of antibacterial effects of prontosil 1945 Sir Alexander Fleming Discovery of penicillin & its purification Ernst Boris Chain Sir Howard Walter Florey 1952 Selman Abraham Waksman Discovery of streptomycin 1982 Sir John R.Vane Discovery of prostaglandins 1999 Alfred G.Gilman Discovery of G proteins & their role in signal transduction in cells Martin Rodbell 1999 Arvid Carlson Discovery that dopamine is neurotransmitter in the brain whose depletion leads to symptoms of Parkinson’s disease Drug nomenclature: i. Chemical name ii. Non-proprietary name iii. Proprietary (Brand) name Source of drugs: Natural – plant /animal derivatives Synthetic/semisynthetic Plant Part Drug obtained Pilocarpus microphyllus Leaflets Pilocarpine Atropa belladonna Atropine Datura stramonium Physostigma venenosum dried, ripe seed Physostigmine Ephedra vulgaris Ephedrine Digitalis lanata Digoxin Strychnos toxifera Curare group of drugs Chondrodendron tomentosum Cannabis indica (Marijuana) Various parts are used ∆9Tetrahydrocannabinol (THC) Bhang - the dried leaves Ganja - the dried female inflorescence Charas- is the dried resinous extract from the flowering tops & leaves Papaver somniferum, P album Poppy seed pod/ Capsule Natural opiates such as morphine, codeine, thebaine Cinchona bark Quinine Vinca rosea periwinkle plant Vinca alkaloids Podophyllum peltatum the mayapple
    [Show full text]
  • Jp Xvii the Japanese Pharmacopoeia
    JP XVII THE JAPANESE PHARMACOPOEIA SEVENTEENTH EDITION Official from April 1, 2016 English Version THE MINISTRY OF HEALTH, LABOUR AND WELFARE Notice: This English Version of the Japanese Pharmacopoeia is published for the convenience of users unfamiliar with the Japanese language. When and if any discrepancy arises between the Japanese original and its English translation, the former is authentic. The Ministry of Health, Labour and Welfare Ministerial Notification No. 64 Pursuant to Paragraph 1, Article 41 of the Law on Securing Quality, Efficacy and Safety of Products including Pharmaceuticals and Medical Devices (Law No. 145, 1960), the Japanese Pharmacopoeia (Ministerial Notification No. 65, 2011), which has been established as follows*, shall be applied on April 1, 2016. However, in the case of drugs which are listed in the Pharmacopoeia (hereinafter referred to as ``previ- ous Pharmacopoeia'') [limited to those listed in the Japanese Pharmacopoeia whose standards are changed in accordance with this notification (hereinafter referred to as ``new Pharmacopoeia'')] and have been approved as of April 1, 2016 as prescribed under Paragraph 1, Article 14 of the same law [including drugs the Minister of Health, Labour and Welfare specifies (the Ministry of Health and Welfare Ministerial Notification No. 104, 1994) as of March 31, 2016 as those exempted from marketing approval pursuant to Paragraph 1, Article 14 of the Same Law (hereinafter referred to as ``drugs exempted from approval'')], the Name and Standards established in the previous Pharmacopoeia (limited to part of the Name and Standards for the drugs concerned) may be accepted to conform to the Name and Standards established in the new Pharmacopoeia before and on September 30, 2017.
    [Show full text]