Global Patent Index - EP 1651235 A4

EP 1651235 A4 20081217 - SIGMA-1 RECEPTOR LIGAND WITH ACETYLCHOLINESTERASE INHIBITION PROPERTIES

Title (en)

SIGMA-1 RECEPTOR LIGAND WITH ACETYLCHOLINESTERASE INHIBITION PROPERTIES

Title (de)

SIGMA-1 REZEPTOR-LIGAND MIT ACETYLCHOLINESTERASE-HEMMENDEN EIGENSCHAFTEN

Title (fr)

LIGAND DU RECEPTEUR SIGMA-1 PRESENTANT DES PROPRIETES D'INHIBITION DE L'ACETYLCHOLINESTERASE

Publication

EP 1651235 A4 20081217 (EN)

Application

EP 04757425 A 20040805

Priority

  • US 2004025295 W 20040805
  • US 49276903 P 20030805

Abstract (en)

[origin: WO2005016276A2] A novel compound and method for preventing or treating neurodegenerative diseases by inhibiting acetylcholinesterase and binding the sigma-1 receptor are disclosed. Dimethylcarbamic acid 2,3-bis-dimethylcarbamoyloxy-6-[4-(4-ethyl-piperazin-yl)-butyryl]-phenyl ester and its derivatives represent a novel therapeutic strategy against beta-amyloid peptide induced neurotoxicity, in inhibiting acetylcholinesterase, in improving cholinergic transmission, in binding the sigma-l receptor, and in releasing a metabolite that is active both as a sigma-1 receptor ligand and an antioxidant.

IPC 8 full level

A61K 31/56 (2006.01); A61K 31/495 (2006.01); A61P 25/28 (2006.01); C07D 241/04 (2006.01)

IPC 8 main group level

A61K (2006.01)

CPC (source: EP)

A61K 31/495 (2013.01); A61P 25/00 (2017.12); A61P 25/28 (2017.12); A61P 43/00 (2017.12)

Citation (search report)

  • [X] US 3284453 A 19661108 - STEPHEN TOMCUFCIK ANDREW, et al
  • [X] US 5143910 A 19920901 - ONOUE HIROSHI [JP], et al
  • [X] GB 846795 A 19600831 - HENRI MORREN
  • [X] FR 2339401 A1 19770826 - ORSYMONDE [FR]
  • [X] US 2003144285 A1 20030731 - BRANN MARK [US], et al
  • [A] EP 0602242 A1 19940622 - YOSHITOMI PHARMACEUTICAL [JP]
  • [X] CHITI W ET AL: "Synthesis of some new p-hydroxypropiophenone derivatives with local anesthetic activity", FARMACO, EDIZIONE SCIENTIFICA, SOCIETA CHIMICA ITALIANA, PAVIA, vol. 15, 1 January 1960 (1960-01-01), pages 773 - 787, XP009108062, ISSN: 0430-0920
  • [X] PERRONE ROBERTO ET AL: "Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT(7) receptor ligands.", JOURNAL OF MEDICINAL CHEMISTRY 13 FEB 2003, vol. 46, no. 4, 13 February 2003 (2003-02-13), pages 646 - 649, XP002502303, ISSN: 0022-2623
  • [X] CHAWLA H P S ET AL: "AGENTS ACTING ON THE CENTRAL NERVOUS SYSTEM. XII. 3-T-AMINOPROPIOPHENONES AS CENTRAL MUSCLE RELAXANTS AND DIURETICS", JOURNAL OF MEDICINAL CHEMISTRY, US AMERICAN CHEMICAL SOCIETY. WASHINGTON, vol. 13, no. 3, 1 January 1970 (1970-01-01), pages 480 - 488, XP001183938, ISSN: 0022-2623
  • [X] KASE YOSHITOSHI ET AL: "Chemical-pharmacological studies on antitussives. II. Site of antitussive action of 1-(3,4-dihydroxyphenacyl)-4-(2-hydroxypropyl)pi perazine dihydrochloride", YAKUGAKU ZASSHI - JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, JP, vol. 825, 1 January 1962 (1962-01-01), pages 1298 - 1302, XP009108068, ISSN: 0031-6903
  • [X] SHAO G X ET AL: "Synthesis of catechol aminoketone and its analogs", YAO HSUEH HSUEH PAO - ACTA PHARMACEUTICA SINICA, BEIJING, CN, vol. 25, no. 2, 1 January 1990 (1990-01-01), pages 101 - 109, XP009108052, ISSN: 0513-4870
  • [X] YOKOYAMA MATATSUGU ET AL: "Phenacylpiperazine derivatives", YAKUGAKU KENKYU - JAPANESE JOURNAL OF PHARMACY AND CHEMISTRY, SN, JP, vol. 33, 1 January 1961 (1961-01-01), pages 752 - 757, XP009108069, ISSN: 0372-7734
  • [X] NATOVA L ET AL: "On the preparation and Structure of some Mannich Basis Prepared from Hydroxy - and Methoxyacetophenons = Synthesis and structure of some Mannich bases obtained from hydroxy- and methoxyacetophenones", GODISNIK NA VISSIA HIMIKOTEHNOLOGICLESKI INSTITUT-SOFIA -ANNUAIRE DE L'INSTITUT CHIMICO-TECHNOLOGIQUE, SOFIA, BG, vol. 24, no. 4, 1 January 1981 (1981-01-01), pages 57 - 66, XP009108051, ISSN: 0489-6211
  • [X] GRINSTEINS V ET AL: "Synthesis and study of potential catechol-O-methyltransferase inhibitors. Synthesis of some nitrogen-containing pyrocatechol derivatives", AKADEMIYA NAUK LATVIISKOI S.S.R. IZVESTIYA. SERIYA KHIMICHESKAYA, IZDEVEJS ZINATNE TURGENEVA, RIGA, LV, no. 5, 1 January 1968 (1968-01-01), pages 593 - 596, XP009108050, ISSN: 0002-3248
  • [A] MATSUNO KIYOSHI ET AL: "SA4503, a novel cognitive enhancer, with sigma-1 receptor agonistic properties", BEHAVIOURAL BRAIN RESEARCH, vol. 83, no. 1-2, 1997, pages 221 - 224, XP002502305, ISSN: 0166-4328
  • See references of WO 2005016276A2

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PL PT RO SE SI SK TR

Designated extension state (EPC)

AL HR LT LV MK

DOCDB simple family (publication)

WO 2005016276 A2 20050224; WO 2005016276 A3 20050707; AU 2004264342 A1 20050224; CA 2534777 A1 20050224; CN 1863536 A 20061115; EP 1651235 A2 20060503; EP 1651235 A4 20081217; JP 2007501254 A 20070125

DOCDB simple family (application)

US 2004025295 W 20040805; AU 2004264342 A 20040805; CA 2534777 A 20040805; CN 200480028827 A 20040805; EP 04757425 A 20040805; JP 2006522719 A 20040805