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Title (En) Benzoxazine and Dihydroquinazoline Derivatives for Use in the Treatment of Alcohol Withdrawal Syndrome

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Title (En) Benzoxazine and Dihydroquinazoline Derivatives for Use in the Treatment of Alcohol Withdrawal Syndrome Title (en) Benzoxazine and dihydroquinazoline derivatives for use in the treatment of alcohol withdrawal syndrome Title (de) Benzoxazin- und Dihydrochinazolinderivate zur Verwendung in der Behandlung von Alkoholentzugssyndrom Title (fr) Dérivés de la benzoxazine et de la dihydroquinazoline pour leur utilisation dans le traitement du syndrome de sevrage alcoolique Publication EP 2179734 A1 20100428 (FR) Application EP 09306018 A 20091027 Priority FR 0857277 A 20081027 Abstract (en) Use of benzoxazine and dihydroquinazoline derivatives (I) and their salts for the prevention or treatment of alcohol withdrawal syndrome, is claimed. Use of benzoxazine and dihydroquinazoline derivatives of formula (I) and their salts for the prevention or treatment of alcohol withdrawal syndrome, is claimed. X : O or N; R 1-R 4 : H, halo (preferably F, Cl, Br or I), OH or 1-2C alkoxyl; R 5, R 6 : H, 1-6C alkyl, 1-6C cycloalkyl or 6C aryl (optionally substituted by at least one halo, OH, 1-2C alkoxyl, trifluoromethyl or nitro); R 7 : H, OH, 1-3C alkyl or 1-3C hydroxyalkyl; R 8 : O or NR 9R 1 0; R 9, R 1 0 : H, OH, 1-3C alkyl or 1-3C hydroxyalkyl; a, d : 0 or 1; and b, c : single bond or double bond. Provided that: when X is an oxygen atom then d is 0, and when X is a nitrogen atom then d is 1; and when R 8 is an oxygen atom then a is 1, b is a single bond and c is a double bond and when R 8 is NR 9R 1 0 then a is 0, b is a double bond and c is a single bond. Independent claims are included for: (1) a composition comprising (I), and at least an additional compound comprising meprobamate, tetrabamate, clomethiazole, acamprosate, a beta-blocker, clonidine, thiamine, and pyridoxine, in combination with a vehicle; and (2) products containing: (I); and the additional compound as a combination product for simultaneous, separate or sequential administration. [Image] ACTIVITY : Antialcoholic; Anticonvulsant; Tranquilizer; Gastrointestinal-Gen.; Hypnotic; CNS-Gen.; Inotropic; Antiarrhythmic; Hypotensive; Anabolic; Eating-Disorders-Gen.; Antiemetic; Nootropic; Neuroleptic; Dermatological. MECHANISM OF ACTION : Gamma-aminobutyric acid A receptor binder. Abstract (fr) La présente invention concerne un composé de formule (I) suivante : ou un sel pharmaceutiquement acceptable de celui-ci, pour son utilisation dans la prévention ou le traitement du syndrome de sevrage alcoolique. IPC 8 full level A61K 31/517 (2006.01); A61K 31/536 (2006.01); A61P 25/32 (2006.01) CPC (source: EP) A61K 31/517 (2013.01); A61K 31/536 (2013.01); A61K 45/06 (2013.01); A61P 25/32 (2018.01) C-Set (source: EP) A61K 31/517 + A61K 2300/00 Citation (applicant) • FR 1571287 A 19690620 • COUZIGOU; LEDINGHEN, GASTROENTEROL. CLIN. BIOL., vol. 26, 2002, pages B163 - B168 • BUCHER; REDETZKI: "La méthode enzymatique", KLIN WOCHENSCHR, vol. 29, 1951, pages 615 - 616 • WATSON; LITTLE, J PHARMACOL EXP THER, vol. 272, 1995, pages 876 - 884 • CRAWLEY; GOODWIN, PHARMACOL BIOCHEM BEHAV, vol. 13, 1980, pages 167 - 170 • WATSON; LITTLE, PSYCHOPHARMACOLOGY, vol. 114, 1994, pages 329 - 336 • MURRAY ET AL., PHARMACOL BIOCHEM BEHAV, vol. 15, 1981, pages 135 - 140 Citation (search report) • [X] WO 2006098969 A2 20060921 - MERCK & CO INC [US], et al • [X] WO 2007109288 A2 20070927 - XYTIS INC [US], et al • [Y] WO 0113921 A1 20010301 - OCKERT DAVID M [US] • [A] EP 1745785 A1 20070124 - BIOCODEX [FR] • [A] EP 1745786 A1 20070124 - BIOCODEX [FR] • [X] SHARMA, A.N.; UGALE, R.R.; CHOPDE, C.T. (INDIAN J PHARMACOL 2005, 37(SUPPL.): S22): "Reversal of ethanol withdrawal anxiety by non-benzodiazepine anxiolytic etifoxine: Role for neurosteroid allopregnanolone", BIOMEDICAL LITERATURE REFERENCE FROM PROUS SCIENCE INTEGRITY., 2005, XP002534089, Retrieved from the Internet <URL:http://integrity.prous.com/integrity/servlet/xmlxsl/ pk_ref_list.xml_show_llistat_refs?> • [Y] SHARMA ET AL: "Chronic progesterone treatment augments while dehydroepiandrosterone sulphate prevents tolerance to ethanol anxiolysis and withdrawal anxiety in rats", EUROPEAN JOURNAL OF PHARMACOLOGY, ELSEVIER BV, NL, vol. 567, no. 3, 27 June 2007 (2007-06-27), pages 211 - 222, XP022132884, ISSN: 0014-2999 • [XP] VERLEYE M ET AL: "The anxiolytic etifoxine protects against convulsant and anxiogenic aspects of the alcohol withdrawal syndrome in mice", ALCOHOL, PERGAMON PRESS, LONDON, GB, vol. 43, no. 3, 1 May 2009 (2009-05-01), pages 197 - 206, XP026021430, ISSN: 0741-8329, [retrieved on 20090423] • [A] MARC VERLEYE ET AL: "Effects of etifoxine on ligand binding to GABAA receptors in rodents", NEUROSCIENCE RESEARCH, ELSEVIER, SHANNON, IR, vol. 44, 1 January 2002 (2002-01-01), pages 167 - 172, XP007908404, ISSN: 0168-0102 Designated contracting state (EPC) AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR Designated extension state (EPC) AL BA RS DOCDB simple family (publication) EP 2179734 A1 20100428; EP 2179734 B1 20140226; FR 2937552 A1 20100430; FR 2937552 B1 20110506 DOCDB simple family (application) EP 09306018 A 20091027; FR 0857277 A 20081027.
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