VERLEYE, MARC,LE GUERN, MARIE-EMMANUELLE,GILLARDIN, JEAN-MARIE,HUBLOT, BERNARD
申请号:
EP09306018.4
公开号:
EP2179734B1
申请日:
2009.10.27
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
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.