| 摘要 |
<p>Benzoxazine or quinazoline derivatives (I) are used to prepare medicaments for preventing or treating cerebral edema. Benzoxazine or quinazoline derivatives of formula (I) are used to prepare medicaments for preventing or treating cerebral edema. a, d : 0 or 1; b, c : single or double bonds; X : O or N, provided that d = 0 when X is O and d = 1 when X is N; R 1-R 4H, halo, OH or 1-2C alkoxy; R 5, R 6H, 1-6C (cyclo)alkyl, or phenyl optionally substituted with halo, OH, 1-2C alkoxy, CF 3or NO 2; R 7H, OH or 1-3C alkyl or hydroxyalkyl; R 8O or NR 9R 10, provided that b is a single bond and c is a double bond when R 8is O and that b is a double bond and c is a single bond when T 8is NR 9R 10; R 9, R 10H, OH or 1-3C alkyl or hydroxyalkyl. Independent claims are also included for: (1) pharmaceutical composition comprising a compound (I) and a another compound (II) intended for preventing or treating cerebral edema, e.g. a glucocorticoid, glycerol, mannitol, furosemide, a barbiturate, an antibiotic, cytidine diphosphate choline, vinpocetin, a calcium inhibitor or an N-methyl-D-aspartate antagonist; (2) product comprising compounds (I) and (II) as a combination product for separate, simultaneous or sequential use for preventing or treating cerebral edema. [Image] ACTIVITY : Antiinflammatory; Cerebroprotective. Rats were treated orally for 5 days with desethyl-etifoxine (50 mg/kg, twice a day) and triethyltin (3 mg/kg). Brain water content was 80.24%, compared with 81.29% in the absence of desethyl-etifoxine MECHANISM OF ACTION : None given.</p> |
