| 摘要 |
<p>Biphenyl derivatives (I) are new. Biphenyl derivatives of formula (I) in free base or acid addition salt form are new. [Image] R1, R2H, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, halo, CF3, trifluoromethoxy, CN or 2-5C alkanoyl; R3H, OH, 1, 1-4C alkoxy, 3-6C cycloalkyloxy, halo, CN, 2-5C alkanoyl, carbamoyl, 1-4C alkyl sulphonyloxy or trifluoromethylsulphonyloxy; R4H, OH or 1-4C alkoxy; R5XNR7R8 or a group of formula (a)-(c); R61-4C alkyl; X : 1-4C alkylene; NR7R8a group of formula (d); Q : O, CH2 or CH2CH2 and R9-R14H, halo, 1-4C alkyl or 1-4C alkoxy. [Image] An independent claim is also included for the preparation of (I). ACTIVITY : Anticonvulsant; cerebroprotective; Vasotropic; Nootropic; Neuroleptic; Antidepressant; Tranquilizer; Antidiabetic; Antiemetic; Analgesic; Antiaddictive; Neuroprotective; Antiparkinsonian. (I) (no further details) reduce ischaemia-induced neuronal damage and ensuing symptoms in the middle cerebral artery (MCA) occlusion model in rats at a dosage of 1-50 mg/kg i.p., i.v. and p.o. MECHANISM OF ACTION : Glutamate Antagonist. (I) exhibit IC50 values of 0.1-100 mu M for binding to the veratridine sensitive sodium channel.</p> |
