| 摘要 |
Atropisomers of formula (Ia) may be used for treating or preventing a condition selected from cerebral deficits subsequent to or resulting from cardiac bypass surgery and grafting, stroke, cerebral ischemia, spinal cord trauma, head trauma, Alzheimer's Disease, Huntington's Chorea, amyotrophic lateral sclerosis, epilepsy, AIDS-induced dementia, perinatal hypoxia, hypoxia, cardiac arrest, hypoglycemic neuronal damage, opiate tolerance, alcohol and drug addiction withdrawal, idiopathic and drug induced Parkinson's Disease or brain edema, muscular spasms, migraine headaches, urinary incontinence, psychosis, convulsions, chronic or acute pain, ocular damage, retinopathy, retinal neuropathy, tinnitus, anxiety, emesis and tardive dyskinesia. In formula Ia, R2 is a phenyl group of the formula Ph2, a six membered containing heterocycle of formula II or a five membered heterocycle of formula III; R3 is hydrogen, halo, CN, NO2, CF3, alkyl or alkoxy; R5 is alkyl, halo, CF3, alkoxy or alkylthio; and R6, R7 and R8 are hydrogen or halo. Examples of compounds of formula (Ia) include: (S)-3-(2-chloro-phenyl)-2-[2-(5-diethylaminomethyl-2-fluoro-phenyl)- vinyl]-6-fluoro-3H-quinazolin-4-one; (S)-3-(2-chloro-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one; (S)-3-(2-chloro-phenyl)-2-[2-(4-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one; (S)-3-(2-chloro-phenyl)-2-[2-(6-ethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one; (S)-3-(2-bromo-phenyl)-2-[2-(6-diethylaminomethyl-pyridin-2-yl)-vinyl]-6-fluoro-3H-quinazolin-4-one; (S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(6-methoxymethyl-pyridin-2-yl)-vinyl]-3H-quinazolin-4-one; (S)-3-(2-chloro-phenyl)-6-fluoro-2-[2-(4-methyl-pyrimidine-2-yI)-vinyl]-3H-quinazolin-4-one; ( S)-3-(2-chloro-phenyl)-6-fluoro-2-{2-[6-(isopropylamino-methyl)-pyridin-2-yl]-ethyl}-3H-quinazolin-4-one; and (S)-6-fluoro-2-[2-(2-methyl-thiazol-4-yl)-vinyl]-3-(2-methyl-phenyl)-3H-quinazolin-4-one.
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