| 摘要 |
<p>Carbostyril derivs. of formula (I) and their salts are new. (R1 is H, lower alkyl, phenyl lower alkyl, lower alkenyl or lower alkynyl. A is CO, CHOH, CH=CR2 or CH2.CHR2. B is lower alkylene. l is 0 or 1, but must be 1 if A is CO or CHOH. Y-Z is -CH2.N(R3)-, -CH2.CR4R5-, or -CH=CR4-. R2 is H or lower alkyl. R3 is phenyl (substd. by 1-3 of halo, lower alkyl, alkoxy, alkoxycarbonyl, alkylthio or alkanoyl, carboxy, hydroxy, nitro, amino or cyano), lower alkylenedioxy-phenyl, phenyl-lower alkyl or 1,2,3,4- tetrahydronaphthyl. R4 is phenyl (substd. by 1-3 of halo, lower alkyl or lower alkoxy or by one lower alkylenedioxy), phenyl-lower alkyl, 1,2,3,4-tetrahydronaphthyl or the gp. (II) R5 is H, hydroxy or alkanoyl. They are made e.g. by reacting a haloacyl- carbostyril with piperazine, piperidine etc. (I) have antihistamine activity (e.g. for treating allergies) and CNS-controlling effects (e.g. useful as hypnotics, sedatives, anxiolytics, antipsychotics, antipyretics, analgesics and antidepressants), but lack the side-effects usual with CNS-active cpds. Additionally, (I) increase the effects of anaesthetics and hypnotics and can be used diagnostically for measuring the secretion of gastric juices.</p> |
