申请人:Otsuka Pharmaceutical Co., Ltd.
公开号:US04482560A1
公开(公告)日:1984-11-13
Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), then R.sup.4 should be neither a hydroxyl group nor a lower alkanoyl group.
具有抗组胺效果并可用作抗组胺剂的新型碳基苯并噻唑衍生物及其盐,由通式(1)表示,其中R1为氢原子,较低的烯基基团,较低的炔基基团或较低的烷基基团,其可以具有苯基(作为取代基);R2为氢原子,较低的烷基基团或苯基;R3为具有苯基(作为取代基)的较低烷基基团,或者是可以具有来自卤素原子,较低烷基基团和较低烷氧基的1至3个取代基的苯基;R4为氢原子,羟基或较低的烷酰基基团;X为卤素原子;Y为较低的烷基烯基基团,其可以具有氢氧基(作为取代基);n为0,1或2;在碳基苯并噻唑骨架中3-和4-位置之间的碳-碳键为单键或双键;前提是当R3为具有苯基(作为取代基)的较低烷基基团时,R4不应为羟基或较低的烷酰基基团。