申请人:ONO PHARMACEUTICAL CO., LTD.
公开号:EP0109255A2
公开(公告)日:1984-05-23
57 Glycerol derivatives of the general formula:
[wherein A represents an oxygen atom or a carbonyloxy group (i.e. -O-CO-, in which the carbonyl group should be attached to a group R3 and the oxa group should be attached to the carbon atom at the third position of the glycerol skeleton), R1 represents an alkyl group of 6 to 22 carbom atoms, or an alkyl group of 2 to 5 carbon atoms being substituted by a phenyl group, R2 represents an azido group (-N3 group), an amino group (-NH2 group) or a group of the general formula: -NHCOR5, - NHCOOR5 or -NHCONHR5, in which R5 represents an alkyl group of 1 to 10 carbon atoms or a phenyl group, with the proviso that, when A represents a carbonyloxy group, R2 does not represent an amino group, R3 represents an alkylene group of 1 to 12 carbon atoms and R4 represents an amino group, or a group of the general formula: -NHCOR6, -NHR7, -N(R7)2 or (R7)3 . , in which R6 represents an alkyl group of 1 to 6 carbon atoms or a phenyl group, R7 represents an alkyl group of 1 to 8 carbon atoms, with the proviso that, when R4 repre- sents a group of the formula: -N(R7)2 or (R7)3. , two or more of R may be same or different to each other, and represents an anion of an acid], and non-toxic acid addition salts thereof, possess antagonistic effect on PAF, hypotensive effect like PAF, inhibitory effect on phospholiphase and inhibitory effect on growth of tumour cell or induction of differentiation, and are, therefore, useful as a platelet aggregation inhibitor, anti-asthmatic agent, anti-allergic agent, anti-inflammatory agent, hypotensive agent and anti-tumour agent for mammals.
57 通式如下的甘油衍生物
[其中A代表氧原子或羰氧基(即-O-CO-,其中羰基应连接到基团R3上,羰基应连接到甘油骨架第三位的碳原子上),R1代表6至22个碳原子的烷基,或被苯基取代的2至5个碳原子的烷基,R2代表叠氮基团(-N3基团)、氨基(-NH2基团)或通式如下的基团:-NHCOR5、-NHCOOR5 或 -NHCONHR5,其中 R5 代表 1 至 10 个碳原子的烷基或苯基,但当 A 代表碳酰氧基时,R2 不代表氨基,R3 代表 1 至 12 个碳原子的亚烷基,R4 代表氨基,或通式如下的基团:-NHCOR6、-NHR7、-N(R7)2 或 (R7)3 。其中 R6 代表 1 至 6 个碳原子的烷基或苯基,R7 代表 1 至 8 个碳原子的烷基:-N(R7)2或(R7)3。其中两个或两个以上的 R 可以相同或互不相同,并代表酸的阴离子]及其无毒酸加成盐,具有拮抗 PAF 的作用、类似 PAF 的降血压作用、抑制磷脂的作用、抑制胰岛素的作用、抑制胰岛素分泌的作用、抑制胰岛素分泌的作用、抑制胰岛素分泌的作用、抑制胰岛素分泌的作用、因此,可用作哺乳动物的血小板聚集抑制剂、抗哮喘剂、抗过敏剂、抗炎剂、降血压剂和抗肿瘤剂。