申请人:Sankyo Company Limited
公开号:EP0238202A2
公开(公告)日:1987-09-23
Glycerol derivatives having at least one heterocyclic group on the 3 or 2 position and a group of formula -Y-D-Q on the 1 position (in which Y represents oxygen, sulphur, -NR3-, -X-CO-R'-, -R4-CO-X-, -NR'-CO-, -CO-NR3-or -X-P-(O) (OH)-O-, where -NR3-is optionally protected imino, R4 represents a direct bond or -NR3; and X represents oxygen or sulphur; D represents optionally substituted C1-C14 alkylene; and Q represents a nitrogen-containing heterocyclic group or an amino group either of which is optionally quatemized) are PAF antagonists which may be used to treat asthma, inflammation and shock. They may be prepared by reacting a glycerol derivative having an active group at the 1-position with an appropriate compound to introduce the desired group.
甘油衍生物在 3 或 2 位上至少有一个杂环基团,在 1 位上有一个式-Y-D-Q 的基团(其中 Y 代表氧、硫、-NR3-、-X-CO-R'-、-R4-CO-X-、-NR'-CO-、-CO-NR3-或 -X-P-(O)(OH)-O-,其中 -NR3- 是可选的受保护亚氨基,R4 代表直接键或 -NR3;X 代表氧或硫;D 代表任选取代的 C1-C14 亚烷基;Q 代表含氮杂环基团或氨基,二者任选其一被藜麦化)是 PAF 拮抗剂,可用于治疗哮喘、炎症和休克。制备方法是将 1 位具有活性基团的甘油衍生物与适当的化合物反应,引入所需的基团。