发明授权
US06743913B2 Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and &agr;-1-blocking action
失效
具有5-羟色胺受体拮抗作用和α-1-阻断作用的吡罗噻嗪和吡咯并噻吩类化合物
- 专利标题: Pyrrolothiazine and pyrrolothiazepine compounds having serotonin-2 receptor antagonistic and &agr;-1-blocking action
- 专利标题(中): 具有5-羟色胺受体拮抗作用和α-1-阻断作用的吡罗噻嗪和吡咯并噻吩类化合物
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申请号: US10421929申请日: 2003-04-24
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公开(公告)号: US06743913B2公开(公告)日: 2004-06-01
- 发明人: Akira Mizuno , Makoto Shibata , Tomoe Kamei , Harukazu Fukami , Norio Inomata
- 申请人: Akira Mizuno , Makoto Shibata , Tomoe Kamei , Harukazu Fukami , Norio Inomata
- 优先权: JP9-366757 19971226
- 主分类号: C07D51304
- IPC分类号: C07D51304
摘要:
A pyrrolesulfonamide compound having the following formula (I): wherein the ring P represented by is a pyrrole ring having the following structure: wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl. The compound (1) has been improved in potency, selectivity to receptors other than serotonin-2 receptors, toxicity, side effects and/or the like over medicines reported to date and equipped with &agr;1-blocking action and serotonin-2 receptor antagonistic action in combination.
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