申请人:Eisai Co., Ltd.
公开号:EP0889037A1
公开(公告)日:1999-01-07
To provide a novel phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative efficacious against diseases in which histamine, leukotrienes, etc. participate.
A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by the following formula are efficacious in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
A nitrogen-containing tricyclic compound represented by the following formula (I), a hydrate thereof or a pharmacologically acceptable salt thereof:
(wherein D represents alkylene, etc.)
wherein R1, R2, R3, R4, R5, R6, R7 and R8 are the same or different from each other and each represents hydrogen, hydroxy, cyano, nitro, optionally substituted carbamoyl, halogeno, optionally halogenated lower alkyl, etc.; Z represents -S-, -SO-, -SO2-, =NO-substituent, -NC(O)- or =NN-substituent; and Q represents, for example, -NR20R21 (wherein R20 and R21 are the same or different from each other and each represents hydrogen, optionally halogenated lower alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, or R20 and R21 may form together with the nitrogen atom to which they are bonded a 3- to 8-membered ring).
提供一种新型吩噻嗪、吖啶坦、吖啶酮肟、吖啶酮腙和二苯并二氮杂卓衍生物,对组胺、白三烯等参与的疾病有效。
下式所代表的吩噻嗪、吖啶酮、吖啶酮肟、吖啶酮腙和二苯并二氮杂卓衍生物可有效预防或治疗组胺和白三烯等化学介质参与的疾病,例如哮喘、过敏性鼻炎、特应性皮炎、荨麻疹、花粉热、胃肠道过敏和食物过敏。
由下式(I)代表的含氮三环化合物、其水合物或药理学上可接受的盐:
(其中 D 代表亚烷基等)
其中 R1、R2、R3、R4、R5、R6、R7 和 R8 彼此相同或不同,且各自代表氢、羟基、氰基、硝基、任选取代的氨基甲酰基、卤代、任选卤代的低级烷基等。Z代表-S-、-SO-、-SO2-、=NO-取代基、-NC(O)-或=NN-取代基;Q代表例如-NR20R21(其中 R20 和 R21 彼此相同或不同,各自代表氢、任选卤代低烷基、任选取代的芳基、任选取代的芳烷基、任选取代的杂芳基或任选取代的杂芳基烷基,或 R20 和 R21 可与它们所键合的氮原子一起形成 3 至 8 元环)。