发明公开
EP0338087A1 FUSED PYRAZOLE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR MEDICINAL USE
失效
熔化在一起的准备和吡唑方法及其使用药物。
- 专利标题: FUSED PYRAZOLE COMPOUNDS, PROCESS FOR THEIR PREPARATION, AND THEIR MEDICINAL USE
- 专利标题(中): 熔化在一起的准备和吡唑方法及其使用药物。
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申请号: EP88908755.7申请日: 1988-10-11
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公开(公告)号: EP0338087A1公开(公告)日: 1989-10-25
- 发明人: OHE, Takanori , SUEOKA, Hiroyuki , HISADOME, Masao , YAMAGAMI, Keiji
- 申请人: Yoshitomi Pharmaceutical Industries, Ltd.
- 申请人地址: 35 Hiranomachi 3-chome Higashi-ku Osaka-shi Osaka 541 JP
- 专利权人: Yoshitomi Pharmaceutical Industries, Ltd.
- 当前专利权人: Yoshitomi Pharmaceutical Industries, Ltd.
- 当前专利权人地址: 35 Hiranomachi 3-chome Higashi-ku Osaka-shi Osaka 541 JP
- 代理机构: von Kreisler, Alek, Dipl.-Chem.
- 优先权: JP257649/87 19871013; JP140147/88 19880607
- 国际公布: WO8903385 19890420
- 主分类号: C07D231/56
- IPC分类号: C07D231/56 ; C07D471/04 ; A61K31/495
摘要:
Novel fused pyrazole compounds represented by general formula (I) (wherein X represents =N- or =CH-, R represents H, alkyl, alkoxy or halogen, Y¹ represents α, phenyl or phenyl substituted by halogen, alkyl or alkoxy, Y² represents β, -A²-B², H, alkyl, substituted alkyl, phenyl or phenyl substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, provided that at least one of Y¹ and Y² represents α or β, Z¹ and Z² each represents -O-, -S- or -NR³ (wherein R³ represents H or alkyl), A¹ and A² each represents alkylene, B¹ and B² each represents carboxyl, alkoxycarbonyl or phenylalkoxycarbonyl wherein the phenyl group may optionally be substituted by a substituent selected from the group consisting of halogen, alkyl and alkoxy, acyl, -OH, acyloxy, γ or λ (wherein R¹ and R² represents H, alkyl, dialkylaminoalkyl, hydroxyalkyl or, when taken together, R¹ and R² represent a group forming a heterocyclic ring together with the adjacent nitrogen atom), and L¹ and L² each represents halogen, alkyl or alkoxy) and salts thereof, a process for their preparation and a medicinal composition containing same are disclosed. The compounds have the action of increasing phagocytosis of leucocytes, that of increasing phagocytosis of macrophage, that of restoring the number of leucocytes, that of activating infection protective function, that of improving immunological competence, an antitumor action, etc.
ABSTRACT
Novel fused pyrazole compounds of the general formula
wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and therefore is of use as a pharmaceutical.
ABSTRACT
Novel fused pyrazole compounds of the general formula
wherein all the symbols are as defined in the specification or its pharmaceutically acceptable salt which possesses a stimulating action on phagocytosis of leukocytes, a stimulating action on phagocytosis of macrophages, a restorative action on leukopenia, a stimulating action on non-specific resistance to infection, an antitumour action, an activating action on immune responses and the like, and therefore is of use as a pharmaceutical.
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