发明公开
EP0795554A2 (Oxo-)xanthene derivatives, their preparation and their use as immunomodulators
失效
(氧代基)呫吨衍生物,其制备方法及其作为免疫调节剂使用
- 专利标题: (Oxo-)xanthene derivatives, their preparation and their use as immunomodulators
- 专利标题(中): (氧代基)呫吨衍生物,其制备方法及其作为免疫调节剂使用
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申请号: EP97301438.4申请日: 1997-03-04
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公开(公告)号: EP0795554A2公开(公告)日: 1997-09-17
- 发明人: Hida, Tsuneaki , Hattori, Masahiko , Kurokawa, Tsutomu , Nakanishi, Atsushi
- 申请人: TAKEDA CHEMICAL INDUSTRIES, LTD.
- 申请人地址: 1-1, Doshomachi 4-chome Chuo-ku, Osaka 541 JP
- 专利权人: TAKEDA CHEMICAL INDUSTRIES, LTD.
- 当前专利权人: TAKEDA CHEMICAL INDUSTRIES, LTD.
- 当前专利权人地址: 1-1, Doshomachi 4-chome Chuo-ku, Osaka 541 JP
- 代理机构: Lewin, John Harvey
- 优先权: JP47795/96 19960305; JP262085/96 19961002
- 主分类号: C07D311/86
- IPC分类号: C07D311/86 ; C07D311/82 ; A61K31/35 ; C07D405/12 ; A61K31/41 ; C07D407/12 ; A61K31/44 ; C07D409/04 ; A61K31/38 ; C07D407/04 ; C12P17/06 ; C12N1/15
摘要:
Xanthene derivatives represented by the general formula:
wherein R 1 is a carboxyl group which may be esterified or amidated; R 2 is a hydrogen atom, a hydroxyl group, or a hydrocarbon group which may be substituted; R 3 and R 4 are the same or different and are a hydroxyl group which may be substituted; R 5 and R 6 are a hydrogen atom or a halogen atom; R 7 is a hydrogen atom, a nitro group, a halogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; n is an integer of 0 to 2; and Y is an oxygen atom or two hydrogen atoms; and when n is 0, R 2 may be a group represented by the formula:
wherein the symbols have the same meanings as defined above, or a salt thereof inhibit a binding of B7-1 to CD28, prevent the B7-1-dependent activation of T cells and inhibit IL-2 production from T cells, thus being used as an immunomodulator such as a graft rejection inhibitor or a pharmaceutical composition for therapeutic treatment of allergy, rheumatoid arthritis, autoimmune disease, nephritis, diabetes mellitus and so on.
wherein R 1 is a carboxyl group which may be esterified or amidated; R 2 is a hydrogen atom, a hydroxyl group, or a hydrocarbon group which may be substituted; R 3 and R 4 are the same or different and are a hydroxyl group which may be substituted; R 5 and R 6 are a hydrogen atom or a halogen atom; R 7 is a hydrogen atom, a nitro group, a halogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; n is an integer of 0 to 2; and Y is an oxygen atom or two hydrogen atoms; and when n is 0, R 2 may be a group represented by the formula:
wherein the symbols have the same meanings as defined above, or a salt thereof inhibit a binding of B7-1 to CD28, prevent the B7-1-dependent activation of T cells and inhibit IL-2 production from T cells, thus being used as an immunomodulator such as a graft rejection inhibitor or a pharmaceutical composition for therapeutic treatment of allergy, rheumatoid arthritis, autoimmune disease, nephritis, diabetes mellitus and so on.
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