发明公开
- 专利标题: Oxamides as IMPDH inhibitors
- 专利标题(中): 草酰胺用作IMPDH抑制剂
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申请号: EP01103521.9申请日: 2001-02-16
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公开(公告)号: EP1127883A3公开(公告)日: 2002-08-07
- 发明人: Broadhurst, Michael John , Hill, Christopher Huw, , Hurst, David Nigel , Jones, Philip Stephen , Kay, Paul Brittain , Kilford, Ian Reginald , McKinnell, Robert Murray
- 申请人: F. HOFFMANN-LA ROCHE AG
- 申请人地址: 4070 Basel CH
- 专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人: F. HOFFMANN-LA ROCHE AG
- 当前专利权人地址: 4070 Basel CH
- 代理机构: Rauber, Beat
- 优先权: GB0004392 20000224; GB0015877 20000628; GB0020322 20000817
- 主分类号: C07D263/32
- IPC分类号: C07D263/32 ; C07D413/12 ; C07D417/12 ; A61K31/421 ; A61K31/422 ; A61K31/4439 ; A61K31/454 ; A61P29/00 ; A61P31/00 ; A61P35/00 ; A61P37/00
摘要:
Disclosed are compounds of the general formula wherein R 1 represents heterocyclyl; R 2 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, hydroxy or cyano; R 3 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R 4 represents hydrogen, lower alkyl, lower cycloalkyl, aryl, or heterocyclyl; R 5 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R 6 represents hydrogen, unsubstituted lower alkyl, lower alkoxy, halo, or cyano; R 7 represents hydrogen, or unsubstituted lower alkyl; R 8 represents hydrogen, or unsubstituted lower alkyl; or R 4 and R 8 together with the nitrogen atom to which they are attached represent heterocyclyl; and pharmaceutically acceptable salts thereof. The disclosed oxamide derivatives are inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH). They can be used as medicaments, especially for treating immune mediated conditions or diseases, viral diseases, bacterial diseases, parasitic diseases, inflammation, inflammatory diseases, hyperproliferative vascular diseases, tumours, and cancer. They can be used alone, or in combination with other therapeutically active agents, for example, an immunosuppressant, a chemotherapeutic agent, an anti-viral agent, an antibiotic, an antiparasitic agent, an anti-inflammatory agent, an anti-fungal agent and/or an anti-vascular hyperproliferation agent.
公开/授权文献
- EP1127883A2 Oxamides as IMPDH inhibitors 公开/授权日:2001-08-29
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