发明授权
- 专利标题: HYDRAZINE DERIVATIVES
- 专利标题(中): HYDRAZINDERIVATE
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申请号: EP98937498.8申请日: 1998-06-18
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公开(公告)号: EP0993442B1公开(公告)日: 2003-04-23
- 发明人: BROADHURST, Michael John , JOHNSON, William, Henry , WALTER, Daryl, Simon
- 申请人: F. HOFFMANN-LA ROCHE AG
- 申请人地址: 124 Grenzacherstrasse 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: 124 Grenzacherstrasse 4070 Basel CH
- 代理机构: Löschner, Thomas
- 优先权: GB9713833 19970630; GB9803335 19980217
- 国际公布: WO99001428 19990114
- 主分类号: C07C311/49
- IPC分类号: C07C311/49 ; A61K31/18 ; C07C259/06 ; C07C281/02 ; C07C281/06 ; C07D209/32 ; C07D209/48 ; C07D211/58 ; C07D211/98 ; C07D213/42 ; C07D213/56
摘要:
Hydrazine derivatives of formula (I) wherein Y signifies CO or SO2; R1 signifies lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 signifies lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y signifies SO¿2? and signifies lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR?5R6¿ when Y signifies CO; and R3 signifies hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonly, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl- lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R?2 and R3¿ together form the residue of a 5-, 6- or 7- membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 signifies lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkly-lower alkyl or a grouping of the formula X-aryl, X-heteroaryl or -(CH¿2?)1-2-CH=CR?7R8¿; X signifies a spacer group; R?5 and R6¿ each individually signify hydrogen, lower alkyl or aryl-lower alkyl; and R?7 and R8¿ together represent a lower alkylene group in which one methylene group is optionally replaced by a hetero atom; and their pharmaceutically acceptable salts inhibit not only the release of tumour necrosis factor (TNF-α) and transforming growth factor (TGF-α) from cells, but also keratinocyte proliferation. They are useful as medicaments, especially for the treatment of inflammation, fever, haemorrhage, sepsis, rheumatoid arthritis, osteoarthritis, multiple sclerosis or psoriasis.
公开/授权文献
- EP0993442A1 HYDRAZINE DERIVATIVES 公开/授权日:2000-04-19
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