发明授权
US5905149A Substituted quinolymethylen-oxindole analogues as tyrosine kinase
inhibitors
失效
取代的喹喔啉甲氧基吲哚类似物作为酪氨酸激酶抑制剂
- 专利标题: Substituted quinolymethylen-oxindole analogues as tyrosine kinase inhibitors
- 专利标题(中): 取代的喹喔啉甲氧基吲哚类似物作为酪氨酸激酶抑制剂
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申请号: US983516申请日: 1998-01-29
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公开(公告)号: US5905149A公开(公告)日: 1999-05-18
- 发明人: Carlo Battistini , Antonella Ermoli , Sergio Vioglio , Franco Buzzetti , Dario Ballinari
- 申请人: Carlo Battistini , Antonella Ermoli , Sergio Vioglio , Franco Buzzetti , Dario Ballinari
- 申请人地址: ITX Milan
- 专利权人: Pharmacia & Upjohn S.p.A
- 当前专利权人: Pharmacia & Upjohn S.p.A
- 当前专利权人地址: ITX Milan
- 优先权: GBX9611797 19960606
- 主分类号: A61K31/00
- IPC分类号: A61K31/00 ; A61K31/47 ; A61K31/4709 ; A61K31/535 ; A61K31/5375 ; A61K31/5377 ; A61K38/00 ; A61P9/00 ; A61P35/00 ; A61P43/00 ; C07D401/06 ; C07D401/14 ; C07K5/06 ; C07K5/078 ; C07D401/02 ; C07D413/14
摘要:
Quinolylmethylen-oxindole derivatives having general formula (I), wherein R is H or --(CH.sub.2).sub.n --COR.sub.7 group in which n is an integer of 1 to 4 and R.sub.7 is hydroxy, amino, C.sub.1 -C.sub.6 alkoxy or --NR.sub.5 R.sub.6 in which one of R.sub.5 and R.sub.6 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.5 and R.sub.6 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle or R.sub.7 is a N-terminally linked peptidyl residue containing from 1 to 3 aminoacids in which the terminal carboxyl group may be present as such, as amide, as alkali metal salt or as a C.sub.1 -C.sub.4 alkyl ester, one or two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from: a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.5 R.sub.6 or --X--(CH.sub.2).sub.m --NHR.sub.8 group; b) --NH--C(.dbd.NH)--NR.sub.5 R.sub.6, --NH--C(.dbd.NH)--NHR.sub.8, --N.dbd.CH--NH.sub.2, --N.dbd.CH--NR.sub.5 R.sub.6 or --N.dbd.CH--NHR.sub.8 group; c) --X--(C.sub.2).sub.n --COR.sub.7 group; d) --COR.sub.a or --COR.sub.9 group; e) --Y--CO--Y'--R.sub.10 group; and f) --NHR.sub.8 or --NHR.sub.11 group and the pharmaceutically acceptable salts thereof, are tyrosine kinase inhibitors.
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