发明授权
- 专利标题: Antifolate agents
- 专利标题(中): 防腐剂
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申请号: US127452申请日: 1987-12-02
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公开(公告)号: US4992444A公开(公告)日: 1991-02-12
- 发明人: Malcolm F. G. Stevens , Roger J. Griffin , Michelle A. Meek
- 申请人: Malcolm F. G. Stevens , Roger J. Griffin , Michelle A. Meek
- 专利权人: Stevens Malcolm F G,Griffin Roger J,Meek Michelle A
- 当前专利权人: Stevens Malcolm F G,Griffin Roger J,Meek Michelle A
- 优先权: GBX8628731 19861202; GBX8721283 19870910; GBX8721284 19870910
- 主分类号: A61K31/505
- IPC分类号: A61K31/505 ; A61P17/00 ; A61P31/04 ; A61P33/02 ; A61P35/00 ; A61P43/00 ; C07D239/48
摘要:
2,4-Diamino-5-phenylpyrimidines in the form of the free base or an acid addition salt thereof are provided having the structural formula (I): ##STR1## wherein R.sup.1 is an alkoxy, aralkoxy or a mono-substituted or disubstituted amino group, R.sup.2 is a nitro group, and R.sup.3 is an alkyl group. The compounds act as antifolate agents and are useful for therapeutic treatment, for example as antitumour agents, antipsoriatic agents, antibacterial agents, antitrypanosomal agents and antimalarial agents. Pharmaceutical preparations comprising these compounds for administration to mammals, and methods for preparing the compounds, are disclosed. Particularly useful new compounds, especially for antitumour therapy, have the structural formula IA: ##STR2## in which formula IA: n is 1-6; R.sub.1 represents hydrogen or alkyl; R.sup.4, R.sup.5 and R.sup.6, which may be identical or different, each represnt hydrogen, alkyl, alkoxy, halo, nitro, perfluoroalkyl, a group of formula --CO.sub.2 R.sup.a wherein R.sup.a represents hydrogen, alkyl or alkoxyalkyl, or a group of formula --COBR.sup.b R.sup.c wherein R.sup.b and R.sup.c which may be identical or different each represent alkyl; and R.sup.3 represents alkyl.
公开/授权文献
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