公开(公告)号：US4992444A

公开(公告)日：1991-02-12

申请号：US127452

申请日：1987-12-02

申请人： Malcolm F. G. Stevens ,  Roger J. Griffin ,  Michelle A. Meek

发明人： Malcolm F. G. Stevens ,  Roger J. Griffin ,  Michelle A. Meek

IPC分类号： A61K31/505 ,  A61P17/00 ,  A61P31/04 ,  A61P33/02 ,  A61P35/00 ,  A61P43/00 ,  C07D239/48

CPC分类号： 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.

摘要翻译： 提供游离碱形式的2,4-二氨基-5-苯基嘧啶或其酸加成盐，其具有结构式（I）：其中R 1是烷氧基，芳烷氧基或单取代或双取代 氨基，R2为硝基，R3为烷基。 化合物作为抗叶酸剂，可用于治疗性治疗，例如作为抗肿瘤剂，抗牛皮癣药，抗菌剂，抗睾丸激素和抗疟药。 公开了包含用于给予哺乳动物的这些化合物的药物制剂及其制备方法。 特别有用的新化合物，特别是用于抗肿瘤治疗，具有结构式IA：其中式IA：n为1-6; R1代表氢或烷基; R 4，R 5和R 6可以相同或不同，各自表示氢，烷基，烷氧基，卤素，硝基，全氟烷基，式-CO 2 R a基团，其中R a表示氢，烷基或烷氧基烷基或式-COBR b R c基团，其中 可以相同或不同的R b和R c表示烷基; 并且R 3表示烷基。