申请人:Richardson-Merrell Inc.
公开号:US04064347A1
公开(公告)日:1977-12-20
The novel bis-basic ketones of fluorene and fluorenone of the present invention have antiviral activity when administered orally and parenterally. These compounds are represented by the following formula: ##STR1## wherein Z is oxygen or H.sub.2 ; each A is a straight or branched alkylene chain having from 1 to about 6 carbon atoms; and each Y is A. the group ##STR2## wherein R.sup.1 and R.sup.2 are individually hydrogen, (lower)alkyl having from 1 to about 6 carbon atoms, cycloalkyl having from 3 to 6 carbon atoms, alkenyl of from 3 to 6 carbon atoms and having the vinyl unsaturation in other than the 1-position of the alkenyl group; or B. the group ##STR3## WHEREIN N IS A WHOLE INTEGER FROM 4 TO 6, AND R.sup.3 is hydrogen, (lower)alkyl of 1 to about 4 carbon atoms, phenyl, or benzyl and can be linked to any one of the carbon atoms of the heterocyclic group; or C. the group ##STR4## wherein X is oxygen or NR.sup.4, and R.sup.4 is hydrogen or (lower)alkyl of from 1 to about 4 carbon atoms; or D. the group ##STR5## WHEREIN P IS A WHOLE INTEGER FROM 2 TO 3, AND M IS A WHOLE INTEGER FROM 1 TO 2; OR A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT OF SAID BASE. These new compounds may be prepared by several different methods which are described.
本发明的芴和芴酮的双碳基酮类化合物在口服和经静脉注射时具有抗病毒活性。这些化合物由以下公式表示:##STR1## 其中Z是氧或H.sub.2;每个A是具有1至约6个碳原子的直链或支链烷基链;每个Y是A。组##STR2##其中R.sup.1和R.sup.2分别是氢,具有1至约6个碳原子的(低)烷基,具有3至6个碳原子的环烷基,具有3至6个碳原子并且具有烯丙基不饱和度在烯丙基组的1-位置以外的烯丙基;或B。组##STR3##其中N是从4到6的整数,R.sup.3是氢,具有1至约4个碳原子的(低)烷基,苯基或苄基,并且可以连接到杂环基的任何一个碳原子;或C。组##STR4##其中X是氧或NR.sup.4,R.sup.4是氢或具有1至约4个碳原子的(低)烷基;或D。组##STR5##其中P是从2到3的整数,M是从1到2的整数;或所述基的药学上可接受的酸加成盐。这些新化合物可以通过几种不同的方法制备,这些方法已经描述。