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.
本发明的萘和萘醌的双碱基酮具有口服和非口服给药时的抗病毒活性。这些化合物由以下式表示:
其中Z为氧或H.sub.2;每个A为具有1到约6个碳原子的直链或支链烷基链;每个Y为A。组
其中R.sup.1和R.sup.2分别为氢、(较低)烷基,具有1到约6个碳原子,环烷基,具有3到6个碳原子,烯烃,具有3到6个碳原子,并且烯烃基团的烯丙烯不在烯烃基团的1位;或B。组
其中N为4到6的整数,R.sup.3为氢、1到约4个碳原子的(较低)烷基,苯基或苄基,并且可以连接到杂环基团的任一碳原子;或C。组
其中X为氧或NR.sup.4,R.sup.4为氢或1到约4个碳原子的(较低)烷基;或D。组
其中P为2到3的整数,M为1到2的整数;或所述碱的药学上可接受的酸加盐。这些新化合物可以通过描述的几种不同方法制备。