申请人:Burroughs Wellcome Co.
公开号:US04999369A1
公开(公告)日:1991-03-12
The present invention relates to compounds of formula (I) ArCH.sub.2 R.sup.1 (I) or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen; R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy; R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl; R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl; R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.
本发明涉及化合物式(I)ArCH.sub.2R.sup.1(I)或其单甲基或单乙基醚(式(I)的化合物包括这些醚,总碳原子数不超过29);它们的醚,酯;酸加成盐;其中Ar是由5元环和6元环组成的融合四环芳香环系,含有至少一个杂原子和3个芳香环,环原子总数不超过18个,或其取代衍生物;杂原子最好是氧、硫或氮;当它是氮时,它被氢、甲基或乙基取代;R.sup.1含有不超过8个碳原子,是一个基团##STR1##其中m为0或1;R.sup.5是氢;R.sup.6和R.sup.7相同或不同,每个都是氢或C.sub.1-5烷基,可选地被羟基取代;R.sup.8和R.sup.9相同或不同,每个都是氢或C.sub.1-3烷基;##STR2##是一个五元环或六元环饱和碳环;R.sup.10是氢、甲基或羟甲基;R.sup.11、R.sup.12和R.sup.13相同或不同,每个都是氢或甲基;R.sup.14是氢、甲基、羟基或羟甲基。