申请人:Burroughs Wellcome Co.
公开号:US05008286A1
公开(公告)日:1991-04-16
The present invention relates to compounds of formula (I) ArCH.sub.2 R.sup.1 (I) or a monomethyl or monethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acide addition salts thereof; wherein Ar is a fused tricyclic aromatic ring system containing a maximum of 14 ring atoms and at least one heteroatom or a fused pentacyclic ring system with at least 4 aromatic rings containing a maximum of 22 ring atoms and at least one heteroatom; or a substituted derivative thereof; for either the tricyclic or pentacyclic ring system there is a maximum of one heteroatom for each ring present but preferably only one or two of the rings contain a heteroatom; the rings forming the tricyclic or the pentacyclic ring system contain five or six atoms; the heteroatoms are conveniently nitrogen, phosphorus, oxygen, sulfur or selenium; suitably the heteroatom is oxygen, sulfur or nitrogen; the tricyclic or the pentacyclic ring system should be planar or deviate only slightly from planarity; suitably the ring system is aromatic or contains one non-aromatic ring; preferably the ring system is aromatic; nitrogen atoms contained in five-membered rings are 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. The compounds have biocidal properties.
本发明涉及化合物的公式(I)ArCH.sub.2 R.sup.1(I)或其单甲基或单乙基醚(公式(I)的化合物包括这些醚,总共不超过29个碳原子);醚,酯;酸盐;其中Ar是含有最多14个环原子和至少一个杂原子的融合三环芳香环系统或至少4个芳香环的含有最多22个环原子和至少一个杂原子的融合五环系统;或其取代衍生物;对于三环或五环系统,每个环最多有一个杂原子,但最好只有一个或两个环含有杂原子;形成三环或五环系统的环包含五个或六个原子;杂原子方便地是氮、磷、氧、硫或硒;适宜的杂原子是氧、硫或氮;三环或五环系统应该是平面的或仅略微偏离平面;合适的环系统是芳香的或包含一个非芳香环;最好环系统是芳香的;五元环中含氮原子被氢、甲基或乙基取代;R.sup.1含有不超过八个碳原子,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,每个是氢或C.sub.1-5烷基,可选择地被羟基取代;R.sup.8和R.sup.9相同或不同,每个是氢或C.sub.1-3烷基;##STR2##是一个五元或六元饱和碳环;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,每个是氢或甲基;R.sup.14是氢、甲基、羟基或羟甲基。这些化合物具有杀生物性能。