申请人:Hamari Chemicals, Ltd.
公开号:US04965064A1
公开(公告)日:1990-10-23
Novel pheophorbide derivatives of the general formula: ##STR1## [wherein Z is O or NH; n is an integer of 1 to 6; Y is NR'R" or ##STR2## wherein R', R" and R'" are the same or different or each represents a C.sub.1 to C.sub.4 lower alkyl group; X.sup.- is a halogen or organic acid ion); R.sub.1 is an ethenyl group; C.sub.1 to C.sub.4 lower alkyl group or ##STR3## (wherein m is an integer of 0 to 6; R.sub.6 is H or a C.sub.1 to C.sub.4 lower alkyl group); R.sub.2 is CH.sub.3, CHO or CH.sub.2 OH; either of R.sub.3 and R.sub.4 is H, with the other being OH, or both of them combine to represent .dbd.O; R.sub.5 is H or CO.sub.2 CH.sub.3) are provided. When administered to a cancer-carrying animal, the derivatives accumulate specifically in cancer tissues and emit characteristic fluorescent spectrum under irradiation of light, which enables one to detect the cancer tissues.
一种新的苊类衍生物的一般公式为:##STR1## [其中Z为O或NH;n为1到6的整数;Y为NR'R"或##STR2## 其中R'、R"和R'"相同或不同,或每个代表C.sub.1到C.sub.4的低碳链基;X.sup.-为卤素或有机酸根离子);R.sub.1为乙烯基;C.sub.1到C.sub.4的低碳链基或##STR3## (其中m为0到6的整数;R.sub.6为H或C.sub.1到C.sub.4的低碳链基);R.sub.2为CH.sub.3、CHO或CH.sub.2 OH;R.sub.3和R.sub.4中的任意一个为H,另一个为OH,或两者结合表示.dbd.O;R.sub.5为H或CO.sub.2 CH.sub.3)。当这些衍生物被用于治疗患有癌症的动物时,它们会特异性地积累在癌组织中,并在光照射下发出特征性的荧光光谱,从而使人们能够检测到癌组织。