公开(公告)号：US4965064A

公开(公告)日：1990-10-23

申请号：US285106

申请日：1988-12-15

申请人： Michito Karasawa ,  Mari Uchimoto ,  Hirofumi Kawabe ,  Takuzo Otani ,  Katsuo Aizawa

发明人： Michito Karasawa ,  Mari Uchimoto ,  Hirofumi Kawabe ,  Takuzo Otani ,  Katsuo Aizawa

IPC分类号： G01N33/50 ,  A61K31/40 ,  A61K41/00 ,  A61K51/00 ,  A61P35/00 ,  C07D487/22

CPC分类号： C07D487/22 ,  A61K41/0071

摘要： 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.

公开(公告)号：US4772681A

公开(公告)日：1988-09-20

申请号：US4333

申请日：1987-01-15

申请人： Yozo Fukuda ,  Takuzo Otani ,  Haruo Yamada ,  Michikazu Sawada ,  Katsuo Aizawa ,  Mari Uchimoto ,  Michito Karasawa

发明人： Yozo Fukuda ,  Takuzo Otani ,  Haruo Yamada ,  Michikazu Sawada ,  Katsuo Aizawa ,  Mari Uchimoto ,  Michito Karasawa

IPC分类号： C07D487/22

CPC分类号： C07D487/22

摘要： Novel porphyrin derivatives of the general formula: ##STR1## wherein R.sub.1 each independently denotes a hydrogen, a C.sub.1 -C.sub.4 alkyl group or an ethenyl group, and R.sub.2 each independently denotes COZ(C.sub.m H.sub.2m)Q, COZCH(C.sub.m H.sub.2m Q).sub.2, --CH.sub.2 --Q [wherein Z is O, S or NH, m is an integer of 1 to 23, and Q is a di-(C.sub.1 -C.sub.4 alkyl)amino group or tri-(C.sub.1 -C.sub.4 alkyl)ammonium halide group] or ##STR2## (wherein X is a halogen); or R.sub.1 each independently denotes --C.sub.2 H.sub.4 --Q (wherein Q is the same as defined above), ##STR3## (wherein X is the same as defined above), and R.sub.2 each independently denotes a carboxyl group or a C.sub.1 -C.sub.4 alkoxycarbonyl group, and the production thereof are described. The quarternary ammonium salt type of the above compounds exhibit affinity and photosensitizing activity for cancer cells and can be employed for diagnosing and treating cancer under irradiation of laser light.

摘要翻译： 其中R1各自独立地表示氢，C1-C4烷基或乙烯基，R2各自独立地表示COZ（CmH2m）Q，COZCH（CmH2mQ）2，-CH2- Q [其中Z为O，S或NH，m为1〜23的整数，Q为二（C1-C4烷基）氨基或三（C1-C4烷基）卤化铵基]或（其中X是卤素）; 或R 1各自独立地表示-C 2 H 4 -Q（其中Q与上述定义相同），＆lt; IMAGE＆gt;（其中X与上述定义相同），R 2各自独立地表示羧基或C 1 -C 4烷氧基羰基， 并描述其生产。 上述化合物的季铵盐类型对癌细胞表现出亲和力和光敏作用，可用于在激光照射下诊断和治疗癌症。