Pheophorbide derivatives

Details Pheophorbide derivatives Pheophorbide derivatives

1988-12-15

1990-10-23

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

In vivo diagnosis or in vivo testing

Magnetic imaging agent

514410, 540145, C07D25700, A61K 3140, A61K 4900

Patent

active

049650645

ABSTRACT:
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.

REFERENCES:
patent: 4849207 (1929-07-01), Sakata et al.
Dougherty, Photochem. and Photobiology, CD. pp. 879-889, 1987.
Gomer et al, Cancer Research, 39, 146-151, Jan. 1979.

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