Pheophorbide derivatives

C - Chemistry – Metallurgy – 07 – D

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167/46, 260/237.

C07D 487/22 (2006.01) A61K 41/00 (2006.01) A61K 49/00 (2006.01)

Patent

CA 1337651

This invention relates to novel pheophorbide derivatives of the general formula: Image wherein Z is O or NH; n is an integer of 1 to 6; Y is NR'R" or Image wherein R', R" and R"' are the same or different or each represents a C1 to C4 lower alkyl group; X- is a halogen or organic acid ion; R1 is an ethenyl group, C1 to C4 lower alkyl group or Image wherein M is an integer of 0 to 6; R6 is H or a C1 to C4 lower alkyl group; R2 is CH3, CHO or CH2OH; either of R3 and R4 is H, with the other being OH, or both of them combine to represent =O; R5 is H or CO2CH3. When administered to a cancer-carrying animal, the derivatives accumulate specifically in cancer tissues and emit a characteristic fluorescent spectrum under irradiation of light, which enables one to detect the cancer tissues.

586168

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