New modified bacterial chlorophyll derivs. - for diagnosis and treatment of tumours

摘要

Bacteriochlorophyll derivs. of formula (A) are new. Ra and Rb are together -CR1R2-CO- (cpds. (I)); or Ra = COCOR2 and Rb = COOR3 (cpds. (II)) or together they are -CO-O-CO- (cpds. (III)); M = H or metal; R1 = residue of oligo-oxyethylene glycol, at least 3C opt. halogenated, linear, branched or cycloaliphatic alcohol; hydroxylated amino acid; sugar alcohol; hydroxylated lipid; linear polyol; aminoalcohol; hydroxycarboxylic acid; nitroxide gp. contg. alcohol; alcohol contg. a chromophore gp. or an alkylbenzylalcohol. R2 = H, OH or COOR4; R4 = 1-12C alkyl or cycloalkyl; R3 = H, OH, or 1-12C alkyl or alkoxy. Specifically, M = Mg, Zn, Ni, Cu or Sn; R1 = fluoroethyl, trifluorobutyl, sorbitoyl, O-serinyl, aminohexyl or pentaoxyethyelne glycol residue; R2 = COOMe; R3 = OH. USE/ADVANTAEG - (A) are useful in diagnosis and treatment of tumour(s) because of their fluoroescent properties and ability to photosensitive generation of singlet oxygen. A wide variety of (A) can be produced simply, some of them having better properties (e.g. as regards IR absorption) than known green chlorophylls. The nature of R1 can be selected to control e.g. water solubility; aggregation; selectivity for target sites; biodegradation etc; and the cpds. absorb in the long wavelength region (up to about 800nm).