Preparation of dihydropyrene derivatives and their uses.

The present invention relates to dihydropyrene derivs. I [n = 0-1; R1 and R11 = H, alkyl, cycloalkyl, etc.; R2-R5 = H, alkyl, cycloalkyl, etc.; X = one or more physiol. acceptable counter anion(s) such as Cl-, PF6-, BF4-, CH3COO-, Br-, F-, SO42-, HSO4-, HPO42-, H2PO4-], processes for prepg. the same and their use in the treatment of pathologies sensitive to singlet oxygen, in particular for use in phototherapy and/or in the treatments of cancers. E.g., a multi-step synthesis of II.2PF6-, starting from 4,9-dibromo-2,7-di-tert-butyl-trans-10b,10c-dimethyl-10b,10c-dihydropyrene, was described. UV-visible irradn. of a soln. of II.2PF6- under air generated compd. III. Singlet oxygen trapping expts. were carried out by NMR (data given). Exemplified compds. I were evaluated in in vitro expts. and cell viability was obsd. Pharmaceutical or diagnostic compn. comprising compd. I was disclosed. [on SciFinder(R)]


Preparation of dihydropyrene derivatives and their uses.
Type de publication
Année de publication
Patent Number
WO 2016193777 A1
Soumis le 23 mai 2018