Diaza heterocyclic compounds for phototherapy

摘要

The invention relates generally to optical agents, including phototherapeutic agents, for biomedical applications, including phototherapy. The invention includes optical agents, and related therapeutic methods, comprising alicyclic diaza compounds, including 1,2 diaza heterocyclic compounds, having a photolabile N—N bond directly or indirectly linked to at least one carbocyclic aromatic and/or heterocyclic aromatic group. In some embodiments, for example, the invention provides alicyclic diaza compounds for phototherapeutic methods having a photolabile N—N bond that undergoes photoactivated cleavage to produce reactive species, such as radicals, ions, etc., that achieve a desired therapeutic effect, such as selective and/or localized tissue damage and/or cell death.

主权项

1. A method of treating cancer, a cancer-associated disorder, inflammation or an inflammation -associated disorder, the method comprising: (i) administering to a patient a therapeutically effective amount of a phototherapeutic agent to a target tissue of said patient, the phototherapeutic agent comprising a compound being of the formula (FX38); and (ii) exposing the phototherapeutic agent administered to the patient at the target tissue to electromagnetic radiation having wavelengths selected over the range of 350 nm and 1300 nm sufficient to result in injury or death to cells at the target tissue; wherein each of R1 and R6 is independently hydrogen, C1-C20 alkyl, C3 -C20 cycloalkyl, C5-C30 aryl, C5-C30 heteroaryl, C1-C20 acyl, C2-C20 alkenyl, C2-C20 alkynyl, C5-C20 alkylaryl, —(CHOH)mR34, —(CH2CH2O)mR35, —CH(R36)CO2H, or —CH(R37)NH2 each of R34 and R35 is independently hydrogen or C1-C10 alkyl; R37 is independently a side chain residue of a natural α-amino acid and m is independently an integer selected from the range of 1 to 100 wherein the exposing cleaves the N—N bond forming two N radicals; and wherein the method is a Type 1 phototherapy procedure.