http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2012503006-A

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filingDate 2009-09-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2012-02-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2012503006-A
titleOfInvention Application of asymmetric meso-substituted porphyrins and chlorins to PDT and a new method
abstract The present invention provides a bioactive compound for use as a photosensitizer applied in diagnosis and therapy. The application is especially for non-cancer indications such as PDT for cancer, infectious diseases and other hyperproliferative diseases, arthritis, inflammatory diseases, viral and bacterial infections, skin diseases, eye diseases, urological diseases Made for fluorescence diagnosis and PDT therapy. The present invention also provides a method for synthesizing those compounds that have reached a pharmaceutically acceptable level. An embodiment includes a method of synthesizing a porphyrin having a meso substituent at a predetermined position and a method of converting the porphyrin system to a chlorin system by dihydroxylation or reduction, whereby a plurality of isomers are formed. If so, it includes a method of separating them by chromatography on normal phase or reverse phase silica. In other embodiments, porphyrin substituents are selected such that specific isomers are selectively synthesized upon reduction or dihydroxylation of chlorin. In another embodiment, an amphiphilic compound having high affinity for a membrane and high PDT effect is provided. In other embodiments, a method of reductive dissociation of an osmic acid (VI) ester that avoids the use of gaseous H 2 S is provided. In other embodiments, a substituent is identified, and the steric and / or electronic effects of the substituent have a selectivity for a dihydroxylation reaction or a reduction reaction with diimine, with one isomer predominating. Indicates. Other embodiments include methods in which the isomer of interest is formulated as an injectable liposomal formulation to avoid undesirable effects such as infusion solubility problems and tetrapyrrole pharmacokinetic delay problems. [Selection] Figure 2
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Total number of triples: 32.