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publicationNumber JP-2010515716-A
titleOfInvention Positively charged water-soluble prodrugs of retinoids and retinoid-like compounds with very high skin permeability
abstract The design and synthesis of a new positively charged prodrug of a retinoid or retinoid-like compound of general formula (31) 'structure 31'. The positively charged amino group of these prodrugs not only significantly increases the solubility of the drug in water, but also binds to a negative charge in the phosphate head group of the membrane. This binding can interfere with the membrane only a little and make room for the lipophilic part of the prodrug. If the membrane molecule moves, it will only 'crack' the membrane due to the binding of the prodrug. This inserts the prodrug into the membrane. Prodrugs can be used pharmaceutically to treat a retinoid or retinoid-like compound treatable condition in humans or animals. Prodrugs can be administered transdermally for any kind of medical treatment and avoid most of the side effects of retinoids or retinoid-like compounds. [Selection] Figure 2
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