Thomas C. Elder, Inc.

Elder Pharmaceuticals Ltd.

Kurt D Kaufman

The invention relates to 5'-aminoalkyl-4'-alkylpsoralens, having essentially no erythematic photosensitizing activity but at the same time having substantial DNA-binding photosensitizing activity, making them of especial interest from the standpoint of suntanning and psoriasis treatment, characteristics which are unpredictable when the compounds are compared with psoralens of similar but different structure.

5'-Aminoalkyl-4'-alkylpsoralens

The invention relates to 8-aminoalkylpsoralens, having essentially no erythematic photosensitizing activity but at the same time having substantial DNA-binding photosensitizing activity, making them of especial interest from the standpoint of suntanning and psoriasis treatment, characteristics which are unpredictable when the compounds are compared with psoralens of similar but different structure.

8-Aminoalkylpsoralens

The invention relates to 5'-aminoalkyl-4',4-dialkylpsoralens having enhanced photosensitizing activity, especially oral activity, including early onset, increased maximum, and rapid decline, as well as low toxicity, when compared with psoralens of different structure.

5'-Aminoalkyl-4',4-dialkylpsoralens

The invention relates to 5'-aminoalkyl-4',4,8-trialkylpsoralens having enhanced photosensitizing activity, especially oral and topical activity, as well as low toxicity, when compared with psoralens of different structure.

5-Aminoalkyl-4,4,8-trialkylpsoralens

The invention relates to 8-aminoalkyl-4-alkylisopsoralens, especially 8-aminomethyl-4-methylisopsoralen, having enhanced photosensitizing activity, especially oral and topical activity, pharmaceutical compositions thereof, and method of effecting photosensitization therewith.

8-Aminoalkyl-4-alkylisopsoralens

The invention relates to 5-benzofuranacrylic acid compounds, preferably loweralkyl-substituted in the benzofuran ring system, which have photosensitizing activity, especially oral and topical activity, as well as low toxicity.

Photosensitizing benzofuranacrylics

The invention relates to 4,5',8-trialkylpsoralens, having a substituent on the 4' carbon atom which is selected from hydroxyalkoxyalkyl and hydroxyalkylaminoalkyl, which are characterized by enhanced photosensitizing activity, especially oral activity, including comparable maxima, early onset, and especially rapid decline, as well as low toxicity, when contrasted with psoralens of different structure.

4'-Substituted-4,5',8-trialkylpsoralens

The invention relates to 8-aminoalkyl-4-alkylpsoralens having enhanced photosensitizing activity, especially oral activity, including early onset, increased maximum, and rapid decline, as well as low toxicity, when compared with psoralens of different structure.

8-Aminoalkyl-4-alkylpsoralens

.alpha.-Loweralkylfurocoumarins are produced by forming a .beta.-haloalk-2-enyl, e.g., .beta.-haloallyl, ether of a hydroxycoumarin having an active hydrogen in the position ortho to the hydroxy group, and heating the formed ether, preferably in dimethylaniline or like basic amine solvent. An abnormal Claisen rearrangement produces a novel o-hydroxy-(.beta.-haloalk-2-enyl) coumarin intermediate which can be dehydrohalogenated directly without isolation to the desired .alpha.-loweralkylfurocoumarin, e.g., .alpha.-methylfurocoumarin.

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Kalamazoo, MI, United States of America

Kurt D Kaufman