Tetrapyrrole therapeutic agents
AssigneeNippon Petrochemicals Company, Limited
InventorsJerry C. Bommer, Bruce F. Burnham
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Abstract
The present invention relates to compounds having the following formula: ##STR1## or the corresponding di- or tetrahydrotetrapyrroles wherein ##STR2## provided that when R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.7 and R.sub.8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole; R is lower alkyl or benzyl; R.sub.6 and R.sub.9, taken together are ##STR3## with the proviso that at least one of R.sub.1 -R.sub.9 includes a free carboxyl group; and salts thereof. These compounds are useful in the photodiagnosis and phototherapy of tumors.
Claims42
A fluorescent mono-, di, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula:
- ##STR57## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole;
- wherein ##STR58## provided that when R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.7 and R.sub.8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole;
- R is lower alkyl or benzyl;
- or
- R.sub.6 and R.sub.9, taken together are ##STR59## with the proviso that at least one of R.sub.1 -R.sub.9 includes a free carboxyl group;
- and salts thereof;
- with the further proviso that said compound is not mesoporphyrin-bis-L-glutamic acid.
A pharmaceutical composition comprising an effective therapeutic amount of a fluorescent mono-, di-, tri- or tetramide of an amino acid containing two carboxy groups and a carboxy containing tetrapyrrole compound of the formula:
- ##STR60## or the corresponding di- or tetrahydrotetrapyrroles, said amide linkage being formed between the amino group of the amino acid and a carboxy-containing substituent attached to the tetrapyrrole;
- wherein ##STR61## provided that when R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.7 and R.sub.8 represent two substituents or are divalent and attached to the same carbon, the respective pyrrole ring to which attached is a dihydropyrrole;
- R is lower alkyl or benzyl;
- or
- R.sub.6 and R.sub.9 taken together are ##STR62## with the proviso that at least one of R.sub.1 -R.sub.9 includes a free carboxyl group;
- and pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier therefor.
Dependencies are inferred from the claim text.