Porphycene compounds for photodynamic therapy
First Claim
1. A porphycene having the structure ##STR4## wherein each R1 is, independently, (a) --(CH2)n -X where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or where X is --Y--(CH2)n -porphycene2, where porphycene2 is a compound of the same said structure, n=1-4 and Y is a direct bond;
- --O--;
or --CH═
CH--;
or(b) where one, two or three of the substituents R1 are C1-6 alkyl or C6-20 carbocyclic aryl and the remaining substituents are as above under (a) and pharmaceutically acceptable salts and metal complexes thereof.
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Abstract
A porphycene having the structure ##STR1## wherein each R1 is, independently, (a) --(CH2)n --X, where n=1-4, X is OR2 and R2 is C1-6 alkyl, aralkyl or aryl; CN; OH; OSO2 R2 ; NH2 ; NHR2 ; NR22 ; SH; SR2 ; S(O)1-2 R2 ; COOH; CO2 R2 ; C(O)NH2 ; C(O)NHR2 ; C(O)NR22 ; halogen; or CHO;
(b) --(CH2)m CH═CH2 where m is 0-2; or
(c) --(CH2)n --O--G where G is a mono- or oligosaccharide;
(d) --(CH2)2n --X, where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or --Y-- (CH2)n -porphycene2 (porphycene2 being a compound of the same structure and Y is a direct bond; --O--; or --CH═CH2); or
(e) where one, two or three of the substituents R1 are C1-6 alkyl or aryl and the remaining substituents are as above under (a)-(d), and salts and metal complexes thereof. The porphycene compounds and pharmaceutical compositions containing the compounds are useful in photodynamic therapy treatment of tumors and psoriasis.
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Citations
15 Claims
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1. A porphycene having the structure ##STR4## wherein each R1 is, independently, (a) --(CH2)n -X where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or where X is --Y--(CH2)n -porphycene2, where porphycene2 is a compound of the same said structure, n=1-4 and Y is a direct bond;
- --O--;
or --CH═
CH--;
or(b) where one, two or three of the substituents R1 are C1-6 alkyl or C6-20 carbocyclic aryl and the remaining substituents are as above under (a) and pharmaceutically acceptable salts and metal complexes thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 12, 13, 14)
- --O--;
- 10. The compound 9-acetoxy-2,7,12,17-tetrakis(methoxyethyl)porphycene.
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15. A porphycene having the structure ##STR5## wherein each R1 is, independently, (a) --(CH2)n -X where X is an amino acid, oligopeptide covalently bonded by an ether-, ester- or amine-bond or where X is --Y--(CH2)n -porphycene2, where porphycene2 is a compound of the same said structure, n=1-4 and Y is a direct bond;
- --O--;
or --CH═
CH--;
or(b) wherein 1, 2, or 3 of the substituents R1 are C1-6 alkyl and the remaining substituents are as above under (a).
- --O--;
Specification