Claims
- 1. A compound of the formula
- 2. The compound of claim 1 where R1, R8 or R11 is
- 3. The compound of claim 1 where R1, R8 or R11 is —(CH2)2CONHphenyleneCH2DTPA.
- 4. The compound of claim 2 where R8 is
- 5. The compound of claim 3 where R8 is —(CH2)2CONHphenyleneCH2DTPA.
- 6. The compound of claim 5 where R2 is —CH3 and R5 is —CH2CH3.
- 7. The compound of claim 1 where R6 is
- 8. The compound of claim 7 where R6 is
- 9. A Technetium99m complex of the compound of claim 2.
- 10. An Indium111 complex of the compound of claim 3.
- 11. A Gadolinium(III) complex of the compound of claim 3.
- 12. The compound of claim 9 wherein the compound is a 99mTc bisaminoethanethiol analog of HPPH.
- 13. The compound of claim 10 wherein the compound is a 111In aminophenyl DTPA analog of HPPH.
- 14. The compound of claim 11 wherein the compound is HPPH-Gd(III)aminophenylDTPA
- 15. The compound of claim 11 wherein the compound is purpurin 18 imide-Gd(III)aminophenylDTPA.
- 16. The compound of claim 11 wherein the compound is a Gd(III)aminophenylDTPA analog of bacteriochlorin.
- 17. A method for the preparation of the compound of claim 14 which comprises:
hydrolizing methyl 3-(hexyloxy)ethyl pheophorbide a with an aqueous solution of LiOH, methanol and tetrahydrofuran to obtain the corresponding carboxylic acid; reacting the carboxylic acid with 4-aminophenyl DTPA penta-tert-butyl ester to produce the tert-butyl aminophenyl DTPA analog; reacting the DTPA analog with trifluoroacetic acid to convert the tertiary butyl groups to carboxylic acid groups; reacting with a solution of Gadolinium hexahydrate.
- 18. A method for the preparation of the compound of claim 15 which comprises:
hydrolizing a methyl ester group of the hexylether derivative of N-hexyl purpurinimide to the corresponding carboxylic acid; reacting the resulting carboxy purpurin imide with a solution of aminophenylDTPA penta-tert-butyl ester; reacting the resulting conjugate with trifluoroacetic acid to obtain a carboxylic acid; and reacting the resulting carboxylic acid with Gadolinium chloride to obtain the desired compound.
- 19. A method for the preparation of the compound of claim 16 which comprises:
hydrogenating 3 vinyl purpurinimide 7 to obtain meso-N-hexyl-purpurin-18-imide; reacting the meso-N-hexyl-purpurin-18-imide with osmiumtetroxide, pyridine and H2S to obtain vic-dihydroxybacteriochlorin; reacting the vic-dihydroxybacteriochlorin with sulfuric acid to obtain a 7-ketobacteriochlorin; hydrolizing a methyl ester group in the 7-ketobacteriochlorin to a carboxy group; reacting the carboxy 7-ketobacteriochlorin with aminophenylDTPA penta-tertiary butyl ester; reacting the resulting product with trifluoroacetic acid to obtain the corresponding carboxylic acid DTPA analog; and reacting the carboxy DTPA analog with Gadolinium chloride to obtain the desired compound.
- 20. A method for the preparation of the compound of claim 12 which comprises:
reacting HPPH with aminobisethanethiol to obtain a thioprotected HPPH conjugate; reacting the conjugate with triethylsilane and TFA to deprotect the thiols; and reacting the conjugate with deprotected thiols with 99mTc pertechnatate reduced by Sn(II) glucoheptonate to obtain the desired compound.
- 21. A method for the preparation of the compound of claim 12 which comprises:
reacting HPPH-aminophenylDTPA with 111In(III)chloride to obtain the desired compound.
Parent Case Info
[0001] This application claims priority from Provisional Patent Application No. 60/171,961 filed Dec. 23, 1999.
Provisional Applications (1)
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Number |
Date |
Country |
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60171961 |
Dec 1999 |
US |