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Title: Carboranylporphyrins and uses thereof

Patent ·
OSTI ID:1175633

The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing 5, 10, 15, 20-tetraphenylporphyrin compounds and methods for their use particularly in boron neutron capture therapy (BNCT) and photodynamic therapy (PDT) for the treatment of tumors of the brain, head, neck, and surrounding tissue. The invention is also directed to using these carborane-containing tetraphenyl porphyrin compounds to methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Research Organization:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
AC02-98CH10886
Assignee:
Brookhaven Science Associates, LLC (Upton, NY)
Patent Number(s):
6,989,443
Application Number:
10/878,138
OSTI ID:
1175633
Country of Publication:
United States
Language:
English

References (17)

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19F NMR Spectra and Structures of Halogenated Porphyrins journal July 1995
Synthesis of carboranyl derivatives of deuteroporphyrin IX journal December 1999
A Carboranyl Porphyrin for Boron Neutron Capture Therapy of Brain Tumors book January 1989
In vivo animal studies with gadolinium (III) texaphyrin as a radiation enhancer journal November 1999
A Straightforward Synthesis of 3,4-Difluoropyrrole journal August 1998
Octabromotetraphenylporphyrin and its metal derivatives: Electronic structure and electrochemical properties journal January 1991
Porphyrin-mediated boron neutron capture therapy: evaluation of the reactions of skin and central nervous system journal January 2003
New Metalloporphyrins with Extremely Altered Redox Properties:  Synthesis, Structure, and Facile Reduction to Air-Stable π-Anion Radicals of Zinc and Nickel β-Heptanitroporphyrins journal July 1997
Synthesis of a porphyrin-labelled carboranyl phosphate diester: a potential new drug for boron neutron capture therapy of cancer journal July 2002
Current status of 10B-neutron capture therapy: Enhancement of tumor dose via beam filtration and dose rate, and the effects of these parameters on minimum boron content: A theoretical evaluation journal April 1985
2,3,7,8,12,13,17,18-Octafluoro-5,10,15,20-tetraarylporphyrins and Their Zinc Complexes:  First Spectroscopic, Electrochemical, and Structural Characterization of a Perfluorinated Tetraarylmetalloporphyrin journal March 1997
Evaluation of carborane-containing porphyrins as tumour targeting agents for boron neutron capture therapy. journal July 1998
Boron Neutron Capture Therapy for Glioblastoma Multiforme: Interim Results from the Phase I/II Dose-Escalation Studies journal June 1999
Syntheses of carboncarbon linked carboranylated porphyrins for boron neutron capture therapy of cancer journal September 2000
Synthesis, dark toxicity and induction of in vitro DNA photodamage by a tetra(4-nido-carboranylphenyl)porphyrin journal November 2002
Biodistribution of Copper Carboranyltetraphenylporphyrins in Rodents Bearing an Isogeneic or Human Neoplasm journal January 2001

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