Title: Porphyrin Based neuton capture agents for cancer therapy

Abstract

The invention describes the synthesis of a panel of novel carbon-carbon linked carboranyl-containing 5,10,15,20-tetraphenylporphyrins bearing 25–44% boron by weight. In certain embodiments, a phenyl porphyrin compound has a carboranyl group attached to the phenyl group by a carbon-carbon linkage, wherein the phenyl group corresponds to the following formula where R7 through R11 are hydrogen, a carboranyl group, or are selected from the group consisting of hydroxyl, NMe₃⁺, PMePh₂⁺, PO(OH)₂, SO₃H, COOH, and NH₂. In this embodiment, the carboranyl group is attached to the phenyl group by a carbon-carbon linkage, either one or two of R7 through R11 are other than hydrogen; and the phenyl porphyrin compound contains at least one phenyl group having at least one of said carboranyl groups.

Inventors:

Vicente, Maria Da; Shetty, Shankar Jayaram; Jaquinod, Laurent; Smith, Kevin M.

Issue Date:

2006-06-27

Research Org.:

Univ. of California, Oakland, CA (United States)

Sponsoring Org.:

USDOE

OSTI Identifier:

1175809

Patent Number(s):

7067653

Application Number:

10/258,948

Assignee:

The Regents of the University of California (Oakland, CA)

Patent Classifications (CPCs):

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

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A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61K - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

A61K41/0071 - {PDT with porphyrins having exactly 20 ring atoms, i.e. based on the non-expanded tetrapyrrolic ring system, e.g. bacteriochlorin, chlorin-e6, or phthalocyanines}
A61K41/0095 - {Boron neutron capture therapy, i.e. BNCT, e.g. using boronated porphyrins}

A - HUMAN NECESSITIES A61 - MEDICAL OR VETERINARY SCIENCE A61P - SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

A61P35/00 - Antineoplastic agents

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07D - HETEROCYCLIC COMPOUNDS

C07D487/22 - in which the condensed system contains four or more hetero rings

C - CHEMISTRY C07 - ORGANIC CHEMISTRY C07F - ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM

C07F5/05 - Cyclic compounds having at least one ring containing boron but no carbon in the ring

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DOE Contract Number:  

98ER62633

Resource Type:

Patent

Country of Publication:

United States

Language:

English

Subject:

60 APPLIED LIFE SCIENCES