Patent US4959356A successfully refreshed from Google Patents.
← Back to Patent Explorer
US4959356A Expired / Lapsed US ⏱️ 0.0 years remaining

Porphyrins for boron neutron capture therapy

Assignee: United States Department of Energy
•
Filing: 1989-05-26
•
Granted: 1990-09-25
•
Expires: 2009-05-26
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract Novel compounds for treatment of brain tumors in Boron Neutron Capture Therapy are disclosed. A method for preparing the compounds as well as pharmaceutical compositions containing said compounds are also disclosed. The compounds are water soluble, non-toxic and non-labile boronated porphyrins which show significant uptake and retention in tumors.

Inventors

  • 👤 Michiko Miura
  • 👤 Detlef Gabel

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 20:50
CPC Classifications
C; C07; C07F; C07F5/00; C07F5/02; C07F5/027; A; A61; A61K; A61K41/00; A61K41/009; A61K41/0095

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 25 words
A compound of the formula ##STR5## wherein R is hydrogen or lower alkyl having 1 to 6 carbon atoms and n is 0 to 10.
Claim 2
Dependent Claim 25 words
A compound of the formula ##STR5## wherein R is hydrogen or lower alkyl having 1 to 6 carbon atoms and n is 0 to 10.
Claim 3
Dependent Claim 9 words
3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)-ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin dimethyl ester.
Claim 4
Dependent Claim 9 words
3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)-ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin dimethyl ester.
Claim 5
Dependent Claim 7 words
3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)-ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin.
Claim 6
Dependent Claim 7 words
3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)-ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin.
Claim 7
Dependent Claim 40 words
A compound of the formula ##STR6## wherein X is 2H or a bindable metal selected from the group consisting of zinc, iron, magnesium, manganese, copper, cobalt, germanium and gadolinium; R' is an alkali metal; and n is 0 to 10.
Claim 8
Dependent Claim 40 words
A compound of the formula ##STR6## wherein X is 2H or a bindable metal selected from the group consisting of zinc, iron, magnesium, manganese, copper, cobalt, germanium and gadolinium; R' is an alkali metal; and n is 0 to 10.
Claim 9
Dependent Claim 8 words
Dipotassium 3,8-(1,1 1 (2,2 1 -bis-(7,8-dicarbaundecaborate)-1))ethenyl)-13,17-dipropionic acid-2,7,12,18-tetramethyl porphyrin.
Claim 10
Dependent Claim 8 words
Dipotassium 3,8-(1,1 1 (2,2 1 -bis-(7,8-dicarbaundecaborate)-1))ethenyl)-13,17-dipropionic acid-2,7,12,18-tetramethyl porphyrin.
Claim 11
Dependent Claim 45 words
A compound of the formula ##STR7## wherein Y is a bindable metal selected from the group consisting of zinc, iron, magnesium, manganese, copper, cobalt, germanium and gadolinium; R" is a lower alkyl group containing 1 to 6 carbon atoms; and n is 0 to 10.
Claim 12
Dependent Claim 45 words
A compound of the formula ##STR7## wherein Y is a bindable metal selected from the group consisting of zinc, iron, magnesium, manganese, copper, cobalt, germanium and gadolinium; R" is a lower alkyl group containing 1 to 6 carbon atoms; and n is 0 to 10.
Claim 13
Dependent Claim 16 words
The compound of claim 6 wherein Y is zinc, R" is methyl and n is 0.
Claim 14
Independent Claim 25 words
A method of treating malignant brain tumors using Boron Neutron Capture Therapy wherein the boron drug employed is 3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin.
Claim 15
Independent Claim 25 words
A method of treating malignant brain tumors using Boron Neutron Capture Therapy wherein the boron drug employed is 3,8-(1,1 1 (2,2 1 -bis-(1,2-dicarbadodecaboranyl)ethenyl) 13,17-dipropionic acid-2,7,12,18-tetramethylporphyrin.
Claim 16
Independent Claim 26 words
A method of treating malignant brain tumors using Boron Neutron Capture Therapy wherein the boron drug employed is dipotassium 3,8-(1,1 1 (2,2 1 -bis-(7,8-dicarbaundecaborate-(-1))ethenyl)-13,17-dipropionic acid-2,7,12,18-tetramethyl porphyrin.
Claim 17
Independent Claim 26 words
A method of treating malignant brain tumors using Boron Neutron Capture Therapy wherein the boron drug employed is dipotassium 3,8-(1,1 1 (2,2 1 -bis-(7,8-dicarbaundecaborate-(-1))ethenyl)-13,17-dipropionic acid-2,7,12,18-tetramethyl porphyrin.
Claim 18
Dependent Claim 127 words
In a method of treating a patient with a malignant tumor which comprises administering to the patient a dose of a generally nontoxic compound which contains an element having an isotope that emits alpha particles when bombarded with neutrons, said compound being administered in a dosage sufficient to accumulate said isotope in the tumor in a concentration of at least 10 ppm; providing a source that emits neutrons having an energy distribution effective for neutron capture, said source having a port through which a beam of neutrons is emitted; and positioning the patient so that said tumor is in the path of said beam for a time sufficient to effect substantial tumor tissue deterioration; the improvement comprising using as the generally nontoxic compound a 3,8-(1,1'(2,2'-bis-(7,8-dicarbaundecaborate(-1)alkenyl) porphyrin derivative.
Claim 19
Dependent Claim 127 words
In a method of treating a patient with a malignant tumor which comprises administering to the patient a dose of a generally nontoxic compound which contains an element having an isotope that emits alpha particles when bombarded with neutrons, said compound being administered in a dosage sufficient to accumulate said isotope in the tumor in a concentration of at least 10 ppm; providing a source that emits neutrons having an energy distribution effective for neutron capture, said source having a port through which a beam of neutrons is emitted; and positioning the patient so that said tumor is in the path of said beam for a time sufficient to effect substantial tumor tissue deterioration; the improvement comprising using as the generally nontoxic compound a 3,8-(1,1'(2,2'-bis-(7,8-dicarbaundecaborate(-1)alkenyl) porphyrin derivative.
Claim 20
Dependent Claim 19 words
A process according to claim 10 wherein the dicarboranyl caged porphyrin comprises dipotassium 3,8-(1,1 1 -(2,2 1 -bis-(7,8-dicarbaundecaborate(-1)ethenyl)-13,17-diproprionic acid-2,7,12,18-tetramethylporphyrin.
Claim 21
Dependent Claim 19 words
A process according to claim 10 wherein the dicarboranyl caged porphyrin comprises 3,8-(1,1 1 (2,2 1 -bis-(7,8-dicarbaundecaborate(-1))ethenyl)-13,17-dipropionic acid -2,7,12,18-tetramethylporphyrin.

References Cited (Backward Citations)

US2858320A Cited
US4386087A Cited
US4500507A Cited
US4516535A Cited
US4675338A Cited
US4693885A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1993-09-24 1994-03-26 1994-09-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1997-09-24 1998-03-26 1998-09-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2001-09-24 2002-03-26 2002-09-25 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag