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Title: |
US5888473:
Liposome compositions for boron neutron capture therapy and methods thereof
[ Derwent Title ]

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Country: |
US United States of America

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Inventor: |
Hawthorne, M. Frederick; Encino, CA
Feakes, Debra Arliene; Los Angeles, CA
Shelly, Kenneth John; Los Angeles, CA

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Assignee: |
The Regents of the University of California, Los Angeles, CA
other patents from UNIVERSITY OF CALIFORNIA, THE REGENTS OF (599425) (approx. 4,840)
News, Profiles, Stocks and More about this company

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Published / Filed: |
1999-03-30
/ 1995-08-03

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Application Number: |
US1995000511073

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IPC Code: |
Advanced:
A61K 9/127;
A61K 33/22;
A61K 41/00;
A61K 51/00;
A61P 35/00;
C07F 5/02;
Core:
C07F 5/00;
more...
IPC-7:
A61K 9/127;
A61K 51/12;
C04F 5/02;

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ECLA Code: |
A61K9/127;

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U.S. Class: |
Current:
424/001.21;
424/450;
564/004;
564/005;
564/008;
Original:
424/001.21;
424/450;
564/004;
564/005;
564/008;

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Field of Search: |
424/1.21,450,657
564/008,4,5
514/064
556/007
568/001,3,4
540/004,128

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Priority Number: |

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Abstract: |
Boron neutron capture therapy can utilize Xy B20 H17 L where X is an alkali metal, y is 1 to 4, and L is a two electron donor such as NH3, and Na2 B10 H9 NCO, among others. These borane salts may be used free or encapsulated in liposomes. Liposomes may have embedded within their bilayers carboranes to increase the amount of delivered 10 B and/or to increase the tumor specificity of the liposome.

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Attorney, Agent or Firm: |
Loeb & Loeb LLP ;

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Primary / Asst. Examiners: |
Hollinden, Gary E.; Hartley, Michael G.

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INPADOC Legal Status: |
None
Family Legal Status Report

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Parent Case: |
This is a division of application Ser. No. 08/071.702 filed on Jun. 3, 1993, now U.S. Pat. No. 5,648,532.

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Designated Country: |
AT BE CH DE DK ES FR GB GR IE IT LI LU MC NL BB BG BR BY CZ FI GE HU KG KP KR KZ LK LV MD MG MN MW NO NZ

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Family: |
Show 13 known family members

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First Claim:
Show all 19 claims |
What is claimed:
1. A tumor treating agent for boron neutron capture therapy comprising a liposome, the liposome having at least one encapsulating bilayer and an internal space defined by the encapsulating bilayer; and a borane compound within the internal space, wherein the borane compound is selected from the group consisting of
- (a) Xy B20 H17 L, wherein X is selected from the group consisting of alkali metals and tetra alkyl ammonium, y is 1 to 4 and L is selected from the group consisting of --NHR1 R2 wherein R1 and R2 are the same or different and are selected from the group consisting of hydrogen, benzyl, alkyl and diamine; --SR3 R4 wherein R3 and R4 are the same or different and are selected from the group consisting of H or alkyl; --CN; --CO; --NCO; --CH2 OH; --CO2 R1 ; -alkyl; --NHCONHR1 ; --COOH and -CONHR1, where R1 is selected from the group consisting of hydrogen, benzyl, alkyl and diamine;
- (b) Xs B10 H9 L, wherein X is selected from the group consisting of alkali metals and tetra alkyl ammonium, s is 1 or 2 and L is selected from the group consisting of --NHR1 R2 wherein R1 and R2 are the same or different and are selected from the group consisting of hydrogen, benzyl, alkyl and diamine; --SR3 R4 wherein R3 and R4 are the same or different and are selected from the group consisting of H or alkyl; --CN; --CO; --NCO; --CH2 OH; --CO2 R1 -alkyl; --NHCONHR1 ; --COOH and --CONHR1, where R1 is selected from the group consisting of hydrogen, benzyl, alkyl and diamine; and
- (c) mixtures of (a) and (b).

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Background / Summary: |
Show background / summary

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Drawing Descriptions: |
Show drawing descriptions

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Description: |
Show description

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Forward References: |
Show 2 U.S. patent(s) that reference this one

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Foreign References: |

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Other Abstract Info: |
CHEMABS 123(07)078659Z
DERABS C1995-036070

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Other References: |
Ji Li et al., "Simple Synthesis and Alkylation Reactions of 3-Iodo-O-Carborane and 9,12-Diiodo-O-Carborane," Inorg. Chem., vol. 30, No. 25, pp. 4866-4868, 1991.
(3 pages)
Cited by 3 patents
[ISI abstract]
M. Frederick Hawthorne et al., "A Study of the Reaction of Hydroxide Ion with B20 H18-2," Journal of the American Chemical Society, 87:21, pp. 4740-4746, Nov. 5, 1965.
Walter R. Hertler, et al., "Chemistry of Boranes XXIV. Carbonylation of Derivatives of B10 H102- and B12 H122- with Oxalyl Chloride," Inorganic Chemistry, vol. 4, No. 3, pp. 288-293, Mar. 1965.
Sol M. Gruner et al., "Materials Properties of Liposomal Bilayers," Princeton University, Princeton, New Jersey, 1990.
K. Shelly et al., "Synthesis of Monosubstituted Derivatives of closo-Decahydrodecaborate(2-), X-ray Crystal Structures of [closo-2-B10 H9 CO]- and [closo-2-B10 H9 NCO]2-," Inorganic Chemistry, vol. 31, No. 13, 1992, pp. 2889-2892.
(4 pages)
Cited by 2 patents
[ISI abstract]
C.A. Presant et al., "Preliminary Report: Imaging of Kaposi Sarcoma and Lymphoma in Aids with Indium-111-Labelled Liposomes," The Lancet, vol. 335, pp. 1307-1309, Jun. 2, 1990.
(3 pages)
Cited by 2 patents
C.A. Presant et al., "Successful Imaging of Human Cancer with Indium-111-Labelled Phospholid Vesicles," Cancer, 62, pp. 905-011, Sep. 1, 1988.
(7 pages)
Cited by 3 patents
S.M. Sullivan, Lipid Particles for Cytoplasmic Delivery of Active Agent-Esp. Oligo-Nucleotide, Are Liposome(s) Having Succinimidyl GPS. Extending from Surface, Abstract (Basic): WO 9205773 A.
F.C. Szoka et al., "Liposome Compsn.--Congt. Encapsulated Antiviral Cpd., E.g. Phosophono-Acetate or Phosphono-Formate, Used to Treat HV and Herpes Simplex Virus-2 Infections," Abstract (Basic), WO 8905152.
C.A. Presant et al., "Liposome(s) for Delivering Imaging Agent or Drug to Tumour Comprising Small Liposome(s) Prepd. from Pure Phospholipid," Abstract (Basic): EP 179444.
H. Hatanaka, "Boron-Neutron Capture Therapy for Tumors," 1986.
M.F. Hawthorne et al., "The Preparation of B10 H102- Ion," vol. IX, Inorgnaic Synthesis, ed. by S. Young Tyree, Jr., McGraw-Hill Publishing Co., Inc., 1967.
Debra A. Feakes et al., Na3 [B20 H17 NH3 ]: Synthesis and liposome delivery to murine tumors, Proc. Natl. Acad. Sci. USA, vol. 91, pp. 3029-3033, Apr. 1994.
(5 pages)
[ISI abstract]
K. Shelly et al., "Model studies directed toward the boron neutron-capture therapy by cancer: Boron delivery to murine tumors with liposomes," Proc. Natl. Acad. Sci. U.S.A., vol. 89, pp. 9039-9043, Oct. 1992.
(5 pages)
Cited by 8 patents
[ISI abstract]
K.C. John et al., The Aklylation and Acylation of B10 H9 NH3-, J. Med. Chem., vol. 12, pp. 54-57, Jan. 1969.

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