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US6143276A Expired / Lapsed US ⏱️ 0.0 years remaining

Methods for delivering bioactive agents to regions of elevated temperatures

Assignee: ImaRx Therapeutics Inc
•
Filing: 1997-03-21
•
Granted: 2000-11-07
•
Expires: 2017-03-21
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Abstract

Abstract Novel methods for delivering bioactive agents to particular regions or tissues of the body of a patient are provided.

Inventors

  • 👤 Evan C. Unger

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 17:36
CPC Classifications
A; A61; A61K; A61K41/00; A61K41/0028; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/543; A61K47/544; A61K49/00; A61K49/22; A61K49/222; A61K49/223; A61K9/00; A61K9/10; A61K9/127; A61K9/1271; Y; Y10; Y10S; Y10S977/00; Y10S977/70; Y10S977/788; Y10S977/797; Y10S977/798; Y10S977/799; Y10S977/801; Y10S977/902; Y10S977/904; Y10S977/906; Y10S977/907; Y10S977/926

Claims Analysis

Total Claims: 62
Claim 1
Independent Claim 54 words
A method for delivering a bioactive agent to a region of elevated temperature in a patient comprising administering to the patient a composition comprising a bioactive agent and a gaseous precursor which undergoes a phase transition to a gas at said region of elevated temperature in the absence of an application of external heat.
Claim 2
Independent Claim 54 words
A method for delivering a bioactive agent to a region of elevated temperature in a patient comprising administering to the patient a composition comprising a bioactive agent and a gaseous precursor which undergoes a phase transition to a gas at said region of elevated temperature in the absence of an application of external heat.
Claim 3
Dependent Claim 14 words
A method according to claim 1 wherein said gaseous precursor is an organic halide.
Claim 4
Dependent Claim 24 words
A method according to claim 2 wherein said halide in said gaseous precursor is selected from the group consisting of fluorine, chlorine and bromine.
Claim 5
Dependent Claim 15 words
A method according to claim 3 wherein said halide in said gaseous precursor is fluorine.
Claim 6
Dependent Claim 40 words
A method according to claim 4 wherein said gaseous precursor is selected from the group consisting of 3-fluorobenzaldehyde, 2-fluoro-5-nitrotoluene, 3-fluorostyrene, perfluoro-2-methyl-2-pentene, 3,5-difluoroaniline, 2,2,2-trifluoroethylacrylate, 3-(trifluoromethoxy)-acetophenone, 1,1,2,2,3,3,4,4-octafluorobutane, 1,1,1,3,3-pentafluorobutane, perfluorocyclohexane, perfluoromethyl-n-butyl ether, perfluoromethylisopropyl ether, perfluoromethyl-t-butyl ether, 1-fluorobutane, 1-bromononafluorobutane, 4-trifluoromethyl perfluorotetrahydrofuran, perfluorotetrahydropyran, and perfluoropentane.
Claim 7
Dependent Claim 15 words
A method according to claim 3 wherein said halide in said gaseous precursor is bromine.
Claim 8
Dependent Claim 23 words
A method according to claim 6 wherein said gaseous precursor is selected from the group consisting of: 1-bromoethane, 6-bromo-1-hexene, 2-bromo-2-nitropropane, 2-bromo-5-nitrothiophene, and 2-bromopropene.
Claim 9
Dependent Claim 15 words
A method according to claim 3 wherein said halide in said gaseous precursor is chlorine.
Claim 10
Dependent Claim 20 words
A method according to claim 8 wherein said gaseous precursor is selected from the group consisting of 3-chloro-5,5-dimethyl-2-cyclohexene and 2-chloro-2-methyl-propane.
Claim 11
Dependent Claim 42 words
A method according to claim 2 wherein said gaseous precursor is selected from the group consisting of 1-chloro-1-fluoro-1-bromomethane, 1,1,1-trichloro-2,2,2-trifluoroethane, 1,2-dichloro-2,2-difluoroethane, 1,1-dichloro-1,2-difluoroethane, 1,2-dichloro-1,1,3-trifluoropropane, 1,1,2,2,3,3,4,4-octafluorobutane, 1,1,1,3,3-pentafluorobutane, 1-bromoperfluorobutane, 1-bromo-2,4-difluorobenzene, 2-iodo-1,1,1-trifluoroethane, 5-bromovaleryl chloride, 1,3-dichlorotetrafluoroacetone, bromine pentafluoride, 1-bromo-1,1,2,3,3,3-hexafluoropropane, 2-chloro-1,1,1,4,4,4-hexafluoro-2-butene, 2-chloropentafluoro-1,3-butadiene, iodotrifluoroethylene, 1,1,2-trifluoro-2-chloroethane, 1,2-difluorochloroethane, 1,1-difluoro-2-chloroethane, 1,1-dichlorofluoroethane, and heptafluoro-2-iodopropane.
Claim 12
Dependent Claim 24 words
A method according to claim 1 wherein the phase transition temperature of said gaseous precursor is from about 28.5° C. to about 56° C.
Claim 13
Dependent Claim 24 words
A method according to claim 11 wherein the phase transition temperature of said gaseous precursor is from about 35° C. to about 52° C.
Claim 14
Dependent Claim 24 words
A method according to claim 12 wherein the phase transition temperature of said gaseous precursor is from about 37° C. to about 48° C.
Claim 15
Dependent Claim 24 words
A method according to claim 13 wherein the phase transition temperature of said gaseous precursor is from about 38° C. to about 42° C.
Claim 16
Dependent Claim 28 words
A method according to claim 1 further comprising a stabilizing material and wherein said stabilizing material is selected from the group consisting of lipids, polymers, proteins, and surfactants.
Claim 17
Dependent Claim 12 words
A method according to claim 15 wherein said stabilizing material comprises lipids.
Claim 18
Dependent Claim 11 words
A method according to claim 16 wherein said lipids comprise phospholipids.
Claim 19
Dependent Claim 21 words
A method according to claim 17 wherein said phospholipids are selected from the group consisting of phosphatidylcholine, phosphatidylethanolamine and phosphatidic acid.
Claim 20
Dependent Claim 21 words
A method according to claim 18 wherein said phosphatidylcholine is selected from the group consisting of dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine.
Claim 21
Dependent Claim 11 words
A method according to claim 19 wherein said phosphatidylcholine comprises dipalmitoylphosphatidylcholine.
Claim 22
Dependent Claim 21 words
A method according to claim 18 wherein said phosphatidylethanolamine is selected from the group consisting of dipalmitoylphosphatidylethanolamine, dioleoylphosphatidylethanolamine, N-succinyldioleoylphosphatidylethanolamine and 1-hexadecyl-2-palmitoylglycerophosphoethanolamine.
Claim 23
Dependent Claim 11 words
A method according to claim 18 wherein said phosphatidylethanolamine comprises dipalmitoylphosphatidylethanolamine.
Claim 24
Dependent Claim 13 words
A method according to claim 18 wherein said phosphatidic acid comprises dipalmitolylphosphatidic acid.
Claim 25
Dependent Claim 12 words
A method according to claim 15 wherein said stabilizing material comprises proteins.
Claim 26
Dependent Claim 11 words
A method according to claim 24 wherein said proteins comprise albumin.
Claim 27
Dependent Claim 12 words
A method according to claim 15 wherein said stabilizing material comprises polymers.
Claim 28
Dependent Claim 13 words
A method according to claim 26 wherein said polymers comprise a hydrophilic polymer.
Claim 29
Dependent Claim 13 words
A method according to claim 27 wherein said hydrophilic polymer comprises polyethylene glycol.
Claim 30
Dependent Claim 83 words
A method according to claim 26 wherein said polymers comprise synthetic polymers or copolymers which are prepared from monomers selected from the group consisting of acrylic acid, methacrylic acid, ethyleneimine, crotonic acid, acrylamide, ethyl acrylate, methyl methacrylate, 2-hydroxyethyl methacrylate, lactic acid, glycolic acid, E-caprolactone, acrolein, cyanoacrylate, cyanomethacrylate, bisphenol A, epichlorhydrin, hydroxyalkylacrylates, siloxane, dimethylsiloxane, ethylene oxide, ethylene glycol, hydroxyalkylmethacrylates, N-substituted acrylamides, N-substituted methacrylamides, N-vinyl-2-pyrrolidone, 2,4-pentadiene-1-ol, vinyl acetate, acrylonitrile, styrene, p-amino-styrene, p-aminobenzylstyrene, sodium styrene sulfonate, sodium 2-sulfoxyethyl-methacrylate, vinyl pyridine, aminoethyl methacrylates, lactides, and 2-methacryloyloxytrimethyl-ammonium chloride.
Claim 31
Dependent Claim 46 words
A method according to claim 29 wherein said polymers comprise synthetic polymers or copolymers selected from the group consisting of polyacrylic acid, polyethyleneimine, polymethacrylic acid, polymethylmethacrylate, polycyanomethacrylate, polysiloxane, polydimethylsiloxane, polylactic acid, poly(ε-caprolactone), epoxy resin, poly(ethylene oxide), poly(ethylene glycol), polyamide, polyvinylidene-polyacrylonitrile, polyvinylidene-polyacrylonitrile-polymethylmethacrylate, polylactide coglycolide, nylon and polystyrene-polyacrylonitrile.
Claim 32
Dependent Claim 11 words
A method according to claim 30 wherein said polymers comprise polycyanomethacrylate.
Claim 33
Dependent Claim 13 words
A method according to claim 15 wherein said stabilizing material comprises a surfactant.
Claim 34
Dependent Claim 22 words
A method according to claim 32 wherein the surfactant is selected from the group consisting of perfluorinated alkylated surfactants and fluorine-containing carbohydrates.
Claim 35
Dependent Claim 17 words
A method according to claim 15 wherein said stabilizing material is in the form of a vesicle.
Claim 36
Dependent Claim 19 words
A method according to claim 34 wherein said vesicles are selected from the group consisting of micelles and liposomes.
Claim 37
Dependent Claim 13 words
A method according to claim 34 wherein said vesicles are formulated from lipids.
Claim 38
Dependent Claim 11 words
A method according to claim 36 wherein said lipids comprise phospholipids.
Claim 39
Dependent Claim 21 words
A method according to claim 37 wherein said phospholipids are selected from the group consisting of phosphatidylcholine, phosphatidylethanolamine and phosphatidic acid.
Claim 40
Dependent Claim 21 words
A method according to claim 38 wherein said phosphatidylcholine is selected from the group consisting of dioleoylphosphatidylcholine, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine.
Claim 41
Dependent Claim 11 words
A method according to claim 39 wherein said phosphatidylcholine comprises dipalmitoylphosphatidylcholine.
Claim 42
Dependent Claim 21 words
A method according to claim 38 wherein said phosphatidylethanolamine is selected from the group consisting of dipalmitoylphosphatidylethanolamine, dioleoylphosphatidylethanolamine, N-succinyldioleoylphosphatidylethanolamine and 1-hexadecyl-2-palmitoylglycerophosphoethanolamine.
Claim 43
Dependent Claim 11 words
A method according to claim 41 wherein said phosphatidylethanolamine comprises dipalmitoylphosphatidylethanolamine.
Claim 44
Dependent Claim 13 words
A method according to claim 38 wherein said phosphatidic acid comprises dipalmitolylphosphatidic acid.
Claim 45
Dependent Claim 13 words
A method according to claim 38 wherein said lipid further comprises a polymer.
Claim 46
Dependent Claim 13 words
A method according to claim 44 wherein said polymer comprises a hydrophilic polymer.
Claim 47
Dependent Claim 13 words
A method according to claim 45 wherein said hydrophilic polymer comprises polyethylene glycol.
Claim 48
Dependent Claim 11 words
A method according to claim 34 wherein said vesicles comprise proteins.
Claim 49
Dependent Claim 11 words
A method according to claim 47 wherein said proteins comprise albumin.
Claim 50
Dependent Claim 11 words
A method according to claim 34 wherein said vesicles comprise polymers.
Claim 51
Dependent Claim 82 words
A method according to claim 49 wherein said polymers comprise synthetic polymers or copolymers which are prepared from monomers selected from the group consisting of acrylic acid, methacrylic acid, ethyleneimine, crotonic acid, acrylamide, ethyl acrylate, methyl methacrylate, 2-hydroxyethyl methacrylate, lactic acid, glycolic acid, E-caprolactone, acrolein, cyanoacrylate, bisphenol A, epichlorhydrin, hydroxyalkylacrylates, siloxane, dimethylsiloxane, ethylene oxide, ethylene glycol, hydroxyalkylmethacrylates, N-substituted acrylamides, N-substituted methacrylamides, N-vinyl-2-pyrrolidone, 2,4-pentadiene-1-ol, vinyl acetate, acrylonitrile, styrene, p-aminostyrene, p-aminobenzylstyrene, sodium styrene sulfonate, sodium 2-sulfoxyethylmethacrylate, vinyl pyridine, aminoethyl methacrylates, lactides and 2-methacryloyloxytrimethyl-ammonium chloride.
Claim 52
Dependent Claim 45 words
A method according to claim 50 wherein said polymers comprise synthetic polymers or copolymers selected from the group consisting of polyacrylic acid, polyethyleneimine, polymethacrylic acid, polymethylmethacrylate, polysiloxane, polydimethylsiloxane, polylactic acid, poly(ε-caprolactone), epoxy resin, poly(ethylene oxide), poly(ethylene glycol), polyamide, polyvinylidene-polyacrylonitrile, polyvinylidene-polyacrylonitrile-polymethylmethacrylate, polylactide coglycolide, nylon and polystyrene-polyacrylonitrile.
Claim 53
Dependent Claim 12 words
A method according to claim 34 wherein said vesicles comprise unilamellar vesicles.
Claim 54
Dependent Claim 12 words
A method according to claim 52 wherein said vesicles comprise one monolayer.
Claim 55
Dependent Claim 20 words
A method according to claim 34 wherein said vesicles are selected from the group consisting of oligolamellar and multilamellar vesicles.
Claim 56
Dependent Claim 22 words
A method according to claim 1 wherein said bioactive agent is selected from the group consisting of pharmaceutical agents, and diagnostic agents.
Claim 57
Dependent Claim 13 words
A method according to claim 55 wherein said bioactive agent is a pharmaceutical.
Claim 58
Dependent Claim 43 words
A method according to claim 56 wherein the pharmaceutical is selected from the group consisting of antibiotics, hormones, vasoactive compounds, antithrombotics, chemotherapeutic agents, bioactive peptides, mitotic inhibitors, antihelminthics, antimalarials, antituberculosis agents, immune sera, antitoxins, antivenins, vaccines, vitamins, anti-coagulants, antiinflammatory agents, RNA and DNA.
Claim 59
Dependent Claim 16 words
A method according to claim 1, further comprising the application of external heat to the region.
Claim 60
Dependent Claim 27 words
The method of claim 1 wherein the region of elevated temperature is associated with a condition selected from the group consisting of disease, infection, inflammation, and injury.
Claim 61
Independent Claim 50 words
A method for treating a region of elevated temperature in a patient comprising administering to the patient a composition comprising a pharmaceutical agent and a gaseous precursor which undergoes a phase transition to a gas at said region of elevated temperature in the absence of an application of external heat.
Claim 62
Independent Claim 50 words
A method for treating a region of elevated temperature in a patient comprising administering to the patient a composition comprising a pharmaceutical agent and a gaseous precursor which undergoes a phase transition to a gas at said region of elevated temperature in the absence of an application of external heat.

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