US5149794A
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Covalent lipid-drug conjugates for drug targeting
Assignee: Oregon Health & Science University
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Filing: 1990-11-01
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Granted: 1992-09-22
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Expires: 2010-11-01
Abstract
Abstract This invention relates to a novel method of drug targeting which comprises covalently binding a drug to a lipid carrier. This composition has the unique ability to both enhance the rate at which an antineoplastic or antiviral drug crosses the plasma membrane, and to direct the drug within the cell to specific organelles. The versatility of these conjugates may be further enhanced by including a spacer group between the drug and the lipid which may act to modulate drug release at the target site.
Inventors
- 👤 Milton B. Yatvin
- 👤 David W. Parks
- 👤 Ronald W. McClard
- 👤 Michael H. B. Stowell
- 👤 John F. Witte
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 14:48
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/543; A61K47/544; A61K47/62; A61K47/65
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
73 words
A composition of matter comprising an antiviral or antineoplastic drug, a polar lipid carrier, two linker functional groups and a spacer, wherein the spacer has a first end and a second end and wherein the polar lipid is attached to the first end of the spacer through a first linker functional group and the antiviral or antineoplastic drug is attached to the second end of the spacer through a second linker functional group.
Claim 2
Dependent Claim
73 words
A composition of matter comprising an antiviral or antineoplastic drug, a polar lipid carrier, two linker functional groups and a spacer, wherein the spacer has a first end and a second end and wherein the polar lipid is attached to the first end of the spacer through a first linker functional group and the antiviral or antineoplastic drug is attached to the second end of the spacer through a second linker functional group.
Claim 3
Dependent Claim
56 words
A composition of matter according to claim 1 wherein the spacer allows the drug to act without being released at an intracellular site and wherein the first linker functional group attached to the first end of the spacer is strong and the second linker functional group attached to the second end of the spacer is weak.
Claim 4
Dependent Claim
58 words
A composition of matter according to claim 1 wherein the spacer allows the drug to facilitate hydrolytic release of the drug at an intracellular site and wherein the first linker functional group attached to the first end of the spacer is strong and the second linker functional group attached to the second end of the spacer is weak.
Claim 5
Dependent Claim
58 words
A composition of matter according to claim 1 wherein the spacer allows the drug to facilitate enzymatic release of the drug at an intracellular site and wherein the first linker functional group attached to the first end of the spacer is strong and the second linker functional group attached to the second end of the spacer is weak.
Claim 6
Dependent Claim
24 words
A composition of matter according to claim 1 wherein the polar lipid is sphingosine, ceremide, phosphatidyl choline, phosphatidyl glycerol, phosphatidyl ethanolamine or phosphatidic acid.
Claim 7
Dependent Claim
38 words
A composition of matter according to claim 1 wherein the spacer is a peptide of formula n , wherein n is an integer between 2 and 25, and the peptide comprises a polymer of a particular amino acid.
Claim 8
Dependent Claim
53 words
A composition of matter comprising an antiviral or antineoplastic drug having a first functional linker group, and a polar lipid carrier having a second functional linker group, wherein the antiviral or antineoplastic drug is covalently linked to the polar lipid carrier by a chemical bond between the first and second functional linker groups.
Claim 9
Dependent Claim
53 words
A composition of matter comprising an antiviral or antineoplastic drug having a first functional linker group, and a polar lipid carrier having a second functional linker group, wherein the antiviral or antineoplastic drug is covalently linked to the polar lipid carrier by a chemical bond between the first and second functional linker groups.
Claim 10
Dependent Claim
36 words
A composition of matter according to claim 7 wherein the first functional linker group is a hydroxyl group, a primary or secondary amino group, a phosphate group or substituted derivatives thereof or a carboxylic acid group.
Claim 11
Dependent Claim
36 words
A composition of matter according to claim 7 wherein the second functional linker group is a hydroxyl group, a primary or secondary amino group, a phosphate group or substituted derivatives thereof or a carboxylic acid group.
Claim 12
Dependent Claim
24 words
A composition of matter according to claim 7 wherein the polar lipid is sphingosine, ceremide, phosphatidyl choline, phosphatidyl glycerol, phosphatidyl ethanolamine or phosphatidic acid.
References Cited (Backward Citations)
No citation records indexed.
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-09-22 | 1996-03-23 | 1996-09-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-09-22 | 2000-03-23 | 2000-09-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-09-22 | 2004-03-23 | 2004-09-22 | $7700.00 | Window Closed / Lapsed |