Patent US5087616A successfully refreshed from Google Patents.
US5087616A
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Cytotoxic drug conjugates and their delivery to tumor cells
Assignee: Battelle Memorial Institute Inc
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Filing: 1987-08-06
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Granted: 1992-02-11
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Expires: 2007-08-06
Abstract
Abstract A therapeutic composition comprising a chemical conjugatge including a first moiety, other than an immunoglobulin or fragment thereof, such as epidermal growth factor, which preferentially binds to a tumor cell, and is internalized by the cell, and a second moiety linked to the first moiety, and comprising a biodegradable polymeric carrier, such as polyglutamic acid, to which one or more cytotoxic molecules, for instance, daunomycin, are attached. The degradation of the carrier by intracellular enzymes releases a cytotoxic agent, resulting in selective destruction of the tumor cells.
Inventors
- 👤 Andre E. Myers
- 👤 Daniel Bichon
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 21:59
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61K47/64; A61K47/645; A61K47/642; A61P; A61P35/00
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
102 words
A therapeutic chemical conjugate including EGF as a first moiety, and a second moiety linked covalently to the EGF, said second moiety comprising a plurality of repeating units, each unit having the structure ##STR12## where L is selected from the group consisting of polyglutamic acid and polyaspartic acid, and T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, cisplatin, adriamycin, daunomycin, and daunorubicin, and where said conjugate has a molecular weight of between 10,000 and 100,000 D and is effective in target cells in vivo and is internalized by tumor cells whereby the latter are inhibited or destroyed.
Claim 2
Dependent Claim
102 words
A therapeutic chemical conjugate including EGF as a first moiety, and a second moiety linked covalently to the EGF, said second moiety comprising a plurality of repeating units, each unit having the structure ##STR12## where L is selected from the group consisting of polyglutamic acid and polyaspartic acid, and T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, cisplatin, adriamycin, daunomycin, and daunorubicin, and where said conjugate has a molecular weight of between 10,000 and 100,000 D and is effective in target cells in vivo and is internalized by tumor cells whereby the latter are inhibited or destroyed.
Claim 3
Dependent Claim
14 words
The conjugate of claim 1 wherein L is polyglutamic acid and T is daunomycin.
Claim 4
Dependent Claim
14 words
The conjugate of claim 1, where the EGF is essentially identical to human EGF.
Claim 5
Dependent Claim
22 words
The conjugate of claim 1, wherein the first moiety is directly linked to the second moiety by means of a peptidyl linkage.
Claim 6
Dependent Claim
45 words
The conjugate of claim 1 wherein the first moiety is linked to the second moiety by a structure having the formula: ##STR13## where R' is: alkylene (C 1 -C 4 ); 1,3-phenylene; cyclohexylene-4-methylene; or alkylene (C 1 -C 4 )-phenylene (1,4); and m=1 or 2.
Claim 7
Dependent Claim
15 words
The conjugate of claim 1, having a molecular weight of less than about 100,000 D.
Claim 8
Dependent Claim
22 words
The conjugate of claim 1 wherein the T is selected from the group consisting of anthracycline drugs, bleomycin, melphalan, chlorambucil, and cisplatin.
Claim 9
Dependent Claim
19 words
The conjugate of claim 7 wherein the T is selected from the group consisting of adriamycin, daunomycin, and daunorubicin.
Claim 10
Dependent Claim
10 words
The conjugate of claim 1 wherein the T is daunomycin.
Claim 11
Dependent Claim
25 words
A therapeutic composition comprising the chemical conjugate of claim 1 and a therapeutically acceptable carrier having a molecular weight of between 10,000 and 100,000 D.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1995-02-10 | 1995-08-12 | 1996-02-11 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-02-10 | 1999-08-12 | 2000-02-11 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-02-10 | 2003-08-12 | 2004-02-11 | $7700.00 | Window Closed / Lapsed |