US4526888A
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Nephrotoxicity inhibitors for aminoglycoside antibiotics
Assignee: Bristol Myers Co
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Filing: 1983-04-29
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Granted: 1985-07-02
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Expires: 2003-04-29
Abstract
Abstract This invention relates to the conjoint use of asparagine or aspartic acid polymers, e.g. poly-l-asparagine or poly-l-aspartic acid polymers, or copolymers thereof, with aminoglycoside antibiotics to inhibit the nephrotoxicity associated with aminoglycoside antibiotics.
Inventors
- 👤 Patricia D. Williams
- 👤 Girard H. Hottendorf
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 14:19
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/02; A61K31/00; A61K31/70; A61P; A61P31/00; A61P31/04; A61P43/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/29
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
105 words
An aminoglycoside composition having reduced nephrotoxicity, which comprises: (a) an aminoglycoside, or pharmaceutically acceptable salt thereof, and (b) at least 0.002 moles, per mole of aminoglycoside, of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the member has a molecular weight of from about 1000 to about 100,000.
Claim 2
Dependent Claim
105 words
An aminoglycoside composition having reduced nephrotoxicity, which comprises: (a) an aminoglycoside, or pharmaceutically acceptable salt thereof, and (b) at least 0.002 moles, per mole of aminoglycoside, of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the member has a molecular weight of from about 1000 to about 100,000.
Claim 3
Dependent Claim
50 words
The composition of claim 1 which comprises: (a) an aminoglycoside, or pharmaceutically acceptable salt thereof, and (b) at least 0.005 moles, per mole of aminoglycoside, of poly-l-asparagine or poly-l-aspartic acid, or a pharmaceutically acceptable salt thereof, wherein the polymer has a molecular weight of from about 5500 to about 16,000.
Claim 4
Dependent Claim
12 words
The composition of claim 2 wherein the aminoglycoside is gentamicin or amikacin.
Claim 5
Dependent Claim
37 words
The composition of claim 1 which comprises gentamicin, or a pharmaceutically acceptable salt thereof, and at least about 0.005 moles, per mole of gentamicin, of poly-l-asparagine having a molecular weight of from about 8000 to about 15,000.
Claim 6
Dependent Claim
44 words
The composition of claim 1 which comprises gentamicin, or a pharmaceutically acceptable salt thereof, and at least about 0.005 moles, per mole of gentamicin, of poly-l-aspartic acid having a molecular weight of from about 8000 to about 15,000, or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
37 words
The composition of claim 1 which comprises amikacin, or a pharmaceutically acceptable salt thereof, and at least about 0.005 moles, per mole of amikacin, of poly-l-asparagine having a molecular weight of from about 8000 to about 15,000.
Claim 8
Dependent Claim
43 words
The composition of claim 1 which comprises amikacin, or pharmaceutically acceptable salt thereof, and at least about 0.005 moles, per mole of amikacin, of poly-l-aspartic acid having a molecular weight of from about 8000 to about 15,000, or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
107 words
An aminoglycoside composition having reduced nephrotoxicity, in unit dosage form, which comprises: (a) a therapeutically effective amount of an aminoglycoside antibiotic and (b) a nephrotoxicity-reducing amount of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the polymer or copolymer has a molecular weight of from about 1000 to about 100,000.
Claim 10
Dependent Claim
107 words
An aminoglycoside composition having reduced nephrotoxicity, in unit dosage form, which comprises: (a) a therapeutically effective amount of an aminoglycoside antibiotic and (b) a nephrotoxicity-reducing amount of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the polymer or copolymer has a molecular weight of from about 1000 to about 100,000.
Claim 11
Dependent Claim
12 words
The composition of claim 8 which additionally contains a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
21 words
The composition of claim 8 wherein the polymer or copolymer has a molecular weight of from about 8000 to about 15,000.
Claim 13
Dependent Claim
12 words
The composition of claim 10 which additionally contains a pharmaceutically acceptable carrier.
Claim 14
Dependent Claim
36 words
The composition of claim 10 wherein the polymer is poly-l-asparagine or poly-l-aspartic acid, or a pharmaceutically acceptable salt thereof, and is present in an amount of at least about 0.005 moles per mole of aminoglycoside antibiotic.
Claim 15
Dependent Claim
12 words
The composition of claim 12 which additionally contains a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
12 words
The composition of claim 12 wherein the aminoglycoside is gentamicin or amikacin.
Claim 17
Dependent Claim
12 words
The composition of claim 14 which additionally contains a pharmaceutically acceptable carrier.
Claim 18
Independent Claim
110 words
A method of reducing the nephrotoxicity of an aminoglycoside antibiotic which comprises concurrently administering to a patient: (a) a therapeutically effective amount of an aminoglycoside antibiotic and (b) a nephrotoxicity-reducing amount of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the member has a molecular weight of from about 1000 to about 100,000.
Claim 19
Independent Claim
110 words
A method of reducing the nephrotoxicity of an aminoglycoside antibiotic which comprises concurrently administering to a patient: (a) a therapeutically effective amount of an aminoglycoside antibiotic and (b) a nephrotoxicity-reducing amount of a member selected from the group consisting of (i) polyasparagine, (ii) polyaspartic acid or a pharmaceutically acceptable salt thereof, (iii) a copolymer of polyasparagine and polyaspartic acid, or a pharmaceutically acceptable salt thereof, and (iv) a copolymer of polyasparagine or polyaspartic acid, or a pharmaceutically acceptable salt thereof, with a pharmaceutically acceptable comonomer, said copolymer containing a substantial amount of asparagine or aspartic acid, wherein the member has a molecular weight of from about 1000 to about 100,000.
Claim 20
Dependent Claim
20 words
The method of claim 16 wherein the aminoglycoside and the polymer or copolymer are administered in a pharmaceutically acceptable carrier.
Claim 21
Dependent Claim
21 words
The method of claim 16 wherein the polymer or copolymer has a molecular weight of from about 8000 to about 15,000.
Claim 22
Dependent Claim
20 words
The method of claim 18 wherein the aminoglycoside and the polymer or copolymer are administered in a pharmaceutically acceptable carrier.
Claim 23
Dependent Claim
35 words
The method of claim 18 wherein the polymer is poly-l-asparagine or poly-l-aspartic acid, or a pharmaceutically acceptable salt thereof, and is present in an amount of at least 0.005 moles per mole of aminoglycoside antibiotic.
Claim 24
Dependent Claim
17 words
The method of claim 20 wherein the aminoglycoside and polymer are administered in a pharmaceutically acceptable carrier.
Claim 25
Dependent Claim
12 words
The method of claim 20 wherein the aminoglycoside is gentamicin or amikacin.
Claim 26
Dependent Claim
17 words
The method of claim 22 wherein the aminoglycoside and polymer are administered in a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-07-01 | 1988-12-31 | 1989-07-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-07-01 | 1992-12-31 | 1993-07-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-07-01 | 1996-12-31 | 1997-07-02 | $7700.00 | Window Closed / Lapsed |