US4645760A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Activated aminoglycosides and aminoglycoside-aminocyclitols pharmaceutical compositions and method of use
Assignee: Health Research Inc
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Filing: 1983-07-20
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Granted: 1987-02-24
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Expires: 2003-07-20
Abstract
Abstract Aminoglycosides and aminoglycoside-aminocyclitols which have been oxygen-radical activated show a broad spectrum of antibacterial activity. The activated compounds are able to penetrate the cell membranes of bacteria and show substantially enhanced activity as compared to the parent unactivated compound.
Inventors
- 👤 Martha Pierson
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 09:06
CPC Classifications
G; G01; G01N; G01N31/00; G01N31/22; G01N31/221; A; A61; A61P; A61P29/00; A61P31/00; A61P31/04; C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; Y; Y10; Y10T; Y10T436/00; Y10T436/14; Y10T436/142222; Y10T436/143333; Y10T436/144444
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
59 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor and which has anti-inflammatory activity and poor solubility in non-polar solvents before oxygen radical-activation, but which is subsequently devoid of anti-inflammatory activity and which is more soluble in non-polar solvents and which exhibits bacteriocidal activity after oxygen radical activation.
Claim 2
Dependent Claim
59 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor and which has anti-inflammatory activity and poor solubility in non-polar solvents before oxygen radical-activation, but which is subsequently devoid of anti-inflammatory activity and which is more soluble in non-polar solvents and which exhibits bacteriocidal activity after oxygen radical activation.
Claim 3
Dependent Claim
15 words
A compound according to claim 1 having a high affinity for the 30S Ribosomal subunit.
Claim 4
Dependent Claim
54 words
A compound according to claim 1 which is an activated aminoglycoside or aminoglycoside-aminocyclitol is soluble in non-polar solvents after incubation in the presence of any reaction which generates O 2 and OH but substantially insoluble in non-polar solvents prior to an oxygen radical reaction and is less soluble in water after modification than before.
Claim 5
Dependent Claim
39 words
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 1, in combination with a pharmaceutically acceptable carrier.
Claim 6
Dependent Claim
46 words
A method of treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 1 in combination with a pharmaceutically acceptable carrier.
Claim 7
Dependent Claim
44 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by reacting an aminoglycoside or an aminoglycoside-aminocyclitol with potassium superoxide in an aqueous medium for about four hours and isolating the substance produced.
Claim 8
Dependent Claim
44 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by reacting an aminoglycoside or an aminoglycoside-aminocyclitol with potassium superoxide in an aqueous medium for about four hours and isolating the substance produced.
Claim 9
Dependent Claim
48 words
An antibacterial composition of matter which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by reacting neomycin B base with potassium superoxide in an aprotic or non-polar medium for from about 4 to about 6 days and isolating the agent produced.
Claim 10
Dependent Claim
48 words
An antibacterial composition of matter which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by reacting neomycin B base with potassium superoxide in an aprotic or non-polar medium for from about 4 to about 6 days and isolating the agent produced.
Claim 11
Dependent Claim
17 words
An antibacterial composition of matter according to claim 7 wherein the medium is 1,4-dioxane or dimethyl sulfoxide.
Claim 12
Dependent Claim
58 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by heating a high concentration of an aminoglycoside or aminoglycoside-aminocyclitol with potassium superoxide in an aqueous medium for up to one month and recovering the substance which precipitates out or which can be partitioned into non-polar solvents.
Claim 13
Dependent Claim
58 words
An aminoglycoside or an aminoglycoside-aminocyclitol which has been oxygen radical-activated at at least one of the primary amino sites therefor produced by heating a high concentration of an aminoglycoside or aminoglycoside-aminocyclitol with potassium superoxide in an aqueous medium for up to one month and recovering the substance which precipitates out or which can be partitioned into non-polar solvents.
Claim 14
Dependent Claim
39 words
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 2, in combination with a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
39 words
A pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 3, in combination with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
46 words
A method of treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 2 in combination with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim
46 words
A method of treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof a therapeutically effective amount of an oxygen radical-activated aminoglycoside or an oxygen radical-activated aminoglycoside-aminocyclitol according to claim 3 in combination with a pharmaceutically acceptable carrier.
References Cited (Backward Citations)
US3896238A
Cited
US4029883A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-02-23 | 1990-08-25 | 1991-02-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-02-23 | 1994-08-25 | 1995-02-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-02-23 | 1998-08-25 | 1999-02-24 | $7700.00 | Window Closed / Lapsed |