US4199570A
Expired / Lapsed
US
⏱️ 0.0 years remaining
1-N-Hetero containing aminoglycoside derivatives
Assignee: Shionogi and Co Ltd
•
Filing: 1978-08-17
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Granted: 1980-04-22
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Expires: 1998-08-17
Abstract
Abstract Novel aminoglycoside derivatives and their salts containing 2-deoxystreptamine moiety, of which the 1-amino group is acylated by a group represented by the formula: ##STR1## wherein R is hydrogen, lower alkyl, aralkyl, or aralkoxycarbonyl; and n is an integer of 1 or 3, effective in treatment and prevention of infectious diseases caused by gram positive and gram negative bacteria.
Inventors
- 👤 Kikuo Igarashi
- 👤 Junji Irisawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 04:57
CPC Classifications
C; C07; C07D; C07D205/00; C07D205/02; C07D205/04; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; C07H; C07H15/00; C07H15/20; C07H15/22; C07H15/222; C07H15/226; C07H15/234
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
112 words
A compound selected from the group consisting of a novel aminoglycoside derivative represented by the formula: ##STR9## wherein R is hydrogen, lower alkyl, aralkyl of 7 to 20 carbon atoms, or aralkoxycarbonyl of 8 to 20 carbon atoms; n is an integer of 1 or 3; R 1 is aminomethyl, hydroxymethyl, 1-aminoethyl, or 1-methylaminoethyl; R 2 , R 3 and R 6 each is hydrogen or hydroxy; R 4 is hydroxy or amino; R 5 is amino or methylamino; R 7 is hydroxy or methyl; R 8 is hydrogen, hydroxymethyl, or carbamoyloxymethyl; and the dotted line represents the presence or absence of a double bond and a non-toxic acid addition salt thereof.
Claim 2
Dependent Claim
112 words
A compound selected from the group consisting of a novel aminoglycoside derivative represented by the formula: ##STR9## wherein R is hydrogen, lower alkyl, aralkyl of 7 to 20 carbon atoms, or aralkoxycarbonyl of 8 to 20 carbon atoms; n is an integer of 1 or 3; R 1 is aminomethyl, hydroxymethyl, 1-aminoethyl, or 1-methylaminoethyl; R 2 , R 3 and R 6 each is hydrogen or hydroxy; R 4 is hydroxy or amino; R 5 is amino or methylamino; R 7 is hydroxy or methyl; R 8 is hydrogen, hydroxymethyl, or carbamoyloxymethyl; and the dotted line represents the presence or absence of a double bond and a non-toxic acid addition salt thereof.
Claim 3
Dependent Claim
13 words
A compound claimed in claim 1 wherein n is an integer of 1.
Claim 4
Dependent Claim
13 words
A compound claimed in claim 1 wherein n is an integer of 3.
Claim 5
Dependent Claim
10 words
A compound claimed in claim 1 wherein R is hydrogen.
Claim 6
Dependent Claim
13 words
A compound claimed in claim 1 wherein R 8 is hydrogen or hydroxymethyl.
Claim 7
Dependent Claim
20 words
A compound claimed in claim 1 wherein R 1 is aminomethyl or hydroxymethyl and R 8 is hydrogen or hydroxymethyl.
Claim 8
Dependent Claim
18 words
A compound claimed in claim 1 wherein R 1 is aminomethyl or hydroxymethyl and R 8 is hydroxymethyl.
Claim 9
Dependent Claim
32 words
A compound claimed in claim 1 wherein R 1 is aminomethyl, R 2 is hydroxy, R 5 is amino, R 6 is hydrogen, R 7 is hydroxy, and R 8 is hydroxymethyl.
Claim 10
Dependent Claim
8 words
A compound claimed in claim 1 namely 1-N-(3-hydroxyazetidine-3-carbonyl)tobramycin.
Claim 11
Dependent Claim
8 words
A compound claimed in claim 1 namely 1-N-(1-benzyloxycarbonyl-3-hydroxyazetidine-3-carbonyl)tobramycin.
Claim 12
Dependent Claim
9 words
A compound claimed in claim 1 namely 1-N-(3-hydroxyazetidine-3-carbonyl)kanamycin A.
Claim 13
Dependent Claim
9 words
A compound claimed in claim 1 namely 1-N-(3-hydroxyazetidine-3-carbonyl)kanamycin B.
Claim 14
Dependent Claim
8 words
A compound claimed in claim 1 namely 1-N-(1-methyl-3-hydroxyazetidine-3-carbonyl)tobramycin.
Claim 15
Dependent Claim
8 words
A compound claimed in claim 1 namely 1-N-(3-hydroxypiperidine-3-carbonyl)tobramycin.
Claim 16
Dependent Claim
8 words
A compound claimed in claim 1 namely 1-N-(1-benzyl-3-hydroxypiperidine-3-carbonyl)tobramycin.
Claim 17
Dependent Claim
21 words
A composition which comprises an antibacterially effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 18
Dependent Claim
41 words
A method for the treatment of a bacterial infectious disease in a human or other species of animal which comprises administering to a host suffering from said bacterial infectious disease an antibacterially effective amount of a compound according to claim 1.
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) | 1983-04-22 | 1983-10-22 | 1984-04-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-04-22 | 1987-10-22 | 1988-04-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-04-22 | 1991-10-22 | 1992-04-22 | $7700.00 | Window Closed / Lapsed |