US4166114A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminoglycoside antibiotic derivatives and method of use
Assignee: Shionogi and Co Ltd
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Filing: 1977-09-29
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Granted: 1979-08-28
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Expires: 1997-09-29
Abstract
Abstract Novel aminoglycoside antibiotic derivatives and their salts containing a 2-deoxystreptamine moiety of which the 1-amino group is substituted by a group represented by the formula: ##STR1## [wherein R is hydrogen atom, lower alkyl or aralkyl; n is an integer 1 or 2] Are effective in treatment and prevention of infectious diseases caused by gram positive and negative bacteria.
Inventors
- 👤 Kikuo Igarashi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 04:57
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; C07H15/222; C07H15/226; C07H15/234; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; C07D211/62; C07D211/66
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
108 words
A member selected from the group consisting of an aminoglycoside derivative of the formula: ##STR6## and a pharmaceutically acceptable salt thereof wherein R is hydrogen, alkyl of C 1 to C 5 or aralkyl of C 7 to C 10 , R 1 is aminomethyl, hydroxymethyl, methylaminomethyl or 1-methylaminoethyl, R 2 , R 3 and R 6 represent independently 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, the dotted line represents the presence or absence of a double bond and n is an integer of 1 or 2.
Claim 2
Dependent Claim
108 words
A member selected from the group consisting of an aminoglycoside derivative of the formula: ##STR6## and a pharmaceutically acceptable salt thereof wherein R is hydrogen, alkyl of C 1 to C 5 or aralkyl of C 7 to C 10 , R 1 is aminomethyl, hydroxymethyl, methylaminomethyl or 1-methylaminoethyl, R 2 , R 3 and R 6 represent independently 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, the dotted line represents the presence or absence of a double bond and n is an integer of 1 or 2.
Claim 3
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 8 is hydrogen or hydroxymethyl.
Claim 4
Dependent Claim
21 words
A compound as claimed in claim 1, wherein R 1 is aminomethyl or hydroxymethyl and R 8 is hydrogen or hydroxymethyl.
Claim 5
Dependent Claim
19 words
A compound as claimed in claim 1, wherein R 1 is aminomethyl or hydroxymethyl and R 8 is hydroxymethyl.
Claim 6
Dependent Claim
33 words
A compound as 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 7
Dependent Claim
11 words
A compound as claimed in claim 1, wherein R is hydrogen.
Claim 8
Dependent Claim
16 words
A compound as claimed in claim 1, wherein R is C 1 to C 5 alkyl.
Claim 9
Dependent Claim
11 words
A compound as claimed in claim 1, wherein R is benzyl.
Claim 10
Dependent Claim
10 words
A compound as claimed in claim 1, namely 1-N-(4-hydroxypiperidine-4-carbonyl)kanamycin A.
Claim 11
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(4-hydroxypiperidine-4-carbonyl)tobramycin.
Claim 12
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(3-hydroxypyrrolidine-3-carbonyl)tobramycin.
Claim 13
Dependent Claim
10 words
A compound as claimed in claim 1, namely 1-N-(3-hydroxypyrrolidine-3-carbonyl)kanamycin A.
Claim 14
Dependent Claim
10 words
A compound as claimed in claim 1, namely 1-N-(3-hydroxypyrrolidine-3-carbonyl)kanamycin B.
Claim 15
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(1-methyl-3-hydroxypyrrolidine-3-carbonyl)tobramycin.
Claim 16
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(1-ethyl-3-hydroxypyrrolidine-3-carbonyl)tobramycin.
Claim 17
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(1-isopropyl-3-hydroxypyrrolidine-3-carbonyl)tobramycin.
Claim 18
Dependent Claim
9 words
A compound as claimed in claim 1, namely 1-N-(1-benzyl-3-hydroxypyrrolidine-3-carbonyl)tobramycin.
Claim 19
Dependent Claim
26 words
A pharmaceutical composition which comprises a bactericidally effective amount of a compound or salt thereof as defined in claim 1 and a pharmaceutically acceptable carrier therefor.
Claim 20
Dependent Claim
36 words
A method for treating a gram-positive or gram-negative bacterial infection which comprises administering to a host suffering from said bacterial infection a bactericidally effective amount of a compound or salt thereof as defined in 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) | 1982-08-27 | 1983-02-26 | 1983-08-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-08-27 | 1987-02-26 | 1987-08-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-08-27 | 1991-02-26 | 1991-08-28 | $7700.00 | Window Closed / Lapsed |