Patent US4199570A successfully refreshed from Google Patents.
← Back to Patent Explorer
US4199570A Expired / Lapsed US ⏱️ 0.0 years remaining

1-N-Hetero containing aminoglycoside derivatives

Assignee: Shionogi and Co Ltd
•
Filing: 1978-08-17
•
Granted: 1980-04-22
•
Expires: 1998-08-17
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

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 06:21
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)

US3940382A Cited
US4051315A Cited
US4104372A Cited

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

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag