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US4214075A Expired / Lapsed US ⏱️ 0.0 years remaining

6'-Epi-fortimicin A and B derivatives

Assignee: Abbott Laboratories
•
Filing: 1977-12-21
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Granted: 1980-07-22
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Expires: 1997-12-21
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Abstract

Abstract 6'-Epi-fortimicin A and B derivatives represented by the formula ##STR1## wherein R 1 is hydrogen or loweralkyl, R 2 is hydrogen or loweralkyl and R 3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, hydroxyloweralkyl, acyl, aminoacyl, hydroxyacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; the pharmaceutically acceptable salts thereof; intermediates useful in their preparation, compositions employing the compounds; and methods of using the compounds. The compounds are useful as antibiotics.

Inventors

  • 👤 John S. Tadanier
  • 👤 Jerry R. Martin

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 14:49
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; C07H15/222; C07H15/224

Claims Analysis

Total Claims: 25
Claim 1
Independent Claim 61 words
A 6'-epi-fortimicins A and B and derivatives of the formula ##STR10## wherein R 1 is hydrogen or lower alkyl, R 2 is hydrogen or loweralkyl and R 3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, aminohydroxyloweralkyl, aminoacyl, hydroxylacyl, acyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim 61 words
A 6'-epi-fortimicins A and B and derivatives of the formula ##STR10## wherein R 1 is hydrogen or lower alkyl, R 2 is hydrogen or loweralkyl and R 3 is selected from the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, aminohydroxyloweralkyl, aminoacyl, hydroxylacyl, acyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue; and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim 10 words
A compound of claim 1 wherein R 3 is hydrogen.
Claim 4
Dependent Claim 10 words
A compound of claim 1 wherein R 3 is glycyl.
Claim 5
Dependent Claim 10 words
A compound of claim 1 wherein R 3 is acyl.
Claim 6
Dependent Claim 10 words
A compound of claim 1 wherein R 3 is loweralkyl.
Claim 7
Dependent Claim 21 words
A compound of claim 1 wherein R 3 is selected from the group consisting of aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl and hydroxy-substituted aminoacyl.
Claim 8
Dependent Claim 13 words
A compound of claim 1 wherein R 3 is an amino acid residue.
Claim 9
Dependent Claim 14 words
A compound of claim 1 wherein R 1 and R 2 each are hydrogen.
Claim 10
Dependent Claim 12 words
A compound of claim 8 wherein R 3 is hydrogen: 6'-epi-fortimicin B.
Claim 11
Dependent Claim 12 words
A compound of claim 7 wherein R 3 is glycyl: 6'-epi-fortimicin A.
Claim 12
Dependent Claim 2 words
4-N-β-Alanyl-6'-epi-fortimicin B.
Claim 13
Dependent Claim 2 words
4-N-β-Alanyl-6'-epi-fortimicin B.
Claim 14
Dependent Claim 2 words
4-N-Sarcosyl-6'-epi-fortimicin B.
Claim 15
Dependent Claim 2 words
4-N-Sarcosyl-6'-epi-fortimicin B.
Claim 16
Dependent Claim 52 words
A compound of the formula ##STR11## wherein R 1 is hydrogen, halogen, 5,5-dimethyl-3-oxo-1-cyclohexenl-yl, or benzyloxycarbonyl; each R 2 are the same or different members of the group consisting of hydrogen, loweralkyl, monocyclicaryl, alkoxycarbonyl or monocyclicaryloxycarbonyl; each R 4 are the same or different members of the group consisting of hydrogen or acetyl.
Claim 17
Dependent Claim 52 words
A compound of the formula ##STR11## wherein R 1 is hydrogen, halogen, 5,5-dimethyl-3-oxo-1-cyclohexenl-yl, or benzyloxycarbonyl; each R 2 are the same or different members of the group consisting of hydrogen, loweralkyl, monocyclicaryl, alkoxycarbonyl or monocyclicaryloxycarbonyl; each R 4 are the same or different members of the group consisting of hydrogen or acetyl.
Claim 18
Dependent Claim 35 words
A compound of the formula ##STR12## wherein R 1 is NH, or, O and each R 2 are the same or different members of the group consisting of hydrogen, lower alkyl, monocyclicaryl, alkoxycarbonyl or monocyclicarylalkoxycarbonyl.
Claim 19
Dependent Claim 35 words
A compound of the formula ##STR12## wherein R 1 is NH, or, O and each R 2 are the same or different members of the group consisting of hydrogen, lower alkyl, monocyclicaryl, alkoxycarbonyl or monocyclicarylalkoxycarbonyl.
Claim 20
Dependent Claim 15 words
A compound of the formula ##STR13## wherein R is benzyloxycarbonyl and R 1 is acetyl.
Claim 21
Dependent Claim 15 words
A compound of the formula ##STR13## wherein R is benzyloxycarbonyl and R 1 is acetyl.
Claim 22
Dependent Claim 16 words
A compound of the formula ##STR14## wherein R is the acetyl and the pharmaceutically acceptable salts.
Claim 23
Dependent Claim 16 words
A compound of the formula ##STR14## wherein R is the acetyl and the pharmaceutically acceptable salts.
Claim 24
Dependent Claim 43 words
A compound of the formula ##STR15## Each R 1 is benzyloxycarbonyl and R 2 is one of a member of the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, hydroxyloweralkyl, acyl, aminoacylhydroxyacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue.
Claim 25
Dependent Claim 43 words
A compound of the formula ##STR15## Each R 1 is benzyloxycarbonyl and R 2 is one of a member of the group consisting of hydrogen, loweralkyl, aminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, hydroxyloweralkyl, acyl, aminoacylhydroxyacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxy-substituted aminoacyl or an amino acid residue.

References Cited (Backward Citations)

US3929762A Cited
US3931400A Cited
US3976768A Cited
US4078138A Cited
US4085208A Cited
US4091032A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-07-22 1984-01-21 1984-07-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-07-22 1988-01-21 1988-07-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-07-22 1992-01-21 1992-07-22 $7700.00 Window Closed / Lapsed

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