US4214075A
Expired / Lapsed
US
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6'-Epi-fortimicin A and B derivatives
Assignee: Abbott Laboratories
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Filing: 1977-12-21
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Granted: 1980-07-22
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Expires: 1997-12-21
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 14:32
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.
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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 |