Patent US4117221A successfully refreshed from Google Patents.
US4117221A
Expired / Lapsed
US
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Aminoacyl derivatives of aminoglycoside antibiotics
Assignee: Merck Sharp & Dohme LLC
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Filing: 1976-10-20
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Granted: 1978-09-26
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Expires: 1996-10-20
Abstract
Abstract Disclosed herein are novel 1-N-X-aminoglycoside anti-bacterial agents produced from antibiotics elaborated by species of the genus Micromonospora wherein X is a member selected from the group consisting of S-3-amino-2-hydroxypropionyl and S-4-amino-2-hydroxybutyryl and S-5-amino-2-hydroxypentanoyl. Also disclosed are novel intermediates in the production of the foregoing.
Inventors
- 👤 Peter J. L. Daniels
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 07:59
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; C07H15/222; C07H15/226; C07H15/234; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 51
Claim 1
Independent Claim
62 words
A 1-N-X-aminoglycoside anti-bacterial agent selected from the group consisting of 1-N-X-gentamicin A, 1-N-X-gentamicin B, 1-N-X-gentamicin B 1 , 1-N-X-gentamicin C 1 , 1-N-X-gentamicin C 1a , 1-N-X-gentamicin C 2 , 1-N-X-gentamicin C 2a , 1-N-X-gentamicin X, 1-N-X-sisomicin, 1-N-X-verdamicin, 1-N-X-antibiotic G-418, 1-N-X-antibiotic 66-40B, 1-N-X-antibiotic 66-40D, 1-N-X-antibiotic JI-20A, 1-N-X-antibiotic JI-20B, 1-N-X-antibiotic G-52 and the pharmaceutically acceptable acid addition salts thereof, wherein X is S-3-amino-2-hydroxypropionyl.
Claim 2
Dependent Claim
62 words
A 1-N-X-aminoglycoside anti-bacterial agent selected from the group consisting of 1-N-X-gentamicin A, 1-N-X-gentamicin B, 1-N-X-gentamicin B 1 , 1-N-X-gentamicin C 1 , 1-N-X-gentamicin C 1a , 1-N-X-gentamicin C 2 , 1-N-X-gentamicin C 2a , 1-N-X-gentamicin X, 1-N-X-sisomicin, 1-N-X-verdamicin, 1-N-X-antibiotic G-418, 1-N-X-antibiotic 66-40B, 1-N-X-antibiotic 66-40D, 1-N-X-antibiotic JI-20A, 1-N-X-antibiotic JI-20B, 1-N-X-antibiotic G-52 and the pharmaceutically acceptable acid addition salts thereof, wherein X is S-3-amino-2-hydroxypropionyl.
Claim 3
Dependent Claim
50 words
A 1-N-X-aminoglycoside anti-bacterial agent selected from the group consisting of 1-N-X-gentamicin A, 1-N-X-gentamicin B, 1-N-X-gentamicin B 1 , 1-N-X-gentamicin C 2a , 1-N-X-gentamicin X, 1-N-X-sisomicin, 1-N-X-verdamicin, 1-N-X-antibiotic G-418, 1-N-X-antibiotic 66-40B, 1-N-X-antibiotic 66-40D, 1-N-X-antibiotic JI-20A, 1-N-X-anti-biotic JI-20B, 1-N-X-antibiotic G-52 and the pharmaceutically acceptable acid addition salts thereof, wherein X is S-4-amino-2-hydroxybutyryl.
Claim 4
Dependent Claim
50 words
A 1-N-X-aminoglycoside anti-bacterial agent selected from the group consisting of 1-N-X-gentamicin A, 1-N-X-gentamicin B, 1-N-X-gentamicin B 1 , 1-N-X-gentamicin C 2a , 1-N-X-gentamicin X, 1-N-X-sisomicin, 1-N-X-verdamicin, 1-N-X-antibiotic G-418, 1-N-X-antibiotic 66-40B, 1-N-X-antibiotic 66-40D, 1-N-X-antibiotic JI-20A, 1-N-X-anti-biotic JI-20B, 1-N-X-antibiotic G-52 and the pharmaceutically acceptable acid addition salts thereof, wherein X is S-4-amino-2-hydroxybutyryl.
Claim 5
Dependent Claim
9 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)sisomicin.
Claim 6
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic 66-40B.
Claim 7
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic 66-40D.
Claim 8
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic G-52.
Claim 9
Dependent Claim
9 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)verdamicin.
Claim 10
Dependent Claim
12 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin C 1 .
Claim 11
Dependent Claim
12 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin C 2 .
Claim 12
Dependent Claim
12 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin C 1a .
Claim 13
Dependent Claim
12 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin C 2a .
Claim 14
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin X.
Claim 15
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin A.
Claim 16
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin B.
Claim 17
Dependent Claim
12 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)gentamicin B 1 .
Claim 18
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic JI-20A.
Claim 19
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic JI-20B.
Claim 20
Dependent Claim
10 words
A compound of claim 1, said compound being 1-N-(S-3-amino-2-hydroxypropionyl)antibiotic G-418.
Claim 21
Dependent Claim
9 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)sisomicin.
Claim 22
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic 66-40B.
Claim 23
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic 66-40D.
Claim 24
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic G-52.
Claim 25
Dependent Claim
9 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)verdamicin.
Claim 26
Dependent Claim
12 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)gentamicin C 2a .
Claim 27
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)gentamicin X.
Claim 28
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)gentamicin A.
Claim 29
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)gentamicin B.
Claim 30
Dependent Claim
12 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)gentamicin B 1 .
Claim 31
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic JI-20A.
Claim 32
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic JI-20B.
Claim 33
Dependent Claim
10 words
A compound of claim 2, said compound being 1-N-(S-4-amino-2-hydroxybutyryl)antibiotic G-418.
Claim 34
Dependent Claim
27 words
A 6'-N-trifluoroacetyl derivative of an aminoglycoside antibiotic selected from the group consisting of gentamicin C 1a , gentamicin B, antibiotic JI-20A, antibiotic 66-40B, antibiotic 66-40D, and sisomicin.
Claim 35
Dependent Claim
27 words
A 6'-N-trifluoroacetyl derivative of an aminoglycoside antibiotic selected from the group consisting of gentamicin C 1a , gentamicin B, antibiotic JI-20A, antibiotic 66-40B, antibiotic 66-40D, and sisomicin.
Claim 36
Dependent Claim
13 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl gentamicin C 1a .
Claim 37
Dependent Claim
11 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl gentamicin B.
Claim 38
Dependent Claim
11 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl antibiotic JI-20A.
Claim 39
Dependent Claim
11 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl antibiotic 66-40B.
Claim 40
Dependent Claim
11 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl antibiotic 66-40D.
Claim 41
Dependent Claim
10 words
A compound of claim 32, said compound being 6'-N-trifluoroacetyl sisomicin.
Claim 42
Dependent Claim
27 words
A 6'-N-t-butoxycarbonyl derivative of an aminoglycoside antibiotic selected from the group consisting of gentamicin C 1a , gentamicin B, sisomicin, antibiotic 66-40B, antibiotic 66-40D and antibiotic JI-20A.
Claim 43
Dependent Claim
27 words
A 6'-N-t-butoxycarbonyl derivative of an aminoglycoside antibiotic selected from the group consisting of gentamicin C 1a , gentamicin B, sisomicin, antibiotic 66-40B, antibiotic 66-40D and antibiotic JI-20A.
Claim 44
Dependent Claim
13 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl gentamicin C 1a .
Claim 45
Dependent Claim
11 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl gentamicin B.
Claim 46
Dependent Claim
10 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl sisomicin.
Claim 47
Dependent Claim
11 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl antibiotic 66-40B.
Claim 48
Dependent Claim
11 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl antibiotic 66-40D.
Claim 49
Dependent Claim
11 words
A compound of claim 39, said compound being 6'-N-t-butoxycarbonyl antibiotic JI-20A.
Claim 50
Dependent Claim
4 words
2',3-di-N-trifluoroacetylgentamicin C 1 .
Claim 51
Dependent Claim
4 words
2',3-di-N-trifluoroacetylgentamicin C 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) | 1981-09-25 | 1982-03-27 | 1982-09-26 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-09-25 | 1986-03-27 | 1986-09-26 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-09-25 | 1990-03-27 | 1990-09-26 | $7700.00 | Window Closed / Lapsed |