US4360665A
Expired / Lapsed
US
⏱️ 0.0 years remaining
4"-N-(Substituted)-apramycin antibiotic derivatives and intermediates therefor
Assignee: Eli Lilly and Co
•
Filing: 1981-12-24
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Granted: 1982-11-23
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Expires: 2001-12-24
Abstract
Abstract Apramycin derivatives substituted at the 4"-amino group with a variety of substituents are broad spectrum antibiotics. Also claimed are intermediates in the synthesis of these apramycin derivatives.
Inventors
- 👤 Herbert A. Kirst
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:40
CPC Classifications
C; C07; C07H; C07H15/00; C07H15/20; C07H15/22; C07H15/222; C07H15/224
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
40 words
A compound of the formula ##STR8## wherein R 1 is C 2 to C 4 -alkyl, C 1 to C 4 -acyl, benzyl, methoxybenzyl, halobenzyl, γ-amino-α-hydroxybutyryl, β-amino-α-hydroxypropionyl, glycyl, 4-amino-2-hydroxybutyl, 3-amino-2-hydroxypropyl or 2-aminoetyl; and the pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim
40 words
A compound of the formula ##STR8## wherein R 1 is C 2 to C 4 -alkyl, C 1 to C 4 -acyl, benzyl, methoxybenzyl, halobenzyl, γ-amino-α-hydroxybutyryl, β-amino-α-hydroxypropionyl, glycyl, 4-amino-2-hydroxybutyl, 3-amino-2-hydroxypropyl or 2-aminoetyl; and the pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim
15 words
A compound of claim 1, wherein R 1 is C 2 to C 4 -alkyl.
Claim 4
Dependent Claim
10 words
The compound of claim 2, wherein R 1 is ethyl.
Claim 5
Dependent Claim
10 words
The compound of claim 1, wherein R 1 is benzyl.
Claim 6
Dependent Claim
15 words
A compound of claim 1, wherein R 1 is C 1 to C 4 -acyl.
Claim 7
Dependent Claim
10 words
The compound of claim 5, wherein R 1 is acetyl.
Claim 8
Dependent Claim
10 words
The compound of claim 1, wherein R 1 is γ-amino-α-hydroxybutyryl.
Claim 9
Dependent Claim
41 words
A compound of the formula ##STR9## wherein R 2 is C 1 to C 4 -acyl, γ-phthalimido-α-hydroxybutyryl, β-phthalimido-α-hydroxypropionyl or N-phthalimidoglycyl; R 3 is benzyloxycarbonyl and R 4 and R 4 ' are each methyl, or, taken together form a cyclohexyl ring.
Claim 10
Dependent Claim
41 words
A compound of the formula ##STR9## wherein R 2 is C 1 to C 4 -acyl, γ-phthalimido-α-hydroxybutyryl, β-phthalimido-α-hydroxypropionyl or N-phthalimidoglycyl; R 3 is benzyloxycarbonyl and R 4 and R 4 ' are each methyl, or, taken together form a cyclohexyl ring.
Claim 11
Dependent Claim
10 words
A compound of claim 8, wherein R 2 is γ-phthalimido-α-hydroxybutyryl.
Claim 12
Dependent Claim
15 words
The compound of claim 9, wherein R 4 and R 4 ' are each methyl.
Claim 13
Dependent Claim
24 words
A compound of the formula ##STR10## wherein R 5 is C 1 -C 4 -acyl, γ-phthaliido-α-hydroxybutyryl, β-phthalimido-α-hydrxypropionyl or N-phthalimidoglycyl; and R 6 is benzyloxycarbonyl.
Claim 14
Dependent Claim
24 words
A compound of the formula ##STR10## wherein R 5 is C 1 -C 4 -acyl, γ-phthaliido-α-hydroxybutyryl, β-phthalimido-α-hydrxypropionyl or N-phthalimidoglycyl; and R 6 is benzyloxycarbonyl.
Claim 15
Dependent Claim
10 words
The compound of claim 11, wherein R 5 is γ-phthalimido-α-hydroxybutyryl.
Claim 16
Dependent Claim
14 words
A compound of the formula ##STR11## wherein R 7 is γ-phthalimido-α-hydroxybutyryl, β-phthalimido-α-hydroxypropionyl or N-phthalimidoglycyl.
Claim 17
Dependent Claim
14 words
A compound of the formula ##STR11## wherein R 7 is γ-phthalimido-α-hydroxybutyryl, β-phthalimido-α-hydroxypropionyl or N-phthalimidoglycyl.
Claim 18
Dependent Claim
10 words
The compound of claim 13, wherein R 7 is γ-phthalimido-α-hydroxybutyryl.
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) | 1985-11-22 | 1986-05-24 | 1986-11-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-11-22 | 1990-05-24 | 1990-11-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-11-22 | 1994-05-24 | 1994-11-23 | $7700.00 | Window Closed / Lapsed |