US4440759A
Expired / Lapsed
US
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20-Amino tylosin derivatives and pharmaceutical compositions containing same
Assignee: Individual
•
Filing: 1983-02-24
•
Granted: 1984-04-03
•
Expires: 2003-02-24
Abstract
Abstract 20-Amino derivatives of tylosin and desmycosin are active against bacteria and Mycoplasma.
Inventors
- 👤 Satoshi Omura
- 👤 Akira Nakagawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 18:08
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08; A; A61; A61P; A61P31/00; A61P31/04
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
145 words
A macrolide of formula (I): ##STR9## where R is mycinosyloxy, where Q is hydrogen or mycarosyl, where X is a group of formula: ##STR10## where: (i) R 10 and R 11 independently represent C 1-4 alkyl, C 3-10 cycloalkyl; or a group of formula: --(CH.sub.2).sub.n --Ph where n is 0, 1 or 2, and Ph is phenyl or phenyl substituted by a C 1-4 alkoxycarbonyl, amino, halogen, C 1-4 alkyl or C 1-4 alkoxy group; (ii) one only of R 10 and R 11 represents hydrogen or a group of formula: ##STR11## where R 12 is hydrogen or C 1-4 alkyl, or (iii) R 10 and R 11 taken together with the adjacent nitrogen atom form a heterocyclic ring selected from piperazino and morpholino; or a pharmaceutically-acceptable salt, or an acyl ester derived from a monocarboxylic acid having from 2 to 7 carbon atoms, thereof.
Claim 2
Dependent Claim
145 words
A macrolide of formula (I): ##STR9## where R is mycinosyloxy, where Q is hydrogen or mycarosyl, where X is a group of formula: ##STR10## where: (i) R 10 and R 11 independently represent C 1-4 alkyl, C 3-10 cycloalkyl; or a group of formula: --(CH.sub.2).sub.n --Ph where n is 0, 1 or 2, and Ph is phenyl or phenyl substituted by a C 1-4 alkoxycarbonyl, amino, halogen, C 1-4 alkyl or C 1-4 alkoxy group; (ii) one only of R 10 and R 11 represents hydrogen or a group of formula: ##STR11## where R 12 is hydrogen or C 1-4 alkyl, or (iii) R 10 and R 11 taken together with the adjacent nitrogen atom form a heterocyclic ring selected from piperazino and morpholino; or a pharmaceutically-acceptable salt, or an acyl ester derived from a monocarboxylic acid having from 2 to 7 carbon atoms, thereof.
Claim 3
Dependent Claim
10 words
A compound of claim 1 in which Q is hydrogen.
Claim 4
Dependent Claim
23 words
A compound of claim 1 in which X represents a group selected from dimethylamino, anilino, N-methylanilino, o-ethoxycarbonylanilino, benzylamino, aminobenzylamino, halobenzylamino, cyclohexylamino and morpholino.
Claim 5
Dependent Claim
8 words
The compound of claim 3 which is 20-deoxo-20-(N-methylanilino)tylosin.
Claim 6
Dependent Claim
8 words
The compound of claim 3 which is 20-deoxo-20-(N-benzylamino)demycarosyltylosin.
Claim 7
Dependent Claim
8 words
The compound of claim 3 which is 20-deoxo-20-(N-morpholino)demycarosyltylosin.
Claim 8
Dependent Claim
34 words
A method of suppressing or treating microbial infections caused by gram-positive bacteria or Mycoplasma in a warm-blooded animal which comprises administering to said warm-blooded animal a chemotherapeutically-effective amount of a compound of claim 1.
Claim 9
Dependent Claim
31 words
A method of suppressing or treating microbial infections caused by Pasteurella in a warm-blooded animal which comprises administering to said warm-blooded animal a chemotherapeutically-effective amount of a compound of claim 2.
Claim 10
Dependent Claim
32 words
A feed premix comprising as an active ingredient an amount of a compound of claim 1 which is effective to suppress or treat microbial infections caused by gram-positive bacteria, Mycoplasma or Pasteurella.
Claim 11
Dependent Claim
43 words
A veterinary formulation which comprises as an active ingredient an amount of a compound of claim 1 which is effective to suppress or treat microbial infections caused by gram-positive bacteria, Mycoplasma or Pasteurella associated with one or more physiologically-acceptable carriers or vehicles therefor.
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) | 1987-04-03 | 1987-10-03 | 1988-04-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-04-03 | 1991-10-03 | 1992-04-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-04-03 | 1995-10-03 | 1996-04-03 | $7700.00 | Window Closed / Lapsed |