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US4092473A
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Tylosin derivatives and their manufacturing process
Assignee: Mercian Corp
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Filing: 1976-07-23
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Granted: 1978-05-30
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Expires: 1996-07-23
Abstract
Abstract New tylosin derivatives having at least one acyl group at the 3- and 4''-positions of tylosin, and the acid addition salts thereof, which inhibit the growth of various microorganisms including drug-resistant bacterial isolants and which produce high blood levels through oral administration are produced by a biochemical reaction using the microorganisms of the genus Streptomyces which are selected for their newly-found ability to acylate at least one of the 3- and 4''-positions of macrolide antibiotics; they are recovered from the reacted mixture by conventional methods for recovering macrolide antibiotics.
Inventors
- 👤 Rokuro Okamoto
- 👤 Tsumoru Fukumoto
- 👤 Akira Takamatsu
- 👤 Tomio Takeuchi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 15:43
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08; C12; C12P; C12P19/00; C12P19/44; C12P19/60; C12P19/62; Y; Y10; Y10S; Y10S435/00; Y10S435/8215; Y10S435/822; Y10S435/886
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
62 words
Acyl derivatives of tylosin having the formula I ##STR4## wherein R 1 is H, acetyl or propionyl, R 2 is H, n-butyryl or isovaleryl, the case where both R 1 and R 2 are H being excluded; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric and phosphoric acid addition salts thereof.
Claim 2
Dependent Claim
62 words
Acyl derivatives of tylosin having the formula I ##STR4## wherein R 1 is H, acetyl or propionyl, R 2 is H, n-butyryl or isovaleryl, the case where both R 1 and R 2 are H being excluded; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric and phosphoric acid addition salts thereof.
Claim 3
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-acetyltylosin, in which R 1 is acetyl and R 2 is H; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 4
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-acetyl-4"-n-butyryltylosin, in which R 1 is acetyl and R 2 is n-butyryl and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 5
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-acetyl-4"-isovaleryltylosin, in which R 1 is acetyl and R 2 is isovaleryl and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 6
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-propionyltylosin, in which R 1 is propionyl and R 2 is H; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 7
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-propionyl-4"-n-butyryltylosin, in which R 1 is propionyl and R 2 is n-butyryl and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 8
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 3-propionyl-4"-isovaleryltylosin, in whih R 1 is propionyl and R 2 is isovaleryl; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 9
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 4"-n-butyryltylosin, in which R 1 is H and R 2 is n-butyryl; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
Claim 10
Dependent Claim
55 words
An acyl derivative of tylosin having the formula I, as claimed in claim 1, wherein the compound is 4"-isovaleryltylosin, in which R 1 is H and R 2 is isovaleryl; and the acid addition salts thereof selected from the group consisting of tartaric, acetic, propionic, citric, succinic, hydrochloric, sulfuric, and phosphoric acid addition salts thereof.
References Cited (Backward Citations)
US3424743A
Cited
US3853842A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-05-29 | 1981-11-28 | 1982-05-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-29 | 1985-11-28 | 1986-05-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-29 | 1989-11-28 | 1990-05-30 | $7700.00 | Window Closed / Lapsed |