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US4264765A Expired / Lapsed US ⏱️ 0.0 years remaining

Salts of erythromycin A esters

Assignee: Abbott Laboratories
•
Filing: 1980-02-20
•
Granted: 1981-04-28
•
Expires: 2000-02-20
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Abstract

Abstract Highly water-soluble erythromycin A derivatives wherein the desosamine moiety is quaternized with an acyloxy-, benzoyloxy- or alkoxycarbonyl-(or carboxy)-acylmethyl iodide, bromine or chloride and esterified in the 2-position with loweralkyl or --(CH 2 ) n CO 2 R", wherein R" is H, loweralkyl or substituted loweralkyl and n is an integer from 1-5. These new esters readily convert to erythromycin A upon administration to warm-blooded animals.

Inventors

  • 👤 Nicholas S. Bodor
  • 👤 Leslie A. Freiberg

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 21:18
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08; A; A61; A61P; A61P31/00; A61P31/04

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 90 words
A quaternary erythromycin salt of erythromycin A 2'-ester wherein the desosamine moiety has a partial structure of the formula ##STR3## wherein (Ery) represents erythromycin A, R is loweralkyl, phenyl or --(CH 2 ) m COOR", R' is loweralkyl, or --(CH 2 ) n COOR", R" is H or loweralkyl, X is bromine, iodine or chlorine, R"' is H or loweralkyl, m and n independently represent an integer from 1 to 5, and said loweralkyl in R, R' and R" and said phenyl may be substituted by Cl, Br or loweralkoxy.
Claim 2
Dependent Claim 90 words
A quaternary erythromycin salt of erythromycin A 2'-ester wherein the desosamine moiety has a partial structure of the formula ##STR3## wherein (Ery) represents erythromycin A, R is loweralkyl, phenyl or --(CH 2 ) m COOR", R' is loweralkyl, or --(CH 2 ) n COOR", R" is H or loweralkyl, X is bromine, iodine or chlorine, R"' is H or loweralkyl, m and n independently represent an integer from 1 to 5, and said loweralkyl in R, R' and R" and said phenyl may be substituted by Cl, Br or loweralkoxy.
Claim 3
Dependent Claim 12 words
A salt as defined in claim 1 wherein R is tert. butyl.
Claim 4
Dependent Claim 13 words
The salt of claim 2 wherein R' is ethoxycarbonylethyl and R"' is H.
Claim 5
Dependent Claim 13 words
The salt of claim 2 wherein R' is carboxyloweralkyl and R"' is H.
Claim 6
Dependent Claim 10 words
The salt of claim 4 wherein said loweralkyl is propyl.
Claim 7
Dependent Claim 13 words
The salt of claim 1 wherein R is phenyl and R"' is H.
Claim 8
Dependent Claim 9 words
The salt of claim 6 wherein R' is ethoxycarbonylethyl.
Claim 9
Dependent Claim 13 words
The salt of claim 6 wherein R' is ethyl and R"' is H.
Claim 10
Dependent Claim 17 words
A salt as defined in claim 1 wherein R is loweralkyl and R' is ethyl or ethoxycarbonylethyl.

References Cited (Backward Citations)

US2857312A Cited
US2881163A Cited
US3558594A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-04-27 1984-10-27 1985-04-28 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-04-27 1988-10-27 1989-04-28 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-04-27 1992-10-27 1993-04-28 $7700.00 Window Closed / Lapsed

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