US4262010A
Expired / Lapsed
US
⏱️ 0.0 years remaining
6-(1-Hydroxyethyl)-2-(2-aminoethylthio)-1,1-disubstituted-1-carbadethiapen-2-em-3-carboxylic acids
Assignee: Merck and Co Inc
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Filing: 1979-12-03
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Granted: 1981-04-14
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Expires: 1999-12-03
Abstract
Abstract Disclosed are 1-substituted-6-(1-hydroxyethyl)-2-(2-aminoethylthio)-1-carbadethiapen -2-em-3-carboxylic acids (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics; such compounds are prepared by total synthesis. <IMAGE> wherein R1 and R2 are, inter alia, substituted and unsubstituted alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl and the spiro substituent formed by the joinder of R1 and R2.
Inventors
- 👤 Burton G. Christensen
- 👤 David H. Shih
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 20:00
CPC Classifications
C; C07; C07D; C07D477/00; C07D477/10; C07D477/12; C07D477/16; C07D477/20; C07C; C07C17/00; C07C17/26; C07C17/272; C07C17/275; C07D205/00; C07D205/02; C07D205/06; C07D205/08; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/10
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
95 words
A compound having the formula: ##STR36## and its pharmaceutically acceptable salts wherein R 1 and R 2 are selected from the group consisting of substituted and unsubstituted: loweralkyl having from 1-6 carbon atoms, phenyl, phenylloweralkyl, cycloalkyl having from 3 to 6 carbon atoms, cycloalkylalkyl having 1 to 6 carbon atoms in the chain and 3-6 carbon atoms in the ring, and spiro cycloalkyl having 3-6 carbon atoms; wherein said substituents on R 1 and R 2 are selected from the group consisting of halogen, hydroxyl, amino, alkoxy having 1-6 carbon atoms, azido, cyano, and carboxyl.
Claim 2
Dependent Claim
95 words
A compound having the formula: ##STR36## and its pharmaceutically acceptable salts wherein R 1 and R 2 are selected from the group consisting of substituted and unsubstituted: loweralkyl having from 1-6 carbon atoms, phenyl, phenylloweralkyl, cycloalkyl having from 3 to 6 carbon atoms, cycloalkylalkyl having 1 to 6 carbon atoms in the chain and 3-6 carbon atoms in the ring, and spiro cycloalkyl having 3-6 carbon atoms; wherein said substituents on R 1 and R 2 are selected from the group consisting of halogen, hydroxyl, amino, alkoxy having 1-6 carbon atoms, azido, cyano, and carboxyl.
Claim 3
Dependent Claim
24 words
A compound according to claim 1 wherein R 1 and R 2 are selected from methyl, phenyl, benzyl, ethyl cyclopropyl, propyl, isopropyl, and spirocyclopropyl.
Claim 4
Dependent Claim
18 words
A compound according to claim 2 wherein R 1 and R 2 are methyl having the structure: ##STR37##
Claim 5
Dependent Claim
10 words
A compound according to claim 2 having the structure: ##STR38##
Claim 6
Dependent Claim
25 words
An antibiotic pharmaceutical composition comprising a therapeutically effective amount of a compound according to claims 1, 2, 3, or 4 and a pharmaceutically carrier therefor.
Claim 7
Independent Claim
21 words
A method of treatment comprising administering an antibiotically effective amount of a compound according to claims 1, 2, 3, or 4.
References Cited (Backward Citations)
BE848545A
Cited
US4181733A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-04-13 | 1984-10-13 | 1985-04-14 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-04-13 | 1988-10-13 | 1989-04-14 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-04-13 | 1992-10-13 | 1993-04-14 | $7700.00 | Window Closed / Lapsed |