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6-(1-Hydroxyethyl)-2-(2-aminoethylthio)-1-substituted-1-carbade-thiapen-2-em-3-carboxylic acids

Assignee: Merck and Co Inc
•
Filing: 1978-10-24
•
Granted: 1980-08-19
•
Expires: 1998-10-24
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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 is, inter alia, substituted and unsubstituted alkyl, aryl and aralkyl.

Inventors

  • 👤 Burton G. Christensen
  • 👤 David H. Shih

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 18:59
CPC Classifications
C; C07; C07D; C07D205/00; C07D205/02; C07D205/06; C07D205/08; C07C; C07C205/00; C07C205/39; C07C205/42; C07D477/00; C07D477/10; C07D477/12; C07D477/16; C07D477/20; C07D477/26; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; C07F9/00; C07F9/02; C07F9/547; C07F9/553; C07F9/568

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 83 words
A compound having the formula: ##STR83## and its pharmaceutically acceptable salts wherein R 1 is 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, and cycloalkylalkyl having 4 to 7 carbon atoms in the chain and 3-6 carbon atoms in the ring; wherein said substituents on R 1 are selected from the group consisting of halogen, hydroxyl, amino, alkyl having 1-6 carbon atoms, azido, cyano, and carboxyl.
Claim 2
Dependent Claim 83 words
A compound having the formula: ##STR83## and its pharmaceutically acceptable salts wherein R 1 is 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, and cycloalkylalkyl having 4 to 7 carbon atoms in the chain and 3-6 carbon atoms in the ring; wherein said substituents on R 1 are selected from the group consisting of halogen, hydroxyl, amino, alkyl having 1-6 carbon atoms, azido, cyano, and carboxyl.
Claim 3
Dependent Claim 18 words
A compound according to claim 1 wherein R 1 is methyl, phenyl, benzyl, ethyl, cyclopropyl, propyl and isopropyl.
Claim 4
Dependent Claim 15 words
A compound according to claim 2 wherein R 1 is methyl having the structure ##STR84##
Claim 5
Dependent Claim 14 words
A compound having the formula: ##STR85## wherein R is H or CH 3 .
Claim 6
Dependent Claim 14 words
A compound having the formula: ##STR85## wherein R is H or CH 3 .
Claim 7
Dependent Claim 25 words
An antibiotic pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1, 2, 3, or 4 and a pharmaceutically carrier therefor.

References Cited (Backward Citations)

US3950357A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1983-08-19 1984-02-18 1984-08-19 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1987-08-19 1988-02-18 1988-08-19 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1991-08-19 1992-02-18 1992-08-19 $7700.00 Window Closed / Lapsed

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