Back to results
US 4,226,870 AGranted
O-, N- and carboxyl derivatives of thienamycin
AssigneeMerck & Co., Inc.
InventorsBurton G. Christensen, John Hannah, William J. Leanza, Ronald W. Ratcliffe, David H. Shih
Life of this patent
Estimating the term…
Abstract
Disclosed are O-, N- and substituted carboxyl derivatives of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
Claims2
The compound having the trans- form of the structure of the following formula:
- ##STR131## wherein r is hydrogen, a pharmaceutically acceptable salt cation, or an easily removable blocking group;
- R.sup.3 is SO.sub.3 H or SO.sub.3 CH.sub.3 ;
- and R.sup.2 is formyl, acetyl, propionyl, butyryl, chloroacetyl, methoxyacetyl, aminoacetyl, methoxycarbonyl, ethoxycarbonyl, methylcarbamoyl, ethylcarbamoyl, phenylthiocarbonyl, 3-aminopropionyl, 4-aminobutyryl, N-methylaminoacetyl, N,N-dimethylaminoacetyl, N,N,N-trimethylaminoacetyl, 3-(N,N-dimethyl)aminopropionyl, 3-(N,N,N-trimethyl)amino propionyl, N,N,N-triethylaminoacetyl, pyridiniumacetyl, guanylthioacetyl, guanidinoacetyl, 3-guanidinopropyl, N.sup.3 -methylguandinopropionyl, hydroxyacetyl, 3-hydroxypropionyl, acryloyl, propynoyl, malonyl, phenoxycarbonyl, amidinoacetyl, acetamidinoacetyl, amidinopropionyl, acetamidopropionyl, guanylureidoacetyl, guanylcarbamoyl, carboxymethylamino-acetyl, sulfoacetylaminoacetyl, phosphonoacetylaminoacetyl, N.sup.3 -dimethylaminoacetamidinopropionyl, ureidocarbonyl, dimethylguanylthioacetyl, 3-(1-methyl-4-pyridinium)propionyl, 3-(5-aminoimidazol-1-yl)propionyl, 3-methyl-1-imidazoliumacetyl, 3-sydnonylacetyl, o-aminomethylbenzoyl, or o-aminobenzoyl.
Dependencies are inferred from the claim text.