|Title:||Combination of 2-substituted carbapenems with dipeptidase inhibitors|
|Abstract:||A combination of a carbapenem of the formula: ##STR1## where R is H or CH.sub.3 and R.sup.1 is ##STR2## with a renal dipeptidase inhibitor is disclosed.|
|Inventor(s):||Kahan; Frederick M. (Scotch Plains, NJ), Kropp; Helmut (Kenilworth, NJ)|
|Assignee:||Merck & Co., Inc. (Rahway, NJ)|
|Filing Date:||Apr 03, 1991|
|Claims:||1. An antibacterial composition comprising a combination of a carbapenem having the following structure: ##STR112## wherein R is hydrogen or methyl, and |
R' is ##STR113## wherein M is CH.sub.3 or H;
and the easily removable pharmaceutically acceptable salt or ester derivatives thereof; and a dipeptidase (E.C.188.8.131.52) inhibitor, of the following structure, ##STR114## wherein R.sup.2 and R.sup.3 are hydrocarbon radicals in the range respectively of 3-10 and 1-15 carbon atoms; in either of these hydrocarbon radicals R.sup.2 and R.sup.3, up to 6 hydrogens may be replaced by halogens, or a non-terminal methylene may be replaced by oxygen or sulphur, including oxidized forms of the latter; a terminal hydrogen in R.sup.3 can also be replaced by a hydroxyl or thiol group, which may be acylated, such as with an alkanoyl acid of 1-8 carbon atoms, or carbamoylated, including alkyl and dialkyl carbamate derivatives; or the hydrogen can be replaced by an amino group, which may be derivatized as in an acylamino, ureido, amidino, guanidino, or alkyl or substituted alkyl amino group, including quaternary nitrogen groupings; or, alternatively, there may be replacement by acid groups such as carboxylic, phosphonic or sulfonic acid groups or esters or amides thereof, as well as cyano; or combinations thereof, such as a terminal amino acid grouping; the ratio of the carbapenem to the dipeptidase inhibitor being within in the range of about 1:3 to 30:1.
2. The composition of claim 1 in which the combination is mixed with a pharmaceutical carrier.
3. The composition of claim 2 in which the carrier is adapted for injection.
4. The composition of claim 1 in which the carbapenem is 2-(1-acetimidoyl-pyrollidin-3-yl-thio)-6-(1-hydroxyethyl)-carbapen-2-em-3- carboxylic acid or sodium carboxylate.
5. The composition of claim 4 wherein the dipeptidase inhibitor is Z-7-(L-amino-carboxyethylthio)-2-(2,2-dimethylcyclopropane carboxamido)-2-heptanoic acid.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.