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filingDate 2000-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c3ff2a2c0daea3bedd669ee95740f4fb
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publicationDate 2002-02-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber DE-10035189-A1
titleOfInvention Drugs for oral administration containing 3-N-formylhydroxylaminopropylphosphonic acid esters or 3-N-acetylhydroxylaminopropylphosphonic acid esters as active ingredient
abstract The drugs 3-N-formylhydroxylaminopropylphosphonic acid (fosmidomycin) and 3-N-acetylhydroxylaminopropylphosphonic acid (FR900098), which have strongly polar functional groups, have an insufficient absorption from the gastrointestinal tract. In addition, there are many esters of these active ingredients, namely the compounds of the formula (I) DOLLAR F1 in which R¶1¶ represents hydrogen and methyl, and in which R¶2¶ and R¶3¶ are selected from the group consisting of from phenyl esters, C¶1-9¶-acyloxy-C¶1-9¶-alkyl groups, phenyl-C¶1-9¶-alkyloxy-C¶1-9¶-alkyl esters, SC¶1-9¶-alkoxythio- C¶1-9¶ alkyl esters, C¶1-9¶ alkyloxybenzyl esters and cyclic esters, in which the two ester-forming oxygen atoms are connected via an alkyl chain with 1 to 5 carbon atoms and the alkyl chain with C¶1-9¶ alkyl , C¶1-9¶ alkoxy, C¶1-9¶ acyl and C¶1-9¶ acyloxy groups may be substituted as suitable prodrugs. On the one hand, these compounds are stable enough to survive the time in the gastrointestinal tract without any noteworthy splitting, on the other hand, they are largely split in the target cell.
priorityDate 2000-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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