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Hilfinger

John Hilfinger, Ann Arbor, MI US

Patent application numberDescriptionPublished
20090270618PHOSPHONYL ESTER CONJUGATES AS PRODRUGS - Cidofovir or foscarnet based compounds having an amino acid or dipeptide esters are provided as prodrugs.10-29-2009
20100093609PRODRUGS OF TRICIRIBINE AND TRICIRIBINE PHOSPHATE - A prodrug composition is provided which includes a pharmaceutical species and an amino acid having a covalent bond to the pharmaceutical species. Particular pharmaceutical species are 6-amino-4-methyl-8-(beta.-D-ribofuranosyl)pyrrolo[4,3,2-de]pyrimido[4,5-c]pyridazine, also known as TCN and by the trade name triciribine; as well as the 5′phosphate of triciribine. TCN and TCNP prodrugs of the present invention have increased bioavailability compared to the parent TCN and TCNP. The inventive prodrug is transported from the gastrointestinal lumen by a specific transporter and is enzymatically cleaved to yield TCN or TCNP, such that TCN or TCNP is delivered to the individual.04-15-2010
20110160127Prodrugs of Neuraminidase Inhibitors - A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.06-30-2011

Patent applications by John Hilfinger, Ann Arbor, MI US

John M. Hilfinger, Ann Arbor, MI US

Patent application numberDescriptionPublished
20110263535TYROSINE-BASED PRODRUGS OF ANTIVIRAL AGENTS - A tyrosine-based (phosphonylmethoxyalkyl)purine or -pyrimidine conjugate is provided. In some embodiments, the conjugate includes tyrosine based amino acid or dipeptide moieties of (S)-9-(3-hydroxy-2-phosphonyl-methoxypropyl)adenine or its cytosine analogue. A method of synthesizing such conjugates based on Boc-protected amino acid or dipeptides is also provided. In addition, a method of isomerizing an (S,S)-diastereoisomer to an (S,R)-diastereoisomer of an amino acid-based or dipeptide-based conjugate by a process including transesterification is provided. A method of inhibiting viral infection and a method of treating viral infection based on (phosphonylmethoxyalkyl)purine or -pyrimidine conjugates is also provided.10-27-2011

Peter Hilfinger, Bad Homburg DE

Patent application numberDescriptionPublished
20100175208Indicating Teeth Cleaning Time - This disclosure relates to toothbrushes and to methods of operating toothbrushes. In some embodiments, a method of operating a toothbrush includes measuring an actual cleaning time of a first teeth cleaning process, comparing the actual cleaning time of the first teeth cleaning process to a standard cleaning time, and determining a target cleaning time of a second, subsequent teeth cleaning process. In certain embodiments, the target cleaning time of the second teeth cleaning process is the standard cleaning time plus additional time when the actual cleaning time of the first cleaning process is less than the standard cleaning time.07-15-2010