PRODRUGS OF PHOSPHONATE NUCLEOTIDE ANALOGUES AND METHODS FOR SELECTING AND MAKING SAME

Prikazana je nova metoda za probiranje prolijekova metoksifosfonatnih analoga nukleotida za identifikaciju prolijekova koji selektivno ciljaju željena tkiva, a imaju antivirusnu ili antitumornu aktivnost. Metoda je vodila identifikaciji novih miješanih ester-amidata PMPA za retrovirusnu ili hepadnav...

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Bibliographische Detailangaben
Hauptverfasser:	Chapman, Harlan H, He, Gong-Xin, Sparacino, Mark L, Cihlar, Tomas, Lee, William A, Kernan, Michael R, Prisbe, Ernest J, Rohloff, John C, Eisenberg, Eugene J, Becker, Mark W
Format:	Patent
Sprache:	hrv ; eng
Schlagworte:	ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM BEER BIOCHEMISTRY CHEMISTRY COMPOSITIONS OR TEST PAPERS THEREFOR CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES DERIVATIVES THEREOF ENZYMOLOGY HUMAN NECESSITIES HYGIENE INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES MEASURING MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS MEDICAL OR VETERINARY SCIENCE METALLURGY MICROBIOLOGY MUTATION OR GENETIC ENGINEERING NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PHYSICS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PROCESSES OF PREPARING SUCH COMPOSITIONS SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SPIRITS SUGARS TESTING VINEGAR WINE
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Beschreibung
Zusammenfassung:	Prikazana je nova metoda za probiranje prolijekova metoksifosfonatnih analoga nukleotida za identifikaciju prolijekova koji selektivno ciljaju željena tkiva, a imaju antivirusnu ili antitumornu aktivnost. Metoda je vodila identifikaciji novih miješanih ester-amidata PMPA za retrovirusnu ili hepadnavirusnu terapiju, uključujući spojeve strukture (5a) koji imaju supstituente koji su ovdje definirani. Prikazani su pripravci tih novih spojeva u farmacetuski prihvatljivim ekscipijensima i njihova upotreba u terapiji ili profilaksi. Također je prikazana poboljšana metoda za upotrebu magenzijevog alkoksida za pripravu polaznih materijala i spojeva za ovdašnju upotrebu. A novel method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. This method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. Also provided is an improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for use herein. A novel method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. This method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. Also provided is an improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for use herein.