Global Patent Index - EP 0428623 A4

EP 0428623 A4 19931208 - PRODUCTION OF RADIOIODINATED 1--G(B)-D-ARABINOFURANOSYL)-5(E)-(2-IODOVINYL)URACIL, AND USES THEREOF, AND RELATED ANALOGUES INCORPORATING ALTERNATIVE HALOGEN RADIONUCLIDES, THE GENERAL RADIOHALOGENATION PRECURSORS, 1-(2,3,5-TRI-O-ACETYL--G(B)-D-ARABINOFURANOSYL)-5(Z AND E)-(2-TRIMETHYLSILYLVINYL)URAC

Title (en)

PRODUCTION OF RADIOIODINATED 1--G(B)-D-ARABINOFURANOSYL)-5(E)-(2-IODOVINYL)URACIL, AND USES THEREOF, AND RELATED ANALOGUES INCORPORATING ALTERNATIVE HALOGEN RADIONUCLIDES, THE GENERAL RADIOHALOGENATION PRECURSORS, 1-(2,3,5-TRI-O-ACETYL--G(B)-D-ARABINOFURANOSYL)-5(Z AND E)-(2-TRIMETHYLSILYLVINYL)URAC

Publication

EP 0428623 A4 19931208 (EN)

Application

EP 89910499 A 19890808

Priority

US 23113788 A 19880810

Abstract (en)

[origin: WO9001324A1] Radioactive antiviral compounds, with 1-( beta -D-arabinofuranosyl)-5(E)-(2-[<*>I]-iodovinyl)uracil, hereinafter referred to as "[<*>I]-IVaraU", as the prototype compound for the class of compounds designated as 1- beta -D-arabinofuranosyl)-5(E)-(2-[<*>X]-halogenovinyl)uracil, hereinafter referred to as "[<*>X]-XVaraU", and novel precursors thereof, 1-(2,3,5-tri-O-acetyl- beta -D-arabinofuranosyl)-5(Z and E)-(2-trimethylsilylvinyl)uracil, hereinafter referred to as "TMSVaraU", and processes for the preparation thereof, and uses thereof, wherein "<*>I" stands for a radionuclide of iodine, and "<*>X" stands for any other appropriate halogen radionuclide. Inclusion of the appropriate gamma or positron emitting iodine, or other appropriate halogen radionuclide, into the structure of [<*>I]-IVaraU, makes this agent useful as a diagnostic tool for detection of herpes virus infections in vitro and in vivo. Inclusion of the appropriate alpha- and/or beta- and/or gamma- emitting, and/or Auger electron decay-associated, (specifically-nuclear-toxic) isotopes of iodine, or other appropriate halogen radionuclides, into the structure of this agent makes the agent useful as a unique radiotherapeutic tool for herpes virus infections by precise targeting of the lethal effects of alpha and/or beta radiation and/or Auger electron decay effects to the site of viral infection.

IPC 1-7

A61K 49/02

IPC 8 full level

A61K 51/04 (2006.01)

CPC (source: EP)

A61K 51/0491 (2013.01); A61K 2121/00 (2013.01); A61K 2123/00 (2013.01)

Citation (search report)

  • ANTIMICROBIAL AGENTS AND CHEMOTHERAPY vol. 29, no. 2, February 1986, pages 320 - 324 J. SAMUEL ET AL 'PHARMACOKINETICS AND METABOLISM OF E-5-(2-Ä131-IÜIODOVINYL)-2'-DEOXYURIDINE IN DOGS'
  • ANTIVIRAL RESEARCH vol. 7, no. 2, February 1987, pages 79 - 86 S. SUZUKI ET AL 'ANTIVIRAL ACTIVITY OF VARIOUS 1-BETA-D-ARABINOFURANOSYL-E-5-HALO GENOVINYLURACILS AND E-5-BROMOVINYL-2'-DEOXYURIDINE AGAINST SALMON HERPES VIRUS, ONCORHYNCHUS MASOU VIRUS (OMV)'
  • JOURNAL OF ORGANIC CHEMISTRY. vol. 48, no. 11, 1983, EASTON US pages 1854 - 1862 M. J. ROBINS ET AL 'NUCLEIC ACID RELATED COMPOUNDS. 39. EFFICIENT CONVERSION OF 5-IODO TO 5-ALKYNYL AND DERIVED 5-SUBSTITUTED URACIL BASES AND NUCLEOSIDES'
  • TETRAHEDRON LETTERS. no. 6, 1974, OXFORD GB pages 543 - 546 R. B. MILLER ET AL 'THE STEREOSPECIFIC SYNTHESIS OF VINYL HALIDES USING A VINYLSILANE AS THE SYNTHETIC PRECURSOR'
  • See references of WO 9001324A1

Designated contracting state (EPC)

AT BE CH DE FR GB IT LI LU NL SE

DOCDB simple family (publication)

WO 9001324 A1 19900222; EP 0428623 A1 19910529; EP 0428623 A4 19931208

DOCDB simple family (application)

US 8903396 W 19890808; EP 89910499 A 19890808