OLIGONUCLEOTIDES CONTAINING 5-ALKYL-, 5-(1-ALKENYL)- OR 5-(1-ALKYNYL)-PYRIMIDINE BASES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR THEIR PREPARATION

The invention relates to 12 to 30 nucleotide-unit long oligodeoxynucleotides containing at least one 5-substituted pyrimidine base, either uracil or cytosine, where the 5-substituent is a C3-14 n-alkyl group, a C2-8 (E)-n-1-alkenyl group, an ethynyl or a C4-12 n-1-alkynyl group. The oligodeoxynucleo...

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Main Authors SAGI,GYULA, OETVOES,LASZLO, FELLEGVARI,IREN, SZABOLCS,OTTONE, SAGI,JANOS, TUEDOES,FERENCNE, EBINGER,KATALIN, RUFF,EVA, SZEMZOE,ATTILA
Format Patent
LanguageEnglish
Published 28.02.1997
Edition6
Subjects
CHEMISTRY
DERIVATIVES THEREOF
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
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Summary:The invention relates to 12 to 30 nucleotide-unit long oligodeoxynucleotides containing at least one 5-substituted pyrimidine base, either uracil or cytosine, where the 5-substituent is a C3-14 n-alkyl group, a C2-8 (E)-n-1-alkenyl group, an ethynyl or a C4-12 n-1-alkynyl group. The oligodeoxynucleotides according to the invention can form double helices with complementary nucleic acids with unaltered or increased stability, possess highly increased stability against 3'-exonucleases as well as strongly increased hydrophobicity and are much better taken up by cells than the unmodified oligodeoxynucleotides. In this way, they can be efficiently used as drugs against various tumours and viruses, including HIV.
Bibliography:Application Number: HU19930000174