Acyclic nucleoside analogs and oligonucleotide sequences containing them
US5576427A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 26, 1995 |
| Grant date | Nov 19, 1996 |
| Priority date | — |
| Expiry date | May 26, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H21/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of formula I; ##STR1## wherein R.sup.1 is hydrogen, or a blocking group that is compatible with oligonucleotide synthesis; PA1 R.sup.2 is hydrogen, nitro, lower alkyl amino, diloweralkyl amino or methyl; PA1 R.sup.3 is hydrogen or --P(R.sup.4)OR.sup.5 ; PA1 R.sup.4 is chlorine, 4-nitroimidazole, imidazole, tetrazole, triazole or di(lower-alkyl)amino-; PA1 R.sup.5 is methyl, 2-cyanoethyl or 2,2,2-trichloroethyl; PA1 n is from 0 to 2 PA1 X is oxygen, sulfur, or --NR.sup.6 ; PA1 R.sup.6 is hydrogen or lower alkyl; PA1 Q is chosen from the group consisting of ##STR2## R.sup.7 is lower-alkyl or loweralkyloxy methylene; and R.sup.8 is hydrogen, benzoyl, anisoyl, or lower-alkyl carbonyl and its pharmaceutically acceptable addition salts are nucleotide analogs. Modified oligonucleotides containing the nucleoside analogs of formula I are stable to nuclease degradation and are useful in inhibiting gene expression, in sequencing, and in mutagenesis.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.