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1. (WO1991008213) OLIGORIBONUCLOSIDE AND OLIGODEOXYRIBONUCLEOSIDE BORANOPHOSPHATES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/008213 International Application No.: PCT/US1990/006949
Publication Date: 13.06.1991 International Filing Date: 29.11.1990
Chapter 2 Demand Filed: 28.06.1991
IPC:
C07H 21/00 (2006.01) ,C12N 15/11 (2006.01) ,C12Q 1/68 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15
Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09
Recombinant DNA-technology
11
DNA or RNA fragments; Modified forms thereof
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES OR MICRO-ORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1
Measuring or testing processes involving enzymes or micro-organisms; Compositions therefor; Processes of preparing such compositions
68
involving nucleic acids
Applicants:
BORON BIOLOGICALS, INC. [US/US]; 533 Pylon Drive P.O. Box 33489 Raleigh, NC 27636-3489, US
DUKE UNIVERSITY [US/US]; Erwin Road Durham, NC 27706, US
THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL [US/US]; 300 Bynum Hall, Campus Box 4100 Chapel Hill, NC 27599-4100, US
Inventors:
Agent:
SIBLEY, Kenneth, D. ; Bell, Seltzer, Park & Gibson P.O. Drawer 34009 Charlotte, NC 28234, US
Priority Data:
443,78130.11.1989US
Title (EN) OLIGORIBONUCLOSIDE AND OLIGODEOXYRIBONUCLEOSIDE BORANOPHOSPHATES
(FR) BORANOPHOSPHATES D'OLIGORIBONUCLEOSIDES ET D'OLIGODESOXYRIBONUCLEOSIDES
Abstract:
(EN) Disclosed are oligonucleoside boranophosphates, or salts thereof, comprising a chain of natural or modified ribonucleotides or deoxyribonucleotides, containing at least one boronated internucleotide phospodiester linkage of formula (III), wherein W is selected from the group consisting of =O, =S, -OPr, and -SPr where Pr is a base-labile protecting group. X is selected from the group consisting of -BH3, -BH2R1, -BHR1R2 and -BR1R2R3. R1 is selected from the group consisting of -R4, -COOH, -COOR4, -CONHR4, -CON(R4)2, -CN+R4, -CN, carboxycholesteryl and carboxybenzyl, wherein R4 is C1 to C18 alkyl. R2 is selected from the group consisting of -R5, -COOH, COOR5, -CONHR5, -CON(R5)2, -CN+R5, -CN, carboxy- cholesteryl and carboxybenzyl, wherein R5 is C1 to C18 alkyl. R3 is selected from the group consisting of C1 to C3 alkyl. Most preferably, X is -BH3 and W is =O. Compounds of formula (III) are useful as antisense agents and probes in molecular biology, and have pharmacological activities including anti-inflammatory, antihyperlipidemic, and antineoplastic activity.
(FR) Sont décrits des boranophosphates d'oligonucléosides, ou des sels de ceux-ci, comprenant une chaîne de ribonucléotides ou de désoxyribonucléotides naturels ou modifiés, contenant au moins une liaison phosphodiester d'internucléotide boraté de la formule (III), dans laquelle W est choisi dans le groupe composé de =O, =S, -OPr, et -SPr, dans lequel Pr représente un groupe protecteur de base-labile. X est choisi dans le groupe composé -BH3, -BH2R1, -BHR1, -BHR1R2 et -BR1R2R3. R1 est choisi dans le groupe composé -R4, -COOH, -COOR4, -CONHR4, -CON(R4)2, -CN+R4, -CN, carboxycholestéryle et carboxybenzyle, dans lequel R4 représente alkyle contenant 1 à 18 atomes de carbone. R2 est choisi dans le groupe -R5, -COOH, -COOR5, -CONHR5, -CON(R5)2, -CN+R5, -CN, carboxy-cholestéryle et carboxybenzyle, dans lequel R5 représente alkyle contenant 1 à 18 atomes de carbone. R3 est choisi dans le groupe composé d'alkyle contenant 1 à 3 atomes de carbone. De préférence, X représente -BH3 et W représente =O. Les composés de la formule (III) sont utiles en tant qu'agents non codants et en tant que sondes en biologie moléculaire, et présentent des activités pharmacologiques parmi lesquelles des activités anti-inflammatoires, antihyperlipidémiques et antinéoplastiques.
Designated States: AU, CA, JP
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0594578CA2069905AU1991070609