Title:
【発明の名称】オリゴリボヌクレオシド及びオリゴデオキシリボヌクレオシドのボラノフォスフェート
Document Type and Number:
Japanese Patent JPH05505178
Kind Code:
A
Abstract:
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 the formula: (III) 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+R4Z-, wherein Z- is an anion, -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+R5Z-, wherein Z- is an anion, -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 =0. 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.
Inventors:
Spiel Vogel Bernard F.
Sudo anup
Hall Iris H.
Shaw Barbara Ramsey
Sudo anup
Hall Iris H.
Shaw Barbara Ramsey
Application Number:
JP50251191A
Publication Date:
August 05, 1993
Filing Date:
November 29, 1990
Export Citation:
Assignee:
Boron Biologicals Inc.
DUKE UNIVERSITY
The University of North Carolina at Chapel Building
DUKE UNIVERSITY
The University of North Carolina at Chapel Building
International Classes:
A61K31/70; A61K31/7135; A61P3/06; A61P29/00; A61P35/00; A61K31/69; C07H21/00; C07H21/04; C07H23/00; C12N15/113; C12Q1/68; (IPC1-7): A61K31/69; A61K31/70; C07H21/00; C07H21/04; C07H23/00
Attorney, Agent or Firm:
Shoichi Hase (1 person outside)