Backbone modified oligonucleotide analogues

• US 5,610,289 A
• Filed: 04/07/1994
• Issued: 03/11/1997
• Est. Priority Date: 07/27/1990
• Status: Expired due to Term

• Current Assignee: ISIS Pharmaceuticals Incorporated
• Original Assignee: ISIS Pharmaceuticals Incorporated
• Inventors: Vasseur, Jean J., Debart, Francoise, Cook, Phillip D., Sanghvi, Yogesh S.
• Primary Examiner(s): Low, Christopher S. F.
• Application Number:
  US08/150,079
• Time in Patent Office: 1,069 Days
• Field of Search: 536/23.1, 536/25.3, 536/25.31, 536/22.1, 536/25.34, 536/25.6, 435/89, 435/87, 435/90, 435/91.1, 435/91.2, 435/91.3, 435/91.5, 514/44, 935/8, 935/9, 935/10
• US Class Current: 536/25.34
• CPC Class Codes: A61K 47/59 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
• CPC Class Codes: A61K 49/0006 Skin tests, e.g. intradermal testing, test strips, delayed hypersensitivity
• CPC Class Codes: C07D 405/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 405/14 containing three or more hetero rings
• CPC Class Codes: C07F 7/1804 Compounds having Si-O-C linkages Si-O-acyl linkages C07F7/1896
• CPC Class Codes: C07H 19/073 with 2-deoxyribosyl as the saccharide radical
• CPC Class Codes: C07H 21/02 with ribosyl as saccharide radical
• CPC Class Codes: C07H 21/04 with deoxyribosyl as saccharide radical

Abstract

Therapeutic oligonucleotide analogues which have improved nuclease resistance and improved cellular uptake are provided. Replacement of the normal phosphorodiester inter-sugar linkages found in natural oligomers with four atom linking groups forms unique di- and poly- nucleosides and nucleotides useful in regulating RNA expression and in therapeutics. Methods of synthesis and use are also disclosed.

Claims