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Title:
オリゴヌクレオチドN3’→P5’ホスホルアミデート:合成および化合物;ハイブリダイゼーションおよびヌクレアーゼ耐性特性
Document Type and Number:
Japanese Patent JP4383720
Kind Code:
B2
Abstract:
PCT No. PCT/US95/03575 Sec. 371 Date Jan. 10, 1997 Sec. 102(e) Date Jan. 10, 1997 PCT Filed Mar. 20, 1995 PCT Pub. No. WO95/25814 PCT Pub. Date Sep. 28, 1995Modified oligonucleotides 3'-NHP(O)(O-)O-5' phosphoramidates were synthesized on a solid phase support. The phosphoramidate analogs were found to have significantly increased resistance toward phosphodiesterase digestion. Thermal dissociation experiments demonstrated that these compounds form more stable duplexes than phosphodiesters with complementary DNA and particularly RNA strands. Further, the phosphoramidate analogs can also form stable triplexes with double-stranded DNA target, where under similar conditions parent phosphodiester compounds failed to do so.

Inventors:
Sergey M. Grinob
Ronald G. Schultz
Changer-Can
Application Number:
JP2002171743A
Publication Date:
December 16, 2009
Filing Date:
June 12, 2002
Export Citation:
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Assignee:
GERON CORPORATION
International Classes:
C07H21/00; A61K31/70; C12Q1/02; A61K31/7042; A61K31/7052; A61K31/7076; A61K31/708; A61K31/7088; A61K31/7125; A61K48/00; A61P29/00; A61P31/04; A61P31/10; A61P31/12; A61P35/00; A61P35/02; A61P43/00; C07H19/06; C07H19/16; C07H19/173; C07H21/04; C12N15/09; C12Q1/68; G01N33/50; G01N33/566
Other References:
Tetrahedron Letters,1993年,Vol.34, No.38,p.6017-6020
Alexei V.Azhayev et al.,Synthesis of phosphoramidate analogues of short oligoribonucleotides,Nucleic Acids Research Symposium Series,英国,IRL Press limited.,1981年,No.9 ,PP251-254
NUCLEIC ACIDS RESEARCH,1987年,Vol.15 No.4,P1699-1715
NUCLEIC ACIDS RESEARCH,1992年,Vol.20 No.13,P3403-3409
Attorney, Agent or Firm:
Hidesaku Yamamoto