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Title:
SYNTHESIS OF ARA-2'-O-METHYL-NUCLEOSIDES, CORRESPONDING PHOSPHORAMIDITES AND OLIGONUCLEOTIDES INCORPORATING NOVEL MODIFICATIONS FOR BIOLOGICAL APPLICATION IN THERAPEUTICS, DIAGNOSTICS, G- TETRAD FORMING OLIGONUCLEOTIDES AND APTAMERS
Document Type and Number:
WIPO Patent Application WO/2010/096201
Kind Code:
A3
Abstract:
The present invention relates to synthesis, purification and methods to obtain high purity novel 2'-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin -1, bearing ara-2'-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents. It is further anticipated that the nucleosides, phosphates and triphosphates of this invention could develop as therapeutic agents.

Inventors:
SRIVASTAVA, Suresh, C. (7 Donald Rd, Burlington, MA, 01803, US)
PANDEY, Divya (7 Alfa Farm, Chini Godam RoadBarabirwa, Kanpur Road, upLucknow, (up), IN)
SRIVASTAVA, Naveen, P. (8 Baron Park Lane, Apt-18Burlington, MA, 01803, US)
SRIVASTAVA, Alok (2 Baron Park Lane, Apt-29Burlington, MA, 01803, US)
Application Number:
US2010/000524
Publication Date:
January 13, 2011
Filing Date:
February 23, 2010
Export Citation:
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Assignee:
CHEMGENES CORPORATION (33 Industrial Way, Wilmington, MA, 01887, US)
SRIVASTAVA, Suresh, C. (7 Donald Rd, Burlington, MA, 01803, US)
PANDEY, Divya (7 Alfa Farm, Chini Godam RoadBarabirwa, Kanpur Road, upLucknow, (up), IN)
SRIVASTAVA, Naveen, P. (8 Baron Park Lane, Apt-18Burlington, MA, 01803, US)
SRIVASTAVA, Alok (2 Baron Park Lane, Apt-29Burlington, MA, 01803, US)
International Classes:
C07H19/02; A61K31/7052; C07H21/00; C12N15/115
Domestic Patent References:
WO2005100375A12005-10-27
Foreign References:
US20050059817A12005-03-17
US5466786A1995-11-14
Other References:
GOTFREDSEN, C. H. ET AL.: "Structure of a DNA Duplex Containing a Single 2'-0-Methyl-beta-D-araT: Combined Use of NMR, Restrained Molecular Dynamics, and Full Relaxation Matrix Refimement", BIOCONJUGATE CHEMISTRY, vol. 7, November 1996 (1996-11-01), pages 680 - 688, XP055078370
GOTFREDSEN, C. H . ET AL.: "Synthesis and properties of alpha- and beta-oligodeoxynucleotides containing alpha- and beta-1-(2-0-Methyl-D-arabino-furanosyl)thymine", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 4, no. 8, 19 August 1996 (1996-08-19), pages 1217 - 1225, XP001107262
See also references of EP 2398815A4
Attorney, Agent or Firm:
ANAND, Indu, M. (15 Green Way, Chelmsford, MA, 01824, US)
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