Abstract: Synthetic processes are provided wherein oligomers are prepared using phosphoramidite compositions. Oligomers having phosphodiester, phosphorothioate, phosphorodithioate covalent linkages are prepared that can include other covalent linkages. Also provided are compositions useful in such processes.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
February 22, 2005
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Vasulinga T. Ravikumar, Daniel C. Capaldi, Douglas L. Cole
Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.
Type:
Grant
Filed:
August 30, 2002
Date of Patent:
February 22, 2005
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Vasulinga T. Ravikumar, Muthiah Manoharan, Daniel C. Capaldi, Achim Krotz, Douglas L. Cole, Andrei Guzaev
Abstract: Modified dimers having a ribose sugar moiety in the 5? nucleoside and a 2? modified sugar in the 3? nucleoside are provided. The modified dimers are useful in the preparation of oligonucleotide analogs having enhanced properties compared to native oligonucleotides, including increased nuclease resistance, enhanced binding affinity and improved protein binding.
Type:
Grant
Filed:
July 15, 2002
Date of Patent:
February 1, 2005
Assignee:
ISIS Pharmaceuticals, Inc.
Inventors:
Phillip Dan Cook, Muthiah Manoharan, Balkrishen Bhat
Abstract: Selectively functionalized oligonucleotides, methods for making same, and compounds useful therefor are disclosed. The oligonucleotides can be selectively functionalized with a first conjugate group at the 3′-terminial position and optionally functionalized with a second conjugate group at the 5′-terminal position and/or one or more internucleotides. Alternatively, the oligonucleotides can be selectively functionalized with a first conjugate group at the 5′-terminal position and optionally functionalized with a second conjugate group at one or more internucleotides. In yet another embodiment, the oligonucleotides can be functionalized with a first conjugate group at one or more internucleotides and with a second conjugate group at one or more different internucleotides.
Abstract: Novel compounds that mimic and/or modulate the activity of wild-type nucleic acids. In general, the compounds are phosphorothioate oligonucleotides wherein the 5′-terminal internucleoside linkage or the 5′- and 3′-terminal linkages are modified.