Nucleoside and nucleotide having nitrogen-containing heterocycle structure
AssigneeShionogi & Co., Ltd.
InventorsYasunori Mitsuoka, Akira Kugimiya, Aiko Yamashita
Life of this patent
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Abstract
The present invention provides compounds shown by the formula: wherein Y1 is CR6 or N, Y2 is CR7 or N, Y3 is CR8 or N, R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.
Claims20
A compound of formula (I) or a salt thereof:
- wherein
- Y1 is CR6 or N,
- Y2 is CR7 or N,
- Y3 is CR8 or N,
- R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylcarbonylamino, substituted or unsubstituted alkenylcarbonylamino, substituted or unsubstituted alkynylcarbonylamino, substituted or unsubstituted alkylcarbamoyl, substituted or unsubstituted alkenylcarbamoyl, or substituted or unsubstituted alkynylcarbamoyl,
- Bx is a nucleic acid base moiety,
- Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group,
- R1 and R2 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R3 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R4 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R5 is a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, and
- n is an integer of 0 to 3, and wherein when n=0, the 4′-position is bonded directly to the 2′ ring.
An oligonucleotide comprising one or more nucleoside structure of formula (II) or a pharmaceutically acceptable salt thereof:
- wherein
- Y1 is CR6 or N,
- Y2 is CR7 or N,
- Y3 is CR8 or N,
- R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylcarbonylamino, substituted or unsubstituted alkenylcarbonyl amino, substituted or unsubstituted alkynylcarbonylamino, substituted or unsubstituted alkylcarbamoyl, substituted or unsubstituted alkenylcarbamoyl or substituted or unsubstituted alkynylcarbamoyl,
- Bx is a nucleic acid base moiety,
- R1 and R2 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R3 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R4 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl,
- R5 is a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl, and
- n is an integer of 0 to 3, and when n=0, the 4′-position is bonded directly to the 2′ring.
Dependencies are inferred from the claim text.