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US 7,115,738 B2Granted
Hydroxyproline/phosphono oligonucleotide analogues, methods of synthesis and methods of use
AssigneeActive Motif, Inc.
InventorsVladimir Efimov, Joseph Fernandez, Dorothy Archdeacon, John Archdeacon, Oksana Chakhmakhcheva, Alla Buryakova, Mikhail Choob, Kyle Hondorp
Life of this patent
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Abstract
Compounds are described and claimed comprising general formula: The compounds have substituents as described herein and are useful, e.g., for their ability to bind nucleic acids and thereby effect purifications, probing techniques and gene inhibition.
Claims4
A compound comprising the structure:
- wherein G is selected from a group consisting of H and a protecting group;
- wherein E is selected from a group consisting of O—, OH, a protecting group, and an activating group;
- wherein each B1 and B2 is independently selected from the group consisting of H and a nucleobaso, and wherein amino groups, if present, are, optionally, protected by amino protecting groups;
- wherein each A1 and each A2 is, independently, a group of formula (Ia), (Ib), or (Ic);
- wherein r and s are, for I(a), I(b), and I(c) independently of one another, values from 0 to 5;
- wherein each R1 and each R2 is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, alkylthio, amino, or halogen;
- wherein each R4 and each R5, is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, amino, aryl, aralkyl, heteroaryl, or an amino acid side chain;
- Y is a single bond, O, S, or NR4;
- and
- X is O, S, Se, NR4, CH2, or C(CH3)2;
- wherein each R6 is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkylthio-substituted (C1–C6)alkyl, aryl, aralkyl, heteroaryl, or an amino acid side chain;
- wherein R7 is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, alkylthio, amino, aryl, aralkyl, heteroaryl, or hydrogen, and R8 is hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, aryl, aralkyl, or heteroaryl;
- or R7 is hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, aryl, aralkyl, or heteroaryl, and R8 is hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, alkylthio, amino, aryl, aralkyl, heteroaryl, or halogen;
- wherein each R9 independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, alkoxy, aryl, arylkyl, or heteroaryl;
- wherein each R10 and each R11 is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, aryl, aralkyl, heteroaryl, or an amino acid side chain;
- wherein each R12, R13, R14, R15, R16, and each R17 is, independently, hydrogen, (C1–C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, alkylthio, aryl, aralkyl, heteroaryl, or an amino acid side chain;
- wherein T is hydrogen, (C1C6)alkyl, hydroxy-, alkoxy-, amino-, or alkythio-substituted (C1–C6)alkyl, hydroxy, alkoxy, alkylthio, aryl, aralkyl, heteroaryl, or an amino acid side chain;
- and
- n is 1 or greater,
- and salts thereof.
17 more elements
Dependencies are inferred from the claim text.