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US 12,653,893 B2Granted
Carbohydrate conjugated RNA agents and process for their preparation
AssigneeAlnylam Pharmaceuticals, Inc.
InventorsJayaprakash K. Nair, Alexander V. Kel'in, Pachamuthu Kandasamy, Kallanthottathil G. Rajeev, Muthiah Manoharan
Life of this patent
Estimating the term…
Abstract
This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.
Claims38
A compound of formula (VIII):
- wherein A is a C6-C14 alkylene linker;
- each R is, independently, an acid protecting group;
- and Rx is an acid protecting group.
A compound of formula (II):
- and a counterion, wherein Z is an acid protecting group;
- n is 0-20;
- and each occurrence of r and s is independently 1-7.
A compound of the formula (XII):
- wherein Z is an acid protecting group;
- n is 0-20;
- each occurrence of r and s is independently 1-7;
- and
- P is an amino protecting group.
2 more elements
A compound of formula (IV):
- wherein Z is an acid protecting group;
- n is 0-20;
- q, r, and s are independently 1-7;
- X is a hydroxy protecting group or hydrogen;
- and
- Y is an amine protecting group.
3 more elements
A compound that is:
Dependencies are inferred from the claim text.