Insulin-oligomer conjugates, formulations and uses thereof

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Insulin; related peptides

Reexamination Certificate

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C514S003100, C530S345000

Reexamination Certificate

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07872095

ABSTRACT:
An insulin compound coupled to a modifying moiety having a formula:in-line-formulae description="In-line Formulae" end="lead"?—X—R1—Y-PAG-Z—R  (Formula VI)in-line-formulae description="In-line Formulae" end="tail"?where,X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond,either R1or R2is is a lower alkyl, optionally including a carbonyl group, and when R1is a lower alkyl, R2is a capping group, andPAG is a linear or branched carbon chain incorporating one or more alkalene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —S—, —O—, —N—, and —C(O)—, andwhere the modifying moiety has a maximum number of 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, or 25 heavy atoms.

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