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US 2014/0275476 A1Published application
Crystalline insulin-conjugates
AssigneeSmartCells, Inc.
InventorsThomas M. Lancaster, Todd C. Zion
Life of this patent
Estimating the term…
Abstract
The present disclosure provides crystalline insulin-conjugates. The present disclosure also provides formulations, methods of treatment, methods of administering, and methods of making that encompass these crystalline insulin-conjugates.
Claims22
A crystalline insulin-conjugate of formula (I):
- wherein:
- each occurrence of
- represents a potential branch within the conjugate;
- each occurrence of
- represents a potential repeat within a branch of the conjugate;
- each occurrence of
- is independently a covalent bond, a carbon atom, a heteroatom, or an optionally substituted group selected from the group consisting of acyl, aliphatic, heteroaliphatic, aryl, heteroaryl, and heterocyclic;
- each occurrence of T is independently a covalent bond or a bivalent, straight or branched, saturated or unsaturated, optionally substituted C1-30 hydrocarbon chain wherein one or more methylene units of T are optionally and independently replaced by —O—, —S—, —N(R)—, —C(O)—, —C(O)O—, —OC(O)—, —N(R)C(O)—, —C(O)N(R)—, —S(O)—, —S(O)2—, —N(R)SO2—, —SO2N(R)—, a heterocyclic group, an aryl group, or a heteroaryl group;
- each occurrence of R is independently hydrogen, a suitable protecting group, or an acyl moiety, arylalkyl moiety, aliphatic moiety, aryl moiety, heteroaryl moiety, or heteroaliphatic moiety;
- —B is -T-LB-X;
- each occurrence of X is independently a ligand that includes a mannose or branched trimannose;
- each occurrence of LB is independently a covalent bond or a group derived from the covalent conjugation of a T with an X;
- -D is -T-LD-W;
- WI is an insulin molecule;
- each occurrence of LD is independently a covalent bond or a group derived from the covalent conjugation of a T with a WI;
- k is an integer from 1 to 12, inclusive;
- each occurrence of p is independently an integer from 1 to 5, inclusive;
- and
- each occurrence of n is independently an integer from 0 to 5, inclusive;
- and
- each occurrence of m is independently an integer from 1 to 5, inclusive;
- and
- each occurrence of v is independently an integer from 0 to 5, inclusive, with the proviso that within each k-branch at least one occurrence of n is ≧1 and at least one occurrence of v is ≧1.
20 more elements
4-5. (canceled)
8-13. (canceled)
16-27. (canceled)
(canceled)
32-38. (canceled)
40-43. (canceled)
A crystalline insulin-conjugate of formula
- wherein:
- WI is an insulin molecule;
- and
- each occurrence of —X is
1 more element
46-77. (canceled)
A crystalline insulin-conjugate comprising a formula selected from the group consisting of:
79-168. (canceled)
Dependencies are inferred from the claim text.