Terminally-functionalized conjugates and uses thereof

• US 8,623,345 B2
• Filed: 01/27/2010
• Issued: 01/07/2014
• Est. Priority Date: 03/20/2009
• Status: Active Grant

• Current Assignee: SmartCells, Inc. (Merck & Co., Inc.)
• Original Assignee: SmartCells, Inc. (Merck & Co., Inc.)
• Inventors: Zion, Todd C., Lancaster, Thomas M.
• Primary Examiner(s): TRAN, SUSAN T
• Application Number:
  US13/257,454
• Publication Number:
  US 20120014908A1
• Time in Patent Office: 1,441 Days
• Field of Search: None
• US Class Current: 424/78.29
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 47/58 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 5/50 for increasing or potentiating the activity of insulin

Abstract

The present disclosure provides inter alia conjugates of formula (I): wherein n, R1, R2, Rx, Z, X, Y and Z are as defined herein. A conjugate of formula (I) can also be converted to a conjugate of formulae (II) or (III) as described herein. Without limitation, the conjugates can be used to make controlled release materials and chemical sensors.

Claims

1. A conjugate having a formula

2. The conjugate of claim 1, wherein at least two occurrences of X include an affinity ligand that comprises a saccharide.

3. The conjugate of claim 2, wherein at least two occurrences of X include an affinity ligand that comprises a saccharide selected from the group consisting of glucose, mannose, glucosamine, mannosamine, methylglucose, methylmannose, ethylglucose, and ethylmannose.

4. The conjugate of claim 2, wherein at least two occurrences of X include an affinity ligand that comprises a bimannose or trimannose.

5. The conjugate of claim 2, wherein at least two occurrences of X include an affinity ligand selected from the group consisting of aminoethylglucose (AEG), aminoethylmannose (AEM), aminoethylbimannose (AEBM) and aminoethyltrimannose (AETM).

6. The conjugate of claim 1, wherein W is a covalently conjugated drug.

7. The conjugate of claim 6, wherein the drug is an insulin molecule.