Claims for Patent: 10,398,781

Summary for Patent: 10,398,781

Title:	Conjugate based systems for controlled drug delivery
Abstract:	Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
Inventor(s):	Zion; Todd C. (Marblehead, MA), Lancaster; Thomas M. (Wenham, MA)
Assignee:	SMARTCELLS, INC. (Kenilworth, NJ)
Application Number:	15/680,262
Patent Claims:	1. A conjugate comprising an insulin molecule conjugated to one or more ligands that are independently selected from the group consisting of aminoethylglucose (AEG), aminoethylmannose (AEM), aminoethylbimannose (AEBM), aminoethyltrimannose (AETM), and .beta.-aminoethyl-N-acetylglucosamine (AEGA), wherein the one or more ligands are indirectly conjugated to the insulin molecule via a conjugate framework. 2. The conjugate of claim 1, wherein the insulin molecule is conjugated via the A1 amino acid residue, via the B1 amino acid residue, via the epsilon-amino group of Lys.sup.B29 or-via the epsilon-amino group of Lys.sup.B3. 3. The conjugate of claim 1, wherein the insulin molecule is conjugated to two or more separate ligands. 4. The conjugate of claim 3, wherein the two or more separate ligands are conjugated to a single conjugate framework that is also conjugated to the insulin molecule. 5. The conjugate of claim 3, wherein the two or more separate ligands and insulin molecule are each located on a separate branch of a single branched conjugate framework. 6. The conjugate of claim 5, wherein the two or more separate ligands and insulin molecule are each located on termini of separate branches of a single branched conjugate framework. 7. The conjugate of claim 3, wherein the two or more separate ligands are conjugated to the insulin molecule via two or more different conjugation points. 8. The conjugate of claim 7, wherein the insulin molecule is conjugated via the A1 amino acid residue and the epsilon-amino group of Lys.sup.B29. 9. The conjugate of claim 8, wherein the insulin molecule is conjugated to two separate conjugate frameworks that are each conjugated to one or more separate ligands. 10. The conjugate of claim 8, wherein the insulin molecule is conjugated to two separate branched conjugate frameworks that are each conjugated to two ligands. 11. The conjugate of claim 10, wherein the ligands are located on separate branches of the branched conjugate frameworks. 12. The conjugate of claim 11, wherein the ligands are located on termini of separate branches of the branched conjugate frameworks. 13. The conjugate of claim 3, wherein the two or more separate ligands are aminoethylglucose (AEG). 14. The conjugate of claim 3, wherein the two or more separate ligands are aminoethylmannose (AEM). 15. The conjugate of claim 3, wherein the two or more separate ligands are aminoethylbimannose (AEBM). 16. The conjugate of claim 3, wherein the two or more separate ligands are aminoethyltrimannose (AETM). 17. The conjugate of claim 3, wherein the two or more separate ligands are O-aminoethyl-N-acetylglucosamine (AEGA). 18. The conjugate of claim 1, wherein the insulin molecule is selected from the group consisting of human insulin, porcine insulin, and bovine insulin. 19. The conjugate of claim 1, wherein the insulin molecule is selected from the group consisting of insulin lispro, insulin aspart, and insulin glulisine. 20. The conjugate of claim 1, wherein the insulin molecule is insulin glargine or insulin detemir.

Details for Patent 10,398,781

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Eli Lilly And Company	HUMALOG	insulin lispro	Injection	020563	June 14, 1996		2037-08-18
Eli Lilly And Company	HUMALOG	insulin lispro	Injection	020563	August 06, 1998		2037-08-18
Eli Lilly And Company	HUMALOG	insulin lispro	Injection	020563	September 06, 2007		2037-08-18
Eli Lilly And Company	HUMALOG	insulin lispro	Injection	020563	June 06, 2017		2037-08-18
Eli Lilly And Company	HUMALOG	insulin lispro	Injection	020563	November 15, 2019		2037-08-18
Novo Nordisk Inc.	NOVOLOG	insulin aspart	Injection	020986	June 07, 2000		2037-08-18