Patent Number: 6,309,633

Title: Amphiphilic drug-oligomer conjugates with hydroyzable lipophile components and methods for making and using the same

Abstract: The invention provides a drug-oligomer conjugate having the following general formula: ##STR1## wherein D is a therapeutic drug moiety; H and H' are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the --H', --L and --H--L substituents; the H--L bond(s) are hydrolyzable and the D--L' bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is 0 and m and n are each at least 1. The therapeutic drug moiety is preferably a therapeutic protein or peptide, preferably insulin or a functional equivalent thereof.

Inventors: Ekwuribe; Nnochiri (Cary, NC), Ramaswamy; Muthukumar (Cary, NC), Rajagopalan; Jayanthi Sethuraman (Cary, NC)

Assignee: Nobex Corporation

International Classification: A61K 47/48 (20060101); A61K 38/00 (20060101); A61K 009/107 (); A61K 038/17 (); A61K 038/28 (); A61K 039/385 (); C07K 001/113 ()

Expiration Date: 10/30/2018