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

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United States of America Patent

PATENT NO 6309633
SERIAL NO

09336548

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Abstract

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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.

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Patent Owner(s)

Patent OwnerAddress
BIOCON LIMITED20TH KM HOSUR ROAD ELECTRONIC CITY P O KARNATAKA BANGALORE 560 100

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ekwuribe, Nnochiri Cary, NC 10 250
Rajagopalan, Jayanthi Sethuraman Cary, NC 1 135
Ramaswamy, Muthukumar Cary, NC 4 270

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