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

来自百度文库

喜欢 0

阅读量：

申请(专利)号：

AU5750000

申请日期：

20000619

公开/公告号：

AU5750000A

公开/公告日期：

20010109

申请(专利权)人：

PROTEIN DELIVERY INC.

发明人：

NNOCHIRI EKWURIBE，MUTHUKUMAR RAMASWAMY，JAYANTHI RAJAGOPALAN

展开

被引量：

296

摘要：

The invention provides a drug-oligomer conjugate having the following general formula: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.

展开