发明名称 Amphiphilic drug-oligomer conjugates with hydroyzable lipophile components and methods for making and using the same
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.
申请公布号 US6309633(B1) 申请公布日期 2001.10.30
申请号 US19990336548 申请日期 1999.06.19
申请人 NOBEX CORPORATION 发明人 EKWURIBE NNOCHIRI;RAMASWAMY MUTHUKUMAR;RAJAGOPALAN JAYANTHI SETHURAMAN
分类号 A61K9/107;A61K38/00;A61K38/22;A61K38/28;A61K47/48;(IPC1-7):A61K9/107;A61K38/17;A61K39/385;C07K1/113 主分类号 A61K9/107
代理机构 代理人
主权项
地址