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1. 发明授权

US06309633B1 Amphiphilic drug-oligomer conjugates with hydroyzable lipophile components and methods for making and using the same 有权
标题翻译：两亲药物 - 低聚物共轭物与可水解的亲油组分和制备和使用它们的方法
公开(公告)号：US06309633B1
公开(公告)日：2001-10-30
申请号：US09336548
申请日：1999-06-19
申请人： Nnochiri Ekwuribe , Muthukumar Ramaswamy , Jayanthi Sethuraman Rajagopalan
发明人： Nnochiri Ekwuribe , Muthukumar Ramaswamy , Jayanthi Sethuraman Rajagopalan
IPC分类号： A61K9107
CPC分类号： A61K47/60 , A61K38/00 , Y02A50/463
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.
摘要翻译：本发明提供具有以下通式的药物 - 低聚物缀合物：其中D是治疗药物部分; H和H'各自为亲水部分，独立地选自具有2至130个PEG亚基的直链或支链PEG聚合物和糖; L是选自具有2-26个碳原子的烷基，胆固醇，金刚烷和脂肪酸的亲脂性部分; o是H上从1到最大数量的共价键合位点的数; 对于-H'，-L和-H-L取代基，m + n + p一起具有至少一个且不超过D的共价键合位置总数的值， H-L键是可水解的，当存在时，D-L'键是可水解的; 该共轭物的进一步特征在于以下之一：（i）m为0且p为至少1; （ii）n为0，p为至少1; （iii）m和n各自为0，p为至少1; （iv）p为0，m和n各自为至少1.治疗药物部分优选为治疗性蛋白质或肽，优选胰岛素或其功能等同物。

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