公开(公告)号：US06271212B1

公开(公告)日：2001-08-07

申请号：US09033996

申请日：1998-03-03

申请人： Chung K. Chu ,  Lakshimi Kotra ,  Kostantine K. Manouilov ,  Jinfa Du ,  Raymond Schinazi

发明人： Chung K. Chu ,  Lakshimi Kotra ,  Kostantine K. Manouilov ,  Jinfa Du ,  Raymond Schinazi

IPC分类号： A61K3170

CPC分类号： A61K31/7076 ,  A61K47/52 ,  C07H19/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

摘要： Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.

摘要翻译： 提供药物前药组合物，其包含能够在体内转化为药物的药物的叠氮衍生物。 具有胺，酮和羟基取代基的药物的叠氮衍生物在体内转化为相应的药物，增加药物的半衰期。 此外叠氮化物前药通常比相应的药物更好地穿透血脑屏障。 特别有用的是虫草素，2'-F-ara-ddI，AraA，阿昔洛韦，喷昔洛韦和相关药物的叠氮衍生物。 有用的叠氮化物前药是治疗脂环族胺，酮和羟基取代的化合物的叠氮化物衍生物，包括芳烷基，杂环芳烷基和环状脂族化合物，其中胺或氧部分在环上，或胺或氧部分在其上 脂肪族侧链，以及治疗性嘌呤和嘧啶，核苷类似物和磷酸化核苷类似物。