会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 7. 发明申请
    • MODIFIED CARBAMATE-CONTAINING PRODRUGS AND METHODS OF SYNTHESIZING SAME
    • 改性含碳酸酯的制剂及其合成方法
    • WO2004043396A2
    • 2004-05-27
    • PCT/US2003/035995
    • 2003-11-07
    • NOBEX CORPORATIONEKWURIBE, Nnochiri, N.RIGGS-SAUTHIER, JenniferDYAKONOV, Tatyana
    • EKWURIBE, Nnochiri, N.RIGGS-SAUTHIER, JenniferDYAKONOV, Tatyana
    • A61K
    • A61K31/325A61K47/54A61K47/58A61K47/60A61K47/61
    • Prodrugs having a hydrolyzable carbamate moiety, compositions including the prodrugs, methods of preparing the prodrugs and methods of treatment using the prodrugs are disclosed. The prodrug has the formula DC(X)XR, where D is a biologically active agent, X is O, S or NR , and R is a moiety that modifies various properties of the biologically active agent. The biologically active agent either includes a functional group such as an amide, thioamide, imide, thioimide, urea, thiourea, carbamate, thiocarbamate, sulfonamide, or sulfonimide group, or includes a hydroxy, amine, carboxylic acid or thiol group that is modified to include such a group. An NH group from the biologically active agent can be coupled to an activated form the C(X)XR moiety to form the prodrugs described herein. Relative to a conventional carbamate group, the presence of the additional carbonyl or sulfonyl group makes the carbamate group more susceptible to hydrolysis. The prodrugs are more stable in certain environments than the biologically active agent, and can permit the drugs to be administered orally, in those embodiments where the biologically active agent must otherwise be administered by injection or intraveneous administration.
    • 公开了具有可水解氨基甲酸酯部分的前药,包含前药的组合物,制备前体药物的方法和使用前药的治疗方法。 前药具有式DC(X)XR,其中D是生物活性剂,X是O,S或NR,R是修饰生物活性剂的各种性质的部分。 生物活性剂还包括官能团,例如酰胺,硫代酰胺,酰亚胺,硫代酰亚胺,脲,硫脲,氨基甲酸酯,硫代氨基甲酸酯,磺酰胺或磺酰亚胺基团,或包括羟基,胺,羧酸或硫醇基, 包括这样一个组。 来自生物活性剂的NH基团可以与C(X)XR部分的活化形式偶联以形成本文所述的前药。 相对于常规氨基甲酸酯基团,另外的羰基或磺酰基的存在使得氨基甲酸酯基团更易于水解。 前药在某些环境中比生物活性剂更稳定,并且可以允许药物口服给药,在那些其中生物活性剂必须通过注射或静脉内给药施用的那些实施方案中。