公开(公告)号：US20050080252A1

公开(公告)日：2005-04-14

申请号：US10939819

申请日：2004-09-13

申请人： Andrew Briggs ,  Charles Dvorak ,  Anthony Prince ,  Keith McCarthy

发明人： Andrew Briggs ,  Charles Dvorak ,  Anthony Prince ,  Keith McCarthy

IPC分类号： C07H19/056

CPC分类号： C07H19/056

摘要： Process and novel intermediates for preparing 2-aminocarboxylic acid esters of the 5-hydroxymethyl group of levovirin (1-(3S,4R-dihydroxy-5S-hydroxymethyl-tetrahydro-furan-2S-yl)-1H-[1,2,4]triazole-3-carboxylic acid amide; Id: R1═R2═R3═H) and acid addition salts thereof. The present process provides the monoesters selectively in high purity with increased efficiency with reduced number of production steps. The process involves condensation of a cyclopentylidene levovirin compound with a N-urethane-N-carboxylic anhydride and subsequent deprotection to directly provide the hydrochloride salt of the product. The mono esters are useful for treatment of viral diseases and are absorbed more efficiently than the parent compound.

摘要翻译： 用于制备左旋病毒5-羟甲基的2-氨基羧酸酯的方法和新型中间体（1-（3S，4R-二羟基-5S-羟甲基 - 四氢 - 呋喃-2S-基）-1H- [1,2,4 ]三唑-3-羧酸酰胺; Id：R 1 = R 2 = R 3 = H）及其酸加成盐。 本方法提供了选择性高纯度的单酯，其生产步骤减少，效率提高。 该方法包括将亚环戊基纤溶蛋白化合物与N-氨基甲酸酯-N-羧酸酐缩合并随后脱保护直接提供产物的盐酸盐。 单酯可用于治疗病毒性疾病，并且比母体化合物更有效地吸收。

公开(公告)号：US20050130915A1

公开(公告)日：2005-06-16

申请号：US10939648

申请日：2004-09-13

申请人： Kondamraj Birudaraj ,  Anthony Prince ,  Keith McCarthy

发明人： Kondamraj Birudaraj ,  Anthony Prince ,  Keith McCarthy

IPC分类号： A61K31/7056 ,  A61K38/21 ,  C07H19/056

CPC分类号： C07H19/056 ,  Y10S514/885

摘要： The present invention relates to the polymorphic crystalline hydrochloride salts of a nucleoside valinate ester according to formula Ib, methods of treating diseases mediated by Hepatitis C Virus and pharmaceutical composition containing Ib.

摘要翻译： 本发明涉及根据式Ib的核苷缬氨酸酯的多晶型结晶盐酸盐，治疗由丙型肝炎病毒介导的疾病的方法和含有Ib的药物组合物。