PARK, Sang-Guk,LIM, Joong-In,KIM, Yong-Jik,KIM, Yong-Duck,KIM, Hoo-Sook,SON, Moon-Ho,KIM, Soon-Hoe,KIM, Jae-Han,KWAK, Woo-Young
申请号：
KRKR2014/005854
公开号：
WO2015/002434A1
申请日:
2014.07.01
申请国别(地区):
WO
年份:
2015
代理人:
摘要：
The present invention relates to a novel tenofovir disoproxil salt and the preparation method thereof. The crystalline form of tenofovir disoproxil orotate according to the present invention is an anhydride and it has superior physicochemical properties that are useful in pharmaceutical preparation as it resolves problems caused by physicochemical properties of tenofovir disoproxil fumarate. Namely, the crystalline form of tenofovir disoproxil orotate according to the present invention has a better than equal light stability compared to tenofovir disoproxil fumarate and has a superior stability especially under extreme stress conditions. Additionally, it is neither corrosive nor harmful to human body, thus making it safe for preparation and easy to manage. All of these characteristics make this invention useful for mass production. The present invention also provides a preparation method with and without using organic solvent, thus providing an industrially applicable and environment-friendly preparation method. Furthermore, tenofovir disoproxil orotate prepared according to the present invention can be used as an antiviral treating agent and can also be made into an anti-HIV treating composition if mixed with other drugs that have anti-HIV activity. The composition can be made into mixtures with one to six of the following other anti-HIV active ingredient medications that include Emtricitabine, Efavirenz, Rilpivirenz, Cobicistat, Elvitegravir, Raltegravir, Ritonavir, Lopinavir, Darunavir, Atazanavir and salts thereof for the treatment of HIV infection.Cette invention concerne un nouveau sel de ténofovir disoproxil et son procédé de préparation. La forme cristalline de lorotate de ténofovir disoproxil selon la présente invention est un anhydride et elle présente des propriétés physicochimiques supérieures qui sont utiles en préparation pharmaceutique dans la mesure où elle résout les problèmes provoqués par les propriétés physicochimiques du fumarate de ténofovir di
