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    • 6. 发明申请
    • A MANUFACTURING PROCESS OF 2',2'-DIFLUORONUCLEOSIDE AND INTERMEDIATE
    • 2',2'-二氟硼烷和中间体的制造方法
    • WO2007069838A1
    • 2007-06-21
    • PCT/KR2006/005372
    • 2006-12-11
    • DONG-A PHARM.CO., LTD.KIM, Moon-SungKIM, Yong-JikCHOI, Jun-HoLIM, Hong-GyuCHA, Dae-Won
    • KIM, Moon-SungKIM, Yong-JikCHOI, Jun-HoLIM, Hong-GyuCHA, Dae-Won
    • C07D307/32
    • C07D307/33C07D307/20C07D405/04C07H19/06Y02P20/55
    • The present invention relates to more improved process for preparing 2'-deoxy-2',2'-difluoronucleoside and its intermediate. The present invention provide a process for preparing an erythro enantiomer in greater than 98% purity, comprising forming a lactone ring by hydrolyzing ethyl (3RS )-2,2-difluoro-3-hydroxy-3-(2,2-dimethyloxolan-4-yl)propionate is hydrolyzed in the presence of hydrolysis reagents selected from acetic acid or chloroacetic acid, water and a mixture of organic solvents selected from the group comprising acetonitrile, dioxane, tetrahydrofuran or toluene, in¬ troducing a substituted benzoyl protecting group at the 3-position and 5-position, and recrys- tallizing said erythro enantiomer. Further, the present invention provides a process for selectively preparing, in greater than 99% purity, a beta-anomer 2'-deoxy-2',2'-difluoronucleoside at the 3'-position and 5'-position that are protected by a substituted benzoyl in a 2:3 alpha/beta anomeric ratio.
    • 本发明涉及制备2'-脱氧-2',2'-二氟核苷及其中间体的更加改进的方法。 本发明提供制备纯度高于98%的赤式对映异构体的方法,包括通过水解(3RS)-2,2-二氟-3-羟基-3-(2,2-二甲基氧基-4- - 基)丙酸酯在选自乙酸或氯乙酸的水解试剂,水和选自乙腈,二恶烷,四氢呋喃或甲苯的有机溶剂的混合物存在下水解,在该溶剂中引入取代的苯甲酰基保护基 3位和5位,并重新显示所述红色对映异构体。 此外,本发明提供了在大于99%的纯度中选择性地制备在3'-位和5'-位上的β-端基异构体2'-脱氧-2',2'-二氟核苷的方法,其被 2:3α/β端基异构体取代的苯甲酰基。
    • 10. 发明申请
    • LIQUID PHARMACEUTICAL COMPOSITION CONTAINING PIROXICAM AND HYALURONIC ACID FOR THE TREATMENT OF OSTEOARTHRITIS
    • 含有PIROXICAM和HYALURONIC酸的液体药物组合物用于治疗OSTEOARTHRITIS
    • WO2014200211A1
    • 2014-12-18
    • PCT/KR2014/004745
    • 2014-05-27
    • DONG-A ST CO., LTD
    • KIM, Soon-HoeSON, Mi-WonJANG, Sun-WooPARK, Chan-WoongMA, Kyung-WanJUNG, Sang-Won
    • A61K31/54A61K31/728A61P19/02A61P19/00
    • A61K31/728A61K9/0019A61K31/5415A61K47/02A61K2300/00
    • The present invention relates to the pharmaceutical composition for the treatment of osteoarthritis comprising piroxicam or pharmaceutically acceptable salt thereof and hyaluronic acid or pharmaceutically acceptable salt thereof at a specific ratio that generates synergistic effect on both anti-inflammatory and analgesic effects simultaneously. The present invention provides a pharmaceutical composition for the treatment of osteoarthritis comprising 0.25-10.0 wt% of piroxicam or its pharmaceutically acceptable salt and 0.5-5.0 wt% of hyaluronic acid or its pharmaceutically acceptable salt, where the weight ratio between piroxicam or its pharmaceutically acceptable salt and hyaluronic acid or its pharmaceutically acceptable salt is between 1:1 and 1:3. The liquid pharmaceutical composition according to the present invention has an outstanding therapeutic effect simultaneously on both inflammation and pain, thus providing an injectable formulation for intra-articular injection with synergistic effect on the treatment of osteoarthritis.
    • 本发明涉及用于治疗骨关节炎的药物组合物,其包含吡罗昔康或其药学上可接受的盐和透明质酸或其药学上可接受的盐,其特定比例同时产生对抗炎和镇痛作用的协同作用。 本发明提供了用于治疗骨关节炎的药物组合物,其包含0.25-10.0重量%的吡罗昔康或其药学上可接受的盐和0.5-5.0重量%的透明质酸或其药学上可接受的盐,其中,炎痛喜酸或其药学上可接受的盐的重量比 盐和透明质酸或其药学上可接受的盐在1:1至1:3之间。 根据本发明的液体药物组合物在炎症和疼痛方面同时具有突出的治疗效果,因此提供关节内注射的可注射制剂,对治疗骨关节炎具有协同作用。