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    • 24. 发明授权
    • Process for the preparation of highly optical pure carvedilol
    • 制备高光学纯卡维地洛的方法
    • US08101781B2
    • 2012-01-24
    • US12280684
    • 2006-08-31
    • Seong-Jin KimChang Woo JongHyun Bin KangByung Hyun MoonLong Guo QuanDuk Kwon WonKyung Yong Jin
    • Seong-Jin KimChang Woo JongHyun Bin KangByung Hyun MoonLong Guo QuanDuk Kwon WonKyung Yong Jin
    • A61K31/403C07D209/88
    • C07D209/88C07D263/24C07D413/12Y02P20/55
    • The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the reaction of N-protected 2-(2-methoxyphenoxy)ethylamine with a chiral glycidol derivative is used as a key intermediate for the preparation of the chiral carvedilol. Specifically, the process for the preparation of the chiral carvedilol comprises a) reacting a compound of formula 2 with a halogenation agent, a sulfonation agent or a mitsunobu reagent to activate a hydroxyl group of the compound of formula 2, followed by nucleophilic substitution reaction with 9H-4-hydroxy carbazole to produce a compound of formula 7, and b) subjecting the obtained compound of formula 7 to a deprotection reaction in a presence of an inorganic base to produce the targeted chiral carvedilol. The process of the present invention can be accomplished in a mild condition. The process neither requires any extraordinary purification procedure, nor involves decrease of optical purity. Therefore, the process of the present invention provides highly optical pure chiral carvedilol in simple and efficient manner.
    • 本发明涉及高效光学纯手性卡维地洛的高效制备方法。 根据本发明,由N-保护的2-(2-甲氧基苯氧基)乙胺与手性缩水甘醇衍生物的反应生成的具有式2的手性恶唑烷-2-酮或恶唑烷-2-硫酮用作关键中间体 用于制备手性卡维地洛。 具体地说,制备手性卡维西洛的方法包括:a)使式2的化合物与卤化剂,磺化剂或mitsunobu试剂反应以活化式2化合物的羟基,然后与 9H-4-羟基咔唑制备式7的化合物,和b)在无机碱的存在下使得到的式7的化合物进行脱保护反应,得到目标的手性卡维地洛。 本发明的方法可以在温和的条件下完成。 该方法既不需要任何非凡的纯化程序,也不涉及降低光学纯度。 因此,本发明的方法以简单有效的方式提供高光学纯手性卡维地洛。
    • 28. 发明授权
    • Pharmaceutical composition comprising Aralia extracts
    • 含有Aralia提取物的药物组合物
    • US06827950B2
    • 2004-12-07
    • US10219613
    • 2002-08-15
    • Eun-Kyung HongYoung-Shin ChungYeong-Bok HanYun Hui ChoiSeong-Jin KimHae-Ri KimBu-Hyeon Kang
    • Eun-Kyung HongYoung-Shin ChungYeong-Bok HanYun Hui ChoiSeong-Jin KimHae-Ri KimBu-Hyeon Kang
    • A61K3578
    • A61K36/25
    • The present invention relates to Aralia extracts and a therapeutic agent comprising Aralia extracts as an active ingredient. The composition and therapeutic agent according to the present invention are effective in preventing cataract, delaying the development of cataract, and treating cataract. According to the present invention, extracts of Aralia are obtained by extraction with alcohol. Addition of myo-inositol or taurine to the extracts will result in a synergistic effect in the treatment of cataract. In addition, oral administration of beverages, galenicals, and nutraceuticals, which comprise Aralia extracts as an active ingredient, will be effective in prevention, delay and treatment of cataract caused by complications of diabetes. Aralia extracts will have the same effect in the case where they are used as an ophthalmic agent. They can also be used as an eye drop or an eye ointment.
    • 本发明涉及Aralia提取物和包含Aralia提取物作为活性成分的治疗剂。 根据本发明的组合物和治疗剂可有效预防白内障,延缓白内障的发展和治疗白内障。 根据本发明,通过用醇萃取获得Aralia的提取物。 将肌醇或牛磺酸加入提取物将导致治疗白内障的协同效应。 此外,含有Aralia提取物作为活性成分的饮料,盖仑制品和营养制品的口服给药将有效预防,延迟和治疗由糖尿病并发症引起的白内障。 在将它们用作眼科剂的情况下,Aralia提取物将具有相同的效果。 它们也可以用作滴眼剂或眼膏。