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    • 16. 发明公开
    • 광학 활성 피페리딘 화합물의 개량된 제조방법
    • 一种改进的光学活性哌啶化合物的制备方法
    • KR1020110028207A
    • 2011-03-17
    • KR1020100049479
    • 2010-05-27
    • 박사룡
    • 박사룡
    • C07D401/10C07D401/02C07D401/12
    • Y02P20/55C07D401/12A61K31/4545C07D213/26C07D213/30
    • PURPOSE: A method for preparing (S)-4-[4-[4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid and additive salts thereof are provided. CONSTITUTION: A method for preparing (S)-4-[4-[4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid and additive salts thereof comprises: a step of reacting (-)-4-chlorophenyl-2-pyridyl-methanol of structural formula b with an alkali metal to obtain a (-)-4-chlorophenyl-2-pyridyl-methoxide of an alkali metal of structural formula b'; a step of reacting the compound of chemical formula b' with 4-halogeno-piperidyl)-butanoic acid derivative of structural formula c to obtain a (S)-4-[4-[4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid derivative of structural formula I'; and a step of removing a carboxylic protection group and reacting with organic acid.
    • 目的:提供(S)-4- [4- [4-氯苯基](2-吡啶基)甲氧基]哌啶子基]丁酸及其添加盐的制备方法。 构成:(S)-4- [4- [4-氯苯基](2-吡啶基)甲氧基]哌啶子基]丁酸及其添加盐的制备方法包括:( - ) - 4-氯苯基-2 结构式b的吡啶基 - 甲醇与碱金属反应,得到结构式b'的碱金属的( - ) - 4-氯苯基-2-吡啶基 - 甲醇盐; 使化学式b'的化合物与结构式c的4-卤代 - 哌啶基) - 丁酸衍生物反应,得到(S)-4- [4- [4-氯苯基](2-吡啶基)甲氧基] 哌啶子基]丁酸衍生物; 以及除去羧基保护基并与有机酸反应的步骤。
    • 18. 发明公开
    • 약물의 생리활성을 증진시킨 개량된 약학적 조성물 및 그제조방법
    • 含有药物活性成分的生理活性改进药物组合物及其制备方法
    • KR1020080037493A
    • 2008-04-30
    • KR1020060113878
    • 2006-11-17
    • 박사룡
    • 박사룡
    • A61K9/10
    • A61K9/10A61K31/366A61K31/40A61K31/436A61K31/505A61K47/10B82Y5/00
    • A co-dissolved mixture of a water-insoluble drug is provided to show enough medicinal effect with a little amount of the drug because of the nano-sized drug being dispersed into a polyhydric alcohol ultra-finely and also show rapid medicinal efficacy. A co-dissolved mixture is characterized in that an ultra-fine nano-sized drug which is hard to be solved in water is dispersed into a polyhydric alcohol or a diluent is further evenly dispersed into the dispersion. In the mixture, the drug is selected from the group consisting of orlistat, atorvastatin and a salt thereof, atorvastatin lactone-type, rosuvastatin and a salt thereof, pivastatin and a salt thereof, simvastatin and tacrolimus, and the polyhydric alcohol is selected from the group consisting of ethyleneglycol, propyleneglycol, glycerin, polyethyleneglycol, monosaccharide and disaccharide.
    • 提供了一种溶于水的不溶性药物的混合溶液,由于纳米级药物被超细分散在多元醇中并显示出快速的药用效能,因此用少量的药物显示出足够的药用效果。 共溶解混合物的特征在于,难以在水中溶解的超细纳米尺寸药物分散在多元醇中,或稀释剂进一步均匀地分散在分散体中。 在该混合物中,药物选自奥利司他,阿托伐他汀及其盐,阿托伐他汀内酯型,瑞舒伐他汀及其盐,妥他他汀及其盐,辛伐他汀和他克莫司,多元醇选自 由乙二醇,丙二醇,甘油,聚乙二醇,单糖和二糖组成的组。