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    • 2. 发明授权
    • 아토르바스타틴의 개선된 제조방법
    • 改进ATORVASTATIN的方法
    • KR100856133B1
    • 2008-09-03
    • KR1020080003530
    • 2008-01-11
    • 조동옥주식회사 다산제약
    • 조동옥권윤자김영숙차경회태현섭
    • C07D207/34A61P3/06
    • Y02P20/55C07D207/34A61K31/40C07D319/06
    • A process for preparing atorvastatin as a therapeutic agent for hyperlipidemia is provided to simplify the preparation process by eliminating a specific function group-introducing process, improve preparation yield and purity by inhibiting production of by-products and performing the process under mild condition, and reduce the preparation time. A process for preparing atorvastatin represented by the formula(1) comprises the steps of: (i) performing N-alkylation reaction between 2-(4-fluorobenzene)-3-phenyl-4-carboaniline-5-isopropyl-pyrrol represented by the formula(2) with cis-t-butyl-7-halo-2-alkoxy-3,5-dioxane-heptanoate represented by the formula(3) to prepare 2-(4-fluorophenyl)-3-phenyl-4-carboaniline-5-isopropyl-1N(cis-t-butyl-2-alkoxy-3,5-dioxane-7-amido-heptanoate)pyrrole represented by the formula(4) wherein R is C1-C6 alkyl group and X is halogen atom; and deprotecting and hydrolyzing the compounds represented by the formula(4) in alcohol solvent in the presence of acid catalyst at 0-25 deg. C.
    • 提供制备阿托伐他汀作为高脂血症治疗剂的方法,以通过消除特定的功能团引入方法,通过抑制副产物的产生和在温和条件下进行该方法来提高制备产率和纯度来简化制备过程,并减少 准备时间。 制备由式(1)表示的阿托伐他汀的方法包括以下步骤:(i)进行2-(4-氟苯)-3-苯基-4-苯胺-5-异丙基 - 吡咯的N-烷基化反应 式(2)与由式(3)表示的顺式叔丁基-7-卤代-2-烷氧基-3,5-二恶烷 - 庚酸酯反应制备2-(4-氟苯基)-3-苯基-4-甲苯胺 (4)所示的5-异丙基-1H-(顺式 - 叔丁基-2-烷氧基-3,5-二恶烷-7-酰氨基 - 庚酸酯)吡咯,其中R是C1-C6烷基,X是卤素原子 ; 并在醇溶剂中,在酸催化剂存在下,在0-25℃,将由式(4)表示的化合物脱保护和水解。 C。
    • 10. 发明公开
    • 슈도에페드린 또는 그의 염의 방출제어형 약제학적 조성물
    • 使用小量的释放控释剂的小剂量的PSEUDOEPHEDRINE或其盐的控制释放药物组合物
    • KR1020040097900A
    • 2004-11-18
    • KR1020040032497
    • 2004-05-08
    • 주식회사 다산제약
    • 류형선박신정
    • A61K9/30
    • A61K9/2866A61K9/2853A61K31/137A61K47/34A61K47/38
    • PURPOSE: A controlled release pharmaceutical composition containing pseudoephedrine or its salt is provided. In particular, the composition comprises a release-controlling layer composed of a small amount of shellac. Therefore, it controls the release of pseudoephedrine or its salt effectively without using any release-controlling agents. CONSTITUTION: The controlled release pharmaceutical composition of pseudoephedrine or its salt comprises: a core: a drug coating layer wherein a therapeutically effective amount of pseudoephedrine or its slat is coated on the surface of the core; and a release-controlling layer wherein 1.5-5 wt.% of shellac is coated on the drug containing layer, based on the total weight of the composition.
    • 目的:提供含有伪麻黄碱或其盐的控释药物组合物。 特别地,组合物包含由少量虫胶组成的释放控制层。 因此,它可以有效地控制伪麻黄碱或其盐的释放,而不使用任何释放控制剂。 构成:伪麻黄碱或其盐的控释药物组合物包括:芯:药物包衣层,其中治疗有效量的伪麻黄碱或其板条涂覆在芯的表面上; 和释放控制层,其中基于组合物的总重量,将1.5-5重量%的虫胶涂覆在含药层上。